甲磺酸沙喹那韦三甲基壳聚糖微球的制备

Preparation of Saquinavir Mesylate Loaded N-trimethyl Chitosan Microspheres

为了提高甲磺酸沙喹那韦的生物利用度,制备了甲磺酸沙喹那韦三甲基壳聚糖微球并考察其体外溶出度。用喷雾干燥法制备甲磺酸沙喹那韦三甲基壳聚糖微球,用红外光谱进行鉴定,采用PBS7.4缓冲液和0.1 mol/L盐酸溶液考察微球的体外药物释放速率,用HPLC法检测药物浓度。结果显示,制备得到的甲磺酸沙喹那韦三甲基壳聚糖微球在体外近中性及酸性条件下能够持续释放,无突释现象。甲磺酸沙喹那韦三甲基壳聚糖微球有利于口服给药后,药物的持续释放。

In order to improve the bioavailability of saquinavir mesylate,saquinavir mesylate loaded N-trimethyl chitosan microspheres was prepared and their vitro dissolution was studied. Saquinavir mesylate loaded N- trimethyl chitosan microspheres was prepared by spray drying. The formation of microspheres were confirmed by infrared spectroscopy（ IR）. The drug release rate of microspheres was studied in P BS7. 4 buffer or 0. 1 mol/L hydrochloric acid solution in vitro,and drug concentrations were detected by HP LC. Results showed that saquinavir mesylate loaded N- trimethyl chitosan microspheres was prepared,which released saquinavir mesylate in neutral and acidic conditions continuously in vitro,without any sudden release. Microspheres were suitable for gastrointestinal drug delivery.