洛伐他汀在巴马香猪体内的绝对生物利用度  

Absolute Bioavailability of Lovastatin in Bama Miniature Pigs

作　　者：曾本华[1] 刘宇[1] 黄亚琴[1] 岑彦艳[1] 郑书全[1] 魏泓[1] 

机构地区：[1]第三军医大学基础部实验动物学教研室,重庆400038

出　　处：《中国实验动物学报》2007年第1期67-69,共3页Acta Laboratorium Animalis Scientia Sinica

基　　金：国家"十五"科技攻关计划重点项目资助课题(2004BA717B-3)

摘　　要：目的选择HMG-CoA还原酶抑制剂洛伐他汀作为模型药物，在巴马香猪体内进行生物利用度及药代动力学研究，探讨巴马香猪对洛伐他汀的处置规律。方法12头6-8月龄健康雄性巴马香猪随机分为灌胃组、静脉组和空白对照组，其中灌胃组和静脉组通过胃管和耳静脉分别给与洛伐他汀8、1．2mg／kg。给药后前腔静脉采血，用RP-HPLC-UV法检测血浆洛伐他汀浓度；用3P97计算药代动力学参数，用统计矩法计算血药浓度．时间曲线下面积（AUC0-∝）。结果灌胃组t1/2和Ke分别为3．43h和0．20h；静脉组C0、Ke、Vd、t1/2和CL分别为180．27ng/mL、0．17h、6．7L/kg、3．97h和66．97mL／min。统计矩法计算得到灌胃组和静脉组的AUC0-∝分别为每小时409．41，1627．78ng／mL，绝对生物利用度F为3．8％。结论洛伐他汀在巴马香猪体内的绝对生物利用度人和犬基本一致，提示巴马香猪与人和犬对药物的处置具有一定的相似性。Objective The absolute bioavailability of lovastatin, an HMG-CoA reductaso, was investigated in order to explore the regularity of lovastatin disposition in Bama miniature pig. Methods A total of 12 health male Bama miniature pigs were randomly divided into intragastrie group, intravenous group and control group. A single dose of lovastatin was administered intragastrically （8.0 mg/kg） and intravenously （1.2 mg/kg） and blood was collected via preeaval vein. Lovastatin concentrations were immediately analyzed by RP-HPLC-UV method and pharmacokinetie parametes were computed by 3p97. AUC0-∝ of intragastrie and intravenous groups were computed by statistical moment method. Results The t1/2 and Ke of intragastrie group were 3.43 h and 0.20 h; the C0, Ke, Vd, t1/2 and CL of intravenous group were 180.27 ng/mL,0.17 h, 6.67 L/kg,3.97 h, 66.97 mL/min/kg. Conclusion The value of absolute bioavailability is similar to that of dog and human, indicating that there is a similarity in lovastatin disposition in Bama miniature pig, dog and human.

关 键 词：巴马香猪 洛伐他汀 血药浓度-时间曲线下面积 绝对生物利用度 

分 类 号：R54[医药卫生—心血管疾病]