盐酸奥昔布宁透皮贴剂的制备及体内外评价  

Preparation and Evaluation of Oxybutynin Hydrochloride Transdermal Patches

作　　者：朱壮志[1] 张晓红[1] 罗华菲[1] 马建芳[1] 王浩[1] 

机构地区：[1]中国医药工业研究总院药物制剂国家工程研究中心,上海201203

出　　处：《中国医药工业杂志》2013年第1期36-40,共5页Chinese Journal of Pharmaceuticals

基　　金：国家"重大新药创制"科技重大专项(2012ZX09304004)

摘　　要：采用溶媒挥发法制备了盐酸奥昔布宁骨架型透皮贴剂。体外透裸鼠皮肤试验表明,该贴剂能维持72 h稳定释药,透皮速率与上市产品Oxytro1相比无显著性差异。测得制品中药物含量为(36.0±0.7)mg,在pH 5.8磷酸盐缓冲液中于24 h内基本释放完全,并且具有较好的含量均匀度和黏附性能。以Oxytro1为参比制剂,考察了自制贴剂在大鼠体内的药动学行为。结果表明自制贴剂给药后能在72 h内维持较恒定的血药浓度,平均相对生物利用度为102.7%。A novel drug-in-adhesive transdermal patch system for oxybutynin hydrochloride was prepared by solvent evaporation method. The results of in vitro permeation test through nude mouse skin showed that the transdermal patches could release for 72 h. The percutaneous rates of oxybutynin between the prepared patches and Oxytrol had no significant difference. The content of oxybutynin hydrochloride in the product was （36.0±0.7） mg and the drug could completely release in pH 5.8 phosphate buffer within 24 h. The product also showed good content uniformity and adhesive performance. The pharmacokinetics of the product in rats was investigated with Oxytrol as the reference preparation. The results showed that the product could maintain the constant plasma concentration within 72 h. The average relative bioavailability was 102.7 %.

关 键 词：盐酸奥昔布宁 透皮贴剂 体外评价 药动学 

分 类 号：R944.9[医药卫生—药剂学]