延胡索乙素单层渗透泵片的制备及体外评价

Preparation and in Vitro Evaluation of Tetrahydropalmatine Monolayer Osmotic Pump Tablets

为了提高难溶性药物—延胡索乙素(THP)的生物利用度,本研究运用了固体分散体技术来提高THP的溶解度,并通过泡腾技术为渗透泵片提供释药源动力,同时综合运用渗透泵技术来制备延胡索乙素单室单层渗透泵片(简称"THP"渗透泵片),然后通过单因素实验来考察和确定最佳的处方工艺,并对最佳处方工艺的体外释药曲线进行模型拟合.结果显示:助悬剂的种类、致孔剂的种类和用量、包衣增重、释药孔径对THP渗透泵片的释药行为有较大影响,而增塑剂用量及桨转速对THP渗透泵片的释药行为无显著影响;实验结果同时还表明:依据最佳处方工艺制备的THP渗透泵片有明显的零级释放特征,r=0.994 7,符合控释制剂的要求.研究表明,THP渗透泵片的制备方法安全可靠,工艺简单,适合工业化生产,本方法为其他难溶性药物渗透泵片的制备提供了新的思路与研究途径.

In order to improve the biodiversity of the insoluble drug tetrahydropalmatine （THP）, solid dispersion technology was used to improve the solubility of THP, and the effervescent technology was used for the osmotic pump to provide drug release power. The integrated use of osmotic pump technology was used to prepare tetrahydropalmatine monolayer osmotic pump tablets （THP osmotic pump tablets）. The single factor experiment was performed to obtain the best prescription technique, and the in vitro release curve of the best prescription was modeled. The results showed that the type of suspending agent, the type and amount of porogen, the weight of coating and the release pore size affect the release behaviour of THP osmotic pump tablets greatly, however, the amount of plasticizer and the speed of propeller had no significant effects on the release behaviour of THP osmotic pump tablets. There were obvious zero-order release characteristics of the THP osmotic pump tablets prepared by best prescription process, r =0. 9947, which meet with the requirements of controlled release preparation. The conclusion can be drawn that the production method of THP osmotic pump tablets is safe and reliable, simple and suitable for industrial production, and the method provides new ideas and research stratdgy for the preparation of other insoluble drug osmotic pump tablets.