磷酸川芎嗪膜控骨架缓释片的研制

目的 :以磷酸川芎嗪为模型药物 ,用乙基纤维素 -壳聚糖混合包衣液对其骨架片进行包衣 ,制备磷酸川芎嗪膜控骨架缓释片 ,以达到对该水溶性药物理想的缓释作用。方法 :用正交设计优选处方 ,以羟丙基甲基纤维素 (HPMC K1 0 0 M)为骨架材料 ,采用湿法制粒压片制备磷酸川芎嗪骨架片 ,用乙基纤维素 -壳聚糖混合包衣液进行包衣处理 ,以调节药物释放速度。用紫外分光光度法在2 95 nm测定吸收度 A来测主药含量 ,根据中国药典 2 0 0 0年版释放度测定法中转篮法测定其体外释放度 ,并对其稳定性作初步考察。结果 :所制备的薄膜包衣缓释片在 12 h内呈现良好的缓释特征 ,符合 Higuchi方程 ,Q=0 .0 95 3 t1 /2 -0 .0 3 87(r=0 .9874) ,且对湿、光、热稳定性良好。结论 :水不溶性材料乙基纤维素和水溶性材料壳聚糖 ,以适当比例混合使用作为包衣材料 ,结合骨架材料 ,对水溶性较大的药物能起到理想的缓释效果。

Studies on Tetramethylpyrazine Sustained-release Matrix Tablets Combined with Blending Coating Materials of Ethylecllulose and Chitosan

Objective: To prepare tetramethylpyrazine phosphate matrix tablet and the tablet was coated with blending solution of ethylcellulose and chitosan. To evaluate in vitro release of this dosage form. Method: Orthogonal design was utilized to choose the best formula. To prepare HPMC hydrogel matrix tablet. Tetramethylpyrazine phosphate was used as model drug. And the tablet was coated with blending solution of ethylcellulose and chitosan to improve sustained-release effect. The concentration of the drug was determined by UV spectrophotometry at 295nm, in vitro release of this dosage form was determined by rotating basket (according to 2000 Chines Pharmacopoeia). Moreover, study on the stability of the tablet. Results: Tetramethylpyraxine phosphate sustained-release tablet showed obvious sustained release effect. The dissolution could be described by Highuchi equation Q=0.0953t\+\{1/2\}-0.0387(r=0.9874). The quality of the tablet was stable at the testing condition. Conclusins: Employed as coating materials, the blending solution of hydrophilic chitason and hydrophobic ethylcellulose could be used as an ideal sustained-release coating material for water-soluble drugs combined with matrix matrials.