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目的:马来酸噻吗洛尔眼用脂质体的研制。方法:采用硫酸铵梯度法结合pH调节法制备马来酸噻吗洛尔脂质体并对其理化性质进行考察;以马来酸噻吗洛尔滴眼液为对照,用改进的Franz立式扩散池进行兔离体角膜渗透性实验,计算渗透参数。结果:以硫酸铵梯度法结合pH调节法制备的脂质体包封率为(93.01±2.09)%,平均粒径为187nm,脂质体的稳态流量和表观渗透系数是滴眼剂的2.19倍。结论:采用硫酸铵梯度法结合pH调节法制备的马来酸噻吗洛尔脂质体包封率较高,制备成脂质体后能够提高马来酸噻吗洛尔的角膜渗透性。
Objective: To study the preparation of liposomes for timolol maleate. Methods: The timolol maleate liposomes were prepared by ammonium sulfate gradient method combined with pH adjusting method. The physical and chemical properties of timolol maleate liposomes were investigated. Taking timolol maleate eye drops as control, The proliferation of rabbit in vitro corneal permeability test, calculate the infiltration parameters. Results: The liposome encapsulation efficiency was (93.01 ± 2.09)% and the average particle size was 187 nm. The steady state flow rate and apparent permeability coefficient of liposomes were 2.19 times. CONCLUSION: The entrapment rate of timolol maleate liposome prepared by ammonium sulfate gradient method and pH adjusting method is high, and the preparation of liposomes can improve the permeability of timolol maleate.