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.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2008年第13期1079-1082,共4页
Chinese Journal of Hospital Pharmacy
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
diammonium glycyrrhizinate
floating sustained-release tabletse pharmacokinetics
relative bioavailability
