检索结果-南通市图书馆

Virtual population pharmacokinetic using physiologically based pharmacokinetic model for evaluating bioequivalence of oral lacidipine formulations in dogs

引用

Asian Journal of Pharmaceutical Sciences 2017年第1期12卷 98-104页

作者： Bin Yang Chunnuan Wu Bin Ji Mingrui Wu Zhonggui He Lei Shang Jin Sun Department of Pharmaceutics School of PharmacyShenyang Pharmaceutical UniversityShenyangChina Department of pharmacy Tianjin Medical University Cancer Institute and HospitalTianjinChina Department of Pharmaceutical analysis School of PharmacyShenyang Pharmaceutical UniversityShenyangChina School of Pharmacy China Medical UniversityShenyangChina Municipal Key Laboratory of Biopharmaceutics School of PharmacyShenyang Pharmaceutical UniversityShenyangChina

The aim of the present study was to investigate virtual population pharmacokinetic using physiologically based pharmacokinetic(PBPK) model for evaluating bioequivalence of oral lacidipine formulations in dogs. The dissolution behaviors of three lacidipine formulations including one commercial product and two self-made amorphous solid dispersions(ASDs)capsules were determined in 0.07% Tween 80 media. A randomized 3-period crossover design in 6 healthy beagle dogs after oral administration of the three formulations at a single dose of 4 mg was conducted. The PBPK modeling was utilized for the virtual bioequivalence study.In vitro dissolution experiment showed that the dissolution behaviors of lacidipine amorphous solid dispersions(ASDs) capsules, which was respectively prepared by HPMC-E5 or Soluplus, as polymer displayed similar curves compared with the reference formulation in 0.07% Tween 80 media. In vivo pharmacokinetics experiments showed that three formulations had comparable maximum plasma drug concentration(Cmax), and the time(Tmax) to reach Cmax of lacidipine tablet, which was prepared by Soluplus, as polymer was slower than other two formulations in consistency with the in vitro dissolution rate. The 90% confidence interval(CI) for the Cmax, AUC0–24 h and AUC0–∞ of the ratio of the test drug to the reference drug exceeded the acceptable bioequivalence(BE) limits(0.80–1.25). However, the 90% CI of the AUC0–24 h, AUC0–∞ and Cmax of the ratio of test to reference drug were within the BE limit,calculated using PBPK modeling when the virtual subjects reached 24 dogs. The results all demonstrated that virtual bioequivalence study can overcome the inequivalence caused by inter-subject variability of the 6 beagle dogs involved in in vivo experiments.

关键词： Physiologically based pharmacokinetic model Virtual population pharmacokinetic Bioequivalence Lacidipine Amorphous solid dispersions

来源：

维普期刊数据库

同方期刊数据库评论

在线全文

学校读者我要写书评

暂无评论

Gut microbiota and Chinese medicine syndrome: altered fecal microbiotas in spleen(Pi)-deficient patients

引用

Journal of Traditional Chinese Medicine 2020年第1期40卷 137-143页

作者： Peng Ying Zhang Shuoying Liu Zhiwei Ji Jia Wu Chunfu Yang Jingyu Li Xiaobo School of Pharmacy Shanghai Jiao Tong UniversityShanghai 200240China School of Pharmacy Shenyang Pharmaceutical UniversityShenyang 110016China

