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目的:测定1%三苯氧胺(TAM)在3种软膏基质中的体外透皮释放,评价三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,λ=235nm处UV测定.结果:在凡士林(Vaseline),聚乙二醇类(PEG)和聚羧乙烯(Carbopol)三种基质中TAM的渗透系数分别在0,1.0677和1.2769μg/(Cm~2h),在24h和46h时的累积释放量分别为0,31.87μg/cm~2和23.48μg/cm~2及0,54.63μg/cm~2和52.44μg/cm~2.结论:TAM在水溶性软膏基质PEG和Carbopol的渗透及释放都优于凡士林软膏基质.
OBJECTIVE: To determine the in vitro transdermal delivery of 1% tamoxifen (TAM) in three ointment bases and evaluate the effects of three ointment bases on the transdermal penetration of the drug.Methods: Franz diffusion cell at λ = 235 nm.Results: The permeation coefficients of TAM in Vaseline, PEG and Carbopol were 0, 1.0677 and 1.2769μg / (Cm ~ 2h), and the cumulative release amounts were 0, 31.87μg / cm ~ 2 and 23.48μg / cm ~ 2 and 0, 54.63μg / cm ~ 2 and 52.44μg / cm ~ 2 at 24h and 46h, respectively. CONCLUSION: TAM is superior to petrolatum ointment in the penetration and release of water-soluble ointment base PEG and Carbopol.