甘草酸二铵脂质复合物泡腾颗粒在犬体内的药代动力学的研究  

Pharmacokinetics research of diammonium glycyrrhizinate effervescent granule in beagle dogs

作　　者：李松龙[1,2] 赵亚[1,2] 茹仁萍[1,2] 

机构地区：[1]杭州市西溪医院 [2]杭州市第六人民医院药剂科,浙江杭州310000

出　　处：《中国临床药理学杂志》2014年第2期131-133,共3页The Chinese Journal of Clinical Pharmacology

基　　金：浙江省卫生厅科研基金资助项目(2011KYA131)

摘　　要：目的比较自制甘草酸二铵脂质复合物泡腾颗粒与甘草酸二铵胶囊在Beagle犬体内的相对生物利用度。方法自身交叉对照设计。Beagle犬(6只)单剂量灌胃甘草酸二铵脂质复合物泡腾颗粒或胶囊剂各300 mg,用HPLC法测定血浆中的甘草酸二铵浓度,DAS 2.1.1程序拟合药代动力学参数。结果泡腾颗粒与胶囊的主要药代动力学参数如下:tmax分别为(3.00±0.00),(3.17±0.41)h;t1/2分别为(6.91±1.45),(6.84±1.51)h;cmax分别为(35.80±3.42),(28.08±3.41)μg·mL-1;AUC0-t分别为(457.67±49.51),(305.84±34.83)μg·h·mL-1;泡腾颗粒相对生物利用度为(149.79±3.79)%。结论 Beagle犬体内甘草酸二铵的药代动力学符合一级吸收二室模型,泡腾颗粒确能显著提高药物的生物利用度。Objective To compare the pharmacokinetics between diammonium glycyrrhizinate （DG） effervescent granule （test） and conventional capsules （reference） in dogs. Methods Six Beagle dogs were given orally a single dose of 300 nag DG in self crossover study. The plasma concentration of DG was assayed by HPLC method and the pharmacokinetie parameters were calculated with DAS 2. 1.1 program by a computer. Results The pharmacokinetic parameters of the test and reference preparations were as follows ： tmax were （ 3.00 ± 0. 00 ）, （3. 17 ± 0. 41 ） h; cmax were （35.80±3.42） and （28.08±3.41）μg·mL-1; t1/2（6.91 ±1.45） and （6.84±1.51） h; AUC0-1, were （457.67±49.51） and （305.84±34.83）μg·h·mL-1, respectively. The relative bioavailability of test preparation was （149. 79 ± 3. 79）% . Conclusion The pharmacokinetics of DG in dogs accord with the two compartment models and with the first absorption after test or reference administration orally, Cmax, AUC0-t and AUC0-∞ of test were all higher than those of reference, and test had a higher bioavailability, which reached the object of this task.

关 键 词：甘草酸二铵 脂质复合物 泡腾颗粒 HPLC 药物动力学 

分 类 号：R969.1[医药卫生—药理学] R975.5[医药卫生—药学]