Aims: A simple and highly sensitive LC-MS method was used to determine the concentrations of losartan, its major active metabolite E3174 and hydrochlorothiazide in human plasma and pharmacokinetic characteristics and ...Aims: A simple and highly sensitive LC-MS method was used to determine the concentrations of losartan, its major active metabolite E3174 and hydrochlorothiazide in human plasma and pharmacokinetic characteristics and metabolism phenotype observation after administration of losartan tablets and losartan/hydrochlorothiazide combination tablets. Methods: An open, randomized cross-over single-dose study was designed in forty healthy male volunteers, A single-dose of 50 mg losartan tablets or 50 mg losartan/12.5 mg hydrochlorothiazide combination tablets was orally given and blood samples were collected at scheduled time. A LC-MS method was established and evaluated for determining the plasma concentrations of losartan, E3174 and hydrochlorothiazide. The pharmacokinetic parameters and characteristic of metabolism phenotypes were calculated and compared via this test. Results: The elimination rate of E3174 (t1/2) was significantly shorter (P 0–t was lower (P 1/2, AUC0–t and AUC0–inf of E3174.展开更多
A sensitive and reproducible liquid chromatography-electrospray ionization-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the quantification of amlodipine in human plasma, with gliclazide a...A sensitive and reproducible liquid chromatography-electrospray ionization-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the quantification of amlodipine in human plasma, with gliclazide as an internal standard (IS). The analyte was extracted with ethyl acetate and analyzed on a Diamond C18 (150 mm× 4.6 mm, 5 μm) column. The mobile phase was composed of methanol ?10 mM ammonium acetate with gradient flow rates and gradient conditions. Amlodipine and IS were ionized by positive ion pneumatically assisted electrospray and detected in the multi-reaction monitoring (MRM) mode using precursor→productions of m/z 409.2→238.1, 294.1 and m/z 324.2→127.3, respectively. The specificity, matrix effect, recovery, sensitivity, linearity, accuracy, precision, and stabilities were all validated over the concentration range of 0.05 - 12 ng/mL. The 90% confidence interval (CI) for AUC0-t, AUC0-∞ and Cmax ratios (test: reference) were all within 80% - 125% interval proposed by FDA. It is concluded that the validated method can successfully fulfill the requirement of clinical bioequivalence study of amlodipine in healthy Chinese subjects after administration of amlodipine/losartan combination tablets and amlodipine tablets, and the test and reference tablets were bioequivalent.展开更多
The objectives of this study are to conduct a comprehensive literature search and bibliometric analysis to identify the breadth and volume of pharmacological and clinical studies on pine pollen(Pinus pollen)and to ide...The objectives of this study are to conduct a comprehensive literature search and bibliometric analysis to identify the breadth and volume of pharmacological and clinical studies on pine pollen(Pinus pollen)and to identify the potential effects and the use of pine pollen.Three Chinese electronic databases and two English electronic databases were searched for pharmacological and clinical studies on pine pollen.Data were extracted and analyzed and included publication year,authors,study type,pharmacological research topics or clinical diseases/conditions,usage and type of preparation,authors’conclusions,and adverse effects.Of 239 publications identified,180 were pharmacological studies,37 were clinical trials,and 22 were reviews.Numbers of publications increased particularly from 2004 onward.The top 10 most frequent topics in pharmacological studies were immune regulation,antisenility,antioxidation,liver protection,inhibiting prostate hyperplasia,inhibiting tumor cell proliferation,lowering blood glucose,lowering blood lipids,antifatigue,and improving intestinal function.The top 10 most frequent clinical diseases treated or where pine pollen was used as an adjuvant were bedsores,diaper dermatitis,hyperlipidemia,oral mucositis,eczema,hyperplasia of prostate,hypertension,prostatitis,type 2 diabetes mellitus,and radiodermatitis.Eight trials reported no adverse events associated with pine pollen,one reported mild gastrointestinal reactions,but symptoms disappeared without special management.There have been an increasing number of publications on pine pollen during the past 20 years.Pharmacological studies have shown many potential benefits,and clinical studies have indicated some positive effects when it is either used as a single herb or as an adjuvant to treat disease.Its use as a topical agent,especially for skin diseases,was notable.展开更多
文摘Aims: A simple and highly sensitive LC-MS method was used to determine the concentrations of losartan, its major active metabolite E3174 and hydrochlorothiazide in human plasma and pharmacokinetic characteristics and metabolism phenotype observation after administration of losartan tablets and losartan/hydrochlorothiazide combination tablets. Methods: An open, randomized cross-over single-dose study was designed in forty healthy male volunteers, A single-dose of 50 mg losartan tablets or 50 mg losartan/12.5 mg hydrochlorothiazide combination tablets was orally given and blood samples were collected at scheduled time. A LC-MS method was established and evaluated for determining the plasma concentrations of losartan, E3174 and hydrochlorothiazide. The pharmacokinetic parameters and characteristic of metabolism phenotypes were calculated and compared via this test. Results: The elimination rate of E3174 (t1/2) was significantly shorter (P 0–t was lower (P 1/2, AUC0–t and AUC0–inf of E3174.
