Salvia miltiorrhiza Bunge,known as red sage or Danshen,is commonly applied in Chinese herbal therapeutics for various biological effects.In 25-220 C.E.,the earliest Chinese Materia Medica referred to as Shengong’s Cl...Salvia miltiorrhiza Bunge,known as red sage or Danshen,is commonly applied in Chinese herbal therapeutics for various biological effects.In 25-220 C.E.,the earliest Chinese Materia Medica referred to as Shengong’s Classic of Materia Medica(Eastern Han Dynasty of China,200 C.E.)initially documented Salvia miltiorrhiza Bunge.Currently,Salvia miltiorrhiza Bunge is one of the most frequently prescribed traditional Chinese medicines in clinics for antidiabetic,antianxiety,antihypertensive,antidepressant,antilipidemic,antiarrhythmic,and anticancer effects.Undoubtedly,it is best known for improving and promoting blood circulation;thus,its recommendation for use in cardiovascular disorders.Regarding this article,important information was sourced both manually and electronically using patent compendium and databases,including Google Scholar,herbal plant monographs,Hindawi,PubMed,Embase,CNKI,pharmacopoeias,Springer,etc.Well-concise details and discussions on the botany,traditional medicinal uses,chemical constituents-phytochemistry,pharmacokinetics,pharmacology,and toxicology information are presented.In perspective,understanding the comprehensive information of the above-stated fields with regards to Salvia miltiorrhiza Bunge would yield an additional positive knowledge on areas that need urgent attention and identify gaps in research and safety for future consideration.展开更多
Metabolomics is a newly developed discipline following genomics,transcriptomics,and proteomics.It is based on the theory of systems biology,supported by modern spectroscopy analysis technology and is analyzed by the e...Metabolomics is a newly developed discipline following genomics,transcriptomics,and proteomics.It is based on the theory of systems biology,supported by modern spectroscopy analysis technology and is analyzed by the external stimulation of organisms.By analyzing the overall changes of metabolites with low molecular weight in organism after being stimulated by the outside world,we can understand the physiological and pathological state of organism,and finally clarify the essence of biological changes of organism.In recent years,metabolomics has developed rapidly.It has been widely used in early toxicity screening of lead compounds,preclinical toxicity of drugs and toxicity evaluation of clinical drugs.The in-depth interpretation of metabolomics results is also developing.This article reviewed the progress of metabolomics technology and its application in the study of toxicity evaluation of traditional Chinese medicine.展开更多
Objective:Inhibition of tumor angiogenesis has become a new targeted tumor therapy.In this study,we established a micellar carrier with a tumor neovascularization-targeting effect modified by the neovascularization-ta...Objective:Inhibition of tumor angiogenesis has become a new targeted tumor therapy.In this study,we established a micellar carrier with a tumor neovascularization-targeting effect modified by the neovascularization-targeting peptide NGR.Methods:The targeted polymer poly(ethylene glycol)-b-poly(lactide-co-glycolide)(PEG-PLGA)modified with Asn–Gly–Arg(NGR)peptide was prepared and characterized by 1H nuclear magnetic resonance and Fourier-transform infrared spectrometry.NGR-PEG-PLGA was used to construct curcumin(Cur)-loaded micelles by the solvent evaporation method.The physicochemical properties of the micelles were also investigated.Additionally,we evaluated the antitumor efficacy of the polymer micelles(PM)using in vitro cytology experiments and in vivo animal studies.Results:The particle size of Cur-NGR-PM was 139.70±2.51 nm,and the drug-loading capacity was 14.37±0.06%.In vitro cytological evaluation showed that NGR-modified micelles showed higher cellular uptake through receptor-mediated endocytosis pathways than did unmodified micelles,leading to the apoptosis of tumor cells.Then,in vivo antitumor experiments showed that the modified micelles significantly inhibited tumor growth and were safe.Conclusions:NGR-modified micelles significantly optimized the therapeutic efficacy of Cur.This strategy offers a viable avenue for cancer treatment.展开更多
Lianqiao(Forsythia suspensa(Thunb.)Vahl,Abbreviated as“F.suspensa”below)is traditional Chinese medicine in China,widely distributed all over the country and also highly rich in resources.The Northwest Territories is...Lianqiao(Forsythia suspensa(Thunb.)Vahl,Abbreviated as“F.suspensa”below)is traditional Chinese medicine in China,widely distributed all over the country and also highly rich in resources.The Northwest Territories is a genuine producing area.There are many chemical components in F.suspensa,including lignans,phenylethanolic glycosides,flavonoids,C6-C2 natural alcohols and their glycosides,phenolic acids,terpenes and volatile oils.Among them,lignans and phenylethanolic glycosides are the main active components.Based on the review of chemical components or constituents and main pharmacological activities,according to the definition of quality marker,the components of quality marker of F.suspensa were predicted and analyzed from the aspects of plant genetics and chemical composition,traditional efficacy,traditional medicine,new efficacy,blood entering composition,measurable composition,effective composition in different compatibility,and the influence of storage conditions of extract.Further research on its medicinal active ingredients will provide scientific basis for the evaluation of F.suspensa quality.展开更多
