Carbopol 934p的亲水膨胀特性及其对曲尼司特缓释片释放行为的影响  

Study on the Hydrating and Swelling Properties of Carbopol 934p and Its Effect on Tranilast Release from the Matrices in Vitro

作　　者：王振国[1] 董皎 韩艳丽[1] 辛益妹[1] 

机构地区：[1]中国人民解放军空军航空医学研究所,北京100036

出　　处：《解放军药学学报》2000年第3期122-125,共4页Pharmaceutical Journal of Chinese People's Liberation Army

摘　　要：目的 :研究Carbopol 934p的凝胶特性及其对曲尼司特缓释片释放行为的影响。方法 :将纯辅料配方和Carbopol 934p为主要辅料的曲尼司特缓释片配方 ,在相同的条件下压片后 ,放入相同的介质中浸泡。采用称重法和体积测量法 ,研究其在不同pH环境、不同浸泡时间的水合度和溶胀度。结果 :辅料片在SGF和SIF中水合速率分别为 1.0 5 3h-1和 2 .75 6h-1,溶胀速率分别为 1.0 33h-1和 2 .45 1h-1,浸泡 5h时溶胀度分别为原有体积的 5 .87倍和 13 .0倍。曲尼司特缓释片在SGF中 ,0 .5h时迅速水合和溶胀 ;而在SIF中 ,5h内随着浸泡时间的增加 ,其重量和体积都缓慢增加 ,5h后重量稍有下降 ,体积基本不变。相同条件下 ,曲尼司特缓释片在人工胃液、人工肠液和梯度pH溶液中 ,10h的释放度分别为 0 .72 %、94.3%和 98.7%。结论 :水凝胶的形成速度和形态与介质的pH关系很大 ;Aim To study the hydrating and swelling properties of Carbopol 934p and its effect on tranilast release from Carbopol matrices.Methods Tablet press method was used to obtain the tranilast sustained release(SR) tablet matrices consisting of Carbopol 934p and small amounts of other excipients and the pure excipient tablets.These tablets were soaked in stimulated intestinal fluid(SIF,pH7.3) and stimulated gastric fluid(SGF,pH1.3) respectively and the weights and dimensions were measured using a gravimetric method and by a micrometer screw gauge during the hydrating and swelling process of the tablets.Results For pure excipient tablets,the hydrating rates were 1.053h -1 in SGF and 2.756h -1 in SIF;the swelling rates were 1.033h -1 in SGF and 2.451h -1 in SIF;at 5 hours the swelled volumes were 5.87 times larger in SGF and 13.0 times larger in SIF than the original volumes for tranilast SR tablets;the weight and dimension increased quickly at the first half hour in SGF and then remained constant;as in SIF,it increased slowly with the prolongation of the immersion within 5 hours and then its dimension remained constant.The extensions of dissolution of tranilast from the SR matrix tablets,to their perfect extent were 0.72%(in SGF),94.3%(in SIF) and 98.7%(in gradient pH) within 10 hours.Conclusion The extent and velocity of hydrating and swelling of matrix were affected by the pH of the dissolution medium and the time of immersion,and the swelling of Carbopol 934p is a rate limiting factor of tranilast release from the matrix.

关 键 词：Carbopol934p 水合作用 曲尼司特 释放度 

分 类 号：R974.3[医药卫生—药品] R944.9[医药卫生—药学]