2种甘草酸二铵制剂的生物等效性研究

Study on Bioequiavailability of 2 Kinds of Diammonium Glycyrrhizinate Preparations

目的:研究甘草酸二铵肠溶片和甘草酸二铵肠溶胶囊的人体药动学及生物等效性。方法:20名健康男性志愿者双周期自身随机交叉、自身对照口服单剂量甘草酸二铵肠溶片(受试制剂)或甘草酸二铵肠溶胶囊(参比制剂)150mg,定时取血,2次用药间隔1周。采用高效液相色谱串联质谱电喷雾(LC-MS/MS)法进行测定,以内标法计算甘草酸血药浓度,用3p97程序计算各项药动学参数。结果:受试制剂与参比制剂的Cmax分别为(61.02±46.78)、(66.30±72.39)μg·L-1,tmax分别为(8.70±2.18)h和(8.60±2.68)h,AUC0～96分别为(1447.24±1071.93)、(1575.49±1543.53)μg·h·L-1,AUC0～∞分别为(1535.69±1118.24)、(1677.82±1630.73)μg·h·L-1;受试制剂相对于参比制剂的生物利用度F0～96、F0～∞分别为(98.16±18.17)%、(97.88±15.43)%。结论:甘草酸二铵肠溶片与草酸二铵肠溶胶囊具有生物等效性。

OBJECTIVE：To study the pharmacokinetics and bioequiavaliability of diammonium glycyrrhizinate enteric tablet and enteric capsule.METHODS：In two-period cross-over design test,20 healthy male volunteers were given 150 mg diammonium glycyrrhizinate enteric tablet（test preparation）or 150 mg diammonium glycyrrhizinate enteric capsule（reference preparation）. Blood samples were collected regularly and medication interval was one week. Plasma concentrations of diammonium glycyrrhizinate were measured by LC-MS/MS method and calculated with internal standard method. Phamacokinetic parameters were calculat-ed with 3p97 process. RESULTS：Main pharmacokinetic parameters of test formulation preparation vs. reference preparation were La1s-0 f17o. 1lB.l9oi3wo）esq：μugi·Cavhm·aa（xlLia6-b11i .lv0its2y.（± o14f 65t.7e7s58t.） 4p9rμ±egp·1ar L5at4-i3o1 .nv5 s3a.）n（dμ6 gr6·e.f3h·e0r±Len-7c1;e2 .A3p9rUe）pCaμ0～rga∞·（tioL1n-5 1w3;5e.rt6me9a （x±F08～1.97 （6101±988.2.21.416）8±）μh1g· 8v.h1s·（.7）L8-%.16 0va±sn.d（2 .1F6 806～）7∞（h7;.98A72.±U88C1±0 ～6193（650..4173 34））4%7μ.g,2·4rh±e·-spectively. CONCLUSION：The results show that test and reference preparations are bioequivalent.