OBJECTIVE:To investigate the fecal microbiota changes in patients with spleen(Pi)-deficiency(SPD),a common Chinese medicine syndrome with digestive and absorptive disturbances and to provide insight into the relationship between Chinese medicine syndrome and gut dysbiosis.METHODS:Fecal microbiotas from the stool samples of 53 SPD patients and 35 healthy subjects were analyzed via 16 S r RNA gene polymerase chain reaction(PCR)-denaturation gradient gel electrophoresis(DGGE).SPD-related marker genes from20 SPD patients and 20 healthy subjects were identified through gene sequencing,while some genes were quantified using quantitative PCR(q PCR).Discriminant analysis was conducted using SPSS software,and the canonical discriminant function formula for Pi-deficiency was established.RESULTS:Alterations in microbiota diversity and composition between the SPD and healthy groups were demonstrated via 16 S r RNA gene PCR-DGGE combined with multivariate statistical analysis.Fecal microbiota changes were also observed among different SPD-subtype patients.Eight SPD-related markers were found,and putative species corresponding to these markers were identified through gene sequencing,which may have potential associations with the common digestive dysfunctions in SPD patients.q PCR methods were established for two of these markers,which were significantly altered in the SPD patients.The canonical discriminant function formula was calculated for SPD,and the validity rates of these markers were over 85%.CONCLUSION:Fecal microbiotas are altered in patients with SPD,which may provide insight for further studies on clinically diagnosing and treating SPD.The results may also provide data to gain a better understanding of Traditional Chinese Medicine syndrome and gut dysbiosis.

关键词： Syndrome differentiation treatment Gastrointestinal microbiome Spleen-deficiency

来源：

维普期刊数据库

同方期刊数据库评论

在线全文

学校读者我要写书评

暂无评论

Predicting factors contributing to knowledge, attitudes and practices relating to Zika virus infection among the general public in Malaysia

引用

Asian Pacific Journal of Tropical Medicine 2020年第7期13卷 314-321页

作者： Kingston Rajiah Mari Kannan Maharajan May Yee Woo Yew Wing Yee Shi Mun Cheah Mai Ya Zhe Department of pharmacy Practice School of PharmacyInternational Medical UniversityKuala Lumpur 57000Malaysia School of Pharmacy International Medical UniversityKuala Lumpur 57000Malaysia

Objective: To identify the predicting factors that contribute to knowledge, attitude and practices relating to Zika virus infection among the general public in Malaysia.Methods: A cross-sectional study was conducted using a validated self-administered questionnaire. Descriptive analysis was done for participants’ socio-demographic profile. Contingency table analysis was done to analyse the associations between knowledge, attitudes, and practices(KAP) scores and socio-demographic profile. A Bonferroni-corrected P-value was used to find the significance of the associations and multiple comparisons were performed in a single data set. To determine the linear relationship between each independent variable and the dependent variable, Spearman rank correlation was performed. Cohen’s correlation coefficient was evaluated to determine the strength of the effect size. Multiple correlations and regression analyses were performed to identify independent variables that predicts the dependent variable.Results: Multiple correlation analyses were conducted between respondents’ KAP score and independent variables(Age >60 years;Female gender;Selangor state;At least 1 pregnant woman per household). The independent variables such as ‘Female gender’, ‘Selangor state’ and ‘At least 1 pregnant woman per household’ were positively and significantly correlated with KAP score whereas, age >60 years was negatively and significantly correlated with the KAP scores.Conclusions: There were associations between four independent factors and the KAP scores, while only three factors contributed to changes in KAP scores among the public. Among these contributing factors, respondents’ age group was the strongest predictor.

关键词： Zika virus Infection Public Malaysia Predictors

来源：

维普期刊数据库评论

在线全文

维普期刊数据库

学校读者我要写书评

暂无评论

Determination of estrogenic activity in the river Chienti(Marche Region, Italy) by using in vivo and in vitro bioassays

引用

Journal of Environmental Sciences 2016年第5期28卷 48-53页

作者： Paolo Cocci Francesco Alessandro Palermo Luana Quassinti Massimo Bramucci Antonino Miano Gilberto Mosconi school of Biosciences and Veterinary Medicine University of Camerino School of Pharmacy University of Camerino

