【摘要】 目的通过制备溶菌酶眼用凝胶制剂提高溶菌酶的稳定性,延长溶菌酶与眼部的作用时间。方法按照部颁标准测定了溶菌酶活性,通过对基质的筛选,确定了最优处方及工艺,考察了溶菌酶眼用凝胶剂的基本性质如:黏度、表面张力、渗透压、体外释放、稳定性,以及眼用凝胶剂的体外抑菌性。结果以质量分数1%HPMC K4M为凝胶基质,制备的溶菌酶眼用凝胶剂的黏度为95.83 m Pa·s,表面张力为39.696 m N·m-1,渗透压为277 m Osm·kg-1,p H为6.56,效价为10 300 U·m L-1,溶菌酶凝胶剂体外释放5 h时,累计释放率接近100%。溶菌酶眼用凝胶剂对革兰氏阳性菌抑菌效果较好,而对革兰氏阴性菌抑菌效果较差。加速试验和长期稳定性试验表明该制剂性质稳定。结论制备的溶菌酶眼用凝胶制剂相关性质均符合眼用制剂标准。更多还原

【Abstract】 Objective To prepare ocular gel formulationwith improvedstability of lysozyme and prolonged residence time of lysozyme on cornea. Methods The activity of lysozyme was determined according to the method listed in Drug Standard of Ministry of Public Health of the People ’s Republic of China. The prescription and preparation technique was optimized by selecting the matrixes. We also studied the viscocity,surface tension,osmotic pressure,cumulative release,stability and antibacterial activity of lysozyme ocular gel. Results We chose 1% HPMC K4 Mas gel matrix. The result stated that the gel had a homogeneous transparent appearance,along with the viscosity of 95. 83 m Pa·s,the surface tension of39. 696 m N·m- 1,the osmotic pressure of 277 m Osm ·kg- 1,the p H of 6. 56 and the potency of10 300 U·m L- 1. A nearly complete accumulative release in vitro could be reached in 5 h. The result of in vitro antibacterial experiments revealed that the lysozyme ophthalmic preparation had better antibacterial effect against Gram-positive bacteria than Gram-negative bacteria. Studies on accelerated stability test and long-term stability test illustrated that the lysozyme ocular gel was stable over storage. Conclusions The lysozyme ocular gel is completely qualified according to the standard of ophthalmic preparation.更多还原