Helicobacter pylori is a risk factor for the development of peptic ulcers with autophagy dysfunction.Omeprazole was widely known as the first-line regimen for H.pylori-associated gastritis.Objectives:The objective of ...Helicobacter pylori is a risk factor for the development of peptic ulcers with autophagy dysfunction.Omeprazole was widely known as the first-line regimen for H.pylori-associated gastritis.Objectives:The objective of this work was to assess the role of omeprazole on cell pyroptosis and autophagy.Methods:The clinical samples were collected.Quantitative polymerase chain reaction,western blotting,enzyme linked immunosorbent assay,and immunofluorescence(IF)analysis were conducted to reveal the mechanism of omeprazole on cell pyroptosis and autophagy.Results:The results revealed that omeprazole could decrease cell pyroptosis,which was attributed to the downregulation of cleaved caspase-1 expression,resulting in the inhibition of gasdermin E and interleukin-18/1βmaturation and secretion as well as the resolution of inflammation.Mechanistically,omeprazole treatment led to drastic downregulation of mammalian target of rapamycin(mTOR)activity was observed in BGC823 cells,leading to enhanced autophagy characterized by increased LC3II expression,which further reduced cell pyroptosis.This omeprazole-mediated phenomenon was enhanced after phosphodiesterase-4(PDE4)inhibitor dipyridamole(DIP)treatment.In addition,activation of mTOR by MHY1485 could rescue the suppression of cell pyroptosis induced by omeprazole.Most importantly,IF analysis suggested that phosphorylation of mTOR and PDE4 activity and caspase-1 were enhanced in H.pylori-infected gastric mucosa.Conclusion:These findings indicate that omeprazole suppresses cell pyroptosis through PDE4-mediated autophagy in gastric epithelial cells,and DIP enhanced the omeprazole-mediated inhibition of cell pyroptosis,implying that DIP is an alternative combined therapy strategy in improving the treatment of patients with H.pylori infection.展开更多
Objective:To investigate the therapeutic effect of omeprazole+amoxicillin in patients with gastric ulcers.Methods:62 cases of patients with gastric ulcers who were treated from January 2022 to December 2022 were recru...Objective:To investigate the therapeutic effect of omeprazole+amoxicillin in patients with gastric ulcers.Methods:62 cases of patients with gastric ulcers who were treated from January 2022 to December 2022 were recruited and randomly divided into groups.Omeprazole+amoxicillin treatment was included in the study group,and amoxicillin treatment was included in the control group.The score of gastric ulcer symptoms,time of symptom resolution,gastrointestinal hormone index,and adverse reactions were compared.Results:The gastric ulcer symptom scores in the study group were lower than those in the control group(P<0.05);the gastric ulcer symptoms and Helicobacter pylori-negative time in the study group were shorter than those in the control group(P<0.05);the gastrointestinal hormone indexes in the study group were better than those in the control group(P<0.05);the adverse reaction rate of gastric ulcer in the study group was lower than that in the control group(P<0.05).Conclusion:Omeprazole+amoxicillin in the treatment of gastric ulcers can regulate gastrointestinal hormones,relieve gastric ulcer symptoms,and shorten the duration of ulcers,which is highly effective and feasible.展开更多
AIM: To clarify whether there is any difference in the symptom relief in patients with reflux esophagitis following the administration of four Proton pump inhibitors (PPIs). METHODS: Two hundred and seventy-four patie...AIM: To clarify whether there is any difference in the symptom relief in patients with reflux esophagitis following the administration of four Proton pump inhibitors (PPIs). METHODS: Two hundred and seventy-four patients with erosive reflux esophagitis were randomized to receive 8 wk of 20 mg omeprazole (n = 68), 30 mg of lansoprazole (n = 69), 40 mg of pantoprazole (n = 69), 40 mg of esomeprazole (n = 68) once a day in the morning. Daily changes in heartburn and acid reflux symptoms in the first 7 d of administration were assessed using a six-point scale (0: none; 1: mild; 2: mild-moderate; 3: moderate; 4: moderate-severe; 5: severe). RESULTS: The mean heartburn score in patients treated with esomeprazole more rapidly decreased than those receiving other PPI. Complete resolution of heartburn was also more rapid in patients treated with esomeprazole for 5 d compared with omeprazole (P = 0.0018, P = 0.0098, P = 0.0027, P = 0.0137, P = 0.0069, respectively), lansoprazole (P = 0.0020, P = 0.0046, P = 0.0037, P = 0.0016, P = 0.0076, respectively), and pantoprazole (P = 0.0006, P = 0.0005, P = 0.0009, P = 0.0031, P = 0.0119, respectively). There were no significant differences between the four groups in the rate of endoscopic healing of reflux esophagitis at week 8. CONCLUSION: Esomeprazole may be more effective than omeprazole, lansoprazole, and pantoprazole for the rapid relief of heartburn symptoms and acid reflux symptoms in patients with reflux esophagitis.展开更多
AIM： To study the effect of proton pump inhibitor （PPI） treatment on patients with reflux esophagitis and its in vivo effect on apoptosis, p53- and epidermal growth factor receptor （EGFR） expression. METHODS： Af...AIM： To study the effect of proton pump inhibitor （PPI） treatment on patients with reflux esophagitis and its in vivo effect on apoptosis, p53- and epidermal growth factor receptor （EGFR） expression. METHODS： After informed consent was obtained, gastric biopsies of the antrum were taken from patients with reflux oesophagitis prior to and after 6 mo of 20 mg omeprazole （n = 24） or 40 mg esomeprazole （n = 22） therapy. Patients did not take any other medications known to affect the gastric mucosa. All patients were Helicobacter pylori negative as confirmed by rapid urease test and histology, respectively. Cell proliferation, apoptosis, EGFR, and p53 expression were measured by immunohistochemical techniques. At least 600 glandular epithelial cells were encountered and results were expressed as percentage of total cells counted. Was considered statistically significant. RESULTS： Although there was a trend towards increase of cell proliferation and EGFR expression both in omeprazole and esomeprazole treated group, the difference was not statistically significant. Neither apoptosis nor p53 expression was affected. CONCLUSION： Long-term PPI treatment does not significantly increase gastric epithelial cell proliferation and EGFR expression and has no effect on apoptosis and p53 expression.展开更多
AIM To investigate and compare the effects of tocotrienol and omeprazole on gastric growth factors in rats exposed to water-immersion restraint stress(WIRS).METHODS Twenty-eight male Wistar rats were randomly assigned...AIM To investigate and compare the effects of tocotrienol and omeprazole on gastric growth factors in rats exposed to water-immersion restraint stress(WIRS).METHODS Twenty-eight male Wistar rats were randomly assigned to four groups of seven rats. The two control groups were administered vitamin-free palm oil(vehicle) and the two treatment groups were given omeprazole(20 mg/kg) or tocotrienol(60 mg/kg) by oral gavage. After 28 d of treatment, rats from one control group and both treated groups were subjected to WIRS one time for 3.5 h. Gastric lesions were measured and gastric tissues were obtained to measure vascular endothelial growth factor(VEGF), epidermal growth factor(EGF), basic fibroblast growth factor(b FGF), and transforming growth factor-alpha(TGF-α) m RNA expression. RESULTS Rats exposed to WIRS for 3.5 h demonstrated the presence of considerable ulcers in the form of gastric erosion. The lesion index in the stressed control(S) group was increased(P < 0.001) compared to the tocotrienol treated and omeprazole treated groups. Stress led to a decrease in gastric VEGF(P < 0.001), b FGF(P < 0.001) and TGF-α(P < 0.001) m RNA levels and caused an increase in EGF m RNA(P < 0.001) that was statistically significant compared to the nonstressed control group. Although both treatment agents exerted similar ulcer reducing ability, only treatment with tocotrienol led to increased expression of VEGF(P = 0.008), b FGF(P = 0.001) and TGF-α(P = 0.002) m RNA.CONCLUSION Tocotrienol provides gastroprotective effects in WIRSinduced ulcers. Compared to omeprazole, tocotrienol exerts a similar protective effect, albeit through multiple mechanisms of protection, particularly through up-regulation of growth factors that assist in repair of gastric tissue injuries.展开更多