Environmental estrogen-like compounds（i.e. xenoestrogens） are a variety of pollutants,ranging from synthetic to natural occurring molecules, that are found in surface and waste waters over a wide range of concentrations. In aquatic environment, the overall estrogenic activity is often due to the presence of a mixture of chemicals and their degraded products which can induce synergistic effects. Current strategies for monitoring estrogen-like chemicals are based on the use of a battery of in vivo and in vitro ecotoxicological tests. In this regard, the aim of the present work was to carry out a bio-monitoring study for testing estrogenicity of the Chienti river（Marche Region, Italy） by using both an E-screen and a vitellogenin（Vtg） induction assay in juvenile goldfish. Three sites were used for analysis,localized at the mouth（sampling point 1）, in the middle（sampling point 2） and at the origin（sampling point 3） of Chienti river. For most of the water samples（i.e. samples collected at sampling points 2 and 3）, clear estrogenic activity was detected in the E-screen assay suggesting different proliferation activities in function of the collecting site. In contrast, the Vtg ELISA demonstrated that water samples collected from each sampling point were estrogenic. Overall, we showed for the first time that the estrogenic activities in water samples from the Chienti river were significant in both in vivo and in vitro; we also observed a different sensitivity between bioassays.

关键词： Xenoestrogens Chienti river Bioassays E-screen Vitellogenin Carassius auratus

来源：

维普期刊数据库

同方期刊数据库评论

在线全文

学校读者我要写书评

暂无评论

Engineering a folic acid-decorated ultrasmall gemcitabine nanocarrier for breast cancer therapy: Dual targeting of tumor cells and tumor-associated macrophages

引用

Acta Pharmaceutica Sinica B 2022年第3期12卷 1148-1162页

作者： Pearl Moharil Zhuoya Wan Apurva Pardeshi Jiang Li Haozhe Huang Zhangyi Luo Sanjay Rathod Ziqian Zhang Yuang Chen Bei Zhang Christian A.Fernandez Jingjing Sun Song Li Center for Pharmacogenetics Department of Pharmaceutical ScienceSchool of PharmacyUniversity of PittsburghPA 15261USA

Combination of passive targeting with active targeting is a promising approach to improve the therapeutic efficacy of nanotherapy.However,most reported polymeric systems have sizes above100 nm,which limits effective extravasation into tumors that are poorly vascularized and have dense stroma.This will,in turn,limit the overall effectiveness of the subsequent uptake by tumor cells via active targeting.In this study,we combined the passive targeting via ultra-small-sized gemcitabine(GEM)-based nanoparticles(NPs)with the active targeting provided by folic acid(FA)conjugation for enhanced dual targeted delivery to tumor cells and tumor-associated macrophages(TAMs).We developed an FAmodified prodrug carrier based on GEM(PGEM)to load doxorubicin(DOX),for co-delivery of GEM and DOX to tumors.The co-delivery system showed small particle size of~10 nm in diameter.The ligand-free and FA-targeted micelles showed comparable drug loading efficiency and a sustained DOX release profile.The FA-conjugated micelles effectively increased DOX uptake in cultured KB cancer cells that express a high level of folate receptor(FR),but no obvious increase was observed in 4T1.2 breast cancer cells that have a low-level expression of FR.Interestingly,in vivo,systemic delivery of FAPGEM/DOX led to enhanced accumulation of the NPs in tumor and drastic reduction of tumor growth in a murine 4T1.2 breast cancer model.Mechanistic study showed that 4T1.2 tumor grown in mice expressed a significantly higher level of FOLR2,which was selectively expressed on TAMs.Thus,targeting of TAM may also contribute to the improved in vivo targeted delivery and therapeutic efficacy.

关键词： Folic acid Gemcitabine Polymeric micelles Breast cancer Dual targeting Tumor associated macrophages Ultrasmall nanocarrier Doxorubicin

来源：

维普期刊数据库

同方期刊数据库评论

在线全文

学校读者我要写书评

暂无评论

Bottlebrush inspired injectable hydrogel for rapid prevention of postoperative and recurrent adhesion

引用

Bioactive Materials 2022年第10期7卷 27-46页

作者： Jushan Gao Jinpeng Wen Datao Hu Kailai Liu Yuchen Zhang Xinxin Zhao Ke Wang School of Pharmacy Health Science CenterXi’an Jiaotong UniversityXi’an710061China

