两种卡泊三醇软膏的体外经皮吸收比较

目的:比较两种不同厂家生产的卡泊三醇软膏(样品A和样品B)的体外透皮吸收情况,并与卡泊三醇搽剂进行比较。方法:采用改良Franz扩散池,小型猪离体皮片分别涂样品A、B和卡泊三醇搽剂(以主药计均为5μg),于给药后2、4、6、8、10、12 h吸取接收液,药物接触的皮片用稀释剂提取。采用高效液相色谱法测定接收液和提取液中卡泊三醇的含量,计算卡泊三醇的皮片保留量、透过百分率和吸收百分率。结果:样品A、B和卡泊三醇搽剂中卡泊三醇在皮片内的保留量分别为(1 519.07±655.88)、(605.83±235.33)、(2 897.29±723.89)ng/g;吸收百分率平均值分别为3.21%、1.25%、6.69%,三者比较差异具有统计学意义(P<0.05);透过百分率均低于0.36%。结论:样品A、B的经皮行为具有明显差异,其中样品A的生物利用度较好。

Comparison of Transdermal Absorption of 2 Kinds of Calcipotriol Ointment in vitro

OBJECTIVE： To compare the transdermal absorption in vitro of 2 kinds of Calcipotriol ointment （sample A and B） from different manufacturers, and compare with Calcipotriol liniment. METHODS： Using modified Franz diffusion cell method, isolated skin of miniature pig was treated with sample A, sample B or Calcipotriol liniment （all 5 μg by main components）, and then absorbed receptor fluid 2, 4, 6, 8, 10, 12 hours after administration; the treated skin was extracted with diluents. HPLC method was adopted to determine the content of calcipotriol in receptor liquid and extract solution. The retention volume, permeation percentage and absorption percentage of calcipotriol were all calculated. RESULTS： The retention volume of calcipotriol from sample A and B and Calcipotriol liniment in skin were （1 519.07 ± 655.88） ng/g, （605.83 ± 235.33） ng/g and （2 897.29 ± 723.89） ng/g, respectively. The average absorption percentages were 3.21%, 1.25 % and 6.69 %, respectively; there was statistical significance （P〈0.05）. The permeation percentages were all lower than 0.36%. CONCLUSIONS： The transdermal potential of sample A and B have significant difference, and sample A is good in bioavailability.