AIM： To study the effect of combined omeprazole（Ome） and domperidone（Dom） therapy on asthma symptoms and pulmonary function in asthmatics with gastroesoph- ageal reflux. METHODS： We selected 198 asthmatics with ...AIM： To study the effect of combined omeprazole（Ome） and domperidone（Dom） therapy on asthma symptoms and pulmonary function in asthmatics with gastroesoph- ageal reflux. METHODS： We selected 198 asthmatics with gastro- esophageal reflux diagnosed by 24-h esophageal pH moni- toring to receive Ome 20 mg twice daily and Dom 10 mg three times daily or placebo for 16 wk （1：1 double-blind randomization）. Spirometry was done at baseline and after 16 wk of treatment. The primary outcome measures were： mean daily daytime and nighttime asthma symptom scores. Mean daily reflux symptom scores, albuterol use as rescue medication （number of puffs）, daytime and nighttime peak expiratory flow rate （PEFR）, postbronchodilator forced expiratory volume in 1 second （FEVl） and postbronchodilator forced vital capacity （FVC） were secondary outcome measures. RESULTS： Comparison of mean change from baseline between antireflux therapy and placebo groups revealed significant reduction in daytime asthma symptom score （17.4% vs 8.9 %）, nighttime asthma symptom score （19.6% vs 5.4%）, reflux symptom score （8.7% vs 1.6%） and rescue medication use （23.2% vs 3.1%） after antireflux therapy compared to mean change in placebo group （P 〈 0.001）. There was significant improvement in morning PEFR （7.9% vs 0.2%）, evening PEFR （9.8% vs 0.5%）, FEW （11.1% vs 3.78%） and FVC （9.3%vs 1.52%） in the antireflux therapy group compared to placebo on comparng the mean change from baseline after 16 wk （P 〈 0.01） CONCLUSION： Combined therapy with Ome and Dom in adult asthmatics with gastroesophageal reflux may be beneficial by reducing asthma symptoms, rescuing medi- cation use, and improving pulmonary function.展开更多
AIM： To evaluate the omeprazole maintenance therapy in patients with recurrent ulcer bleeding after surgery for duodenal ulcer. METHODS： We studied 15 consecutive patients with recurrent ulcer bleeding after surgery...AIM： To evaluate the omeprazole maintenance therapy in patients with recurrent ulcer bleeding after surgery for duodenal ulcer. METHODS： We studied 15 consecutive patients with recurrent ulcer bleeding after surgery for duodenal ulcer. Omeprazole （20 mg/d） maintenance therapy was given after ulcer healing. In addition to clinical follow-up, ambulatory 24-h gastric pH assay was performed before and during omeprazole therapy in those patients and controls with previous duodenal ulcer surgery but no ulcer recurrence. RESULTS： All the 15 ulcers were healed after being treated with omeprazole （40 mg/d） for 2 too. Eleven patients with two （1-9） episodes of recurrent ulcer bleeding completed the follow-up （43, 12-72 too）. None of them had a bleeding episode while on omeprazole. One patient discontinued the therapy and had recurrent bleeding. The median 24-h fraction time of gastric pH 〈4 in patients was 80, 46-95%, and was reduced to 32, 13-70% by omeprazole （P= 0.002）. CONCLUSION： Long-term maintenance therapy with omeprazole （20 rag/day） is effective in preventing recurrent ulcer bleeding.展开更多
AIM To explore the effects of omeprazole on chemoradiotherapy efficacy and tumor recurrence in rectal cancer. METHODS The medical data of 125 rectal cancer patients who received the same neoadjuvant chemoradiotherapy(...AIM To explore the effects of omeprazole on chemoradiotherapy efficacy and tumor recurrence in rectal cancer. METHODS The medical data of 125 rectal cancer patients who received the same neoadjuvant chemoradiotherapy(CRT) followed by surgery were retrospectively collected. Patients who received omeprazole(OME) orally at a dose of 20 mg at least once daily for six days and/or intravenously at 40 mg a day were recognized as eligible OME users(EOU). Otherwise, patients were regarded as non-eligible OME users(non-EOU).Moreover, a preferred OME dose cut-off of 200 mg on tumor recurrence was obtained by receiver operating characteristic(ROC) curves. Patients were divided into two groups: the effective OME group(EOG, OME ≥ 200 mg) and the non-effective OME group(non-EOG, OME < 200 mg). RESULTS The good response rate of CRT efficacy(50.8%) in EOU was significantly increased compared with nonEOU(30.6%)(P = 0.02). The recurrence rate in the EOG was 10.3%, which was significantly lower compared with 31.3% in non-EOG(P = 0.025). The good response rate of CRT efficacy in EOG was 55.2%, which was obviously higher compared with 36.5% in non-EOG, with a significant difference(P = 0.072). Multivariate Cox analysis demonstrated that OME(nonEOG and EOG) was an independent and significant impact factor for DFS(P = 0.048, HR = 0.30, 95%CI: 0.09-0.99).CONCLUSION When applied as an adjuvant drug in cancer treatment for relieving common side effects of chemotherapy, omeprazole has a synergetic effect in improving CRT efficacy and decreasing rectal cancer recurrence.展开更多
AIM: One-week triple therapy with proton pump inhibitors, clarithromycin and amoxicillin has recently been proposed as the first-line treatment for Helicobacter pylori (H pylori) infection; however, data regarding the...AIM: One-week triple therapy with proton pump inhibitors, clarithromycin and amoxicillin has recently been proposed as the first-line treatment for Helicobacter pylori (H pylori) infection; however, data regarding the effects of this regimen in China are scarce. The aim of this prospective and randomized study was to compare the efficacy of clarithromycin and metronidazole when they were combined with omeprazole and amoxicillin on eradication of H pylori and ulcer healing in Chinese peptic ulcer patients. METHODS: A total of 103 subjects with Hpylori-positive peptic ulcer were randomly divided into two groups, and accepted triple therapy with omeprazole 20 mg, amoxicillin 1 000 mg and either clarithromycin 500 mg (OAC group, n = 58) or metronidazole 400 mg (0AM group, n - 45). All drugs were given twice daily for 7 d. Patients with active peptic ulcer were treated with omeprazole 20 mg daily for 2-4 wk after anti-H pylori therapy. Six to eight weeks after omeprazole therapy, all patients underwent endoscopies and four biopsies (two from the antrum and two others from the corpus of stomach) were taken for rapid urease test and histological analysis (with modified Giemsa staining) to examine H pylori. Successful eradication was defined as negative results from both examination methods. RESULTS: One hundred patients completed the entire course of therapy and returned for follow-up. The eradication rate of H pylori for the per-protocol analysis was 89.3% (50/56) in OAC group and 84.1% (37/44) in 0AM group. Based on the intention-to-treat analysis, the eradication rate of H pylori was 86.2% (50/58) in OAC group and 82.2% (37/45) in 0AM group. There were no significant differences in eradication rates between the two groups on either analysis. The active ulcer-healing rate was 96.7% (29/30) in OAC group and 100% (21/21) in 0AM group (per-protocol analysis, P>0.05). Six patients in OAC group (10.3%) and five in OAM group (11.1%) reported adverse events (P>0.05). CONCLUSION: One-week triple therapy with omeprazole and amoxicillin in combination with either clarithromycin or metronidazole is effective for the eradication of H pylori. The therapeutic regimen comprising metronidazole with low cost, good compliance and mild adverse events may offer a good choice for the treatment of peptic ulcers associated with H pylori infection in China.展开更多
