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28mg/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;T1/2β分别为(55±27)min和(28±23)min;Vc分别为(1580±265)mL和(2460±2200)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。
Aim To prepare the breviscapine liposomes and study the pharmacokinetics of breviscapine liposomes in Beagle dogs. Methods The 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. Results The 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 ; T1/2α 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 Ti/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）. Conclusion Compared 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.
出处
《药学学报》
CAS
CSCD
北大核心
2006年第1期24-29,共6页
Acta Pharmaceutica Sinica
基金
国家高技术研究发展计划(863计划)重大科技专项资助(2004AA2Z3230)
江苏省自然科学基金重点项目资助(BK2001210)
