健康人伏立康唑血浆浓度与唾液浓度的相关性

目的研究健康人伏立康唑(抗真菌药)血浆和唾液浓度的相关性。方法20名男性健康志愿者分别单剂量口服伏立康唑片200 mg,用液相色谱-串联质谱法测定伏立康唑血浆和唾液浓度,用DAS 2.0软件计算药代动力学参数,用SPSS 10.0比较2种浓度及药代动力学参数的相关性。结果伏立康唑血浆浓度(Cp)和唾液浓度(Cs)的相关性公式Cs=0.69Cp-35.96,γ=0.9710,血浆浓度和唾液浓度呈显著的正向相关关系(P<0.01),Cs/Cp为0.59±0.53。Cs和Cp的药代动力学参数t1/2Ka、t1/2、Tmax较为接近,无显著性差异(P>0.05)。结论可用唾液浓度代替血浆浓度进行伏立康唑的药物浓度监测和人体药代动力学研究。

Correlation between plasma and saliva concentration of voriconazole in healthy volunteers

Objective To study correlation between plasma and saliva concentration of voriconazole in healthy volunteers.MethodsA single oral dose of 200 mg voriconazole tablet was given to 20 healthy male volunteers respectively.The drug concentrations in plasma and saliva were determined by LC-MS/MS method;The pharmacokinetic parameters calculated by DAS 2.0.The two concentrations and pharmacokinetic parameters were compared respectively by SPSS 10.0.ResultsThe linear regression equation of voriconazole salivary(Cs) and plasma(Cp) concentration were Cs=0.69Cp-35.96,γ=0.9710,and there was a significant positive correlation between them(P<0.01).The ration of Cs/Cp was 0.59±0.53.The pharmacokinetic parameters t1/2Ka,t1/2,Tmax calculated by Cs and Cp respectively were similar,there were no significant differences between them(P>0.05).ConclusionThe drug concentration can be monitored and its pharmacokinetics in human body can be studied by the saliva concentration replacing the plasma concentration.