Postsurgical adhesion is a common clinic disease induced by surgical trauma,accompanying serious subsequent complications.Current non-surgical approaches of drugs treatment and biomaterial barrier administration only show limited prevention effects and couldn’t effectively promote peritoneum repair.Herein,inspired by bottlebrush,a novel self-fused,antifouling,and injectable hydrogel is fabricated by the free-radical polymerization in aqueous solution between the methacrylate hyaluronic acid(HA-GMA)and N-(2-hydroxypropyl)methacrylamide(HPMA)monomer without any chemical crosslinkers,termed as H-HPMA hydrogel.The H-HPMA hydrogel can be tuned to perform excellent self-fused properties and suitable abdominal metabolism time.Intriguingly,the introduction of the ultra-hydrophilic HPMA chains to the H-HPMA hydrogel affords an unprecedented antifouling capability.The HPMA chains establish a dense hydrated layer that rapidly prevents the postsurgical adhesions and recurrent adhesions after adhesiolysis in vivo.The H-HPMA hydrogel can repair the peritoneal wound of the rat model within 5 days.Furthermore,an underlying mechanism study reveals that the H-HPMA hydrogel significantly regulated the mesothelial-to-mesenchymal transition(MMT)process dominated by the TGF-β-Smad2/3 signal pathway.Thus,we developed a simple,effective,and available approach to rapidly promote peritoneum regeneration and prevent peritoneal adhesion and adhesion recurrence after adhesiolysis,offering novel design ideas for developing biomaterials to prevent peritoneal adhesion.

关键词： Bottlebrush polymer Rapid healing Antifouling MMT Postoperative adhesion prevention

来源：

维普期刊数据库评论

在线全文

维普期刊数据库

学校读者我要写书评

暂无评论

Fructus Zanthoxyli extract improves glycolipid metabolism disorder of type 2 diabetes mellitus via activation of AMPK/PI3K/Akt pathway:Network pharmacology and experimental validation

引用

Journal of Integrative Medicine 2022年第6期20卷 543-560页

作者： Ting Zhang Qing Zhang Wei Zheng Ting Tao Ruo-lan Li Li-yu Wang Wei Peng Chun-jie Wu School of Pharmacy Chengdu University of Traditional Chinese MedicineChengdu 611137Sichuan ProvinceChina

Objective:This study investigated the potential mechanisms behind the beneficial effects of Fructus Zanthoxyli(FZ)against type 2 diabetes mellitus(T2DM)based on network pharmacology and experimental validation.Methods:Ultra-high-performance liquid chromatography coupled with hybrid quadrupole-orbitrap high-resolution mass spectrometry,and gas chromatography-mass spectrometry were used to identify the constituents of FZ.Next,the differentially expressed genes linked to the treatment of diabetes with FZ were screened using online databases(including Gene Expression Omnibus database and Swiss Target Prediction online database),and the overlapping genes and their enrichment were analyzed by Kyoto Encyclopedia of Genes and Genomes(KEGG).Finally,the pathway was verified by in vitro experiments,and cell staining with oil red and Nile red showed that the extract of FZ had a therapeutic effect on T2DM.Results:A total of 43 components were identified from FZ,and 39 differentially expressed overlapping genes were screened as the possible targets of FZ in T2DM.The dug component-target network indicated that PPARA,PPARG,PIK3R3,JAK2 and GPR88 might be the core genes targeted by FZ in the treatment of T2DM.Interestingly,the enrichment analysis of KEGG showed that effects of FZ against T2DM were closely correlated with the adenosine monophosphate-activated protein kinase(AMPK)and phosphatidylinositol-3-kinase(PI3K)/protein kinase B(Akt)signaling pathways.In vitro experiments further confirmed that FZ significantly inhibited palmitic acid-induced lipid formation in Hep G2 cells.Moreover,FZ treatment was able to promote the AMPK and PI3K/Akt expressions in Hep G2 cells.Conclusion:Network pharmacology combined with experimental validation revealed that FZ extract can improve the glycolipid metabolism disorder of T2DM via activation of the AMPK/PI3K/Akt pathway.