Objective:To observe the protective effect of omeprazole on gastric mucosal of cirrhotic portal hypertension rats.Methods:All rats were randomly divided into normal control group,cirrhosis and treatment group.Thioacet...Objective:To observe the protective effect of omeprazole on gastric mucosal of cirrhotic portal hypertension rats.Methods:All rats were randomly divided into normal control group,cirrhosis and treatment group.Thioacetamide was used to establish rat model of cirrhotic portal hypertension.The necrotic tissue of gastric mucosa ulcer focus,degree of neutrophils infiltration at the ulcer margin,portal pressure,portal venous flow,abdominal aortic pressure,abdominal aortic blood flow at front end,gastric mucosal blood flow（GMBF）,glycoprotein（GP）of gastric mucosa,basal acid secretion,H’ back-diffusion,gastric mucosal damage index,NO,prostaglandin E2（PGE2） and tumor necrosis factor-α（TNF-α） were determined respectively,and the pathological changes of gastric mucosa were also observed by microscope.Results:Compared with cirrhosis group and the control group,the ulcer bottom necrotic material,gastric neutrophil infiltration and UI of the treatment group were all decreased significantly（P【0.01）,GMBF value,GP values,serum NO,PGE2,TNF- a were all significantly increased.Conclusions:Omeprazole has an important protective effect on gastric mucosal and it can increase gastric mucosal blood flow and related to many factors.展开更多
Background: This study evaluated the effect of omeprazole or pantoprazole on platelet reactivity in non-STsegment elevation acute coronary syndrome(NSTE-ACS) patients receiving clopidogrel.Methods: Consecutive patient...Background: This study evaluated the effect of omeprazole or pantoprazole on platelet reactivity in non-STsegment elevation acute coronary syndrome(NSTE-ACS) patients receiving clopidogrel.Methods: Consecutive patients with NSTE-ACS(n =620) from general hospital of Shenyang Military Command were randomized to the omeprazole or pantoprazole(20mg/d) group(1:1), and received routine dual antiplatelet treatment. Patients' reversion rate of adenosine diphosphate-induced platelet aggregation(ADP-PA) was assessed at baseline, 12 to 24 h after administration of medication, and after 72 h of percutaneous coronary intervention(PCI). The primary endpoint of the study was platelet reactivity assessed with ADP-PA at 30 days after PCI. Adverse events(AEs) were recorded for 30-day and 180-day follow-up periods.Results: There were no significant differences between both the groups in platelet response to clopidogrel at 12–24h after drug administration(54.09%±18.90% vs. 51.62%±19.85%, P=0.12), 72 h after PCI(52.15%±19.45% vs. 49.66%±20.05%, P=0.18), and 30 days after PCI(50.44%±14.54% vs. 48.52%±15.08%, P=0.17). The rate of AEs did not differ significantly between groups during the 30-day(15.2% vs. 14.8%, P=0.91) and 180-day(16.5% vs. 14.5%, P=0.50) follow-up periods after PCI.Conclusion: The addition of omeprazole or pantoprazole to clopidogrel did not restrict the effect of platelet aggregation by reducing the conversion of clopidogrel. Compared with clopidogrel alone, pantoprazole-clopidogrel and omeprazoleclopidogrel combinations did not increase the incidence of adverse clinical events during 30-day and 180-day follow-up periods after PCI.展开更多
Recent reports have demonstrated that the new commercially available immobilized-type chiral stationary phases（CSPs） containing amylose tris（3-chloro-5-methylphenylcarbamate）（ACMPC） as a selector exhibit not onl...Recent reports have demonstrated that the new commercially available immobilized-type chiral stationary phases（CSPs） containing amylose tris（3-chloro-5-methylphenylcarbamate）（ACMPC） as a selector exhibit not only an exceptionally high enantioselectivity in high-performance liquid chromatography（HPLC） but they are also applicable to a wide range of chiral analytes. Herein, we report the results obtained in the HPLC analysis of omeprazole and its impurities B and E on the ACMPC-based Chiralpak IG-3 CSP（CSP） under polar organic conditions. A systematic evaluation of the retention characteristics of the selected benzimidazole chiral probes was carried out by changing the composition of the mobile phase and the column temperature. It is worth emphasizing that the high affinity of both enantiomers of all analytes recorded in pure methanol mode dramatically decreased incorporating small volumes of either basic or acid additives in the mobile phase. Unspecified sites of the IG-3 CSP presumably involved in strong and non-stereoselective H-bonding contacts with chiral analytes are assumed responsible for the unproductive retention process.展开更多
AIM： To compare the effect of intravenous and oral omeprazole in patients with bleeding peptic ulcers without high-risk stigmata.METHODS： This randomized study included 211 patients [112 receiving iv omeprazole prot...AIM： To compare the effect of intravenous and oral omeprazole in patients with bleeding peptic ulcers without high-risk stigmata.METHODS： This randomized study included 211 patients [112 receiving iv omeprazole protocol （Group 1）, 99 receiving po omeprazole 40 mg every 12 h （Group 2）] with a mean age of 52.7. In 144 patients the ulcers showed a clean base, and in 46 the ulcers showed fiat spots and in 21 old adherent clots. The endpoints were re-bleeding, surgery, hospital stay, blood transfusion and death. After discharge, re-bleeding and death were reevaluated within 30 d.RESULTS： The study groups were similar with respect to baseline characteristics. Re-bleeding was recorded in 5 patients of Group 1 and in 4 patients of Group 2 （P = 0.879）. Three patients in Group 1 and 2 in Group 2 underwent surgery （P = 0.773）. The mean length of hospital stay was 4.6 ± 1.6 d in Group 1 vs 4.5 ± 2.6 d in Group 2 （P = 0.710）; the mean amounts of blood transfusion were 1.9 ±1.1 units in Group 1 vs 2.1 ±1.7 units in Group 2 （P = 0.350）. Four patients, two in each group died （P = 0.981）. After discharge, a new bleeding occurred in 2 patients of Group 1 and in 1 patient of Group 2, and one patient from Group 1 died.CONCLUSION： We demonstrate that the effect of oral omeprazole is as effective as intravenous therapy in terms of re-bleeding, surgery, transfusion requirements, hospitalization and mortality in patients with bleeding ulcers with low risk stigmata. These patients can be treated effectively with oral omeprazole.展开更多
A randomized, two-way, crossover study was conducted in 18 fasting, healthy, algerian volunteers to compare the bioavailability of two brands of Omeprazole 20 mg Gastro-Resistant Capsules where MOPRAL （Astra Zeneca）...A randomized, two-way, crossover study was conducted in 18 fasting, healthy, algerian volunteers to compare the bioavailability of two brands of Omeprazole 20 mg Gastro-Resistant Capsules where MOPRAL （Astra Zeneca） was the reference product. The study was performed at the bioequivalence center of the national control laboratory for pharmaceuticals product. The drug was administered on two treatment days separated by one week washout period. After dosing, serial blood samples were collected for a period of 12 h. A reliable and robust LC-MS/MS （liquid chromatography-tandem mass spectrometry） method has been developed and validated for the estimation of Omeprazole in human plasma. The assay was found to be linear over the range of 5-1,000 ng/mL. The pharmacokinetical and statistical analysis was conducted with Kinetica 4.4.1. AUC0.t, AUC0-∞ and Cmax were tested for bioequivalence. No significant difference was found based on ANOVA; 90% confidence interval （[97.14%-117..85%] for AUC0.t, [97.17%-117.67%] for AUC0-∞） of test/reference ratio for these parameters were found within bioequivalence acceptance range of 80%-125%. But for the Cmax, it was not in this acceptance range [73,5%-100.54%]. The results of PK analysis suggested that the reference and test formulations of Omeprazole 20 mg Gastro-Resistant Capsules were not bioequivalent during fasting state in these healthy Algerian volunteers.展开更多
