摘要
以聚丙烯酸钠及聚乙烯吡咯烷酮为凝胶基质,以维生素E为透皮吸收促进剂制备标题化合物。采用紫外分光光度法测定西咪替丁含量;以剥离强度和黏着力为检测指标,通过单因素和正交实验优选标题化合物的最优处方;而后对其进行体外性能研究。标题化合物较优处方(质量百分比)为:5.5%聚丙烯酸钠、0.15%聚乙烯吡咯烷酮、1.4%氢氧化铝、1.2%羧甲基纤维素钠、1.5%酒石酸、30%甘油、1%维生素E和1.5%西咪替丁;固化温度为50℃,固化时间为2 h。此时其24 h的药物累积释放率为23.65%,26 h药物累积透皮渗透量达1 010.22μg/cm2。结果表明,以聚丙烯酸钠/聚乙烯吡咯烷酮基为高分子骨架的水凝胶基质易于涂布,涂布后有足够的强度,适合用作贴剂的水凝胶基质;含有1%维生素E的标题化合物中药物具有很好的小鼠皮肤透过性。标题化合物是一种具有发展潜力的新剂型。
To prepare cimetidine hydrogel patch and assess the quality. Cimetidine hydrogel patch for target medication were prepared using sodium polyacrylate / polyvinylpyrrolidone polymer with good biocompatibility as skeleton material of hydrogel and vitamin E as the skin penetration enhancer. The drug content was determined by ultraviolet（ UV） spectrophotometer. The prescription of cimetidine hydrogel patch was designed by single factor and orthogonal experiments with gel strength and initial adhesion as testing index. The quality of cimetidine hydrogel patch was assessed by the cimetidine skin permeability and release in vitro. The results indicated that the optimal prescription of cimetidine hydrogel patch（ mass percent） was as following： sodium polyacrylate5. 5%,aluminum hydroxide 1. 4%,sodium carboxymethyl cellulose 1. 2%,tartaric acid 1. 5%,polyvinylpyrrolidone 0. 15%,glycerol 30%,vitamin E 1% and cimetidine 1. 5%,curing temperature 50 ℃,curing time 2 h. Approximately 23. 65% cimetidine was released from hydrogel patch within 24 h. Drug cumulative transdermal osmotic quantity was 1 010. 22 μg / cm2 after 26 h. Sodium polyacrylate / polyvinylpyrrolidone polymer based hydrogel patch is easy to coat and has enough strength,indicating that sodium polyacrylate / polyvinylpyrrolidone polymer is suitable as hydrogel matrix. The cimetidine hydrogel patch containing 1% vitamin E possesses excellent drug skin permeability. Thus,cimetidine hydrogel patch is a new potential formulations.
出处
《化学试剂》
CAS
北大核心
2015年第9期785-790,794,共7页
Chemical Reagents
基金
国家级大学生创新基金资助项目(201310595025)