关键词： Fructus Zanthoxyli Zanthoxylum bungeanum Maxim Type 2 diabetes mellitus Network pharmacology Glucose and lipid metabolism Phosphatidylinositol-3-kinase AMPK/PI3K/Akt

来源：

维普期刊数据库

同方期刊数据库评论

在线全文

学校读者我要写书评

暂无评论

Bile duct ligation differently regulates protein expressions of organic cation transporters in intestine,liver and kidney of rats through activation of farnesoid X receptor by cholate and bilirubin

引用

Acta Pharmaceutica Sinica B 2023年第1期13卷 227-245页

作者： Shijin Hong Shuai Li Xiaoyan Meng Ping Li Xun Wang Mengxiang Su Xiaodong Liu Li Liu Center of Drug Metabolism and Pharmacokinetics School of PharmacyChina Pharmaceutical UniversityNanjing 210098China Tianjin Institutes of Pharmaceutical Research Tianjin 300301China Departments of Pharmaceutical Analysis School of PharmacyChina Pharmaceutical UniversityNanjing 210098China

Body is equipped with organic cation transporters(OCTs).These OCTs mediate drug transport and are also involved in some disease process.We aimed to investigate whether liver failure alters intestinal,hepatic and renal Oct expressions using bile duct ligation(BDL)rats.Pharmacokinetic analysis demonstrates that BDL decreases plasma metformin exposure,associated with decreased intestinal absorption and increased urinary excretion.Western blot shows that BDL significantly downregulates intestinal Oct2 and hepatic Oct1 but upregulates renal and hepatic Oct2.In vitro cell experiments show that chenodeoxycholic acid(CDCA),bilirubin and farnesoid X receptor(FXR)agonist GW4064 increase OCT2/Oct2 but decrease OCT1/Oct1,which are remarkably attenuated by glycine-β-muricholic acid and silencing FXR.Significantly lowered intestinal CDCA and increased plasma bilirubin levels contribute to different Octs regulation by BDL,which are confirmed using CDCA-treated and bilirubin-treated rats.A disease-based physiologically based pharmacokinetic model characterizing intestinal,hepatic and renal Octs was successfully developed to predict metformin pharmacokinetics in rats.In conclusion,BDL remarkably downregulates expressions of intestinal Oct2 and hepatic Oct1 protein while upregulates expressions of renal and hepatic Oct2 protein in rats,finally,decreasing plasma exposure and impairing hypoglycemic effects of metformin.BDL differently regulates Oct expressions via Fxr activation by CDCA and bilirubin.

关键词： Bilirubin Chenodeoxycholic acid Farnesoid X receptor Liver failure Organic cation transporters Bile duct ligation Physiologically based pharmacokinetic model

来源：

维普期刊数据库

同方期刊数据库评论

在线全文

学校读者我要写书评

暂无评论

Liquisolid technique and its applications in pharmaceutics

引用

Asian Journal of Pharmaceutical Sciences 2017年第2期12卷 115-123页

作者： Mei Lu Haonan Xing Jingzheng Jiang Xiao Chen Tianzhi Yang Dongkai Wang Pingtian Ding School of Pharmacy Shenyang Pharmaceutical UniversityShenyangChina Department of Basic Pharmaceutical Sciences School of PharmacyHusson UniversityBangorMEUSA

Most of the newly developed drug candidates are lipophilic and poorly water-soluble. Enhancing the dissolution and bioavailability of these drugs is a major challenge for the pharmaceutical industry. Liquisolid technique, which is based on the conversion of the drug in liquid state into an apparently dry, non-adherent, free flowing and compressible powder,is a novel and advanced approach to tackle the issue. The objective of this article is to present an overview of liquisolid technique and summarize the progress of its applications in pharmaceutics. Low cost, simple processing and great potentials in industrial production are main advantages of this approach. In addition to the enhancement of dissolution rate of poorly water-soluble drugs, this technique is also a fairly new technique to effectively retard drug release. Furthermore, liquisolid technique has been investigated as a tool to minimize the effect of pH variation on drug release and as a promising alternative to conventional coating for the improvement of drug photostability in solid dosage forms. Overall, liquisolid technique is a newly developed and promising tool for enhancing drug dissolution and sustaining drug release, and its potential applications in pharmaceutics are still being broadened.

