沈阳药科大学学报

2001, (05) 324-326+380

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释放分割法体外评价释放特征符合Higuchi方程的缓释制剂药物动力学
The Release-Division method:a novel in vitro pharmacokinetic evaluation method for the sustained release dosage forms with a release profile characterized by the Higuchi equation

张继稳,钟大放,毕殿洲
ZHANG Ji wen; ZHONG Da fang; BI Dian zhou (College of Pharmacy;

摘要(Abstract):

提出一种Higuchi释放缓释制剂药物动力学体外评价方法 ,将Higuchi释放以高斯 牛顿法分割成零级释放、一级释放和速释部分 ,每部分释放对体内药物动力学的贡献值则通过经典的药物动力学计算获得。方法学研究证明了释放分割法与基于零级释放药物动力学的剂量分割法效果相当 ,释放分割法计算得到的血药浓度 (CRD)与剂量分割法计算得到的血药浓度 (CDD)间的相关方程为CDD=-0 2 5 88+1 0 1 4CRD(r=0 993 6)。由于任意Higuchi释放曲线可以通过归一化的Higuchi释放曲线线性化表达 ,所以归一化Higuchi释放曲线的分割系数可作为非归一化的Higuchi释放的体外评价的模数。释放分割法可以对制剂的体外释放行为进行经济的评价 ,适用于缓释制剂的处方筛选、体内外相关性研究等
A novel in vitro pharmacokinetic method was established to evaluate the sustained release systems characterized by the Higuchi equation. The normalized Higuchi release profile was divided into parts of typical zero order release, first order release and instant release by the Gauss Newton method, the pharmacokinetic behavior of each part was predictable by traditional pharmacokinetics. The methodology studies showed that the Release Division method was identical to the Dose Division method. The expectance of the plasma levels obtained by the Dose Division method ( C DD ) and that obtained by the Release Division method ( C RD ) were well correlated ( C DD = -0 258 8 + 1 014 C RD , r = 0 993 6 ). Since any Higuchi release is linear to the normalized Higuchi release, the release division to the normalized Higuchi release will be the essential Mode Number to the Higuchi releases. The Release Division method is possibly an economic way for the formula and the production process optimization and validation, and might be utilized in the in vivo in vitro correlation analysis.

关键词(KeyWords): 缓释制剂;释放分割法;剂量分割法;药物动力学;释放度;Higuchi方程
sustained release systems; Release Division method; Dose Division method; pharmacokinetics; release; Higuchi equation

Abstract:

Keywords:

基金项目(Foundation): 国家自然科学基金资助项目 (3 993 0 1 80 )

作者(Authors): 张继稳,钟大放,毕殿洲
ZHANG Ji wen; ZHONG Da fang; BI Dian zhou (College of Pharmacy;

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