Gastrodin(4-hydroxymethylphenyl-β-d-glucopyranoside)is an active ingredient with high content,which is isolated from the rhizome of Gastrodia elata.Gastrodin injections,tablets and capsules are currently the main gas...Gastrodin(4-hydroxymethylphenyl-β-d-glucopyranoside)is an active ingredient with high content,which is isolated from the rhizome of Gastrodia elata.Gastrodin injections,tablets and capsules are currently the main gastrodin-related preparations in clinical practice,and gastrodin injections are the most widely used.This article will summarize pharmacology and adverse reactions of gastrodin to evaluate its safety,effectiveness and quality control.Gastrodin has pharmacological effects on central nervous system(vertigo,headache,insomnia,neurasthenia,convulsions and epilepsy,etc.),cardiovascular system and other diseases(osteoporosis,osteoarthritis and bone injury,etc.),but we still need to pay attention to its clinical adverse reactions(some patients may have dry mouth and nose,dizziness and stomach discomfort).In addition,further research is needed in other fields,such as health products,food,cosmetics,etc.We also need to further develop and explore the new pharmacological effects of gastrodin and expand its medicinal value.展开更多
Baicalein(BE) is one of the main active flavonoids representing the variety of pharmacological effects including anticancer, anti-inflammatory and cardiovascular protective activities, but it's very low solubility...Baicalein(BE) is one of the main active flavonoids representing the variety of pharmacological effects including anticancer, anti-inflammatory and cardiovascular protective activities, but it's very low solubility, dissolution rate and poor oral absorption limit the therapeutic applications. In this work, a nano-cocrystal strategy was successfully applied to improve the dissolution rate and bioavailability of BE. Baicalein-nicotinamide(BE-NCT) nanococrystals were prepared by high pressure homogenization and evaluated both in vitro and in vivo. Physical characterization results including scanning electron microscopy, dynamic light scattering, powder X-ray diffraction and differential scanning calorimetry demonstrated that BE-NCT nano-cocrystals were changed into amorphous state with mean particle size of 251.53 nm. In the dissolution test, the BE-NCT nano-cocrystals performed 2.17-fold and 2.54-fold enhancement than BE coarse powder in FaSSIF-V2 and FaSSGF. Upon oral administration, the integrated AUC0-t of BE-NCT nano-cocrystals(6.02-fold) was significantly higher than BE coarse powder(1-fold), BE-NCT cocrystals(2.87-fold) and BE nanocrystals(3.32-fold). Compared with BE coarse powder, BE-NCT cocrystals and BE nanocrystals, BENCT nano-cocrystals possessed excellent performance both in vitro and in vivo evaluations.Thus, it can be seen that nano-cocrystal is an appropriate novel strategy for improving dissolution rate and bioavailability of poor soluble natural products such as BE.展开更多
Blindness and vision impairment are the most devastating global health problems resulting in a substantial economic and social burden.Delivery of drug to particular parts of the anterior or posterior segment has been ...Blindness and vision impairment are the most devastating global health problems resulting in a substantial economic and social burden.Delivery of drug to particular parts of the anterior or posterior segment has been a major challenge due to various protective barriers and elimination mechanisms associated with the unique anatomical and physiological nature of the ocular system.Drug administration to the eye by conventional delivery systems results in poor ocular bioavailability(<5%).The designing of a novel approach for a safe,simple,and effective ocular drug delivery is a major concern and requires innovative strategies to combat the problem.Over the past decades,several novel approaches involving different strategies have been developed to improve the ocular delivery system.Among these,the ophthalmic in-situ gel has attained a great attention over the past few years.This review discussed and summarized the recent and the promising research progress of in-situ gelling in ocular drug delivery system.展开更多
Diabetic retinopathy is the most common microvascular complication of diabetes mellitus and the primary reason for blindness all over the world,which is a lesion of blood vessels,neurons,and glial cells that constitut...Diabetic retinopathy is the most common microvascular complication of diabetes mellitus and the primary reason for blindness all over the world,which is a lesion of blood vessels,neurons,and glial cells that constitute the complete structure of the retina.Patients may have vision loss and irreversible blindness.With the increase in the number of diabetes mellitus patients and the extension of lifespan,the incidence rate gradually increases.The clinical diagnosis of diabetic retinopathy mainly relies on regular examinations of ocular fundus and subjective patient descriptions,and once diabetic retinopathy is diagnosed,it is difficult to reverse.It is necessary to find the early markers of diabetic retinopathy.In this paper,data collection,data analysis of metabolomics and its research progress in diabetic retinopathy are summarized and prospected.In recent years,metabolomics has made some progress in the discovery of biomarkers,the exploration of pathogenesis,and the evaluation of diabetic retinopathyug efficacy of diabetic retinopathy.However,there are currently few metabolomics studies on the progression of diabetes mellitus to diabetic retinopathy.The determination of diabetic retinopathy-related specific biomarkers also requires data which a large number of animal experiments and clinical trials provide.In addition,despite the rapid development of metabolomics as an emerging discipline,there are still some problems,which need to be further improved in terms of analysis technology,data acquisition and data analysis.In general,there is still a lot of work to be done to apply metabolomics to clinical work.展开更多
