他莫昔芬软膏在3种基质中的体外透皮释药比较

Comparison of percutaneous release of tamoxifen ointment in three stromata in vitro

目的 :测定 1%他莫昔芬在 3种软膏基质中的体外透皮释放 ,评价 3种软膏基质对主药经皮渗透的影响。方法 :以人离体皮肤为渗透释药模型 ,试验用Franz扩散池 ,2 35nm处UV测定。结果 :在凡士林、聚乙二醇和聚羧乙烯 3种基质中他莫昔芬的渗透系数分别为 0 ,( 1.0 6± 0 .2 1)和 ( 1.2 8± 0 .2 0 ) μg/ (cm2 ·h) ,在 2 4h和 46h时的累积释放量分别为 0 ,( 31.9± 2 .4)和 ( 2 3.5± 2 .9) μg/cm2 及0 ,( 5 5± 3)和 ( 5 2± 4) μg/cm2 。结论

AIM: To determine the percutaneous release of 1% tamoxifen (Tam) in three different stromata in vitro, and evaluate the affection of the treansdermal permeation of Tam from the three stromata in vitro. METHODS: The Franz diffusion cell was applied, and the samples was measured by UV(235 nm). RESULTS: In the different stromata of vaseline, PEG and carbopol, the permeation coefficient of Tam were 0, ( 1.06 ± 0.21 ) and ( 1.28 ± 0.20) μg/(cm 2·h), respectively. The cumulative amounts of release were 0, (31.9±2.4) and (23.5±2.9) μg/cm 2 in 24 h, and 0, (55±3) and (52±4) μg/cm 2 in 46 h, respectively. CONCLUSION: Hydrophilic ointment stromata for Tam, such as PEG and carbopol were better than vaseline stromata in the percutanous release.