Bassani August S, Banov Daniel, Lehman Paul A
Professional Compounding Centers of America, Houston, Texas.
Int J Pharm Compd. 2008 May-Jun;12(3):270-3.
For several years, pharmacists have been using vehicles such as Pluronic lecithin organogel and Lipoderm for the delivery of medication, including promethazine, through the skin. This study evaluated the percutaneous absorption pharmacokinetics of promethazine hydrochloride 25 mg/g in Pluronic lecithin organogel and the commercial base Lipoderm,in vitro, in human ex vivo skin, using the finite dose technique and Franz Diffusion Cells. Due to the polar nature of promethazine hydrochloride, it was theorized that this drug would present a transdermal challenge for these two commonly utilized compounding bases. An amount of 5 mcL/cm squared of each formulation was applied to triplicate sections of skin from three different ex vivo skin donors. At 4, 8, 12, 24, 32, and 48 hours post-application, the reservoir solution in the Franz Cell was removed and analyzed. Lipoderm performed better than Pluronic lecithin organogel based on total absorption into the reservoir solution (2.86% +/- 0.79 vs. 1.73% +/-0.85) (P less than 0.2). Total permeation through and beyond the stratum corneum (epidermis, dermis, and reservoir solution) after 48 hours was significantly greater for Lipoderm than for Pluronic lecithin organogel (23.06% +/- 3.33 vs. 10.31% +/- 5.44), with the Student's t-test showing statistical significance (P less than 0.001). These data indicate that promethazine hydrochloride does penetrate into and through human ex vivo skin in vitro using Lipoderm and Pluronic lecithin organogel, with Lipoderm showing better results.
几年来，药剂师一直在使用诸如普朗尼克卵磷脂有机凝胶和Lipoderm等载体，通过皮肤来递送包括异丙嗪在内的药物。本研究采用有限剂量技术和弗兰兹扩散池，在体外人离体皮肤中评估了25mg/g盐酸异丙嗪在普朗尼克卵磷脂有机凝胶和市售基质Lipoderm中的经皮吸收药代动力学。由于盐酸异丙嗪的极性性质，理论上认为这种药物对这两种常用的配制剂基质会构成经皮挑战。将每种制剂5 μL/cm²的量应用于来自三名不同离体皮肤供体的皮肤的三个重复切片上。在给药后4、8、12、24、32和48小时，取出弗兰兹扩散池中的储库溶液并进行分析。基于进入储库溶液的总吸收量，Lipoderm的表现优于普朗尼克卵磷脂有机凝胶（2.86%±0.79对1.73%±0.85）（P小于0.2）。48小时后，Lipoderm透过角质层（表皮、真皮和储库溶液）的总渗透量显著高于普朗尼克卵磷脂有机凝胶（23.06%±3.33对10.31%±5.44），学生t检验显示具有统计学显著性（P小于0.001）。这些数据表明，使用Lipoderm和普朗尼克卵磷脂有机凝胶时，盐酸异丙嗪在体外确实能渗透进入并透过人离体皮肤，且Lipoderm显示出更好的结果。