Idiopathic pulmonary fibrosis(IPF)is a serious and fatal pulmonary inflammatory disease with an increasing incidenceworldwide.The drugs nintedanib and pirfenidone,are listed as conditionally recommended drugs in the“...Idiopathic pulmonary fibrosis(IPF)is a serious and fatal pulmonary inflammatory disease with an increasing incidenceworldwide.The drugs nintedanib and pirfenidone,are listed as conditionally recommended drugs in the“Evidence-Based Guidelines for the Diagnosis and Treatment of Idiopathic Pulmonary Fibrosis”.However,these two drugs have many adverse reactions in clinical application.Salvianolic acid B(Sal B),a water-soluble component of Salvia miltiorrhiza,could alleviate bleomycin-induced peroxidative stress damage,and prevent or delay the onset of IPF by regulating inflammatory factors and fibrotic cytokines during the disease’s progression.However,Sal B is poorly absorbed orally,and patient compliance is poor when administered intravenously.Therefore,there is an urgent need to find a new non-injection route of drug delivery.In this study,Sal B was used as model drug and l-leucine(LL)as excipient to prepare Sal B dry powder inhaler(Sal B-DPI)by spray drying method.Modern preparation evaluation methods were used to assess the quality of Sal B-DPI.Sal B-DPI is promising for the treatment of IPF,according to studies on pulmonary irritation evaluation,in vivo and in vitro pharmacodynamics,metabolomics,pharmacokinetics,and lung tissue distribution.展开更多
The characteristics of PF are diffuse alveolitis and disruption of alveolar structure leading to pulmonary interstitial fibrosis.At the same time,pulmonary fibrosis reduces lung volume and restricts ventilation,ultima...The characteristics of PF are diffuse alveolitis and disruption of alveolar structure leading to pulmonary interstitial fibrosis.At the same time,pulmonary fibrosis reduces lung volume and restricts ventilation,ultimately leading to hypoxemia and respiratory failure.In clinical guidelines,Nintedanib or Pirfenidone is often used for treatment.However,the two drugs,although they may slow the progression of the disease,cannot stop,or reverse fibrosis and generally result in a variety of toxic side effects.In 184-220 A.D.,it was already recorded in Supplementary Records of Famous Physicians that the function of SMB was to invigorate blood circulation and disperse blood stasis.In modern medical research,the active ingredients of SMB have likewise been found to be used in treatments such as anti-fibrosis,anti-inflammatory,antithrombotic,antioxidant,microcirculatory improvement,and antineoplastic.In this review,a comprehensive search of the former literature on SMB and pulmonary fibers was conducted using databases including PubMed,CNKI,the National Science and Technology Library,Hindawi,Chinese Science and Technology Journal Database,and the Scientific Network Database.Meanwhile,this review presents the mechanisms of the active ingredients in SMB which have anti-pulmonary fibrosis effects through the signal pathways,cytokines,inflammation response,oxidative stress,apoptosis,and matrix metalloproteinases.SMB could offer a direction for therapy for pulmonary fibrosis by identifying the possible active components and exploring the potential mechanisms.Those could provide a reference for further research and application of SMB in the treatment of pulmonary fibrosis.展开更多
Objective: To investigate the effects of fluidized bed granulation with dextrin on moisture sorption and diffusion of Zexie Decoction granules.Methods: The particle characterization was studied by the particle size, s...Objective: To investigate the effects of fluidized bed granulation with dextrin on moisture sorption and diffusion of Zexie Decoction granules.Methods: The particle characterization was studied by the particle size, scanning electron microscopy(SEM), differential scanning calorimetry(DSC), and Fourier transform infrared(FTIR). The moisture sorption isotherm, equilibrium moisture content(EMC), and moisture diffusion coefficients were determined by using the saturated salt solution method.Results: The particle size increased from 6.04 μm(powder) to 1201.47 μm(granule). The glass transition temperature of dextrin, Zexie Decoction powder, and granule was 107.13 °C, 94.82 °C, and 126.25 °C. As the increase of temperature, the initial rate of moisture sorption become higher. Furthermore, the initial rate of moisture sorption of Zexie Decoction granules was lower than those of powders and dextrin. The EMC and moisture diffusion coefficients were reduced significantly after granulation(P < 0.01). Critical relative humidity and diffusion activation energy of granules were higher than powders.Conclusion: Results suggested that fluidized bed granulation with dextrin could reduce the hygroscopicity of the Zexie Decoction extract powders and inhibited moisture diffusion, which is mainly related to the microstructure reorganization by fluidized bed granulation and anti-plasticizing effects of dextrin.展开更多
