盐酸小檗碱在鸡体内的药动学研究

Pharmacokinetic Study of Berberine Hydrochloride in chickens

关键词:  盐酸小檗碱  鸡  HPLC  药动学

Key words:  Berberine Hydrochloride  Chicken  HPLC  Pharmacokinetics

摘要:

目的：探讨盐酸小檗碱在鸡体内的药动学特征。方法：鸡以3mg•kg-1和50mg•kg-1剂量静脉注射和口服给药，采用HPLC法测定血浆中盐酸小檗碱的质量浓度。血药浓度一时间数据经DAS药代动力学分析软件处理，计算出药动学参数。结果：盐酸小檗碱静脉注射药时曲线符合三室开放模型，主要药动学参数分别为：t1/2β为0.41±0.24 h，t1/2γ为3.66±1.06 h，AUC为78.92±30.58（μg•L-1•h），Vc为25.49±21.77（L•kg-1），CL为43.20±16.21 （L•h-1•kg-1）。盐酸小檗碱口服给药的药时曲线符合二室开放模型，主要药动学参数分别为：t1/2α为1.86±0.76 h，t1/2β为4.18±3.13 h，t1/2ka为0.89±0.46 h ，Tmax为2.65±0.63 h，Cmax为4.09±1.13（μg•L-1），AUC为26.18±10.73（μg•L-1•h），绝对生物利用度为2.03%。结论：鸡口服盐酸小檗碱的生物利用度低，消除较快。

Abstract:

Objective To investigate the pharmacokinetics of berberine hydrochloride in chickens. Methods The plasma concentration of berberine was determined by HPLC method.The plasma concentration-time data of berberine hydrochloride was analyzed by Drug and Statistics (DAS). Results Following intravenous administration(3mg•kg-1),the drug concentration-time data was best described by a three -compartment open model , t1/2β , t1/2γ, Vc, CL and AUC were 0.41±0.24 h,3.66±1.06 h ,25.49±21.77（L•kg-1）,43.20±16.21（L•h-1•kg-1）and 78.92±30.58（μg•L-1•h）respectively. The drug concentration-time data was best described by a two -compartment open model after oral administration of 50 mg•kg-1, t1/2α, t1/2β,t1/2ka,Tmax,Cmax and AUC were 1.86±0.76 h , 4.18±3.13 h, 0.89±0.46 h ,2.65±0.62 h, 4.09±1.13（μg•L-1）and 26.18±10.73（μg•L-1•h）, respectively. The absolute bioavailability is 2.03% after oral administration. Conclusion Berberine hydrochloride has a low rate of bioavailability by oral administration, and its elimination is fast.