丹七注射液中丹参素钠在Beagle犬体内药代动力学及生物利用度研究

Pharmacokinetics and bioavailability of danshensu-sodium in beagle dogs

目的研究丹七注射液中丹参素钠在Beagle犬体内的药代动力学。方法液相色谱-紫外光谱法,乙腈-1%的冰醋酸水溶液(8∶92)为流动相,测定一次性静脉注射丹七注射液(28.4 mg.kg-1)和一次性口服丹七丸(114.7 mg.kg-1)后Beagle犬血浆中丹参素钠含量。采用BAPP2.3生物利用度数据处理通用程序中的模型拟合与统计矩法计算药物的药代动力学参数。结果静注和口服丹七制剂中的丹参素钠在Beagle犬体内的药代动力学均符合二室模型,T1/2为0.573、2.258 h,AUC分别为29.792、77.84 h.μg.ml-1,口服生物利用度为63.8%。结论丹七注射液中丹参素钠在Beagle犬体内呈快吸收慢消除动力学特征。

Aim To investigate the pharmacokinetics of danshensu-sodium in Beagle dogs and the main pharmacokinetic parameters. Methods An HPLC-UV method was used. Acetonitrile-1% ammonium acetate （8 ： 92） was used as the mobile phase. According to the BAPP2.3 pharmacokinetic program,the main parameters were calculated. Results The danshensu-sodium pharmacokinetics conforms to a two-compartment model after a single iv（28.4 mg · kg^-1）and oral（ 114.7 mg · kg^-1） dose of danshensu-sodium in Beagle dogs. The parameters were as followings ： T1/2 were 0.573 and 2. 258 h, AUC were 29. 792 and 77.84 h ·μg · ml^-1, respectively. The oral administration bioavailability of danshensu-sodium capsule was 63.8%. Conclusion The pharmacokinetics of danshensu-sodium after iv. and oral administration showed a rapid absorption and slow elimination process in beagle dogs.