Salidroside(SAL)is a phenolic substance with high solubility and low permeability,which make it easy to cause the efflux effect of P-glycoprotein and degradation of intestinal flora,resulting in lower bioavailability....Salidroside(SAL)is a phenolic substance with high solubility and low permeability,which make it easy to cause the efflux effect of P-glycoprotein and degradation of intestinal flora,resulting in lower bioavailability.The aim of this study was to develop and optimize a water-in-oil nanoemulsion of SAL(w/o SAL-N)to explore its suitability in oral drug delivery systems.In this work,SAL-N was successfully prepared by water titration method at K_(m)=1 to construct the pseudo-ternary phase diagrams.Physical characterization including the average viscosity,pH,refractive index,particle size,PDI,TEM,DSC,the content of SAL,and stability study were performed.It was evaluated for drug release in vitro and pharmacokinetic studies in vivo.The optimized nanoemulsion formulation consisted of Labrafil M 1944 CS(63%),Span-80/Tween-80/EtOH(27%)and 200 mg·mL^(-1) SAL solution(SAL-SOL)(10%).Low viscosity and suitable pH were expected for the nanoemulsion.The spherical morphology and nanoscale size of SAL-N enhanced the stability of the nanoemulsion system.In vitro drug release showed that SAL-N had a better controlled release property than SAL-SOL at earlier time points.The pharmacokinetic studies exhibited that SAL-N had significantly higher in t_(1/2)(2.11-fold),AUC_(0-48 h)(1.75-fold)and MRT0-48 h(2.63-fold)than SAL-SOL(P<0.01).The w/o SAL-N prepared in this work can be effectively delivered via the oral route.It can be seen w/o nanoemulsion is a strategy for the drug with polyphenols to delay the release,enhance oral absorption and reduce metabolic rate.展开更多
The aim of this paper was to develop a cataplasma matrix that can be applicable to both watersoluble and liposoluble drugs.The gellan gum and konjaku were employed as the scaffold materials of the matrix.With polyacry...The aim of this paper was to develop a cataplasma matrix that can be applicable to both watersoluble and liposoluble drugs.The gellan gum and konjaku were employed as the scaffold materials of the matrix.With polyacrylic acid sodium and oligosaccharides as tacktifier,the formula of the cataplasma matrix was optimized in the orthogonal method as:gellan gum 0.4 g,xanthan gum 0.03 g,konjac glue 0.1 g,glycerin 4 g,Gluco-Adhesive T(GAT)6 g,Gluco-Adhesive E(GAE)6 g,polyacrylic acid sodium 0.22 g,and sorbitol 3 g.The 180°peel strength,the tensile strength and the elongation at break was 3.043 N,0.275 MPa and 91.05%,respectively.Furthermore,the drug-compatibilities of the matrix were investigated with baicalin,berberine and curcumin,which were used as the models of hydrophilic,poor-water-soluble and hydrophobic ingredients.The drug contents could reach 4.12%,2.42%and 3.75%,while the in vitro release rate were measured as,361.79,55.85 and 104.41μg·cm^(-2)·h^(-1)for baicalin,berberine and curcumin,respectively.These results indicated that the obtained matrix had good drug-compatibility and drug-release properties for different ingredients.展开更多
Objective To apply the response surface-central composite design to developing and optimizing the oral fast disintegrating tablets(ODT) formulation for Jiawei Qing'e, a kind of prescription of Chinese herbal medic...Objective To apply the response surface-central composite design to developing and optimizing the oral fast disintegrating tablets(ODT) formulation for Jiawei Qing'e, a kind of prescription of Chinese herbal medicine.Methods The bitterness of Jiawei Qing'e was masked using Eudragit E-100 by solvent evaporation technique.Response surface approach was applied to investigating the interaction of formulation parameters in optimizing the formulation. The independent variables were Eudragit E-100/drug ratio(X1), amount of disintegrants(X2), and the amount of diluents(X3). The disintegration time(Y1), hardness(Y2), and weight variations of the tablets were characterized. Results The models predicted levels of X1=4.63%, X2=5.25%, and X3=34.33%, for the optimal formulation having a hardness of 3.0 kg with the disintegration time of 30 s within experimental region. The observed response of Y1=26.5 s and Y2=3.14 kg reasonably agreed with the predicted response. Conclusion Response surface methodology shows the good predictability and reliability in optimizing the formulation. The optimized ODT of Jiawei Qing'e has acceptable taste, rapid disintegrating ability, and good mechanical strength.展开更多
Objective: A selective and sensitive ultra performance liquid chromatography-tandem mass spectrometry(UPLC-MS/MS) method was employed to study the pharmacokinetics of ginsenoside Re(GRe) in rabbits after vaginal admin...Objective: A selective and sensitive ultra performance liquid chromatography-tandem mass spectrometry(UPLC-MS/MS) method was employed to study the pharmacokinetics of ginsenoside Re(GRe) in rabbits after vaginal administration of Xiaomi suppository to evaluate the systemic exposure of the suppository for the local treatment.Methods: Chromatographic separation was on an ACQUITY UPLC?BEH C18 column, and acetonitrile-0.1%formic acid was used as mobile phase in gradient elution. The plasma samples were deproteinized by acetonitrile, and the pharmacokinetic parameters were calculated by Winnonlin 6.4.Results: Calibration curve of GRe showed a good linearity over the concentration range from 5 ng/mL to500 ng/mL(r = 0.9999). The low limit of quantification of 5 ng/m L could satisfy the experimental requirement. The intra-day and inter-day precision of GRe at three concentrations were less than 1.96%, and the average recoveries of GRe were more than 64.0%. The pharmacokinetic parameters for vaginal administration were as follows: Tm ax, 0.5 h; C max, 20.88 ng/mL; AUC0-t, 64.71 h · ng/mL and the residence time was3.06 h. By using deconvolution calculation method, the cumulative absorption fraction of GRe was about0.89%.Conclusion: The systemic exposure of GRe was minimal after vaginal administration of Xiaomi suppository.展开更多
基金Scientific Research Project of Tianjin Municipal Education Commission(No.2019KJ083).
