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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 drug release curves of three batches of diltiazem hydrochloride controlled-release Xiaowan Orally Disintegrating Tablets were determined and fitted with different mathematical models to investigate their drug release mechanism. The results showed that the cumulative release rate of this product within 4 h was less than 10%. The in vitro release of 0-24 h was better fitted with the zero-order model, and the in vitro release of 5-24 h fitted with the Higuchi model better. Pharmacokinetics in six healthy volunteers were compared with that of a commercially available controlled release capsule (Herbesser, reference formulation). The results showed that compared with the reference formulation, the release of this product in vivo was delayed 4 ~ 5 h compared with the reference formulation, reaching the preset pulse and controlled release effect. The in vivo absorption rate was calculated by Loo-Riegelman method, and was linearly correlated with the in vitro release data at the corresponding time. The correlation coefficient of the equation was 0.997 0, suggesting a significant correlation in vitro and in vivo.