吕文莉, 郭健新, 平其能, 李锦, 赵雏微, 张兰. 注射用灯盏花素脂质体在Beagle犬体内的药代动力学J. 药学学报, 2006, 41(1): 24-29.
引用本文: 吕文莉, 郭健新, 平其能, 李锦, 赵雏微, 张兰. 注射用灯盏花素脂质体在Beagle犬体内的药代动力学J. 药学学报, 2006, 41(1): 24-29.
Lü Wen-li, GUO Jian-xin, PING Qi-neng, LI Jin, ZHAO Chu-wei, ZHANG Lan. Pharmacokinetics of breviscapine liposomes following intravenous injection in Beagle dogsJ. Acta Pharmaceutica Sinica, 2006, 41(1): 24-29.
Citation: Lü Wen-li, GUO Jian-xin, PING Qi-neng, LI Jin, ZHAO Chu-wei, ZHANG Lan. Pharmacokinetics of breviscapine liposomes following intravenous injection in Beagle dogsJ. Acta Pharmaceutica Sinica, 2006, 41(1): 24-29.

注射用灯盏花素脂质体在Beagle犬体内的药代动力学

Pharmacokinetics of breviscapine liposomes following intravenous injection in Beagle dogs

  • 摘要: 目的制备灯盏花素脂质体,研究灯盏花素脂质体在Beagle犬体内的药代动力学。方法采用双周期交叉试验法,6只Beagle犬分别单剂量(以灯盏乙素计为28 mg/只)静脉注射自制灯盏花素脂质体和市售普通注射液,用反相高效液相色谱法测定不同时间血浆中灯盏乙素的浓度,采用3P97计算药代动力学参数,并进行统计学分析。结果脂质体和市售注射液的T1/2α分别为(4.4±0.7) min和(1.8±1.3) min;T1/2<>分别为(55±27) min和(28±23) min;Vc分别为(1 580±265) mL和(2 460±2 200) mL;CLs分别为(88±10) mL·min-1和(324±69) mL·min-1; AUC0-720分别为(363±42) μg·min·mL-1和(102±19) μg·min·mL-1。两种制剂的T1/2α,CLs及AUC0-720经方差分析后均存在极显著或显著性差异。结论与市售普通注射液相比,灯盏花素脂质体Beagle犬静脉注射给药后,大大提高了血药浓度,显著改善了灯盏乙素原药的药代动力学性质,具有缓释作用。

     

    Abstract: AimTo prepare the breviscapine liposomes and study the pharmacokinetics of breviscapine liposomes in Beagle dogs. MethodsThe cross-over design (two periods) was employed. Six Beagle dogs were administrated a single intravenous dosage of 28 mg of breviscapine liposomes and reference preparation, respectively, scutellarin in plasma of 6 dogs at different sampling time was determined by RP-HPLC. The pharmacokinetic parameters were calculated by 3P97 program and compared by statistic analysis. ResultsThe mean concentration-time curves of breviscapine liposomes and reference preparation were both fitted to two-compartment model with the main pharmacokinetic parameters as follows: T1/2α were (4.4±0.7) min and (1.8±1.3) min respectively; T1/2<> were (55±27) min and (28±23) min respectively; Vc were (1 580±265) mL and (2 460±2 200) mL respectively; CLs were (88±10) mL·min-1 and (324±69) mL·min-1 respectively; and AUC0-720 were (363±42) μg·min·mL-1 and (102±19) μg·min·mL-1 respectively. The T1/2α, CLs and AUC0-720 of breviscapine liposomes all had significant difference from those of reference preparation, after the data were examined by a one-way analysis of variance (ANOVA). ConclusionCompared with the reference preparation, breviscapine liposomes had a much more higher concentration in plasma and contained characteristic of sustained-release, which ameliorated the pharmacokinetic properties of scutellarin.