文摘Salvia miltiorrhiza Bunge,known as red sage or Danshen,is commonly applied in Chinese herbal therapeutics for various biological effects.In 25-220 C.E.,the earliest Chinese Materia Medica referred to as Shengong’s Classic of Materia Medica(Eastern Han Dynasty of China,200 C.E.)initially documented Salvia miltiorrhiza Bunge.Currently,Salvia miltiorrhiza Bunge is one of the most frequently prescribed traditional Chinese medicines in clinics for antidiabetic,antianxiety,antihypertensive,antidepressant,antilipidemic,antiarrhythmic,and anticancer effects.Undoubtedly,it is best known for improving and promoting blood circulation;thus,its recommendation for use in cardiovascular disorders.Regarding this article,important information was sourced both manually and electronically using patent compendium and databases,including Google Scholar,herbal plant monographs,Hindawi,PubMed,Embase,CNKI,pharmacopoeias,Springer,etc.Well-concise details and discussions on the botany,traditional medicinal uses,chemical constituents-phytochemistry,pharmacokinetics,pharmacology,and toxicology information are presented.In perspective,understanding the comprehensive information of the above-stated fields with regards to Salvia miltiorrhiza Bunge would yield an additional positive knowledge on areas that need urgent attention and identify gaps in research and safety for future consideration.
文摘Metabolomics is a newly developed discipline following genomics,transcriptomics,and proteomics.It is based on the theory of systems biology,supported by modern spectroscopy analysis technology and is analyzed by the external stimulation of organisms.By analyzing the overall changes of metabolites with low molecular weight in organism after being stimulated by the outside world,we can understand the physiological and pathological state of organism,and finally clarify the essence of biological changes of organism.In recent years,metabolomics has developed rapidly.It has been widely used in early toxicity screening of lead compounds,preclinical toxicity of drugs and toxicity evaluation of clinical drugs.The in-depth interpretation of metabolomics results is also developing.This article reviewed the progress of metabolomics technology and its application in the study of toxicity evaluation of traditional Chinese medicine.
基金supported by Scientific Research Project of Tianjin Municipal Education Commission (No.2019KJ080).
文摘Objective:Inhibition of tumor angiogenesis has become a new targeted tumor therapy.In this study,we established a micellar carrier with a tumor neovascularization-targeting effect modified by the neovascularization-targeting peptide NGR.Methods:The targeted polymer poly(ethylene glycol)-b-poly(lactide-co-glycolide)(PEG-PLGA)modified with Asn–Gly–Arg(NGR)peptide was prepared and characterized by 1H nuclear magnetic resonance and Fourier-transform infrared spectrometry.NGR-PEG-PLGA was used to construct curcumin(Cur)-loaded micelles by the solvent evaporation method.The physicochemical properties of the micelles were also investigated.Additionally,we evaluated the antitumor efficacy of the polymer micelles(PM)using in vitro cytology experiments and in vivo animal studies.Results:The particle size of Cur-NGR-PM was 139.70±2.51 nm,and the drug-loading capacity was 14.37±0.06%.In vitro cytological evaluation showed that NGR-modified micelles showed higher cellular uptake through receptor-mediated endocytosis pathways than did unmodified micelles,leading to the apoptosis of tumor cells.Then,in vivo antitumor experiments showed that the modified micelles significantly inhibited tumor growth and were safe.Conclusions:NGR-modified micelles significantly optimized the therapeutic efficacy of Cur.This strategy offers a viable avenue for cancer treatment.
