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采用前体脂质体技术提高缬沙坦的口服生物利用度。采用薄膜水化法制备了磷脂∶药物∶胆固醇比例不同的前体脂质体,并考察其粒径、包封率、形态、体外释药、体外渗透性和体内药动学等特性。优化所得的前体脂质体粒径为(364.1±14.9)nm,包封率(95.6±2.9)%。采用透析袋法考察了优化制品与原料药混悬液在模拟胃液(pH 1.2)和纯水中的释放行为,结果优化制品在2种介质中12 h的累积释放率均较高。分别采用平行人工
Use of liposomal precursor technology to increase the oral bioavailability of valsartan. The precursor liposomes with different proportions of drug and cholesterol were prepared by the membrane hydration method. The particle size, encapsulation efficiency, morphology, in vitro drug release, in vitro permeability and in vivo pharmacokinetics were also investigated. The optimized liposome size was (364.1 ± 14.9) nm and encapsulation efficiency (95.6 ± 2.9)%. The dialysis bag method was used to investigate the release behavior of the optimized products and API suspensions in simulated gastric fluid (pH 1.2) and pure water. The results showed that the cumulative release rate of optimized products in both media was high at 12 h. Respectively using parallel artificial