罗替戈汀压敏胶分散型贴剂的制备及质量评价  

Preparation and Quality Evaluation of Drug-in-adhesive Patches of Rotigotine

作　　者：李燕[1] 赵利刚[2] 彭宏峰[3] 王慧丽[1] 吕立勋[2] 

机构地区：[1]唐山市妇幼保健院药剂科,河北唐山063000 [2]河北联合大学药学院,河北唐山063000 [3]河北联合大学口腔医学院,河北唐山063000

出　　处：《中国医药工业杂志》2015年第6期601-605,共5页Chinese Journal of Pharmaceuticals

基　　金：河北省自然科学基金石药联合基金"α-萜品醇脂肪酸酯类衍生物经皮促透作用的可逆性及其机理研究"(H2013209098)

摘　　要：制备了含不同促透剂[月桂氮酮、油酸、N-甲基吡咯烷酮(NMP)、薄荷醇、萜品醇、庚酸薄荷醇酯(M-HEP)或油酸薄荷醇酯(M-OA)]的罗替戈汀压敏胶分散型贴剂。采用双室扩散池,以离体大鼠皮肤为屏障进行体外渗透试验,考察了压敏胶和促透剂的种类及浓度对贴剂中药物渗透行为的影响。结果表明,以丙烯酸树脂压敏胶Duro-Tak 87-2677为基质,3%M-OA与10%NMP联用时贴剂中罗替戈汀的累积透过量较高且无释放时滞。初步稳定性考察结果表明,该制品在30℃、相对湿度60%环境放置6个月,黏附性和透皮性能无显著改变。市售制剂Neupro(规格2.4 mg/10 cm2)和自制品(规格5 mg/10 cm2)的24 h累积透过量为(254.34±46.16)和(499.36±53.27)?g/cm2。The drug-in-adhesive patches of rotigotine with azone, oleic acid, N-methylpyrrolidone （NMP）, menthol, terpineol, 2-isopropyl-5-methylcyclohexyl heptanoate （M-HEP） or （E）-2-isopropyl-5-methylcyclohexyl octadec-9-enoate （M-OA） as penetration enhancer were prepared, respectively. The in vitro permeability test was carried out with two-chamber cells and excised rat skin to investigate the effects of pressure sensitive adhesives （PSA） and enhancers on permeation behavior of the drug in patches. The results showed that the optimal patches with Duro-Tak 87-2677 as the matrix and combined enhancers of 3 % M-OA and 10% NMP had a higher penetration amount and no time lag in release. The results of preliminary stability study showed that the adhesion and in vitro transdermal property of the product stored at 30 ~C and relative humidity of 60% for 6 months had no significant changes. The penetration amounts at 24 h of the commercial patches （Neupro, 2.4 mg/10 cm2） and the self-made patches （5 mg/10 cm^2） were （254.344±46.16） and （499.364±53.27） μg/cm^2.

关 键 词：罗替戈汀 压敏胶分散型贴剂 体外透皮 促透剂 制备 质量评价 

分 类 号：R944.9[医药卫生—药剂学]