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巴氯芬在泊洛沙姆卵磷脂有机凝胶中的释放及透皮渗透情况

The release and transdermal penetration of baclofen formulated in a poloxamer lecithin organogel.

作者信息

Arnold John J, Asbill Scott

机构信息

McWhorter School of Pharmacy, Samford University, Birmingham, Alabama.

出版信息

Int J Pharm Compd. 2009 Nov-Dec;13(6):569-71.

Abstract

The purpose of this study was to evaluate the in vitro release and ex vivo penetration of baclofen following incorporation into a 2% poloxamer lecithin organogel. Franz cells were utilized for both the release and penetration studies. Semi-permeable dialysis membranes were used as the model skin for the penetration study. Baclofen release and penetration at predetermined time points were assessed using high-performamce liquid chromatographic analysis. Results demonstrated that baclofen release from the poloxamer lecithin organogel was significantly higher than its penetration through porcine skin. The amount of baclofen released by the poloxamer lecithin organogel was linear up to 12 hours. Approximately 20% of applied drug was released over the duration of the study period. In comparison with drug released, the ex vivo penetration of baclofen through porcine skin was very low with only minute detectable quantities (significantly less than 1%) after the 12-hour study period. These results suggest that the request to include baclofen into a compounded poloxamer lecithin organogel should be approached cautiously by compounding pharmacists.

摘要

本研究的目的是评估巴氯芬在被掺入2%泊洛沙姆卵磷脂有机凝胶后的体外释放和离体渗透情况。采用Franz扩散池进行释放和渗透研究。半透性透析膜用作渗透研究的模型皮肤。使用高效液相色谱分析法评估在预定时间点的巴氯芬释放和渗透情况。结果表明,巴氯芬从泊洛沙姆卵磷脂有机凝胶中的释放显著高于其透过猪皮的渗透。泊洛沙姆卵磷脂有机凝胶释放的巴氯芬量在长达12小时内呈线性。在研究期间,约20%的给药药物被释放。与释放的药物相比,巴氯芬透过猪皮的离体渗透非常低,在12小时研究期后仅能检测到微量(显著低于1%)。这些结果表明,复方药剂师在将巴氯芬纳入复方泊洛沙姆卵磷脂有机凝胶时应谨慎对待。

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