摘要
目的探讨依那普利的口颊黏膜给药系统的制备。方法使用粘膜粘附性多聚物、通过溶剂涂布技术,将依那普利配制成口腔贴膜的形式,同时在体外释放研究和透过性研究中评价了其多种理化特点。结果所有配方均显示有高的药物百分含量(96.45%至98.49%)。有良好膨胀特性的配方显示有良好的驻留时间。在体外,发现包括贴膜(F2)在内的高粘性羧甲纤维素钠(SCMC-HV)的药物释放率最高(药物释放很快,在1.5小时内释放92.24%)、其次是贴膜F4(含有聚乙烯吡咯烷酮K-90 1%w/v个SCMC(HV)1%w/v)。研究发现,在10小时结束时,F2和F4的活体外药物穿透率分别为82.24%和89.90%。结论根据最高的膨胀度、最高的驻留时间和最长体外驻留时间选择将配方F4用于构建口颊贴膜,可用于对心血管病的治疗。
Objective To study the preparation of buccal mucosa delivery systems of enalapril. Methods Using solvent coating technology and mucous membrane adhesive polymer,enalapril were prepared in forms of buccal mucoadhesive films.Meanwhile,their various physical and chemical characteristics were evaluated in release and permeability studies in vitro. Results All formulas showed high percentage composition of drug（ 96. 45 ~ 98. 49%）. The formula with good expansion characteristics displayed favorable residence time. In vitro,the rate of drug release in sodium carboxymethyl cellulose with high viscosity（ SCMC-HV）,including mucoadhesive film（ F2）,was the highest（ fast drug release,with 92. 24% in 1. 5 hours）,followed by mucoadhesive film F4（ containing polyvinylpyrrolidone K-90 1% w / v,SCMC（ HV） 1% w / v）. It was found that by the end of 10 hours,drug penetration rate of F2 and F4 in vitro were 82. 24% and 89. 90% respectively. Conclusions In view of the highest degree of expansion,the maximum absorption and the longest residence time in vitro,the formula F4 was adopted in the preparation of buccal mucosa delivery system,which could be applied in the treatment of cardiovascular disease.
作者
贺文帅
赵兴胜
南景龙
鲁亚南
温霞
蔡佳飞
HE Wen-shuai ZHAO Xing-sheng NAN Jing-long et al(Inner Mongolia People＇s Hostipal. Inner Mongolia 010017, China)
出处
《心脑血管病防治》
2016年第4期267-269,272,共4页
CARDIO-CEREBROVASCULAR DISEASE PREVENTION AND TREATMENT
关键词
依那普利
口颊黏膜
制备
Enalapril
Buccal mucosa
Preparation
