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目的制备白花前胡甲素脂质体并进一步研究其在大鼠体内的药动学。方法采用乙醇注入法制备白花前胡甲素脂质体,采用正交设计优化处方。白花前胡甲素脂质体按5、10、20mg·kg~(-1)低、中、高3个剂量经大鼠颈静脉给药后检测一定时间点的血药浓度,对照组为10mg·kg~(-1)的白花前胡甲素溶液。结果制备的脂质体含药量为2g·L~(-1),包封率为93.2%,脂质体高、中、低剂量组及对照组的t_(1/2)分别为(136.58±22.86),(74.12±6.97),(44.93±7.47),(51.26±5.13)min;AUC_(0-∞)分别为(215.93±33.24),(91.75±26.47),(29.22±4.47),(66.90±14.54)min·mg·L~(-1)。结论成功制备了白花前胡甲素脂质体,制得的白花前胡甲素脂质体在大鼠体内半衰期显著延长,生物利用度有明显的提高。
Objective To prepare the promethazine liposomes and further study its pharmacokinetics in rats. Methods The ethanol injection method was used to prepare the promethazine liposomes, and the orthogonal design was used to optimize the prescription. The plasma concentrations of POMA liposomes at low, medium and high doses of 5, 10, and 20 mg · kg -1 were measured by the jugular vein at a dose of 10 mg · kg -1 ~ (-1) of the solution of the white before. Results The liposomes contained 2g · L -1 and the entrapment efficiency was 93.2%. The t 1/2 of liposomes in high, medium and low dose groups and the control group were (136.58 ± 22.86), (74.12 ± 6.97), (44.93 ± 7.47) and (51.26 ± 5.13) min, respectively. The AUC 0-∞ values were (215.93 ± 33.24), (91.75 ± 26.47), (29.22 ± 4.47) and ± 14.54) min · mg · L -1. Conclusion The preparation of the white melatonin liposomes, the prepared promethazine liposomes in rats significantly extended the half-life, bioavailability was significantly improved.