Omeprazole sodium(OMS), a typical non-hydrogen bond donors API, is only available in solvates so far, including monohydrate, ethanol solvate and methanol solvate. The methanol solvate was found for the first time. Sol...Omeprazole sodium(OMS), a typical non-hydrogen bond donors API, is only available in solvates so far, including monohydrate, ethanol solvate and methanol solvate. The methanol solvate was found for the first time. Solvate transformation thermodynamics of OMS was studied in this paper. First, the ternary phase diagrams forming two solvates for OMS in binary solvent mixtures including methanol + water, ethanol + water, and methanol+ ethanol were measured at temperature ranging of T =(278.15 to 313.15) K under atmospheric pressure. Further, the standard equilibrium constants of the solvate transformation reactions were evaluated according to the chemical reaction isothermal equation. The standard molar Gibbs free energy, the standard molar enthalpy, and the standard molar entropy of solvate transformation reactions were then calculated based on van't Hoff equation. Moreover, the thermodynamic stability of the OMS solvate was analyzed based on phase diagram. The results are of great importance to develop a crystallization process for manufacturing OMS solvate, and could be helpful to other solvate transformation research.展开更多
Omeprazole is a potent proton pump inhibitor with powerful inhibition of secretion of gastric juice. Oral site-specific drug delivery systems have recently attracted a great interest for the local treatment of bowel d...Omeprazole is a potent proton pump inhibitor with powerful inhibition of secretion of gastric juice. Oral site-specific drug delivery systems have recently attracted a great interest for the local treatment of bowel disease and for improving systemic absorption of drugs which are unstable in the stomach. However, microenvironment in the gastrointestinal tract and varying absorption mechanisms cause hindrance for the formulation and optimization of oral drug delivery. The objective of the study was to develop and optimize enteric coating process for omeprazole tablets. Different batches of core tablets were sub coated, one set sub coated with opadry and another with a mixture of light magnesium oxide, magnesium stearate and absolute alcohol omeprazole magnesium. Seal coating was applied by using opadry to achieve certain weight gain and to protect omeprazole from acidic coating polymers. A comparative dissolution test was performed. The variation of thickness and diameter were observed to be minimal with a weight gain of 3% - 4% of enteric polymer. Disintegration test showed that in each tested batch the enteric coated layer remained intact in 0.1N HCl for 2 hours and when exposed to alkaline media of phosphate buffer pH 6.8, it dissolved within few minutes. Dissolution release was 98.8% to 102.4% within two hours when the product was exposed to phosphate buffer pH 6.8 after 2 hours. The similarity and dis-similarity factors were calculated and observed to be 54 to 61 and 4 to 5 respectively. Therefore a simple and good enteric coating process was developed and tested with potential for transfer this technology into local pharmaceutical industries using cheap and easily available materials.展开更多
Objective:To investigate the effect of somatostatin combined with omeprazole on serum inflammatory factors and intestinal mucosal barrier function in severe acute pancreatitis. Methods: patients with severe acute panc...Objective:To investigate the effect of somatostatin combined with omeprazole on serum inflammatory factors and intestinal mucosal barrier function in severe acute pancreatitis. Methods: patients with severe acute pancreatitis who were treated in Zigong Third People's Hospital between August 2014 and December 2017 were chosen and divided into two groups by random number table method. Control group received conventional + omeprazole treatment, combined group received conventional + somatostatin + omeprazole treatment and the treatment lasted for 1 week. The differences in serum levels of inflammatory factors, chemokines and intestinal mucosal barrier function indexes were compared between the two groups immediately after admission and after 1 week of treatment.Results: After 1 week of treatment, serum IL-1β, IL-8, IL-18, hs-CRP, MCP-1, FKN, CINC, D-Lactate, DAO, Endotoxin and FABP levels of both groups significantly decreased and serum IL-1β, IL-8, IL-18, hs-CRP, MCP-1, FKN, CINC, D-Lactate, DAO, Endotoxin and FABP levels of combined group were significantly lower than those of control group.Conclusion: Somatostatin combined with omeprazole therapy for severe acute pancreatitis can effectively alleviate the inflammatory response and protect the intestinal mucosal barrier function.展开更多
Objective:To investigate the TNF-α、IL-6、IL-1βeffect of omeprazole combined with amoxicillin on cytokines in gingival crevicular fluid of patients with periodontal disease.Methods:102 patients with periodontal dise...Objective:To investigate the TNF-α、IL-6、IL-1βeffect of omeprazole combined with amoxicillin on cytokines in gingival crevicular fluid of patients with periodontal disease.Methods:102 patients with periodontal disease who were treated in our hospital from June 2016 to March 2018 were selected.Randomly divided into two groups,the control group was treated with omeprazole alone,and the research group was treated with omeprazole combined with amoxicillin.The levels of inflammatory cytokines(TNF-α、IL-6、IL-1β),therapeutic effects and adverse reactions to drugs were compared between the two groups.Results:the levels of inflammatory factors(TNF-α、IL-6、IL-1β)in the study group were lower than those in the control group(P<0.05).The therapeutic effect(82.4%)of the control group was lower than that of the study group(96.1%)(P<0.05).The incidence of adverse reactions to drugs in the study group(3.8%)was lower than that in the control group(21.5%)(P<0.05).Conclusion:joint take omeprazole amoxicillin treatment of periodontal disease patients achieved ideal therapeutic efficacy.展开更多
Objective:To investigate the clinical efficacy and safety of Banxia Xiexin decoction and omeprazole in the treatment of gastroesophageal reflux disease(GERD).Methods:EMbase,Cochrane,PubMed,CNKI,Wan Fang and VIP databa...Objective:To investigate the clinical efficacy and safety of Banxia Xiexin decoction and omeprazole in the treatment of gastroesophageal reflux disease(GERD).Methods:EMbase,Cochrane,PubMed,CNKI,Wan Fang and VIP database were searched from inception to November 2018 according to the search strategy.Eligible randomized controlled clinical trials related to the efficacy of omeprazole compared with Banxia Xiexin decoction in the treatment of GERD were included according to the inclusion and exclusion criteria.Total effective rate,pathological improvement rate,total symptom score,acid reflux symptoms,heartburn symptoms,improvement of post-sternal pain symptoms,and incidence of adverse reactions were evaluated.Data analysis was performed with RevMan5.3 software provided by Cochrane Collaboration.Results:A total of 15 studies were enrolled,including 1,532 patients.Meta-analysis results showed that the total effective rate of Banxia Xiexinfang was higher than that of omeprazole in the treatment of GERD(odds ratio(OR)=3.99,95%confidence intervals(CI)(2.58,6.15),P<0.00001).Pathological improvement under endoscopy was not obvious(OR=1.98,95%CI(0.94,4.19),P=0.07)between the two groups.The total symptom score improved significantly,indicating that Banxia Xiexin decoction has an objective advantage over omeprazole in the treatment of GERD(standardised mean difference(SMD)=?2.56,95%CI(?3.86,?1.26),P=0.0001),The incidence of adverse reactions in patients treated with Banxia Xiexin decoction is lower than omeprazole group(OR=0.09,95%CI(0.02,0.39),P=0.001].In addition,total effective rate of Banxia Xiexin decoction combined with omeprazole was higher than omeprazole alone(OR=6.31,95%CI(2.86,13.92),P<0.00001).Conclusion:Banxia Xiexin decoction is superior to omeprazole in total effective rate,total symptom score and adverse reaction rate in the treatment of GERD.The clinical efficacy of Banxia Xiexin decoction combined with omeprazole is better than that of omeprazole alone.However,due to the low quality of the included literatures,large-scale and high-quality RCTs are still needed for further confirmation.展开更多
基金supported by National Natural Science Foundation of China(No.82200607)Guangdong Basic and Applied Basic Research Foundation(Nos.2020A1515110109,2021A1515012194,2023A1515030064)+3 种基金Basic and Applied Research Project of Guangzhou Municipal Science and Technology Project(No.202201020631)Guangzhou Medical Key Disciplines and Specialties(No.011006003)Guangzhou Key Laboratory of Pediatric Inflammatory Bowel Disease(No.2023A03J0866)National Health Commission Key Laboratory of Tropical Disease Prevention and Control(2022NHCTDCKFKT21001).
