抽脂患者皮下注射利多卡因血清与唾液浓度的相关性及其药代动力学研究

本文利用高效液相色谱法对12名抽脂健康患者皮下注射利多卡因的血清、唾液及脂肪浓度进行了测定,探讨了血清与唾液中药物浓度的相关性,并比较了二者之间的药代动力学参数。患者的平均给药剂量为20mg/kg,单剂量给药。实验结果表明血清与唾液中药物浓度呈线性关系:r=0.8043(p<0.01),C_(血清)=0.3433C_(唾液)+0.2620(n=78).唾液与血清药物浓度比值为2.37±0.857(比值范围:1.02～4.09,n=78).测得血清及唾液药代动力学参数分别为:吸收速率常数(Ka)0.573±0.583h~(-1),0.478±0.270h~(-1);消除半衰期(t_(1/2)k)6.41±2.08h,5.68±1.76h;达峰时间(T_(max))6.63±1.46h,6.67±1.80h;峰浓度(C_(max))2.52±0.926μg/ml,6.31±2.30μg/ml.血清与唾液的动力学参数除峰浓度(C_(max))外,统计学上均无明显差异(P>0.05).患者被抽出脂肪的药物含量为给药总量的31.84%(20.69～47.90%).

THE CORRELATIONS OF SALIVA AND SERUM CONCENTRATIONS AND THE CLINICAL PHARMACOKINETIC ON SUBCUT ANEOUS INJECTION LIDOCAIN IN HEALTHY VOLUNTEERS DEFATTED

The concentrations of Lidocain in saliva, serum and fat tissue from 12 healthy volunteers who were evacuated of their fat tissue were determined by means of High Performance Liquid Chromatography. The correlation between and pharmacokinetic parameters of lidocain concentration in saliva and serum were studied and compared. When a separate dose of 20mg/kg (mean) of lidocain was given subcutaneously, a linear relation was observed of lidocain in saliva to that in serum r=0.8043(p<0.01), C_(?)=0.3433C_(?)+0.2620. The ratio of the concentration of lidocain in saliva to that in serum was 2.37±0.857 (n=78). The pharmacokinetic parameters of serum and saliva for the 12 healthy volunteers were Ka 0.573±0.583h~(-1), 0.478±0.270h~(-1); t(1/2)k 6.41±2.08h, 5.68±1.76h; T(max) 6.63±1.46h, 6.67±1.80h, C_(max)2.52± 0.926 μg/ml, 6.31±2.30μg/ml. A comparison between the pharmacokinetic parameters of saliva and serum showed that there was no major difference except in C_(max) (P>0.05). The drug content in the fat tissue drawn from the healthy volunteers was 31.84% of the dose given.