检索结果-南通市图书馆

Influence of omeprazole on pharmacokinetics of domperidone given as free base and maleate salt in healthy Chinese patients

引用

Acta Pharmacologica Sinica 2007年第8期28卷 1243-1246页

作者： Yi-fan ZHANG~1 Xiao-yan CHEN~1 Xiao-jian DAI~1 Yi-ni ZHANG~(1,2) Qi-zhi LIU~3 Hua-ling YU~2 Da-fang ZHONG~(1,4) ~1Shanghai Institute of Materia Medica,Chinese Academy of Sciences,Shanghai 201203,china ~2shenyang pharmaceutical university,shenyang 110016,china ~3Beijing Hanmi Pharm,Beijing 101312,china Shanghai Institute of Materia Medica Chinese Academy of Sciences Shanghai China shenyang pharmaceutical university Shenyang China Beijing Hanmi Pharm Beijing China

Aim:To investigate the influence of omeprazole on the pharmacokinetics ofdomperidone given as free base and maleate ***:An open,randomized,2-period crossover study with a washout period of 7 d was conducted in 10healthy Chinese,male *** each study period,the patients were adminis-tered a single oral dose of 10 mg domperidone as free base or maleate salt on d 1,20 mg omeprazole twice daily on d 2 and 3,and once on d 4.A single dose of 10 mgdomperidone as free base or maleate salt was taken at 4 h after administration ofomeprazole on d *** samples were collected on d 1 and 4 after the adminis-tration of domperidone,and the plasma concentrations of domperidone were de-termined by a sensitive liquid chromatography-tandem mass spectrometry ***:For free-base domperidone,pretreatment with omeprazole resulted in a16% decrease in maximum concentration(Cmax),compared with administrationalone（P2,no pharmacokinetic parameters were significantly *** the free baseand maleate salt were administered alone,no differences were found in any param-eters between the 2 *** contrast,when they were administered in thepresence of omeprazole,the Cmaxof domperidone given as free base was lower（25.9%）than that given as maleate salt（P<0.05）.Conclusion:Pretreatment ofomeprazole does not affect the absorption of domperidone maleate,but leads to amoderately decreased rate of absorption of the free base.

关键词： domperidone omeprazole maleate salt free base pharmacokinetics

来源：

同方期刊数据库评论

在线全文

同方期刊数据库

学校读者我要写书评

暂无评论

Biotransformation of metoprolol by the fungus Cunninghamella blakesleeana

引用

Acta Pharmacologica Sinica 2007年第7期28卷 1067-1074页

作者： Bin MA~(1,2),Hai-hua HUANG~2,Xiao-yan CHEN~1,Yu-ming SUN~2,Li-hong LIN~2,Da-fang ZHONG~(1,3)~1 Center for Drug Metabolism and Pharmacokinetics Research,Shanghai Institute of Materia Medica,Chinese Academy of Sciences,Shang-hai 201203,china ~2 shenyang pharmaceutical university,shenyang 110016,china Center for Drug Metabolism and Pharmacokinetics Research Shanghai Institute of Materia Medica Chinese Academy of Sciences Shanghai China shenyang pharmaceutical university Shenyang China

Aim:To investigate the biotransformation of metoprolol,a β1-cardioselectiveadrenoceptor antagonist,by filamentous fungus,and to compare the parallelsbetween microbial transformation and mammalian ***:Fivestrains of Cunninghamella （C elegans AS 3.156,C elegans AS 3.2028,C echinulataAS 3.2004,C blakesleeana AS 3.153 and AS 3.910） were screened for the ability totransform *** metabolites of metoprolol produced by C blakesleeanaAS 3.153 were separated and assayed by liquid chromatography-tandem massspectrometry （LC/MS~n）.The major metabolites were isolated by semipreparativeHPLC and the structures were identified by a combination of LC/MS~n and nuclearmagnetic resonance ***:Metoprolol was transformed to 7metabolites;2 were identified as new metabolites and 5 were known metabolites ***:The microbial transformation of metoprolol was similar tothe metabolism in *** fungi belonging to Cunninghamella speciescould be used as complementary models for predicting in vivo metabolism andproducing quantities of metabolite references for drugs like metoprolol.

