正交实验优选苦参碱胃内漂浮颗粒的制备工艺

Optimization Preparing Procedures of Gastric Floating Granules Loaded with Matrine

目的制备苦参碱胃内漂浮颗粒,并对其性能进行研究。方法以羟丙基甲基纤维素(hydroxy propyl methylcellulose HPMC)、十八醇(octadecyl alcohol OA)为主要材料,采用L9(34)正交试验法优选制备工艺,对其漂浮性和释药特性进行评价。结果优选的最佳工艺为羟丙基甲基纤维素与总辅料的质量比:2:3;十八醇:7%;含0.8%的PEG-4000的包衣液乙基纤维素(ethyl cellulose,EC)浓度:4%;包衣增重:1:6。所制备的漂浮颗粒在12 h内具有明显的漂浮性,并呈现良好的缓释特性,释药过程符合一级动力学方程。结论该制剂有明显的胃内漂浮性和缓释效果,可作为胃部肿瘤治疗的给药剂型。

OBJECTIVE To prepare the gastric floating granules loaded matrine and to evaluate its properties. METHODS Using HPMC and octadecyl alcohol OA as major matrix, the optimal formulation of gastric floating granules loaded matrine was selected by L9（34） orthogonal design. Also, the two main properties of cumulative release and floating ability were comprehensively considered. RESULTS The optimum preparing procedures for this granules were followed as 2 ： 3 HPMC, 7% OA, 4% coating EC contained 0.8% PEG-4000, and coating weight gain approaching 1 ： 6. The granules presented satisfactory sustained release characteristics within 12 h in vitro, and occupied a significant floating characteristic, the release behavior followed with first-order kinetics. CONCLUSION The granules showed sustained release effect and floating ability. This nroduct could be used as a new theraneutic dosage form for stomach tumor.