文摘Helicobacter pylori is a risk factor for the development of peptic ulcers with autophagy dysfunction.Omeprazole was widely known as the first-line regimen for H.pylori-associated gastritis.Objectives:The objective of this work was to assess the role of omeprazole on cell pyroptosis and autophagy.Methods:The clinical samples were collected.Quantitative polymerase chain reaction,western blotting,enzyme linked immunosorbent assay,and immunofluorescence(IF)analysis were conducted to reveal the mechanism of omeprazole on cell pyroptosis and autophagy.Results:The results revealed that omeprazole could decrease cell pyroptosis,which was attributed to the downregulation of cleaved caspase-1 expression,resulting in the inhibition of gasdermin E and interleukin-18/1βmaturation and secretion as well as the resolution of inflammation.Mechanistically,omeprazole treatment led to drastic downregulation of mammalian target of rapamycin(mTOR)activity was observed in BGC823 cells,leading to enhanced autophagy characterized by increased LC3II expression,which further reduced cell pyroptosis.This omeprazole-mediated phenomenon was enhanced after phosphodiesterase-4(PDE4)inhibitor dipyridamole(DIP)treatment.In addition,activation of mTOR by MHY1485 could rescue the suppression of cell pyroptosis induced by omeprazole.Most importantly,IF analysis suggested that phosphorylation of mTOR and PDE4 activity and caspase-1 were enhanced in H.pylori-infected gastric mucosa.Conclusion:These findings indicate that omeprazole suppresses cell pyroptosis through PDE4-mediated autophagy in gastric epithelial cells,and DIP enhanced the omeprazole-mediated inhibition of cell pyroptosis,implying that DIP is an alternative combined therapy strategy in improving the treatment of patients with H.pylori infection.
文摘Objective:To investigate the therapeutic effect of omeprazole+amoxicillin in patients with gastric ulcers.Methods:62 cases of patients with gastric ulcers who were treated from January 2022 to December 2022 were recruited and randomly divided into groups.Omeprazole+amoxicillin treatment was included in the study group,and amoxicillin treatment was included in the control group.The score of gastric ulcer symptoms,time of symptom resolution,gastrointestinal hormone index,and adverse reactions were compared.Results:The gastric ulcer symptom scores in the study group were lower than those in the control group(P<0.05);the gastric ulcer symptoms and Helicobacter pylori-negative time in the study group were shorter than those in the control group(P<0.05);the gastrointestinal hormone indexes in the study group were better than those in the control group(P<0.05);the adverse reaction rate of gastric ulcer in the study group was lower than that in the control group(P<0.05).Conclusion:Omeprazole+amoxicillin in the treatment of gastric ulcers can regulate gastrointestinal hormones,relieve gastric ulcer symptoms,and shorten the duration of ulcers,which is highly effective and feasible.
文摘AIM: To clarify whether there is any difference in the symptom relief in patients with reflux esophagitis following the administration of four Proton pump inhibitors (PPIs). METHODS: Two hundred and seventy-four patients with erosive reflux esophagitis were randomized to receive 8 wk of 20 mg omeprazole (n = 68), 30 mg of lansoprazole (n = 69), 40 mg of pantoprazole (n = 69), 40 mg of esomeprazole (n = 68) once a day in the morning. Daily changes in heartburn and acid reflux symptoms in the first 7 d of administration were assessed using a six-point scale (0: none; 1: mild; 2: mild-moderate; 3: moderate; 4: moderate-severe; 5: severe). RESULTS: The mean heartburn score in patients treated with esomeprazole more rapidly decreased than those receiving other PPI. Complete resolution of heartburn was also more rapid in patients treated with esomeprazole for 5 d compared with omeprazole (P = 0.0018, P = 0.0098, P = 0.0027, P = 0.0137, P = 0.0069, respectively), lansoprazole (P = 0.0020, P = 0.0046, P = 0.0037, P = 0.0016, P = 0.0076, respectively), and pantoprazole (P = 0.0006, P = 0.0005, P = 0.0009, P = 0.0031, P = 0.0119, respectively). There were no significant differences between the four groups in the rate of endoscopic healing of reflux esophagitis at week 8. CONCLUSION: Esomeprazole may be more effective than omeprazole, lansoprazole, and pantoprazole for the rapid relief of heartburn symptoms and acid reflux symptoms in patients with reflux esophagitis.
基金Supported by the National Science Foundation (OTKA Grant No:T 034345)
文摘AIM： To study the effect of proton pump inhibitor （PPI） treatment on patients with reflux esophagitis and its in vivo effect on apoptosis, p53- and epidermal growth factor receptor （EGFR） expression. METHODS： After informed consent was obtained, gastric biopsies of the antrum were taken from patients with reflux oesophagitis prior to and after 6 mo of 20 mg omeprazole （n = 24） or 40 mg esomeprazole （n = 22） therapy. Patients did not take any other medications known to affect the gastric mucosa. All patients were Helicobacter pylori negative as confirmed by rapid urease test and histology, respectively. Cell proliferation, apoptosis, EGFR, and p53 expression were measured by immunohistochemical techniques. At least 600 glandular epithelial cells were encountered and results were expressed as percentage of total cells counted. Was considered statistically significant. RESULTS： Although there was a trend towards increase of cell proliferation and EGFR expression both in omeprazole and esomeprazole treated group, the difference was not statistically significant. Neither apoptosis nor p53 expression was affected. CONCLUSION： Long-term PPI treatment does not significantly increase gastric epithelial cell proliferation and EGFR expression and has no effect on apoptosis and p53 expression.