关键词： metoprolol biotransformation Cun-ninghamella blakesleeana liquid chromatographytandem mass spectrometry

来源：

同方期刊数据库评论

在线全文

同方期刊数据库

学校读者我要写书评

暂无评论

Biotransformation of indomethacin by the fungus Cunninghamella blakesleeana

引用

Acta Pharmacologica Sinica 2006年第8期27卷 1097-1102页

作者： Peng ZHANG~2 Li-hong LIN~4 Hai-hua HUANG~3 Hai-yan XU~2 Da-fang ZHONG~(2,3,5) ~2Laboratory of Drug Metabolism and Pharmacokinetics,shenyang pharmaceutical university,shenyang 110016.china ~3Shanghai Institute of Materia Medica.Chinese Academy of Sciences,Shanghai 201203,china ~4Department of Microbiology,shenyang pharmaceutical university,shenyang 110016,china Laboratory of Drug Metabolism and Pharmacokinetics Shenyang Pharmaceutical University Shenyang 110016 China Shanghai Institute of Materia Medica Chinese Academy of Sciences Shanghai 201203 China Department of Microbiology Shenyang Pharmaceutical University Shenyang 110016 China

Aim:To investigate the biotransformation of indomethacin,the first of the newernonsteroidal anti-inflammatory drugs,by filamentous fungus and to compare thesimilarities between microbial transformation and mammalian metabolism ***:Five strains of Cunninghamella（C elegans AS 3.156,C elegans AS 3.2028,C blakesleeana AS 3.153,C blakesleeana AS 3.910 andC echinulata AS 3.2004）were screened for their ability to catalyze the biotransfor-mation of *** was partially metabolized by five strains ofCunninghamella,and C blakesleeana AS 3.910 was selected for *** metabolites produced by C blakesleeana AS 3.910 wereisolated using semi-preparative HPLC,and their structures were identified by acombination analysis of LC/MS~n and NMR *** three metabolites wereseparated and quantitatively assayed by liquid chromatography-ion trap ***:After 120 h of incubation with C blakesleeana AS 3.910,approximately 87.4% of indomethacin was metabolized to three metabolites:O-desmethylindomethacin（DMI,M1,67.2%）,N-deschlorobenzoylindomethacin（DBI,M2,13.3%）and O-desmethyl-N-deschlorobenzoylindomethacin（DMBI,M3,6.9%）.Three phase I metabolites of indomethacin produced by C blakesleeanaAS 3.910 were identical to those obtained in ***:C blakesleeanacould be a useful tool for generating the mammalian phase I metabolites ofindomethacin.

关键词： indomethacin microbial transformation Cunninghamella blakesleeana liquid chromatography mass spectrometry

来源：

同方期刊数据库评论

在线全文

同方期刊数据库

学校读者我要写书评

暂无评论

Influence of dosage forms on pharmacokinetics of daidzein and its main metabolite daidzein-7-O-glucuronide in rats

引用

Acta Pharmacologica Sinica 2005年第9期26卷 1145-1152页

作者： Feng QIU~2 Xiao-yan CHEN~2 Bo SONG~2 Da-fang ZHONG~3 Chang-xiao LIU~4 2 Laboratory of Drug Metabolism and Pharmacokinetics,shenyang pharmaceutical university,shenyang 110016,china Laboratory of Drug Metabolism and Pharmacokinetics Shenyang Pharmaceutical University Shenyang China Tianjin Key Laboratory of Drug Metabolism and Pharmacokinetics Tianjin Institute of Pharmaceutical Research Tianjin China

