甘草酸二铵胃内滞留漂浮型缓释片兔体内的药动学  

Pharmacokinetics of diammonium glycyrrhizinate floating sustained-release tablets in rabbits

作　　者：李松龙[1] 茹仁萍[1] 上官盈盈[2] 庄辉耀[1] 

机构地区：[1]杭州市第六人民医院药剂科,浙江杭州310014 [2]浙江医学高等专科学校,浙江杭州310053

出　　处：《中国医院药学杂志》2008年第13期1079-1082,共4页Chinese Journal of Hospital Pharmacy

摘　　要：目的:比较自制甘草酸二铵胃内滞留漂浮型缓释片和市售胶囊剂兔体内药动学、相对生物利用度。方法:用6只新西兰兔自身交叉对照、单剂量灌胃甘草酸二铵胃内滞留漂浮型缓释片或市售胶囊剂各200mg,采用高效液相色谱法测定血浆甘草酸二铵浓度,DAS2.0程序拟合血药浓度-时间数据。结果:甘草酸二铵胃内滞留漂浮型缓释片和市售胶囊剂给药后,药动学参数tmax分别为2h和4h,Cmax分别为(2.8±0.5)mg·L-1和(2.5±0.18)mg·L-1,AUC(0-t)分别为(18.4±2.4)mg·L-1.h,和(27.0±2.2)mg·L-1.h,漂浮片相对生物利用度为(149.0±11.2)%。结论:家兔体内甘草酸二铵的药动学规律均符合一级吸收二室模型,与市售胶囊剂相比,漂浮片释药平稳,tmax、AUC(0-t)均较胶囊剂高,说明漂浮片能显著提高药物的生物利用度,初步达到设计要求。OBJECTIVE To compare the pharmacokinetics between diammonium glycyrrhizinate floating sustained-release tablets （A） and conventional capsules （R）. METHODS Six New Zealand rabbits were given orally with A and R,with a single dose of 200 mg diammonium glycyrrhizinate in selfcrossover study. The plasma concentration of diammonium glycyrrhizinate was assayed by HPLC and the pharmacokinetic parameters were calculated with DAS2. 0 program by a computer. RESULTS The tmax were 2 and 4 h; Cmax were （2. 8 ± 0. 5） and （2. 6 ± 0. 18）mg· L^-1; AUC（0-t） were （18.4 ± 2. 4） and （27. 0 ± 2. 2）mg· L^-1· h ; the relative bioavailability of A was （149. 0 ± 11.2）% . CONCLUSION The pharmacokinetics of diammonium glycyrrhizinate in rabbits accord with the two compartment models and with the first absorption after A or R administration tmax and AUC（0-t） of A were all higher than those of R,and A had a higher bioavailability.

关 键 词：甘草酸二铵 胃内滞留漂浮型缓释片 药动学 相对生物利用度 

分 类 号：R969.1[医药卫生—药理学]