摘要
目的 研制了马来酸曲美布汀 (TMB)缓释片家犬药动学 ,为人体生物利用度研究提供依据和参考。方法 以市售普通片为参比制剂 ,采用HPLC法测定了两制剂在家犬的血药浓度 ,按单剂量给药、多剂量给药方案进行研究并计算药动学参数。结果 单剂量给药 ,6只家犬的双周期交叉试验后 ,Tmax、MRT有极其显著性差异 ,相对生物利用度为 10 2 .5 % ,TMB缓释片具有缓释作用。多剂量试验给予TMB缓释片和TMB普通片达稳态后 ,缓释片与普通片比较 ,稳态达峰时间极显著延长 (P <0 .0 1) ,稳态达峰浓度显著降低 (P <0 .0 5 ) ,Css、Cmin、T1/ 2 、AUC0 ∞ 等药动学参数的改变没有显著意义。表明受试制剂TMB缓释片与参比制剂达稳态的程度相同 ,TMB缓释片稳态血药浓度的波动程度较小。结论 该缓释片在家犬体内具有缓释作用。
AIM Pharmacokinetics study on trimebutine maleate sustained-release tablets in dogs was carried out. METHODS An ion-pairing reversed-phase HPLC method was developed for determination of trimebutine in dogs plasma. Pharmacokinetics and bioavailability studies were compared with TMB sustained-release tablets and TMB conventional tablets. RESULTS The pharmacokinetic parameters in six dogs after single-dose oral administration of conventional tablets and sustained-release tablets of TMB were calculated. T max and MRT had significant difference(P<0.01). Relative bioavailability was 102.5. The pharmacokinetic parameters in six dogs after multiple-dose oral administration of conventional tablets and sustained-release tablets of TMB:T max 、C max 、FI had significant difference(P<0.05). CONCLUSION The TMB sustained-release tablets were able to maintain a sustained release for 12 h.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2001年第2期122-126,共5页
Journal of China Pharmaceutical University