Aim:To investigate the influence of dosage forms on the pharmacokinetics ofdaidzein and its main metabolite daidzein-7-O-glucuronide in Wistar ***:After administration of two typical dosage forms(daidzein solution andsuspension),the concentrations of daidzein and daidzein-7-O-glucuronide weredetermined by an LC-MS-MS *** pharmacokinetic parameters were cal-culated and analyzed statistically using the Student’s ***:Absorp-tion of daidzein after administration of daidzein solution(tmax=0.46 h)was morerapid than that of the suspension(tmax=5.00 h).The peak plasma concentrationsof daidzein after administration of daidzein solution and suspension were 601.1 μg/Land 127.3 μg/L,respectively,and those of daidzein-7-O-glucuronide were 3000 μg/Land 192.6 μg/L,*** absolute bioavailabilities of free daidzein in ratsafter administration of daidzein solution and suspension were 12.8% and6.1%,respectively,which were calculated to be 47.0% and 12.2%,respectively,inthe form of total daidzein(free plus conjugated daidzein).Conclusion:Absorp-tion of daidzein solution was better than absorption of suspension(P<0.05).

关键词： daidzein daidzein-7-O-glucuronide influence dosage forms pharmacokinetics rats

来源：

同方期刊数据库评论

在线全文

同方期刊数据库

学校读者我要写书评

暂无评论

Phase II metabolites of etofesalamide in filamentous fungi

引用

Acta Pharmacologica Sinica 2005年第7期26卷 893-896页

作者： Hai-hua HUANG Gui-lei MA Yu-ming SUN~2 Qiang LI~2 Da-fang ZHONG~(2,3) Department of pharmaceutical Microbiology 2 Laboratory of Drug Metabolism and Pharmacokinetics,shenyang pharmaceutical university,shenyang 110016,china Department of pharmaceutical Microbiology Shenyang Pharmaceutical University Shenyang China Laboratory of Drug Metabolism and Pharmacokinetics Shenyang Pharmaceutical University Shenyang China

Aim:To study phase Ⅱ metabolites of etofesalamide in filamentous ***:Seven fungi were screened to transform *** metabolites ofetofesalamide were assayed using liquid chromatography coupled to *** major metabolite was subject to enzymatic hydrolysis to con-firm its ***:Etofesalamide was converted into two phase Ⅱmetabolites:glucoside and riboside *** conjugate was themajor product with a yield greater than 90%;no phase I metabolites were ***:Glucoside and riboside conjugations of etofesalamide in filamentousfungi differ from the phase Ⅱ metabolism of glucuronidation in mammals.

关键词： etofesalamide Cunninghamella metabolite transformation: mass spectrum analysis

来源：

同方期刊数据库评论

在线全文

同方期刊数据库

学校读者我要写书评

暂无评论

TGF-β_1 in retinal ganglion cells in rats with chronic ocular hypertension: its expression and anti-apoptotic effect

引用

International Journal of Ophthalmology(English edition) 2011年第4期4卷 396-401页

作者： Yong-Jian Tao 1, Dian-Wen Gao 1, Miao Yu 2 1Department of Ophthalmology, Shengjing Hospital of china Medical university, shenyang 110004, Liaoning Province, china 2 shenyang pharmaceutical university, shenyang 110016, Liaoning Province, china Department of Ophthalmology Shengjing Hospital of China Medical University Shenyang 110004 Liaoning Province China.