基金Supported by Universiti Kebangsaan Malaysia Research Fund,No.UKM-DLP-066-2011 and No.FF-032-2012
文摘AIM To investigate and compare the effects of tocotrienol and omeprazole on gastric growth factors in rats exposed to water-immersion restraint stress(WIRS).METHODS Twenty-eight male Wistar rats were randomly assigned to four groups of seven rats. The two control groups were administered vitamin-free palm oil(vehicle) and the two treatment groups were given omeprazole(20 mg/kg) or tocotrienol(60 mg/kg) by oral gavage. After 28 d of treatment, rats from one control group and both treated groups were subjected to WIRS one time for 3.5 h. Gastric lesions were measured and gastric tissues were obtained to measure vascular endothelial growth factor(VEGF), epidermal growth factor(EGF), basic fibroblast growth factor(b FGF), and transforming growth factor-alpha(TGF-α) m RNA expression. RESULTS Rats exposed to WIRS for 3.5 h demonstrated the presence of considerable ulcers in the form of gastric erosion. The lesion index in the stressed control(S) group was increased(P < 0.001) compared to the tocotrienol treated and omeprazole treated groups. Stress led to a decrease in gastric VEGF(P < 0.001), b FGF(P < 0.001) and TGF-α(P < 0.001) m RNA levels and caused an increase in EGF m RNA(P < 0.001) that was statistically significant compared to the nonstressed control group. Although both treatment agents exerted similar ulcer reducing ability, only treatment with tocotrienol led to increased expression of VEGF(P = 0.008), b FGF(P = 0.001) and TGF-α(P = 0.002) m RNA.CONCLUSION Tocotrienol provides gastroprotective effects in WIRSinduced ulcers. Compared to omeprazole, tocotrienol exerts a similar protective effect, albeit through multiple mechanisms of protection, particularly through up-regulation of growth factors that assist in repair of gastric tissue injuries.
基金a research grant from the University of Delhi, No. 52301/01Glaxo Smithkline Pharmaceuticals Limited and Dr. Reddy's Laboratories Ltd, No. 9834512
文摘AIM： To study the effect of combined omeprazole（Ome） and domperidone（Dom） therapy on asthma symptoms and pulmonary function in asthmatics with gastroesoph- ageal reflux. METHODS： We selected 198 asthmatics with gastro- esophageal reflux diagnosed by 24-h esophageal pH moni- toring to receive Ome 20 mg twice daily and Dom 10 mg three times daily or placebo for 16 wk （1：1 double-blind randomization）. Spirometry was done at baseline and after 16 wk of treatment. The primary outcome measures were： mean daily daytime and nighttime asthma symptom scores. Mean daily reflux symptom scores, albuterol use as rescue medication （number of puffs）, daytime and nighttime peak expiratory flow rate （PEFR）, postbronchodilator forced expiratory volume in 1 second （FEVl） and postbronchodilator forced vital capacity （FVC） were secondary outcome measures. RESULTS： Comparison of mean change from baseline between antireflux therapy and placebo groups revealed significant reduction in daytime asthma symptom score （17.4% vs 8.9 %）, nighttime asthma symptom score （19.6% vs 5.4%）, reflux symptom score （8.7% vs 1.6%） and rescue medication use （23.2% vs 3.1%） after antireflux therapy compared to mean change in placebo group （P 〈 0.001）. There was significant improvement in morning PEFR （7.9% vs 0.2%）, evening PEFR （9.8% vs 0.5%）, FEW （11.1% vs 3.78%） and FVC （9.3%vs 1.52%） in the antireflux therapy group compared to placebo on comparng the mean change from baseline after 16 wk （P 〈 0.01） CONCLUSION： Combined therapy with Ome and Dom in adult asthmatics with gastroesophageal reflux may be beneficial by reducing asthma symptoms, rescuing medi- cation use, and improving pulmonary function.
文摘AIM： To evaluate the omeprazole maintenance therapy in patients with recurrent ulcer bleeding after surgery for duodenal ulcer. METHODS： We studied 15 consecutive patients with recurrent ulcer bleeding after surgery for duodenal ulcer. Omeprazole （20 mg/d） maintenance therapy was given after ulcer healing. In addition to clinical follow-up, ambulatory 24-h gastric pH assay was performed before and during omeprazole therapy in those patients and controls with previous duodenal ulcer surgery but no ulcer recurrence. RESULTS： All the 15 ulcers were healed after being treated with omeprazole （40 mg/d） for 2 too. Eleven patients with two （1-9） episodes of recurrent ulcer bleeding completed the follow-up （43, 12-72 too）. None of them had a bleeding episode while on omeprazole. One patient discontinued the therapy and had recurrent bleeding. The median 24-h fraction time of gastric pH 〈4 in patients was 80, 46-95%, and was reduced to 32, 13-70% by omeprazole （P= 0.002）. CONCLUSION： Long-term maintenance therapy with omeprazole （20 rag/day） is effective in preventing recurrent ulcer bleeding.
文摘AIM To explore the effects of omeprazole on chemoradiotherapy efficacy and tumor recurrence in rectal cancer. METHODS The medical data of 125 rectal cancer patients who received the same neoadjuvant chemoradiotherapy(CRT) followed by surgery were retrospectively collected. Patients who received omeprazole(OME) orally at a dose of 20 mg at least once daily for six days and/or intravenously at 40 mg a day were recognized as eligible OME users(EOU). Otherwise, patients were regarded as non-eligible OME users(non-EOU).Moreover, a preferred OME dose cut-off of 200 mg on tumor recurrence was obtained by receiver operating characteristic(ROC) curves. Patients were divided into two groups: the effective OME group(EOG, OME ≥ 200 mg) and the non-effective OME group(non-EOG, OME < 200 mg). RESULTS The good response rate of CRT efficacy(50.8%) in EOU was significantly increased compared with nonEOU(30.6%)(P = 0.02). The recurrence rate in the EOG was 10.3%, which was significantly lower compared with 31.3% in non-EOG(P = 0.025). The good response rate of CRT efficacy in EOG was 55.2%, which was obviously higher compared with 36.5% in non-EOG, with a significant difference(P = 0.072). Multivariate Cox analysis demonstrated that OME(nonEOG and EOG) was an independent and significant impact factor for DFS(P = 0.048, HR = 0.30, 95%CI: 0.09-0.99).CONCLUSION When applied as an adjuvant drug in cancer treatment for relieving common side effects of chemotherapy, omeprazole has a synergetic effect in improving CRT efficacy and decreasing rectal cancer recurrence.
基金Supported by the Scientific Research Foundation for Foreign- Returned Chinese Scholars, State Education Ministry, China
文摘AIM: One-week triple therapy with proton pump inhibitors, clarithromycin and amoxicillin has recently been proposed as the first-line treatment for Helicobacter pylori (H pylori) infection; however, data regarding the effects of this regimen in China are scarce. The aim of this prospective and randomized study was to compare the efficacy of clarithromycin and metronidazole when they were combined with omeprazole and amoxicillin on eradication of H pylori and ulcer healing in Chinese peptic ulcer patients. METHODS: A total of 103 subjects with Hpylori-positive peptic ulcer were randomly divided into two groups, and accepted triple therapy with omeprazole 20 mg, amoxicillin 1 000 mg and either clarithromycin 500 mg (OAC group, n = 58) or metronidazole 400 mg (0AM group, n - 45). All drugs were given twice daily for 7 d. Patients with active peptic ulcer were treated with omeprazole 20 mg daily for 2-4 wk after anti-H pylori therapy. Six to eight weeks after omeprazole therapy, all patients underwent endoscopies and four biopsies (two from the antrum and two others from the corpus of stomach) were taken for rapid urease test and histological analysis (with modified Giemsa staining) to examine H pylori. Successful eradication was defined as negative results from both examination methods. RESULTS: One hundred patients completed the entire course of therapy and returned for follow-up. The eradication rate of H pylori for the per-protocol analysis was 89.3% (50/56) in OAC group and 84.1% (37/44) in 0AM group. Based on the intention-to-treat analysis, the eradication rate of H pylori was 86.2% (50/58) in OAC group and 82.2% (37/45) in 0AM group. There were no significant differences in eradication rates between the two groups on either analysis. The active ulcer-healing rate was 96.7% (29/30) in OAC group and 100% (21/21) in 0AM group (per-protocol analysis, P>0.05). Six patients in OAC group (10.3%) and five in OAM group (11.1%) reported adverse events (P>0.05). CONCLUSION: One-week triple therapy with omeprazole and amoxicillin in combination with either clarithromycin or metronidazole is effective for the eradication of H pylori. The therapeutic regimen comprising metronidazole with low cost, good compliance and mild adverse events may offer a good choice for the treatment of peptic ulcers associated with H pylori infection in China.