文摘Lianqiao(Forsythia suspensa(Thunb.)Vahl,Abbreviated as“F.suspensa”below)is traditional Chinese medicine in China,widely distributed all over the country and also highly rich in resources.The Northwest Territories is a genuine producing area.There are many chemical components in F.suspensa,including lignans,phenylethanolic glycosides,flavonoids,C6-C2 natural alcohols and their glycosides,phenolic acids,terpenes and volatile oils.Among them,lignans and phenylethanolic glycosides are the main active components.Based on the review of chemical components or constituents and main pharmacological activities,according to the definition of quality marker,the components of quality marker of F.suspensa were predicted and analyzed from the aspects of plant genetics and chemical composition,traditional efficacy,traditional medicine,new efficacy,blood entering composition,measurable composition,effective composition in different compatibility,and the influence of storage conditions of extract.Further research on its medicinal active ingredients will provide scientific basis for the evaluation of F.suspensa quality.
文摘Gastrodin(4-hydroxymethylphenyl-β-d-glucopyranoside)is an active ingredient with high content,which is isolated from the rhizome of Gastrodia elata.Gastrodin injections,tablets and capsules are currently the main gastrodin-related preparations in clinical practice,and gastrodin injections are the most widely used.This article will summarize pharmacology and adverse reactions of gastrodin to evaluate its safety,effectiveness and quality control.Gastrodin has pharmacological effects on central nervous system(vertigo,headache,insomnia,neurasthenia,convulsions and epilepsy,etc.),cardiovascular system and other diseases(osteoporosis,osteoarthritis and bone injury,etc.),but we still need to pay attention to its clinical adverse reactions(some patients may have dry mouth and nose,dizziness and stomach discomfort).In addition,further research is needed in other fields,such as health products,food,cosmetics,etc.We also need to further develop and explore the new pharmacological effects of gastrodin and expand its medicinal value.
文摘Baicalein(BE) is one of the main active flavonoids representing the variety of pharmacological effects including anticancer, anti-inflammatory and cardiovascular protective activities, but it's very low solubility, dissolution rate and poor oral absorption limit the therapeutic applications. In this work, a nano-cocrystal strategy was successfully applied to improve the dissolution rate and bioavailability of BE. Baicalein-nicotinamide(BE-NCT) nanococrystals were prepared by high pressure homogenization and evaluated both in vitro and in vivo. Physical characterization results including scanning electron microscopy, dynamic light scattering, powder X-ray diffraction and differential scanning calorimetry demonstrated that BE-NCT nano-cocrystals were changed into amorphous state with mean particle size of 251.53 nm. In the dissolution test, the BE-NCT nano-cocrystals performed 2.17-fold and 2.54-fold enhancement than BE coarse powder in FaSSIF-V2 and FaSSGF. Upon oral administration, the integrated AUC0-t of BE-NCT nano-cocrystals(6.02-fold) was significantly higher than BE coarse powder(1-fold), BE-NCT cocrystals(2.87-fold) and BE nanocrystals(3.32-fold). Compared with BE coarse powder, BE-NCT cocrystals and BE nanocrystals, BENCT nano-cocrystals possessed excellent performance both in vitro and in vivo evaluations.Thus, it can be seen that nano-cocrystal is an appropriate novel strategy for improving dissolution rate and bioavailability of poor soluble natural products such as BE.
文摘Blindness and vision impairment are the most devastating global health problems resulting in a substantial economic and social burden.Delivery of drug to particular parts of the anterior or posterior segment has been a major challenge due to various protective barriers and elimination mechanisms associated with the unique anatomical and physiological nature of the ocular system.Drug administration to the eye by conventional delivery systems results in poor ocular bioavailability(<5%).The designing of a novel approach for a safe,simple,and effective ocular drug delivery is a major concern and requires innovative strategies to combat the problem.Over the past decades,several novel approaches involving different strategies have been developed to improve the ocular delivery system.Among these,the ophthalmic in-situ gel has attained a great attention over the past few years.This review discussed and summarized the recent and the promising research progress of in-situ gelling in ocular drug delivery system.
文摘Diabetic retinopathy is the most common microvascular complication of diabetes mellitus and the primary reason for blindness all over the world,which is a lesion of blood vessels,neurons,and glial cells that constitute the complete structure of the retina.Patients may have vision loss and irreversible blindness.With the increase in the number of diabetes mellitus patients and the extension of lifespan,the incidence rate gradually increases.The clinical diagnosis of diabetic retinopathy mainly relies on regular examinations of ocular fundus and subjective patient descriptions,and once diabetic retinopathy is diagnosed,it is difficult to reverse.It is necessary to find the early markers of diabetic retinopathy.In this paper,data collection,data analysis of metabolomics and its research progress in diabetic retinopathy are summarized and prospected.In recent years,metabolomics has made some progress in the discovery of biomarkers,the exploration of pathogenesis,and the evaluation of diabetic retinopathyug efficacy of diabetic retinopathy.However,there are currently few metabolomics studies on the progression of diabetes mellitus to diabetic retinopathy.The determination of diabetic retinopathy-related specific biomarkers also requires data which a large number of animal experiments and clinical trials provide.In addition,despite the rapid development of metabolomics as an emerging discipline,there are still some problems,which need to be further improved in terms of analysis technology,data acquisition and data analysis.In general,there is still a lot of work to be done to apply metabolomics to clinical work.