AIM: To investigate the anti-apoptotic effect of transforming growth factor beta-1 (TGF-β1) on chronic ocular hypertension. METHODS: The expression of TGF-β1 in retinal ganglion cells (RCGs) was measured using the immunohistochemiscal S-P method and real-time PCR in the normally control group, the ocular hypertension group (experimental group A), the ocular hypertension plus antibody intervention group (experimental group B) and the ocular hypertension plus antigen intervention group (experimental group C) at 1, 2, 3 and 4 weeks postoperatively. The count of apoptotic RCGs was measured using the TUNEL method. RESULTS: The expression of TGF-β1 was significantly higher in experimental group C than that in other three groups (P<0.05). The expression was the lowest in experimental group B (4.17%). A statistically significant difference was noted between the four groups (P <0.01). The count of apoptotic RCGs was statistically significantly lower in experimental group C than that in the experimental groups A and B (P <0.01). A statistically significant difference was noted in the count of apoptotic RCGs between these three experimental groups (P <0.01). CONCLUSION: TGF-β1 can inhibit the apoptosis of RCGs in rats with chronic ocular hypertension.

关键词： glaucoma nerve protect TGF-β1 retinal ganglion cells chronic ocular hypertension

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

A model of 3D-structure of H+, K+-ATPase catalytic subunit derived by homology modeling

引用

Acta Pharmacologica Sinica 2004年第4期25卷 76-81页

作者： Dong YAN, Yuan-dong HU1, Song LI1, Mao-sheng CHENG2 shenyang pharmaceutical university, shenyang 110016 1Academy of Military Medical Sciences, Beijing 100850, china shenyang pharmaceutical university Shenyang 110016 Academy of Military Medical Sciences 北京 100850

AIM: To build a model of 3D-structure of H+, K+-ATPase catalytic subunit for theoretical study and anti-ulcer drug design. METHODS: The model was built on the basis of structural data from the Ca2+-ATPase. Structurally conserved regions were defined by amino acid sequence comparisons, optimum interconnecting loops were se- lected from the protein databank, and amino (N)- and carboxyl (C)-terminal ends were generated as random coil structures. Applying molecular mechanics method then minimized the model energy. Molecular dynamics tech- nique was used to do further structural optimization. RESULTS: The model of 3D-structure of H+, K+-ATPase was derived. The model is reasonable according to several validation criteria. There were ten transmembrane helices (TM1-TM10) in the model and inhibitor-binding site was identified on the TM5-8 riched negatively charged residues. CONCLUSION: The 3D-structure model from our study is informative to guide future molecular biology study about H+, K+-ATPase and drug design based on database searching.

关键词： peptic ulcer H(+)-K(+)-exchanging ATPase protein structural homology drug design

来源：

同方期刊数据库评论

在线全文

同方期刊数据库

学校读者我要写书评

暂无评论

Pharmacokinetic behaviors and oral bioavailability of oridonin in rat plasma

引用

Acta Pharmacologica Sinica 2006年第12期27卷 1642-1646页

作者： Wen XU~2 Jin SUN~2 Ting-ting ZHANG~2 Bo MA~2 Sheng-miao CUI~3 Da-wei CHEN~2 Zhong-gui HE~(2,4)2 Department of Pharmaceutics,School of Pharmacy,shenyang pharmaceutical university,shenyang 110016,china 3 Department of Pharmacy,Guangdong pharmaceutical university,Guangzhou 510006,china Department of Pharmaceutics School of Pharmacy Shenyang Pharmaceutical University Shenyang China Department of Pharmacy Guangdong Pharmaceutical University Guangzhou China

Aim:To study the intravenous and oral pharmacokinetic behavior of oridonin andits extent of absolute oral bioavailability in ***:Oridonin was adminis-tered to rats via iv(5,10 and 15 mg/kg),po(20,40 and 80 mg/kg)or ip administra-tion(10 mg/kg).The concentrations of oridonin in rat plasma were determined bya high performance liquid chromatography with electrospray ionization mass spec-trometric detection(HPLC/ESI-MS)method and the pharmacokinetic parameterswere determined by non-compartmental ***:The plasma concen-tration of oridonin after intravenous administration decreased polyexponentially,and the pharmacokinetic parameters of oridonin were dose-independent withinthe examined *** was absorbed rapidly after oral gavage with a t(max)ofless than 15 min;the extent of absolute bioavailability of oridonin following oraladministration was 4.32%,4.58% and 10.8%.The extent of absolute bioavailabilityof oridonin following intraperitoneal administration was 12.6%.Conclusion:Firstorder rate pharmacokinetics were observed for oridonin within the range of ivdoses,while the extent of absolute oral bioavailability was rather low and *** low and dose-dependent extent of oral bioavailability may be dueto the saturation of first-pass effects.