关键词： Liquisolid technique Dissolution enhancement Poorly water-soluble drugs Sustained release pH variation Photostability

来源：

维普期刊数据库

同方期刊数据库评论

在线全文

学校读者我要写书评

暂无评论

Polymyxin B as an inhibitor of lipopolysaccharides contamination of herb crude polysaccharides in mononuclear cells

引用

Chinese Journal of Natural Medicines 2017年第7期15卷 487-494页

作者： LU Xiao-Xiao JIANG Yi-Fan LI Hong OU Ying-Ye ZHANG Zhi-De DI Hong-Ye CHEN Dao-Feng ZHANG Yun-Yi Department of Pharmacology School of Pharmacy Fudan University Shanghai 201203 China Department of Pharmacognosy School of Pharmacy Fudan University Shanghai 201203 China

Lipopolysaccharides(LPS) contamination in herbal crude polysaccharides is inevitable. The present study was performed to explore the effect of polymyxin B on abolishing the influence of LPS contamination in mononuclear cells. LPS was pretreated with polymyxin B sulfate(PB) at different concentrations for 1, 5 or 24 h, and then used to stimulate RAW264.7 and mouse peritoneal macrophages(MPMs). The nitric oxide(NO) and tumor necrosis factor-α(TNF-α) in cell culture supernatant, as the indications of cell response, were assayed. Bupleurum chinensis polysaccharides(BCPs) with trace amount contamination of LPS was treated with PB. 30 μg·mL^(–1) of PB, treating LPS(10 and 1000 ng·mL^(–1) in stimulating RAW264.7 and MPMs respectively) at 37 ℃ for 24 h, successfully abolished the stimulating effect of LPS on the cells. When the cells were stimulated with LPS, BCPs further promoted NO production. However, pretreated with PB, BCPs showed a suppression of NO production in MPMs and no change in RAW264.7. In the in vitro experiments, LPS contamination in polysaccharide might bring a great interference in assessing the activity of drug. Pretreatment with PB(30 μg·mL^(–1)) at 37 °C for 24 h was sufficient to abolish the effects of LPS contamination(10 and 1 000 ng·mL^(–1)).

关键词： Lipopolysaccharide Polymyxin B Bupleurum chinensis polysaccharides Mouse peritoneal macrophages RAW264.7 cells

来源：

维普期刊数据库

同方期刊数据库评论

在线全文

学校读者我要写书评

暂无评论

欢迎您,

建议与咨询留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

时间限定

文献类型

馆藏选择

核心期刊

语言

文献类型

帮助

文字说明：

检索规则说明：

检索范例：

分类表

所选分类

限定检索结果

文献类型

馆藏范围

日期分布

学科分类号

主题

机构

作者

语言

在线全文

在线全文

在线全文

在线全文

在线全文

在线全文

在线全文

在线全文

在线全文

在线全文

请选择保存的检索档案：

请选择收藏分类：

通借通还

欢迎您,

建议与咨询 留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

时间限定

文献类型

馆藏选择

核心期刊

语言

文献类型

帮助

文字说明：

检索规则说明：

检索范例：

分类表

所选分类

限定检索结果

文献类型

馆藏范围

日期分布

学科分类号

主题

机构

作者

语言

在线全文

在线全文

在线全文

在线全文

在线全文

在线全文

在线全文

在线全文

在线全文

在线全文

请选择保存的检索档案： 新增检索档案 确定 取消

请选择收藏分类： 新增自定义分类 确定 取消

通借通还

建议与咨询留下您的常用邮箱和电话号码，以便我们向您反馈解决方案和替代方法

请选择保存的检索档案：

请选择收藏分类：