摘要
目的研究八宝素在Beagle犬体内的药代动力学。方法用高效液相色谱法,以蒽为内标,苯甲酰氯为衍生剂,甲醇-水(64∶36)为流动相,测定一次性静脉注射10.6和21.3 mg.kg-1八宝素后,Beagle犬血液中八宝素的含量。采用3P97程序计算药物代谢动力学参数。结果八宝素iv在Beagle犬体内的药代动力学符合二室开放模型,两剂量组T1/2α为2.3和2.1 m in,T1/2β分别为1.9和2.0 h,Vc均为0.54 L.kg-1,AUC分别为1.8和4.1 g.m in.L-1,CL分别为0.004 8和0.005 6 L.kg-1.m in-1。结论八宝素在Beagle犬体内分布和消除较快,呈一级动力学特征。
Aim To investigate the pharmacokinetics ot hylotelephln in Beagle dogs and obtain the main pharmacokinetic parameters. Methods An HPLC method with UV detection was developed to study the pharmacokinetics of hylotelephin in dogs by joining an internal standard （anthracene）. Benzoyl chloride was used to the pre-column derivatization of hylotelephin and methanol-water （64： 36） was used as the mobile phase. According to the 3P97 pharmacokinetic program, the main parameters were calculated. Results The hylotelephin pharmacokinetics conforms to a two-compartment open model after a single iv dose of hylotelephin 10.6 or 21.3 mg·kg^-1 in Beagle dogs. The parameters of two groups were as follows： T1/2α were 2.3 and 2. 1 min, T1/2β were 1.9 and 2.0 h, K12 were 0. 12 and 0. 11 min, K21 were0.17 and0.21 rain, K10 were 0. 011 and 0. 009 4 min＇ Vo were 0. 54 and 0. 54 L· kg^-1, AUC were 1.8and4.1 g·min·L^-1 CL were 0. 004 8 and 0. 005 6 L . kg^-1 .min^-1 MRT were 2.10 and 2. 4 h respectively. Conclusion The pharmacokinetics of hylotelephin after iv administration showed a rapid distribution and elimination process in Beagle dogs and was of first order kinetics.
出处
《药学学报》
CAS
CSCD
北大核心
2006年第7期680-683,共4页
Acta Pharmaceutica Sinica