关键词： oridonin pharmacokinetics intravenous oral bioavailability intraperitoneal injections rats

来源：

同方期刊数据库评论

在线全文

同方期刊数据库

学校读者我要写书评

暂无评论

Effect of melatonin on endogenous circadian rhythm

引用

沈阳药科大学学报 2008年第S1期25卷 126-127页

作者： XU Feng,WANG Min,ZANG Ling-he(shenyang pharmaceutical university,shenyang 110016,china)

Objective To further authenticate the role of melatonin on endogenous biologic clock *** Pinealectomized mice were used in the experiments,a series of circadian rhythm of physiology index,such as glucocorticoid,amino acid neurotransmitter,immune function,sensitivity of algesia and body temperature were *** Effects of melatonin on endogenous circadian rhythm roughly appeared four forms:1)The model of inherent rhythm was invariant,but midvalue was removed.2)Pacing function:pinealectomy and melatonin administration changed amplitude of the circadian vibration of aspartate,peripheral blood WBC and serum hemolysin.3)Phase of rhythm changed,such as the effects on percentage of lymphocyte and sensitivity of algesia.4)No effect,the circadian rhythm of body temperature belong to this *** Melatonin has effects some circadian rhythm,and it can adjust endogenous inherent rhythm and make the rhythm keep step with environmental *** may be a kind of Zeitgeber,Pineal gland might being a rhythm bearing organ to some circadian rhythm.

关键词： pineal gland melatonin circadian rhythm

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

Effects of nine antihypertensive drugs on blood pressure variability in sinoaortic-denervated rats

引用

Acta Pharmacologica Sinica 2006年第8期27卷 1013-1017页

作者： Jin Wang~(2,3) Fu-ming SHEN~2 Mm-wei WANG~3 Ding-feng SU~(2,4) ~2 Department of Pharmacology,Second Military Medical university,Shanghai 200433 ~3Department of" Pharmacology,shenyang pharmaceutical university,shenyang 110016,china Department of Pharmacology Second Military Medical University Shanghai China Department of Pharmacology Shenyang Pharmaceutical University Shenyang China

Aim:The present work was designed to investigate the effects of nine commonlyused antibypertensive drugs on blood pressure(BP)and blood pressure variabil-ity(BPV)in conscious sinoaortic-denervated(SAD)***:Seventy-twoSAD rats were randomly divided into nine *** were respectively givennifedipine 3 mg/kg,nitrendipine 5 mg/kg,amlodipine 1mg/kg,clonidine 10 μg/kg,prazosin 0.5 mg/kg,atenolol 20 mg/kg,telmisartan 20 mg/kg,hydrochlorothiazide40 mg/kg or captopril 50 mg/*** drugs were given via a catheter previouslyimplanted into the *** was recorded for 5 h from 1 h before drug admin-istration to 4 h after drug administration in conscious,freely moving ***:It was found that all these nine drugs significantly decreased BP in SAD *** these drugs(nifedipine,nitrendipine,amlodipine,clonidine,prazosin andatenolol)significantly decreased BPV in SAD rats,but the remaining three drugsdid *** and atenolol increased the heart period and the others did *** drugs affected the heart period ***:Among nine antihy-pertensive drugs from different classes,calcium antagonists and sympatheticinhibitors decreased BPV in SAD rats.

关键词： antihypertensive drugs blood pressure blood pressure variability sinoaortic denervation

来源：

同方期刊数据库评论

在线全文

同方期刊数据库

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：