摘要
目的比较川芎嗪长循环脂质体和川芎嗪普通脂质体在大鼠体内的药动学行为。方法 12只SD大鼠随机分为2组,分别单剂量注射给予川芎嗪长循环脂质体和川芎嗪普通脂质体,采用高效液相色谱法测定各时间点的血药浓度,应用DAS2.1软件计算药动学参数,并采用SPSS13.0软件分析2组数据的差异性。结果川芎嗪长循环脂质体和川芎嗪普通脂质体在大鼠体内的药动学行为符合二室模型,主要药动学参数t1/2β分别为(7.56±1.53)h和(0.07±0.05)h,MRT0-∞分别为(5.57±1.76)h和(2.96±1.04)h,AUC0-∞分别为(24.64±1.30)mg·L-1·h和(7.58±0.95)mg·L-1·h,2组之间比较差异具有统计学意义;与川芎嗪普通脂质体相比,川芎嗪长循环脂质体的相对生物利用度为(325.07±10.2)%。结论与川芎嗪普通脂质体相比,川芎嗪长循环脂质体显著延长川芎嗪在大鼠血液循环系统中的驻留时间,具有长循环作用,亦显著提高川芎嗪在大鼠体内的生物利用度。
Objective To study the pharmacokinetics and relative bioavailability of tetramethylpyrazine long- circulating liposomes and tetramethylpyrazine conventional liposomes in rats.Methods 12 rats were randomly divided into two groups.Single dose of tetramethyl-pyrazine long-circulating liposomes and tetramethylpyrazine conventional liposomes were intravenously administrated to the rats respectively. The tetramethylpyrazine concentration in plasma was determined by HPLC, and the phannaeokinetic parameters were calculated and analyzed by DAS 2.1 and SPSS13.0 software. Results The pharmacokinetics of tetramethylpyrazine long- circulating liposomes and tetramethylpyrazine conventional liposomes in rats were both accont with the two compartment models, The main pharmacokinetic parameters were as tbllows ： t1/2β （ 7.56_± 1.53） h and （ 0.07 ± 0. 05） h,MRT0-∞ （ 5.57± 1.76） h and （ 2.96± 1.04） h,AUC0-∞ （ 24.64± 1.30） mg· L^-1 h and（7.58±0.95） mg · L^-1 · h, there were significantly differences between two preparations. And the relative bioavailability of tetramethylpyrazine long-circulating liposomes to tetramethylpyrazine conventional liposomes was （325.07± 10. 2）%. Conclusion Compared with tetramethylpyrazine common liposomes, tetrame-thylpyrazine long- circulating liposomes have longer release time and higher bioavailability.
出处
《广东药学院学报》
CAS
2014年第2期150-152,共3页
Academic Journal of Guangdong College of Pharmacy
