泼尼松择时释放片的制备及其体内外评价
Preparation and evaluation of Prednisone modified-release tablets in vitro and in vivo
作者：范晓茹;邓杰;宗太丽;姜和;
Author：
收稿日期： 年卷（期）页码：2017,32(02):-139-142
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：泼尼松;风湿性关节炎;择时释放片;延迟释放;压制包衣;LC-MS/MS;药动学
Key words：
基金项目：
中文摘要
目的制备泼尼松择时释放片,评价其体内外的释药。方法采用水不溶性包衣材料,干法压制包衣制备泼尼松择时释放片,用HPLC法测定泼尼松体外释放度,LC-MS/MS测定Beagle犬随机交叉口服单剂量泼尼松择时释放片与泼尼松普通速释片后血浆中泼尼松的浓度,计算药动学参数。结果所制泼尼松择时释放片的体外时滞时间为4~5 h,时滞后药物可达到0.5 h内释放大于85%的爆破型脉冲释药效果。受试制剂与参比制剂泼尼松在Beagle犬体内的AUC_(0-t)分别为62.01±3.57、59.96±2.72 ng·mL~(-1)·h;AUC_(0-∞)分别为63.35±3.51、62.76±3.27ng·mL~(-1)·h;t_(1/2)分别为1.00±0.16、1.22±0.54 h;T_(max)分别为4.67±0.26、0.97±0.30 h;C_(max)分别为27.84±3.03、28.05±1.94 ng·mL~(-1);T_(lag)分别为3.83±0.26、0 h。结论犬体内外的结果均证明该制剂具有延迟释放特性,其设计方案可行。
参考文献
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