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目的:研制酮洛芬(KPF)脂质体凝胶,并进行体外经皮渗透动力学研究。方法:通过均匀实验设计筛选KPF脂质体的最佳处方,采用薄膜分散法制备脂质体,再以泊洛沙姆-407为基质制成脂质体凝胶;以影响因素试验考察该制剂的稳定性,并用Franz扩散池研究KPF脂质体凝胶与KPF普通凝胶的经皮渗透规律。结果:KPF脂质体平均粒径为(886.2±12.08) nm,Zeta电位为(-15.05±2.36)mV,平均包封率为(76.13±1.27)%(n=3);KPF脂质体凝胶为类白色细腻粘稠胶体,对试验光照及温度条件稳定。体外透皮试验表明脂质体能促进药物的透皮吸收,脂质体凝胶在皮肤中的蓄积量为普通凝胶的2倍。结论:KPF脂质体凝胶制备工艺可行,质量稳定,检测方法可靠,能促进药物透皮渗透,值得进一步研究。
OBJECTIVE: To develop ketoprofen (KPF) liposome gel and investigate the in vitro percutaneous permeability kinetics. Methods: The optimum formulation of KPF liposomes was screened through uniform experimental design. The liposomes were prepared by the method of film dispersion and pololimus gel was made with Poloxamer-407 as the substrate. The stability of KPF liposome gel and KPF gel were studied by Franz diffusion cell. RESULTS: The average particle size of KPF liposomes was (886.2 ± 12.08) nm and the zeta potential was (-15.05 ± 2.36) mV, the average encapsulation efficiency was (76.13 ± 1.27)% (n = 3) Gum as a class of white viscous gel, the test light and temperature conditions stable. In vitro transdermal experiments showed that liposomes can promote the transdermal absorption of the drug, and the volume of the liposome gel in the skin is twice that of the ordinary gel. Conclusion: KPF liposome gel preparation process is feasible, stable quality, reliable detection method, can promote drug transdermal penetration, worthy of further study.