摘要
目的研究葛根素固体分散体的制备及其在家兔体内药动学,以提高葛根素口服给药的生物利用度。方法采用溶出度法,确定葛根素固体分散体的最佳制备处方;采用HPLC法,测定家兔血浆中葛根素的含量,药动学参数经3P97药动学软件处理。结果葛根素固体分散体的最佳制备处方为葛根素:PEG6000:pluronicF-68=1:4:1(m/m/m);葛根素及葛根素固体分散体的血药浓度-时间过程均符合二室模型,主要药动学参数:α分别为(2.040±0.327)、(0.870±0.191)·h^(-1),β分别为(0.21 2±0.021)、(0.351±0.022)·h^(-1),AUC_(0-∞)分别为(11.966±1.370)、(91.419±3.531)mg·L^(-1)·h,t_(max)分别为(0.491±0.026)、(1.423±0.035)h,ρ_(max)分别为(3.917±0.066)、(20.416±1.870)mg·L^(-1)。葛根素固体分散体对葛根素的相对生物利用度为763.99%。结论葛根素固体分散体可提高葛根素口服给药在家兔体内的生物利用度。
AIM To study the preparation of puerarin solid dispersions and pharmacokinetics in rabbits so as to increase the bioavailability of puerarin for oral.METHODS Dissolution test was used to determine the preparation prescription,puerarin concentrations in blood were determined by HPLC,and pharmacokinetic parameters were calculated using 3P97 pharmacokinetic program software.RESULTS The best preparation prescription was puerarin：PEG6000：pluronicF-68 =1：4：1（m/m/m）.The concentration-time profiles of puerarin and puerarin solid dispersions were shown to fit two-compartment model absorption.The main pharmacokinetics parameters of puerarin and puerarin solid dispersions were：α（2.040±0.327）,（0.870±0.191）·h^（-1）;β（0.212±0.021）,（0.351±0.022）·h^（-1）;AUC_（0-∞）（11.966±1.370）,（91.419±3.531） mg·L^（-1）·h; t_（max）（0.491±0.026）,（1.423±0.035） h;ρ_（max）（3.917±0.066）,（20.416±1.870） mg·L^（-1）.The relative bioavailability of puerarin solid dispersions was 763.99%.CONCLUSION Puerarin solid dispersions can effectively enhance puerarin absorption in rabbits in vivo.
出处
《中国新药与临床杂志》
CAS
CSCD
北大核心
2011年第4期294-297,共4页
Chinese Journal of New Drugs and Clinical Remedies
基金
黑龙江省教育厅科学技术研究项目(11521060)
关键词
葛根素
固体分散体
药动学
色谱法
高压液相
生物利用度
puerarin
solid dispersions
pharmacokinetics
chromatography
high pressure liquid
biological availability
