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分别以丙烯酸树脂压敏胶和硅酮压敏胶为基质制备托特罗定压敏胶分散型贴剂,结果采用硅酮压敏胶的制品中药物稳态渗透速率较高。又制备了以硅酮压敏胶为基质、含不同促透剂[月桂氮酮、N-甲基吡咯烷酮(NMP)、薄荷醇、油酸薄荷醇酯(M-OA)或庚酸薄荷醇酯(M-HEP)]的制品,结果促渗透作用由大到小依序为:M-OA>NMP>M-HEP,月桂氮酮及薄荷醇对托特罗定均无明显促透作用。大鼠药动学研究结果表明,空白组及加入M-OA的贴剂组大鼠稳态血药浓度(css)分别为0.69和0.97 g/ml;计算得相应的稳态血药浓度预测值(cssP)分别为0.60和0.93 g/ml,表明该制品具有良好的体内外相关性。
Respectively, acrylic pressure-sensitive adhesive and silicone pressure-sensitive adhesive as the base preparation of tolterodine pressure-sensitive adhesive dispersion patch, the results using silicone pressure-sensitive adhesive products in the drug steady state penetration rate higher. Also prepared a silicone pressure-sensitive adhesive as a matrix containing different permeation enhancers [Azone, N-methyl pyrrolidone (NMP), menthol, menthol oleate (M-OA) or heptyl heptanoate (M-HEP)]. The results showed that the promoting osmotic effect was M-OA> NMP> M-HEP in descending order. Azone and menthol had no obvious osmotolerance to tolterodine. Pharmacokinetic studies in rats showed that steady-state plasma concentration (css) was 0.69 and 0.97 g / ml for the blank group and the M-OA-added patch group, respectively, and the corresponding steady-state plasma concentration predictive value (cssP) were 0.60 and 0.93 g / ml, respectively, indicating that the product has good in vivo and in vitro relevance.