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目的制备9-硝基喜树碱自微乳化静脉注射给药系统(9-NCME),并考察其在大鼠体内的药动学情况。方法采用伪三元相图确定油相制剂组成,以正交设计优化处方组成,评价了9-NCME制剂的稳定性,并考察了正常大鼠尾静脉注射后体内的药动学行为。结果以注射用大豆油为油相、EPC/Tween80为乳化剂、无水乙醇为助乳化剂等成分组成的新型注射剂9-NCME,在临用前用5%葡萄糖注射液稀释20倍后可自发形成平均粒径38.3±4.0nm稳定微乳,大鼠尾静脉给予9-NCME药动学参数为:t1/2(0.97±0.14h),AUC0–8(372.77±49.62ng·h·mL–1)andMRT(1.40±0.21h),分别是对照溶液剂的1.4、1.65和1.4倍(P<0.01)。结论9-NCME具有较好的物理和化学稳定性,有望成为新型的9-NC静脉注射剂。
Objective To prepare a 9-nitrocamptothecin self-microemulsifying intravenous injection system (9-NCME) and study its pharmacokinetics in rats. Methods The composition of the oil phase was determined by pseudo-ternary phase diagram. The composition of the formulation was optimized by orthogonal design. The stability of 9-NCME formulation was evaluated. The pharmacokinetics of the 9-NCME formulation was also investigated. Results The new injectable agent 9-NCME, which was composed of soybean oil as injection phase, EPC / Tween80 as emulsifier and absolute ethanol as co-emulsifier, was spontaneously The pharmacokinetic parameters of 9-NCME were given to the tail vein of rats with t1 / 2 (0.97 ± 0.14h) and AUC0-8 (372.77 ± 49.62ng · h · mL-1) ) andMRT (1.40 ± 0.21h), 1.4, 1.65 and 1.4 times (P <0.01), respectively, relative to the control solution. Conclusion 9-NCME has good physical and chemical stability and is expected to become a new 9-NC intravenous injection.