多单元口崩脉冲控释片的研制.Ⅲ.盐酸地尔硫脉冲小丸口崩片的释药机制及其初步体内评价  

Preparation of Multiple-unit,Pulsatile Controlled-release Orally Disintegrating Tablets.Ⅲ.Release Mechanism and Preliminary in vivo Evaluation of Orally Disintegrating Tablets Containing Diltiazem Hydrochloride Pulsatile Controlled-release Pellets

作　　者：梁超峰 周焘 陈桐楷 郑映燕 钟国平[2] 

机构地区：[1]广州医药工业研究院,广东广州510240 [2]中山大学药学院,广东广州510006

出　　处：《中国医药工业杂志》2012年第12期1007-1011,共5页Chinese Journal of Pharmaceuticals

摘　　要：测定了3批盐酸地尔硫脉冲控释小丸口崩片的体外药物释放曲线,并采用不同的数学模型进行拟合,探讨其释药机制。结果表明,本品在4 h内的累积释放率低于10%,0～24 h的体外释放度用零级模型拟合效果较好,5～24 h的体外释放度用Higuchi模型拟合效果较好。并考察其与市售控释胶囊(Herbesser,参比制剂)在6名健康志愿者体内的药动学。结果表明,与参比制剂相比,本品在体内的释药较参比制剂推迟4～5 h,达到了预设的脉冲和控释效果。用Loo-Riegelman法计算本品体内吸收率,并与相应时间的体外释放数据进行线性回归,所得方程的相关系数为0.997 0,提示其体内外具有显著的相关性。The in vitro release curves of three batches of orally disintegrating tablets containing diltiazem hydrochloride pulsatile controlled-release pellets were drawn and different mathematical models were applied to fit above data so that the release mechanism was investigated. The results showed that the cumulative release during the first 4 h was below 10 %, the zero model and Higuchi model fit well with the release data during 0 - 24 h and 5 - 24 h, respectively. The pharmacokinetics of the orally disintegrating tablets in six health volunteers was investigated with the commercial controlled-release capsules （Herbesser） as the reference. The results showed that the product with the lag time of 4 - 5 h had an expected pulsatile and controlled release effect compared with reference preparation. The Loo-Riegelman method was used to calculate the in vivo absorption percentage, and linear regression was made with in vitro release data of corresponding time. The correlation coefficient was 0.997 0 of the regression equation. It revealed that there was a significant correlation between in vitro release and in vivo absorption.

关 键 词：盐酸地尔硫 脉冲控释小丸 口崩片 释药机制 药动学 体内外相关性 

分 类 号：R944.9[医药卫生—药剂学]