控释制剂释放动力学评价理论研究

Novel evaluation theories of kinetics for controlled-release drug delivery systems

目的:建立控释制剂释放动力学的评价新理论和模型。方法:针对控释制剂具有零级释放动力学基本特征,结合控释制剂释放度及其变化速率的曲线特征,阐明控释制剂释放动力学评价的原理。采用新建立的模型,评价市售非洛地平渗透泵片在不同转速下的控释特征。结果:依据控释制剂释放动力学原理,提出控释度(ICR)、早期释放差异指数(IR-Di)、末端释放差异指数(IRDt)等指标。非洛地平渗透泵片在75,100,150r/min时的体外ICR分别为70.8%,74.8%和64.2%;IRDi和IRDt定量反映了测定因素转速对非洛地平渗透泵片的控释特征的影响。结论:本文提出的控释制剂释放动力学评价理论,可以对控释制剂的不同释放阶段及整体的控释动力学进行定量评价,相关参数为剂型定量设计和优化提供了方法学基础。

Aim：To study the theory and kinetic modeling for the release characteristics of the controlled-release drug delivery systems. MethodS：On the basis of the zero-order release kinetics, the principles and models were established focusing on the characteristics of the release profile and its differential function. The controlled-release kinetics of felodipine osmotic drug delivery systems were assessed using this method as an illustration. Results： The including index of controlled release （ICR）, index for release difference of the initial phase （IRDi） and index for release difference of the terminal phase （IRDt）, were established. The results indicated their utility in the quantification of the release difference of the felodipine osmotic drug delivery system as a function of the rotation speeds. ICRs approached 70, 8%, The new approach is 74.8%, and 64.2% at the rotation speed of 75,100 and 150 r/min, respectively. Conclusion： effective in the evaluation of the release kinetics of different release phases as well as a whole profile in the quantitative design of the controlled-release drug delivery systems.