基金supported by Medical Scientific Research of Health Department of Hebei Province(No 02199)
文摘Objective:To observe the protective effect of omeprazole on gastric mucosal of cirrhotic portal hypertension rats.Methods:All rats were randomly divided into normal control group,cirrhosis and treatment group.Thioacetamide was used to establish rat model of cirrhotic portal hypertension.The necrotic tissue of gastric mucosa ulcer focus,degree of neutrophils infiltration at the ulcer margin,portal pressure,portal venous flow,abdominal aortic pressure,abdominal aortic blood flow at front end,gastric mucosal blood flow（GMBF）,glycoprotein（GP）of gastric mucosa,basal acid secretion,H’ back-diffusion,gastric mucosal damage index,NO,prostaglandin E2（PGE2） and tumor necrosis factor-α（TNF-α） were determined respectively,and the pathological changes of gastric mucosa were also observed by microscope.Results:Compared with cirrhosis group and the control group,the ulcer bottom necrotic material,gastric neutrophil infiltration and UI of the treatment group were all decreased significantly（P【0.01）,GMBF value,GP values,serum NO,PGE2,TNF- a were all significantly increased.Conclusions:Omeprazole has an important protective effect on gastric mucosal and it can increase gastric mucosal blood flow and related to many factors.
基金supported by National Key Technology R&D Program in the "Twelfth Five-Year" Plan of China(2011BAI11B07)
文摘Background: This study evaluated the effect of omeprazole or pantoprazole on platelet reactivity in non-STsegment elevation acute coronary syndrome(NSTE-ACS) patients receiving clopidogrel.Methods: Consecutive patients with NSTE-ACS(n =620) from general hospital of Shenyang Military Command were randomized to the omeprazole or pantoprazole(20mg/d) group(1:1), and received routine dual antiplatelet treatment. Patients' reversion rate of adenosine diphosphate-induced platelet aggregation(ADP-PA) was assessed at baseline, 12 to 24 h after administration of medication, and after 72 h of percutaneous coronary intervention(PCI). The primary endpoint of the study was platelet reactivity assessed with ADP-PA at 30 days after PCI. Adverse events(AEs) were recorded for 30-day and 180-day follow-up periods.Results: There were no significant differences between both the groups in platelet response to clopidogrel at 12–24h after drug administration(54.09%±18.90% vs. 51.62%±19.85%, P=0.12), 72 h after PCI(52.15%±19.45% vs. 49.66%±20.05%, P=0.18), and 30 days after PCI(50.44%±14.54% vs. 48.52%±15.08%, P=0.17). The rate of AEs did not differ significantly between groups during the 30-day(15.2% vs. 14.8%, P=0.91) and 180-day(16.5% vs. 14.5%, P=0.50) follow-up periods after PCI.Conclusion: The addition of omeprazole or pantoprazole to clopidogrel did not restrict the effect of platelet aggregation by reducing the conversion of clopidogrel. Compared with clopidogrel alone, pantoprazole-clopidogrel and omeprazoleclopidogrel combinations did not increase the incidence of adverse clinical events during 30-day and 180-day follow-up periods after PCI.
基金funding from the European Community's Seventh Framework Programme under the grant agreement 602051 (Project HERACLES: Humancystic Echinococcosis Rese Arch in Centra L and Eastern Societies http://www.Heracles-fp7.eu/)
文摘Recent reports have demonstrated that the new commercially available immobilized-type chiral stationary phases（CSPs） containing amylose tris（3-chloro-5-methylphenylcarbamate）（ACMPC） as a selector exhibit not only an exceptionally high enantioselectivity in high-performance liquid chromatography（HPLC） but they are also applicable to a wide range of chiral analytes. Herein, we report the results obtained in the HPLC analysis of omeprazole and its impurities B and E on the ACMPC-based Chiralpak IG-3 CSP（CSP） under polar organic conditions. A systematic evaluation of the retention characteristics of the selected benzimidazole chiral probes was carried out by changing the composition of the mobile phase and the column temperature. It is worth emphasizing that the high affinity of both enantiomers of all analytes recorded in pure methanol mode dramatically decreased incorporating small volumes of either basic or acid additives in the mobile phase. Unspecified sites of the IG-3 CSP presumably involved in strong and non-stereoselective H-bonding contacts with chiral analytes are assumed responsible for the unproductive retention process.
文摘AIM： To compare the effect of intravenous and oral omeprazole in patients with bleeding peptic ulcers without high-risk stigmata.METHODS： This randomized study included 211 patients [112 receiving iv omeprazole protocol （Group 1）, 99 receiving po omeprazole 40 mg every 12 h （Group 2）] with a mean age of 52.7. In 144 patients the ulcers showed a clean base, and in 46 the ulcers showed fiat spots and in 21 old adherent clots. The endpoints were re-bleeding, surgery, hospital stay, blood transfusion and death. After discharge, re-bleeding and death were reevaluated within 30 d.RESULTS： The study groups were similar with respect to baseline characteristics. Re-bleeding was recorded in 5 patients of Group 1 and in 4 patients of Group 2 （P = 0.879）. Three patients in Group 1 and 2 in Group 2 underwent surgery （P = 0.773）. The mean length of hospital stay was 4.6 ± 1.6 d in Group 1 vs 4.5 ± 2.6 d in Group 2 （P = 0.710）; the mean amounts of blood transfusion were 1.9 ±1.1 units in Group 1 vs 2.1 ±1.7 units in Group 2 （P = 0.350）. Four patients, two in each group died （P = 0.981）. After discharge, a new bleeding occurred in 2 patients of Group 1 and in 1 patient of Group 2, and one patient from Group 1 died.CONCLUSION： We demonstrate that the effect of oral omeprazole is as effective as intravenous therapy in terms of re-bleeding, surgery, transfusion requirements, hospitalization and mortality in patients with bleeding ulcers with low risk stigmata. These patients can be treated effectively with oral omeprazole.
