摘要
目的研究毕格犬静脉注射不同剂量N,N-双乙酰胱氨酸(DiNAC)后的药动学。方法毕格犬12只随机分成3组,分别静脉注射DiNAC25,12.5,6.25mg/kg,在设定的时间点采血,反相高效液相色谱法测定血浆中的DiNAC浓度,DAS程序计算其药动学参数。结果毕格犬静脉给予DiNAC后,其血药浓度-时间曲线符合二室模型一级动力学过程。AUC0→∞分别为3849.7±157.7,1683.0±90.5,757.1±344.2mg/(L·min),与给药剂量成良好的线性关系(r=0.9993);Cmax分别为91.99±15.13,53.37±3.88,23.20±7.07mg/L,与给药剂量呈线性关系(r=0.993);而t1/2α为1、1~1.9min,t1/2β为34.2~47.3min,分布容积(Vd)为0、38~0.49L/kg,显示非剂量依赖性特征。结论DiNAC在毕格犬体内的药动学过程为二室模型一级动力学过程,具有分布快,消除迅速的特点。
Purpose To study the iv pharmacokinetics of N, N-diacetylcystine (DiNAC)in Beagle dogs. Methods 12 Beagle dogs were divided into 3 groups.A single dose of 25, 12.5 and 6.25 mg/kg of DiNAC was given by iv. Serial blood samples were collected at the designed time points. The plasma DiNAC concentration was measured by RP-HPLC. Pharmacokinetic parameters were computerized by DAS program. Results After intravenous injection of single dose DiNAC, the plasma concentration versus time curves of DiNAC conformed to two-compartment model. The AUC0→∞ and Cmax were lined with the iv dose ( r = 0. 999 3 and 0.993, respectively) ; t1/2α was 1.1-1.9 min, t1/2β was 34.2-47.3 min and Vd was 0.38-0.49 L/kg, which had no significant deviation between groups ( P 〉 0.05 ). Condusion The pharmacokinetics of DiNAC con- formed to two-compartment model in Beagle dogs after single dose iv. Distribution and elimination of DiNAC were rapid.
出处
《中国生化药物杂志》
CAS
CSCD
2007年第2期113-115,共3页
Chinese Journal of Biochemical Pharmaceutics