Yang Yong-Ge, Song Li-Xue, Jiang Nan, Xu Xue-Ting, Di Xiao-Hui, Zhang Mei
Department of Pharmacy, Beijing Military Region General Hospital Beijing, China.
Int J Clin Exp Med. 2015 Oct 15;8(10):18744-50. eCollection 2015.
To investigate the pharmacokinetics of Ambroxol and Clenbuterol Tablets in Chinese healthy volunteers after a single or multiple dosages oral administration.
A total of 9 healthy adult subjects were given Ambroxol and Clenbuterol Tablets in a single dosage or multiple dosages respectively. LC/MS/MS were used for the determination of Ambroxol and Clenbuterol of in plasma. The important pharmacokinetic parameters were calculated by DAS 2.0 software (compartment model).
Single and multiple dosage groups of Ambroxol and Clenbuterol were all fitted two-compartment model. The pharmacokinetics fitted first order kinetics process. No difference in pharmacokinetics of Ambroxol in single and multiple dosage groups volunteers was observed, Which showed no marked changes, suggesting that multiple dosing did not influence the velocity of drug metabolism. Moreover, parameters of Clenbuterol had significant difference between the single and multiple dosage groups (P<0.05), showing there was accumulation in the body. 9 subjects had completed single or multiple dosages oral administration test, with no adverse drug reactions appeared during the test.
There was no obvious accumulation of Ambroxol after repeated dosing. But obvious accumulation of Clenbuterol was noted in multiple-dose administration. The established method is sensitive, accurate, reliable and specific, and it can meet the requirement of clinical pharmacokinetic trial.
研究氨溴索克仑特罗片在中国健康志愿者单次及多次口服给药后的药代动力学。
9名健康成年受试者分别单次或多次服用氨溴索克仑特罗片。采用液相色谱-串联质谱法测定血浆中氨溴索和克仑特罗的含量。重要的药代动力学参数通过DAS 2.0软件（房室模型）计算。
氨溴索和克仑特罗的单次和多次给药组均拟合二房室模型。药代动力学符合一级动力学过程。单次和多次给药组志愿者氨溴索的药代动力学无差异，无明显变化，提示多次给药不影响药物代谢速度。此外，克仑特罗的参数在单次和多次给药组之间有显著差异（P<0.05），表明体内有蓄积。9名受试者完成了单次或多次口服给药试验，试验期间未出现药物不良反应。
氨溴索重复给药后无明显蓄积。但克仑特罗在多次给药时有明显蓄积。所建立的方法灵敏、准确、可靠、特异，能满足临床药代动力学试验的要求。
