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目的研究艾可清颗粒不同给药方式对大鼠高效抗逆转录病毒治疗(highly active antiretroviral therapy,HAART)中齐多夫定(zidovudine,AZT)药代动力学的影响。方法将36只大鼠分为3组进行灌胃给药:Ⅰ组采用HAART,即拉米夫定(3TC,31.5 mg/kg)加AZT(31.5 mg/kg)加依非韦伦(EFV,63.0 mg/kg);Ⅱ组在HAART给药同时给予艾可清颗粒(525 mg/kg);Ⅲ组在HAART治疗后间隔120 min后给予等量艾可清颗粒。采用液质联用法分别测定各组大鼠给予HAART前及给药后0.5、1、2、3、4、6、8、10、12h时AZT血药浓度;采用DAS 2.0软件计算药物半衰期(t_(1/2))、达峰浓度时间(T_(max))、药物达峰浓度(C_(max))、从0~t时间内的血药浓度-时间曲线下面积(AUC_(0-t))及药物清除率(plasma clearance rate,CL)等药代动力学参数。结果 AZT的回归方程线性关系良好,精密度、回收率、稳定性都得到确定。Ⅱ组、Ⅲ组血药浓度曲线高于Ⅰ组,3组t_(1/2)、T_(max)、C_(max)、AUC_(0-12h)、AUC_(0-∞)及CL比较,差异无统计学意义(P>0.05)。结论艾可清颗粒联合HAART可提高AZT最高血药浓度。
Objective To study the effects of different administration methods of Ai Ke Qing granules on the pharmacokinetics of zidovudine (AZT) in highly active antiretroviral therapy (HAART) rats. Methods 36 rats were divided into 3 groups for intragastric administration: group Ⅰ was treated with HAART (3TC, 31.5 mg / kg) plus AZT (31.5 mg / kg) plus efavirenz (EFV, 63.0 mg / kg). In group Ⅱ, patients were treated with HAART simultaneously with ECK (525 mg / kg). Patients in group Ⅲ were treated with equal doses of iczygine 120 minutes after HAART. The serum concentrations of AZT before and at 0.5, 1, 2, 3, 4, 6, 8, 10 and 12 hours after administration of HAART in each group were determined by liquid chromatography-mass spectrometry. The half- (AUC_ (0-t)), time to peak concentration (T max), peak drug concentration (C max) )) And drug clearance (plasma clearance rate, CL) and other pharmacokinetic parameters. Results The regression equation of AZT had a good linear relationship, and the precision, recovery and stability were all confirmed. The blood concentration curve of group Ⅱ and group Ⅲ was higher than that of group Ⅰ. The t 1/2, T max, C max, AUC 0-12h, AUC 0-0, The difference was not statistically significant (P> 0.05). Conclusion Ai Ke Qing particles combined with HAART can increase the highest plasma AZT concentration.