中文摘要：

目的 制备羟丝肽（JBP 485）口服微乳,并考察其形态、稳定性及体内药动学性质.方法采用伪三元相图绘制法来筛选JBP 485微乳制备的处方,以微乳的载药量、稳定性及黏度作为综合评定的指标,优选最佳处方.给大鼠分别灌胃JBP 485水溶液和JBP 485微乳,比较药物在大鼠体内的生物利用度.结果筛选出JBP 485微乳的最佳处方,以三油酸甘油酯-单辛/癸酸甘油酯（ODO-L）-乙醇-水（Km＝1：1）体系作为JBP 485微乳的载药体系,JBP 485微乳热力学稳定性良好,粒径60～120 nm,载药量35 μg·mL-1.药动学结果表明所制备的JBP 485微乳在大鼠体内的相对生物利用度达到191.3%.结论制备的JBP 485微乳稳定性良好,相对于水溶液,生物利用度有较明显的提高.

英文摘要：

Objective To prepare JBP 485-loaded oral microemulsion, and to study the shape characteristics,in vitrostability,and its pharmacokinetics in rats. Methods Pseudo ternary phase diagram was adopted to optimize the formula of JBP485 microemulsion. Drug loading capability, stability and viscosity were used as the indexes for the assessment of the bestformula. Rats were used in the study to compare the oral bioavailability of JBP 485 solution and JBP 485 microemulsion. Results Glycerol trioleate/ ODO-L/ EtOH/ H2 O （Km = 1：1） was selected as the delivery system of JBP 485. The prepared JBP485 microemulsion was stable in thermodynamic assessment. The particle diameter was 60 - 120 nm and the drug-loadingcapability was 35 μg·mL-1 . The relative bioavailability of the prepared JBP 485 microemulsion reached 191. 3% compared withthe JBP 485 solution. Conclusion The prepared JBP 485 microemulsion is stable, of low toxity, and can prolong thecirculation time in vivo and improve the bioavailability.