介质pH,药物浓度,月桂氮艹(左)卓(右)酮对二氢埃托啡透皮(蛇皮)作用的影响

郭庆东;陈小平;石庭森;

中国药学杂志 ›› 1997, Vol. 32 ›› Issue (06) : 349-352.

中国药学杂志 ›› 1997, Vol. 32 ›› Issue (06) : 349-352.
药剂

介质pH,药物浓度,月桂氮艹(左)卓(右)酮对二氢埃托啡透皮(蛇皮)作用的影响

  • 郭庆东;陈小平;石庭森;
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Effect of vehicle pH, drug concentration and Azone on the snake skin permeation of dihydroetorphine hydrochloride

  • Guo Qingdong
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摘要

目的:采用鸟梢蛇腹部皮肤研究pH,药物浓度和月桂氮艹(左)卓(右)酮对二氢埃托啡(DHE)体外透皮作用的影响。方法:采用改良Franz直立式释放池对DHE的体外释放作了研究。有效释放面积为2.5 cm2,按设定的时间间隔取样直至24 h,取样童为100μl,并用液闪法分析DHE透过量。结果:pH对DHE渗透的影响很复杂,在pH 3和9透皮流率明显快于pH 5和7。不同浓度DHE的透皮流率也不同,在实验选择的DHE浓度范围内,DHE的透皮流率与DHE浓度成正比。月桂氮艹(左)卓(右)酮对DHE的渗透有很强的促进作用。结论:通过乌梢蛇皮腹部皮肤研究了不同因素对DHE透皮作用影响,发现pH、药物浓度和促渗剂对DHE的透皮作用影响复杂。其结果为进一步研究DHE透皮给药系统提供了有益的参考。

Abstract

OBJECTIVE: To investigate the effects of pH, donor phase drug concentration and Atone on in vitro skin permeation of dihydroetorphine hydrochloride(DHE)using excised abdominal Zaocys dhumnades(Cantor ) skin. METHODS: The DHE permeation study was carried out using modified Franz-type vertical diffusion cells with an effective diffusional area of 2.5 cm2 .Samples of 100μl were with drawn from the receptor solution at appropriate time intervals over 24 h and assayed for DHE by liquid scintillation method. RESULTS: The influence of pH on the permeation of DHE was very complex. The permeation flux at pH 3 and 9 was significantly faster than that at pH 5 and 7. The permeation flux at different DHE concentrations was rather steady, so the DHE permeated was in direct proportional to DHE concentrations of the selected DHE concentrations. Atone had a strong effect on the DHE permeation. CONCLUSION: The different factors that affect DHE permeation through Zaocys dhumandes skin were tested. It was found that the factors like pH, drug concentration and enhancer had intricated effect on DHE permeation. The results were useful for further research of DHE transdermal delivery system.

关键词

透皮吸收 / 二氢埃托啡 / 乌梢蛇 / 月桂氮艹(左)卓(右)酮

Key words

percutaneous absorption / dihydroetorphine hydrochloride / Zaocys dhumandes (Cantor) / Atone

引用本文

导出引用
郭庆东;陈小平;石庭森;. 介质pH,药物浓度,月桂氮艹(左)卓(右)酮对二氢埃托啡透皮(蛇皮)作用的影响[J]. 中国药学杂志, 1997, 32(06): 349-352
Guo Qingdong . Effect of vehicle pH, drug concentration and Azone on the snake skin permeation of dihydroetorphine hydrochloride[J]. Chinese Pharmaceutical Journal, 1997, 32(06): 349-352

参考文献

1 葛云.李密.孙文林,等.盐酸二氢埃托啡身体依赖性潜力的临床评价.药学学报,1994,29(4): 256. 2 Chen XP, Guo QD, Shi TS. Transdermal permeation of DHE influence of pH, concentration and surfactants on in vitro permeation. J Chin Pharm Sci, 1995, 4(4):187. 3 Kasting GB. Effect of pH, counter ion and oil vehicle on the skin penetration of triprolidine. Pharm Res, 1990,7:S112. 4 Liu P, Nightingale JAS, Kurihara-Bergatrom, T. Variation of human skin permeation in vitro: ionic vs neutral compounds. Int J Pharm, 1993,90: 171. 5 Chien Y W, Siddiqui O, Shi WM. et al, Direct current iontophoretic transdermal delivery of peptide and protein drugs. JPS, 1989,78(5):376.

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