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薄荷醇对盐酸尼卡地平从羟丙基纤维素凝胶透过离体大鼠表皮的经皮通量的促渗作用。

Penetration enhancing effect of menthol on the percutaneous flux of nicardipine hydrochloride through excised rat epidermis from hydroxypropyl cellulose gels.

作者信息

Krishnaiah Y S R, Satyanarayana V, Karthikeyan R S

机构信息

Department of Pharmaceutical Sciences, Andhra University, Visakhapatnam-530003, India.

出版信息

Pharm Dev Technol. 2002;7(3):305-15. doi: 10.1081/pdt-120005727.

Abstract

The aim of the present investigation is to study the penetration enhancing effect of menthol on the percutaneous flux of nicardipine hydrochloride through the excised rat epidermis from 2% w/w hydroxypropyl cellulose (HPC) gel system. The HPC gel formulations containing nicardipine hydrochloride and selected concentrations of menthol (0-12% w/w) were prepared, and evaluated for in vitro permeation of the drug through excised rat abdominal epidermis. The percutaneous flux of nicardipine hydrochloride across rat epidermis was enhanced markedly by the addition of menthol to the HPC gels. A maximum flux of nicardipine hydrochloride (227.70 +/- 1.30 micrograms cm-2 hr-1) was observed with an enhancement ratio of 7.12 when menthol was incorporated at a concentration of 8% w/w in a reservoir HPC system. The differential scanning calorimetry and Fourier transform-infrared spectroscopy data indicated that menthol increased the percutaneous flux of nicardipine hydrochloride through the rat skin by partial extraction of lipids in the stratum corneum. The results suggest that menthol may be useful for increasing the skin permeability of nicardipine hydrochloride from transdermal therapeutic system containing HPC gel as a reservoir.

摘要

本研究的目的是研究薄荷醇对盐酸尼卡地平从2%w/w羟丙基纤维素(HPC)凝胶体系经离体大鼠表皮的经皮通量的渗透促进作用。制备了含有盐酸尼卡地平及选定浓度薄荷醇(0 - 12%w/w)的HPC凝胶制剂,并评估了药物经离体大鼠腹部表皮的体外渗透情况。向HPC凝胶中添加薄荷醇可显著提高盐酸尼卡地平经大鼠表皮的经皮通量。当在储库型HPC体系中以8%w/w的浓度加入薄荷醇时,观察到盐酸尼卡地平的最大通量为(227.70±1.30微克·厘米⁻²·小时⁻¹),增强比为7.12。差示扫描量热法和傅里叶变换红外光谱数据表明,薄荷醇通过部分提取角质层中的脂质增加了盐酸尼卡地平经大鼠皮肤的经皮通量。结果表明,薄荷醇可能有助于提高含HPC凝胶作为储库的透皮治疗系统中盐酸尼卡地平的皮肤渗透性。

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