基金supported by Innovation Team and Talents Cultivation Program of National Administration of Traditional Chinese Medicine (No. ZYYCXTD-D-202002)Scientific Research Project of Tianjin Municipal Education Commission (No.2019KJ083)
文摘Idiopathic pulmonary fibrosis(IPF)is a serious and fatal pulmonary inflammatory disease with an increasing incidenceworldwide.The drugs nintedanib and pirfenidone,are listed as conditionally recommended drugs in the“Evidence-Based Guidelines for the Diagnosis and Treatment of Idiopathic Pulmonary Fibrosis”.However,these two drugs have many adverse reactions in clinical application.Salvianolic acid B(Sal B),a water-soluble component of Salvia miltiorrhiza,could alleviate bleomycin-induced peroxidative stress damage,and prevent or delay the onset of IPF by regulating inflammatory factors and fibrotic cytokines during the disease’s progression.However,Sal B is poorly absorbed orally,and patient compliance is poor when administered intravenously.Therefore,there is an urgent need to find a new non-injection route of drug delivery.In this study,Sal B was used as model drug and l-leucine(LL)as excipient to prepare Sal B dry powder inhaler(Sal B-DPI)by spray drying method.Modern preparation evaluation methods were used to assess the quality of Sal B-DPI.Sal B-DPI is promising for the treatment of IPF,according to studies on pulmonary irritation evaluation,in vivo and in vitro pharmacodynamics,metabolomics,pharmacokinetics,and lung tissue distribution.
基金supported by Scientific Research Project of Tianjin Municipal Education Commission(No.2019KJ083).
文摘The characteristics of PF are diffuse alveolitis and disruption of alveolar structure leading to pulmonary interstitial fibrosis.At the same time,pulmonary fibrosis reduces lung volume and restricts ventilation,ultimately leading to hypoxemia and respiratory failure.In clinical guidelines,Nintedanib or Pirfenidone is often used for treatment.However,the two drugs,although they may slow the progression of the disease,cannot stop,or reverse fibrosis and generally result in a variety of toxic side effects.In 184-220 A.D.,it was already recorded in Supplementary Records of Famous Physicians that the function of SMB was to invigorate blood circulation and disperse blood stasis.In modern medical research,the active ingredients of SMB have likewise been found to be used in treatments such as anti-fibrosis,anti-inflammatory,antithrombotic,antioxidant,microcirculatory improvement,and antineoplastic.In this review,a comprehensive search of the former literature on SMB and pulmonary fibers was conducted using databases including PubMed,CNKI,the National Science and Technology Library,Hindawi,Chinese Science and Technology Journal Database,and the Scientific Network Database.Meanwhile,this review presents the mechanisms of the active ingredients in SMB which have anti-pulmonary fibrosis effects through the signal pathways,cytokines,inflammation response,oxidative stress,apoptosis,and matrix metalloproteinases.SMB could offer a direction for therapy for pulmonary fibrosis by identifying the possible active components and exploring the potential mechanisms.Those could provide a reference for further research and application of SMB in the treatment of pulmonary fibrosis.
基金financial support provided for this research by Tianjin Municipal Education Commission Research Project(Grant No.2017KJ134)
文摘Objective: To investigate the effects of fluidized bed granulation with dextrin on moisture sorption and diffusion of Zexie Decoction granules.Methods: The particle characterization was studied by the particle size, scanning electron microscopy(SEM), differential scanning calorimetry(DSC), and Fourier transform infrared(FTIR). The moisture sorption isotherm, equilibrium moisture content(EMC), and moisture diffusion coefficients were determined by using the saturated salt solution method.Results: The particle size increased from 6.04 μm(powder) to 1201.47 μm(granule). The glass transition temperature of dextrin, Zexie Decoction powder, and granule was 107.13 °C, 94.82 °C, and 126.25 °C. As the increase of temperature, the initial rate of moisture sorption become higher. Furthermore, the initial rate of moisture sorption of Zexie Decoction granules was lower than those of powders and dextrin. The EMC and moisture diffusion coefficients were reduced significantly after granulation(P < 0.01). Critical relative humidity and diffusion activation energy of granules were higher than powders.Conclusion: Results suggested that fluidized bed granulation with dextrin could reduce the hygroscopicity of the Zexie Decoction extract powders and inhibited moisture diffusion, which is mainly related to the microstructure reorganization by fluidized bed granulation and anti-plasticizing effects of dextrin.
