恩诺沙星固体分散体片的制备及体外溶出度的研究

Preparation and in Vitro Dissolution of Enrofloxacin Solid Dispersions

为了提高恩诺沙星在水中的溶解度、溶出度 ,加速内服药物的溶解、扩散、吸收 ,达到速效、高效的目的 ,以 PEG60 0 0等高分子材料为载体 ,制备恩诺沙星的固体分散体 ,分别测定固体分散体与原料药的溶解度以及固体分散体片剂与普通片剂的溶出度 ,恩诺沙星 - PEG60 0 0固体分散体的体外溶出度均达到 95%以上 ,而普通片剂 (自制 )为 50 %左右 ,市售片剂为 1 1 %左右。 ENRO在水中溶解度为 1 .0 2 58,而恩诺沙星 - PEG60 0 0 ( 1∶ 6)为 1 .873,恩诺沙星 - PEG60 0 0 ( 1∶ 1 2 )为3.859( 2 5℃ )。结果显示固体分散体能显著提高恩诺沙星的溶解度、溶出度 ,经方差分析 ( p<0 .0 1 ) 。

To improve the dissolution of enrofloxacin, enrofloxacin solid dispersions were prepared using coevaporation method with PEG 6000 and Urea as carriers,and its dissolution characteristics were studied in simulated gastric juice. In PEG 6000 enrofloxacin solid dispersion, enrofloxacin existed as fine crystalline. In vitro dissolution results showed that the higher carriers enrofloxacin ratio the faster drug dissolution. Statistical analysis showed significant difference between the dissolution of the drug and the solid dispersion. PEG 6000 is potent in improving the solubility and dissolution of enrofloxacin and has the potential for practical use.