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目的:用巯基化羧甲基壳聚糖载醋甲唑胺纳米球制备滴眼剂,以派立明滴眼剂(Alcon)做对照,比较二者对家兔的降眼压作用。方法:将巯基化羧甲基壳聚糖为载体包裹醋甲唑胺得到载药纳米球,制备成滴眼剂,以桨法测定该制剂中醋甲唑胺体外释放情况;家兔眼局部用药,以压陷式眼压计测量法测定眼压变化。结果:在体外释放试验中,前6 h内醋甲唑胺从纳米球中快速释放出80%的药量,到9 h总共释放出约90%的药量。方程拟合以一级动力学方程拟合效果最好。1%醋甲唑胺纳米球滴眼剂降眼压效果在给药后1 h达峰值,其眼压变化值为(-3.69±0.0)mm Hg,之后降眼压效果逐渐减弱,持续时间为5 h。未见眼刺激性。结论:巯基化羧甲基壳聚糖载醋甲唑胺纳米球滴眼剂有明显降眼压效果。
OBJECTIVE: To prepare eye drops with sulfamidomecarbazolme acetate-loaded nanospheres and to compare the intraocular pressure (IOP) reduction of the two with Alconol. Methods: The drug-loaded nanospheres were coated with thiolated carboxymethyl chitosan as the carrier and the eye drops were prepared. The in vitro release of methadzamide was determined by paddle method. , To determine the change of intraocular pressure with a compression tonometer. Results: In the in vitro release test, methazolamide rapidly released 80% of the drug from the nanosphere within the first 6 hours and a total of about 90% of the dose was released by 9 hours. Equations fitted by the first-order kinetic equation fitted best. The intraocular pressure (IOP) of 1% metformin nanosphere eye drops peaked at 1 hour after administration, and the change of intraocular pressure was (-3.69 ± 0.0) mm Hg. The IOP decreased gradually and the duration was 5 h. No eye irritation. CONCLUSION: The thiolated carboxymethyl chitosan mesagotline nanometer spherical eye drops have a significant ocular hypotensive effect.