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目的建立测定家兔体内甘草酸和甘草次酸血药浓度的HPLC法,进行家兔体内复方甘草酸苷片的药动学研究和生物等效性评价。方法采用双周期自身交叉给药方案,12只新西兰家兔按300mg/kg剂量ig给药,采用HPLC法测定不同时间的血-药浓度,经3p97药动学软件计算药动学参数。结果单剂量ig复方甘草酸苷片受试制剂和参比制剂后,受试制剂和参比制剂的药动学参数分别为:(1)甘草酸的MRT为(44.29±22.89)、(50.31±35.09)h,t1/2为(28.34±17.89)、(33.22±25.96)h,tmax为(10.9±5.8)、(7.3±3.9)h,Cmax分别为(1.81±0.69)、(1.84±0.54)mg/L,AUC0～t为(37.37±9.76)、(39.11±9.88)mg.h/L,相对生物利用度为(99.5±29.0)%;(2)甘草次酸的MRT为(37.93±32.97)、(31.42±21.81)h,t1/2为(18.22±23.67)、(16.50±16.60)h,tmax为(18.10±6.20)、(12.20±5.00)h,Cmax分别为(0.54±0.25)、(0.50±0.16)mg/L,AUC0～t为(9.15±3.88)、(8.69±2.30)mg.h/L,相对生物利用度为(110.4±46.3)%。结论建立的HPLC法简便、准确,重现性好,复方甘草酸苷片受试制剂和参比制剂在家兔体内生物等效。
Objective To establish a HPLC method for determination of blood concentration of glycyrrhizic acid and glycyrrhetinic acid in rabbits and to study the pharmacokinetics and bioequivalence of compound glycyrrhizin tablets in rabbits. Methods Two-cycle self-cross-dosing regimen was used. Twelve New Zealand rabbits were administered ig at a dose of 300 mg/kg. The blood-drug concentrations at different times were determined by HPLC and the pharmacokinetic parameters were calculated using 3p97 pharmacokinetic software. Results The pharmacokinetic parameters of the test and reference preparations were as follows: (1) The MRT of glycyrrhizic acid was (44.29±22.89), (50.31±) 35.09) h, t1/2 is (28.34±17.89), (33.22±25.96) h, tmax is (10.9±5.8), (7.3±3.9) h, Cmax is (1.81±0.69), (1.84±0.54) Mg/L, AUC0-t were (37.37±9.76), (39.11±9.88) mg.h/L, relative bioavailability was (99.5±29.0)%; (2) MRT of glycyrrhetinic acid was (37.93±32.97). ), (31.42±21.81) h, t1/2 was (18.22±23.67), (16.50±16.60) h, tmax was (18.10±6.20), (12.20±5.00) h, and Cmax was (0.54±0.25), respectively. (0.50±0.16) mg/L, AUC0-t were (9.15±3.88), (8.69±2.30) mg.h/L, and the relative bioavailability was (110.4±46.3)%. Conclusion The established HPLC method is simple, accurate, and reproducible. The test preparation and reference preparation of compound glycyrrhizin tablets are bioequivalent in rabbits.