香芹酮对尼莫地平从膜控型经皮治疗系统中渗透的影响。

Effect of carvone on the permeation of nimodipine from a membrane-moderated transdermal therapeutic system.

作者信息

Krishnaiah Y S R, Bhaskar P, Satyanarayana V

机构信息

Department of Pharmaceutical Sciences, Andhra University, Visakhapatnam, India.

出版信息

Pharmazie. 2003 Aug;58(8):559-63.

PMID:12967033

Abstract

The purpose of this investigation was to develop a membrane-moderated transdermal therapeutic system (TTS) of nimodipine using 2% w/w hydroxypropylmethylcellulose (HPMC) gel as a reservoir system containing 10% w/w of carvone (penetration enhancer) in 60% v/v ethanol. The flux of nimodipine through an ethylene vinyl acetate (EVA) copolymer membrane was found to increase with an increase in vinyl acetate content in the copolymer. The effect of a pressure-sensitive adhesive (TACKWHITE A 4MED) on the permeability of nimodipine through an EVA 2825 membrane (28% w/w vinyl acetate) or an EVA 2825 membrane/skin composite was also studied. An EVA 2825 membrane coated with TACKWHITE 4A MED was found to provide the required flux of nimodipine (117 +/- 5 microg/cm2/h) across rat abdominal skin. Thus a new transdermal therapeutic system for nimodipine was formulated using EVA 2825 membrane, coated with a pressure-sensitive adhesive TACKWHITE 4A MED, and 2% w/w HPMC gel as reservoir containing 10% w/w of carvone as a penetration enhancer. Studies in healthy human volunteers indicated that the TTS of nimodipine, designed in the present study, provided steady-state plasma concentration of the drug with minimal fluctuations.

摘要

本研究的目的是开发一种膜调节型尼莫地平透皮治疗系统（TTS），该系统使用2%（w/w）羟丙基甲基纤维素（HPMC）凝胶作为储库系统，在60%（v/v）乙醇中含有10%（w/w）香芹酮（渗透促进剂）。发现尼莫地平通过乙烯-醋酸乙烯酯（EVA）共聚物膜的通量随共聚物中醋酸乙烯酯含量的增加而增加。还研究了压敏胶（TACKWHITE A 4MED）对尼莫地平透过EVA 2825膜（28%（w/w）醋酸乙烯酯）或EVA 2825膜/皮肤复合物的渗透性的影响。发现涂有TACKWHITE 4A MED的EVA 2825膜可提供尼莫地平穿过大鼠腹部皮肤所需的通量（117±5μg/cm²/h）。因此，使用EVA 2825膜、涂有压敏胶TACKWHITE 4A MED以及2%（w/w）HPMC凝胶作为含有10%（w/w）香芹酮作为渗透促进剂的储库，配制了一种新的尼莫地平透皮治疗系统。对健康人类志愿者的研究表明，本研究设计的尼莫地平TTS可提供药物的稳态血浆浓度，波动最小。