摘要
目的 探讨血啉甲醚在动物体内的药代动力学规律。方法 将 15只家兔分成 3组 ,每组 5只 ,分别静脉注射血啉甲醚 10、2 0、40mg/kg后 ,以荧光分光光度法测定血药浓度 ,并根据血药浓度 时间数据计算药代动力学参数。结果 血啉甲醚血浆浓度为 10、2 0和 40 μg/ml时 ,重复测定 5次 ,方法回收率的均值和变异系数分别为 97 2 0 %、2 19% ,97 30 %、2 2 6 % ,98 6 0 %、2 0 3%。静脉给药后 ,血啉甲醚在家兔体内的药代动力学符合开放三房室模型。各组主要药代动力学参数 :10mg/kg组 ,T1/ 2π(分布半衰期 ) =3.0 5 1min ,T1/ 2α(分布半衰期 ) =15 77min ,T1/ 2 β(消除半衰期 ) =149 84min ,Vc(中央室表观分布容积 ) =0 75 7L/kg ,Cl(清除率 ) =0 0 6 5 2L·kg-1·min-1,AUC(血药浓度 时间曲线下面积 ) =15 3μg·min-1·ml-1;2 0mg/kg组 ,T1/ 2π=1 845min ,T1/ 2α=2 0 46min ,T1/ 2 β=15 9 71min,Vc =0 0 74L/kg ,Cl=0 0 2 0 0L·kg-1·min-1,AUC =998μg·min-1·ml-1;40mg/kg组 ,T1/ 2π=2 6 17min ,T1/ 2α=2 1 5 7min ,T1/ 2 β=35 3 0 1min ,Vc =0 0 40L/kg,Cl=0 0 0 84L·kg-1·min-1,AUC =476 4μg·min-1·ml-1。结论 血啉甲醚静脉注射后 ,在家兔体内的药时过程为线性一级动力学?
Objective To study the pharmacokinetic rule of hematoporphyrin monomethyl ether(HMME) in animal after intravenous injection. Methods Fifteen rabbits were randomly and equally divided into 3 groups. The tested rabbits were injected intravenously with 10, 20 or 40 mg/kg of HMME, respectively. The plasma concentration of HMME in rabbits after intravenous injection was determined by fluorospectrophotometry. The excitation and emission wavelengths were 395 and 613 nm, respectively. The pharmacokinetic parameters of HMME in rabbits were calculated by computer according to the plasma cocentration time data. Results The average recovery of HMME from plasma was 97 20% (CV=2 19%), 97 30%(CV=2 26%) and 98 60 (CV=2 03%) at concentration of 10, 20 and 40 μg/ml, respectively. It was indicated that the pharmacokinetics of HMME in rabbits after intravenous injection was fit for a three compartment open model. The principal pharmacokinetic parameters were T 1/2π =3.051 min, T 1/2α =15.77 min, T 1/2β =149.84 min, Vc=0.757 L/kg, Cl=0.065 2 L·kg -1 ·min -1 , AUC=153 μg·min -1 ·ml -1 (10 mg/kg); T 1/2π =1.845 min, T 1/2α =20.46 min, T 1/2β =159.71 min, Vc=0.074 L/kg, Cl=0.020 0 L·kg -1 ·min -1 , AUC=998 μg·min -1 ·ml -1 (20 mg/kg); T 1/2π =2.617 min, T 1/2α =21.57 min, T 1/2β =353.01 min, Vc=0.040 L/kg, Cl=0.008 4 L·kg -1 ·min -1 , AUC=4 764 μg·min -1 ·ml -1 (40 mg/kg), respectively. Conclusions It was suggested that the plasma concentration time course of HMME in rabbits after intravenous injection was a first order linear kinetic process. The data of the first distribution phase and the second distribution phase showed that HMME was distributed rapidly to the peripheral compartment from the central compartment in rabbits after intravenous injection. The data of the elimination phase showed that HMME was eliminated more quickly and was not accumulated, thus significantly reducing the systematic side effects.
出处
《中国激光医学杂志》
CAS
CSCD
2000年第2期105-108,共4页
Chinese Journal of Laser Medicine & Surgery
关键词
光化学疗法
抗肿瘤药
药代动力学
血淋甲醚
Photochemotherapy
Antineoplastic agents
Pharmacokinetics
Hematoporphyrin monomethyl ether
