手性药物经皮吸收与代谢的立体选择性及其影响因素

被引：1

作者：

叶金翠 ^{[1
,2
]}

陈国神 ^{[2
]}

曾苏 ^{[1
]}

机构：

[1] 浙江大学药学院

[2] 浙江省医学科学院药物研究所

来源：

中国药学杂志 | 2009年 / 44卷 / 01期

关键词：

手性药物; 皮肤渗透; 立体选择性;

D O I：

暂无

中图分类号：

R96 [药理学];

学科分类号：

100602 ; 100706 ;

摘要：

目的综述手性药物经皮吸收与代谢的立体选择性及其影响因素。方法分析评述近年来国内、外相关文献资料。结果皮肤的组成潜在地提供了一个手性环境,手性药物对映体与皮肤手性物质的选择性结合会引起对映体间渗透性的不同。除皮肤手性环境外,其他一些因素如对映体与消旋体熔点的差异、手性促进剂的构象、手性辅料的对映体选择性吸附、前体药物的对映体选择性皮肤代谢等均可能引起对映体选择性皮肤渗透。结论手性药物皮肤吸收与代谢的对映体选择性及其影响因素研究可为其经皮给药制剂的研制及其前体药物的设计提供理论与技术支持。

引用

页码：6 / 10

页数：5

共 49 条

[1]

Differential permeation ofpropranolol enantiomers across human skin in vitro fromformulations containing an enantioselective excipient. SUEDEE R,BRAIN K R,HEARD C M. Chirality . 1999

[2] Piperazinylalkyl prodrugs of naproxen improve in vitro skin permeation [J].

Rautio, J ;

Nevalainen, T ;

Taipale, H ;

Vepsäläinen, J ;

Gynther, J ;

Laine, K ;

Järvinen, T .

EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2000, 11 (02) :157-163

[3]

Evaluation of Stereoselective Transdermal Transport and Concurrent Cutaneous Hydrolysis of Several Ester Prodrugs of Propranolol: Mechanism of Stereoselective Permeation[J] . Shamim Ahmed,Teruko Imai,Masaki Otagiri. &nbspPharmaceutical Research . 1996 (10)

[4]

Relationship among physicochemical properties , skin permeability , and topical activity of the racemic compound and pure enantiomers of a new antifungal. Wearley L,Antonacci B,Cacciapuoti A,et al. Pharmacological Research . 1993

[5]

Relationship Among Physicochemical Properties, Skin Permeability, and Topical Activity of the Racemic Compound and Pure Enantiomers of a New Antifungal[J] . Lorraine Wearley,Barry Antonacci,Anthony Cacciapuoti,Seb Assenza,Imtiaz Chaudry,Charles Eckhart,Nancy Levine,David Loebenberg,Christine Norris,Raolo Parmegiani,Joel Sequeira,Taisa Yarosh-Tomaine. &nbspPharmaceutical Research . 1993 (1)

[6]

Oleic Acid: Its Effects on Stratum Corneum in Relation to (Trans)Dermal Drug Delivery[J] . Michael L. Francoeur,Guia M. Golden,Russell O. Potts. &nbspPharmaceutical Research . 1990 (6)

[7]

Transdermal delivery from eutectic systems: enhanced permeation of a model drug, ibuprofen. Stott PW,Williams AC,Barry BW. Journal of Controlled Release . 1998

[8]

Evaluation of stereoselective dissolutionof racemic salbutamol matrices prepared with commonly usedexcipients and 1H-NMR study. SRICHANA T,SUEDEE R. Drug Development and Industrial Pharmacy . 2001

[9]

Transdermal drug delivery enhanced and controlled by erbium:YAG laser:a comparative study of lipophilic and hydrophilic drugs. LEE W R,SHENS C,LAI HH,et al. J Controlled Re-lease . 2001

[10]

Chirality and its implication in transdermal drug development. Reddy IK,Kommuru TR,Zaghloul AA,Khan MA. Critical Reviews in Therapeutic Drug Carrier Systems . 2000

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