文摘A sensitive and reproducible liquid chromatography-electrospray ionization-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the quantification of amlodipine in human plasma, with gliclazide as an internal standard (IS). The analyte was extracted with ethyl acetate and analyzed on a Diamond C18 (150 mm× 4.6 mm, 5 μm) column. The mobile phase was composed of methanol ?10 mM ammonium acetate with gradient flow rates and gradient conditions. Amlodipine and IS were ionized by positive ion pneumatically assisted electrospray and detected in the multi-reaction monitoring (MRM) mode using precursor→productions of m/z 409.2→238.1, 294.1 and m/z 324.2→127.3, respectively. The specificity, matrix effect, recovery, sensitivity, linearity, accuracy, precision, and stabilities were all validated over the concentration range of 0.05 - 12 ng/mL. The 90% confidence interval (CI) for AUC0-t, AUC0-∞ and Cmax ratios (test: reference) were all within 80% - 125% interval proposed by FDA. It is concluded that the validated method can successfully fulfill the requirement of clinical bioequivalence study of amlodipine in healthy Chinese subjects after administration of amlodipine/losartan combination tablets and amlodipine tablets, and the test and reference tablets were bioequivalent.
基金supported by the fund from Beijing University of Chinese Medicine for the Project on Research and Development of Evidence-Based Medicine of Clinical Scientific Research Capacity and International Development in TCM(No.2016-ZXFZJJ-011,No.1000061020008)partially supported by the NCCIH grant(AT001293 with Sub Award No.020468C)funded by Overseas Expertise Project,Ministry of Education of China(MS20180009)。
文摘The objectives of this study are to conduct a comprehensive literature search and bibliometric analysis to identify the breadth and volume of pharmacological and clinical studies on pine pollen(Pinus pollen)and to identify the potential effects and the use of pine pollen.Three Chinese electronic databases and two English electronic databases were searched for pharmacological and clinical studies on pine pollen.Data were extracted and analyzed and included publication year,authors,study type,pharmacological research topics or clinical diseases/conditions,usage and type of preparation,authors’conclusions,and adverse effects.Of 239 publications identified,180 were pharmacological studies,37 were clinical trials,and 22 were reviews.Numbers of publications increased particularly from 2004 onward.The top 10 most frequent topics in pharmacological studies were immune regulation,antisenility,antioxidation,liver protection,inhibiting prostate hyperplasia,inhibiting tumor cell proliferation,lowering blood glucose,lowering blood lipids,antifatigue,and improving intestinal function.The top 10 most frequent clinical diseases treated or where pine pollen was used as an adjuvant were bedsores,diaper dermatitis,hyperlipidemia,oral mucositis,eczema,hyperplasia of prostate,hypertension,prostatitis,type 2 diabetes mellitus,and radiodermatitis.Eight trials reported no adverse events associated with pine pollen,one reported mild gastrointestinal reactions,but symptoms disappeared without special management.There have been an increasing number of publications on pine pollen during the past 20 years.Pharmacological studies have shown many potential benefits,and clinical studies have indicated some positive effects when it is either used as a single herb or as an adjuvant to treat disease.Its use as a topical agent,especially for skin diseases,was notable.