文摘A randomized, two-way, crossover study was conducted in 18 fasting, healthy, algerian volunteers to compare the bioavailability of two brands of Omeprazole 20 mg Gastro-Resistant Capsules where MOPRAL （Astra Zeneca） was the reference product. The study was performed at the bioequivalence center of the national control laboratory for pharmaceuticals product. The drug was administered on two treatment days separated by one week washout period. After dosing, serial blood samples were collected for a period of 12 h. A reliable and robust LC-MS/MS （liquid chromatography-tandem mass spectrometry） method has been developed and validated for the estimation of Omeprazole in human plasma. The assay was found to be linear over the range of 5-1,000 ng/mL. The pharmacokinetical and statistical analysis was conducted with Kinetica 4.4.1. AUC0.t, AUC0-∞ and Cmax were tested for bioequivalence. No significant difference was found based on ANOVA; 90% confidence interval （[97.14%-117..85%] for AUC0.t, [97.17%-117.67%] for AUC0-∞） of test/reference ratio for these parameters were found within bioequivalence acceptance range of 80%-125%. But for the Cmax, it was not in this acceptance range [73,5%-100.54%]. The results of PK analysis suggested that the reference and test formulations of Omeprazole 20 mg Gastro-Resistant Capsules were not bioequivalent during fasting state in these healthy Algerian volunteers.
基金Supported by the National Natural Science Foundation of China(21776203 and 21576187)the Tianjin Municipal Natural Science Foundation(18JCYBJC21100)
文摘Omeprazole sodium(OMS), a typical non-hydrogen bond donors API, is only available in solvates so far, including monohydrate, ethanol solvate and methanol solvate. The methanol solvate was found for the first time. Solvate transformation thermodynamics of OMS was studied in this paper. First, the ternary phase diagrams forming two solvates for OMS in binary solvent mixtures including methanol + water, ethanol + water, and methanol+ ethanol were measured at temperature ranging of T =(278.15 to 313.15) K under atmospheric pressure. Further, the standard equilibrium constants of the solvate transformation reactions were evaluated according to the chemical reaction isothermal equation. The standard molar Gibbs free energy, the standard molar enthalpy, and the standard molar entropy of solvate transformation reactions were then calculated based on van't Hoff equation. Moreover, the thermodynamic stability of the OMS solvate was analyzed based on phase diagram. The results are of great importance to develop a crystallization process for manufacturing OMS solvate, and could be helpful to other solvate transformation research.
文摘Omeprazole is a potent proton pump inhibitor with powerful inhibition of secretion of gastric juice. Oral site-specific drug delivery systems have recently attracted a great interest for the local treatment of bowel disease and for improving systemic absorption of drugs which are unstable in the stomach. However, microenvironment in the gastrointestinal tract and varying absorption mechanisms cause hindrance for the formulation and optimization of oral drug delivery. The objective of the study was to develop and optimize enteric coating process for omeprazole tablets. Different batches of core tablets were sub coated, one set sub coated with opadry and another with a mixture of light magnesium oxide, magnesium stearate and absolute alcohol omeprazole magnesium. Seal coating was applied by using opadry to achieve certain weight gain and to protect omeprazole from acidic coating polymers. A comparative dissolution test was performed. The variation of thickness and diameter were observed to be minimal with a weight gain of 3% - 4% of enteric polymer. Disintegration test showed that in each tested batch the enteric coated layer remained intact in 0.1N HCl for 2 hours and when exposed to alkaline media of phosphate buffer pH 6.8, it dissolved within few minutes. Dissolution release was 98.8% to 102.4% within two hours when the product was exposed to phosphate buffer pH 6.8 after 2 hours. The similarity and dis-similarity factors were calculated and observed to be 54 to 61 and 4 to 5 respectively. Therefore a simple and good enteric coating process was developed and tested with potential for transfer this technology into local pharmaceutical industries using cheap and easily available materials.
文摘Objective:To investigate the effect of somatostatin combined with omeprazole on serum inflammatory factors and intestinal mucosal barrier function in severe acute pancreatitis. Methods: patients with severe acute pancreatitis who were treated in Zigong Third People's Hospital between August 2014 and December 2017 were chosen and divided into two groups by random number table method. Control group received conventional + omeprazole treatment, combined group received conventional + somatostatin + omeprazole treatment and the treatment lasted for 1 week. The differences in serum levels of inflammatory factors, chemokines and intestinal mucosal barrier function indexes were compared between the two groups immediately after admission and after 1 week of treatment.Results: After 1 week of treatment, serum IL-1β, IL-8, IL-18, hs-CRP, MCP-1, FKN, CINC, D-Lactate, DAO, Endotoxin and FABP levels of both groups significantly decreased and serum IL-1β, IL-8, IL-18, hs-CRP, MCP-1, FKN, CINC, D-Lactate, DAO, Endotoxin and FABP levels of combined group were significantly lower than those of control group.Conclusion: Somatostatin combined with omeprazole therapy for severe acute pancreatitis can effectively alleviate the inflammatory response and protect the intestinal mucosal barrier function.
文摘Objective:To investigate the TNF-α、IL-6、IL-1βeffect of omeprazole combined with amoxicillin on cytokines in gingival crevicular fluid of patients with periodontal disease.Methods:102 patients with periodontal disease who were treated in our hospital from June 2016 to March 2018 were selected.Randomly divided into two groups,the control group was treated with omeprazole alone,and the research group was treated with omeprazole combined with amoxicillin.The levels of inflammatory cytokines(TNF-α、IL-6、IL-1β),therapeutic effects and adverse reactions to drugs were compared between the two groups.Results:the levels of inflammatory factors(TNF-α、IL-6、IL-1β)in the study group were lower than those in the control group(P<0.05).The therapeutic effect(82.4%)of the control group was lower than that of the study group(96.1%)(P<0.05).The incidence of adverse reactions to drugs in the study group(3.8%)was lower than that in the control group(21.5%)(P<0.05).Conclusion:joint take omeprazole amoxicillin treatment of periodontal disease patients achieved ideal therapeutic efficacy.
文摘Objective:To investigate the clinical efficacy and safety of Banxia Xiexin decoction and omeprazole in the treatment of gastroesophageal reflux disease(GERD).Methods:EMbase,Cochrane,PubMed,CNKI,Wan Fang and VIP database were searched from inception to November 2018 according to the search strategy.Eligible randomized controlled clinical trials related to the efficacy of omeprazole compared with Banxia Xiexin decoction in the treatment of GERD were included according to the inclusion and exclusion criteria.Total effective rate,pathological improvement rate,total symptom score,acid reflux symptoms,heartburn symptoms,improvement of post-sternal pain symptoms,and incidence of adverse reactions were evaluated.Data analysis was performed with RevMan5.3 software provided by Cochrane Collaboration.Results:A total of 15 studies were enrolled,including 1,532 patients.Meta-analysis results showed that the total effective rate of Banxia Xiexinfang was higher than that of omeprazole in the treatment of GERD(odds ratio(OR)=3.99,95%confidence intervals(CI)(2.58,6.15),P<0.00001).Pathological improvement under endoscopy was not obvious(OR=1.98,95%CI(0.94,4.19),P=0.07)between the two groups.The total symptom score improved significantly,indicating that Banxia Xiexin decoction has an objective advantage over omeprazole in the treatment of GERD(standardised mean difference(SMD)=?2.56,95%CI(?3.86,?1.26),P=0.0001),The incidence of adverse reactions in patients treated with Banxia Xiexin decoction is lower than omeprazole group(OR=0.09,95%CI(0.02,0.39),P=0.001].In addition,total effective rate of Banxia Xiexin decoction combined with omeprazole was higher than omeprazole alone(OR=6.31,95%CI(2.86,13.92),P<0.00001).Conclusion:Banxia Xiexin decoction is superior to omeprazole in total effective rate,total symptom score and adverse reaction rate in the treatment of GERD.The clinical efficacy of Banxia Xiexin decoction combined with omeprazole is better than that of omeprazole alone.However,due to the low quality of the included literatures,large-scale and high-quality RCTs are still needed for further confirmation.