基金supported by Tianjin City High School Science Technology Fund Planning Project(No.2017KJ134)。
文摘Salidroside(SAL)is a phenolic substance with high solubility and low permeability,which make it easy to cause the efflux effect of P-glycoprotein and degradation of intestinal flora,resulting in lower bioavailability.The aim of this study was to develop and optimize a water-in-oil nanoemulsion of SAL(w/o SAL-N)to explore its suitability in oral drug delivery systems.In this work,SAL-N was successfully prepared by water titration method at K_(m)=1 to construct the pseudo-ternary phase diagrams.Physical characterization including the average viscosity,pH,refractive index,particle size,PDI,TEM,DSC,the content of SAL,and stability study were performed.It was evaluated for drug release in vitro and pharmacokinetic studies in vivo.The optimized nanoemulsion formulation consisted of Labrafil M 1944 CS(63%),Span-80/Tween-80/EtOH(27%)and 200 mg·mL^(-1) SAL solution(SAL-SOL)(10%).Low viscosity and suitable pH were expected for the nanoemulsion.The spherical morphology and nanoscale size of SAL-N enhanced the stability of the nanoemulsion system.In vitro drug release showed that SAL-N had a better controlled release property than SAL-SOL at earlier time points.The pharmacokinetic studies exhibited that SAL-N had significantly higher in t_(1/2)(2.11-fold),AUC_(0-48 h)(1.75-fold)and MRT0-48 h(2.63-fold)than SAL-SOL(P<0.01).The w/o SAL-N prepared in this work can be effectively delivered via the oral route.It can be seen w/o nanoemulsion is a strategy for the drug with polyphenols to delay the release,enhance oral absorption and reduce metabolic rate.
基金the National Natural Science Foundation of China for the financial support(Grant No.20606024).
文摘The aim of this paper was to develop a cataplasma matrix that can be applicable to both watersoluble and liposoluble drugs.The gellan gum and konjaku were employed as the scaffold materials of the matrix.With polyacrylic acid sodium and oligosaccharides as tacktifier,the formula of the cataplasma matrix was optimized in the orthogonal method as:gellan gum 0.4 g,xanthan gum 0.03 g,konjac glue 0.1 g,glycerin 4 g,Gluco-Adhesive T(GAT)6 g,Gluco-Adhesive E(GAE)6 g,polyacrylic acid sodium 0.22 g,and sorbitol 3 g.The 180°peel strength,the tensile strength and the elongation at break was 3.043 N,0.275 MPa and 91.05%,respectively.Furthermore,the drug-compatibilities of the matrix were investigated with baicalin,berberine and curcumin,which were used as the models of hydrophilic,poor-water-soluble and hydrophobic ingredients.The drug contents could reach 4.12%,2.42%and 3.75%,while the in vitro release rate were measured as,361.79,55.85 and 104.41μg·cm^(-2)·h^(-1)for baicalin,berberine and curcumin,respectively.These results indicated that the obtained matrix had good drug-compatibility and drug-release properties for different ingredients.
基金Major Projects of National Science and Technology on"New Drug Creation and Development"(2012ZX09103201-0462012ZX09101212)
文摘Objective To apply the response surface-central composite design to developing and optimizing the oral fast disintegrating tablets(ODT) formulation for Jiawei Qing'e, a kind of prescription of Chinese herbal medicine.Methods The bitterness of Jiawei Qing'e was masked using Eudragit E-100 by solvent evaporation technique.Response surface approach was applied to investigating the interaction of formulation parameters in optimizing the formulation. The independent variables were Eudragit E-100/drug ratio(X1), amount of disintegrants(X2), and the amount of diluents(X3). The disintegration time(Y1), hardness(Y2), and weight variations of the tablets were characterized. Results The models predicted levels of X1=4.63%, X2=5.25%, and X3=34.33%, for the optimal formulation having a hardness of 3.0 kg with the disintegration time of 30 s within experimental region. The observed response of Y1=26.5 s and Y2=3.14 kg reasonably agreed with the predicted response. Conclusion Response surface methodology shows the good predictability and reliability in optimizing the formulation. The optimized ODT of Jiawei Qing'e has acceptable taste, rapid disintegrating ability, and good mechanical strength.
文摘Objective: A selective and sensitive ultra performance liquid chromatography-tandem mass spectrometry(UPLC-MS/MS) method was employed to study the pharmacokinetics of ginsenoside Re(GRe) in rabbits after vaginal administration of Xiaomi suppository to evaluate the systemic exposure of the suppository for the local treatment.Methods: Chromatographic separation was on an ACQUITY UPLC?BEH C18 column, and acetonitrile-0.1%formic acid was used as mobile phase in gradient elution. The plasma samples were deproteinized by acetonitrile, and the pharmacokinetic parameters were calculated by Winnonlin 6.4.Results: Calibration curve of GRe showed a good linearity over the concentration range from 5 ng/mL to500 ng/mL(r = 0.9999). The low limit of quantification of 5 ng/m L could satisfy the experimental requirement. The intra-day and inter-day precision of GRe at three concentrations were less than 1.96%, and the average recoveries of GRe were more than 64.0%. The pharmacokinetic parameters for vaginal administration were as follows: Tm ax, 0.5 h; C max, 20.88 ng/mL; AUC0-t, 64.71 h · ng/mL and the residence time was3.06 h. By using deconvolution calculation method, the cumulative absorption fraction of GRe was about0.89%.Conclusion: The systemic exposure of GRe was minimal after vaginal administration of Xiaomi suppository.
