复方对乙酰氨基酚维生素C泡腾片人体生物等效性研究

The clinical pharmacokinetics and bioequivalence of paracetamol and Vitamin C compound effervescent tablet

目的:研究复方对乙酰氨基酚维生素C泡腾片人体生物等效性。方法:18名健康男性志愿受试者,随机分为2组,分别于早晨空腹一次口服供试品2片(每片含对乙酰氨基酚330mg和维生素C200mg)或对照品必理通1片(每片含对乙酰氨基酚500mg)+维生素C4片(每片含维生素C100mg),用200ml水服用。1周后再交叉服药。受试者分别于服药前和服药后0.25、0.5、1、1.5、2、3、4、6、8、10、12和24h抽取静脉血3ml,以高效液相法(HPLC)测定对乙酰氨基酚血药浓度。结果:两药均符合口服一级吸收二房室开放模型。主要参数:对乙酰氨基酚供试品和对照品Tmax为(0.29±0.10)和(0.68±0.46)h,Cmax为(16.87±3.81)和(8.69±3.25)μg·ml-1,AUC为(36.33±8.70)和(26.22±8.33)μg·ml-1·h。各参数间除Tmax和Cmax差异有十分显著性外(P<0.01)其它差异均无显著性。供试品相对生物利用度为109.81%±11.44%,RSD为10.42%。结论:生物等效性检验后认为两药AUC体内生物等效性相同,Tmax和Cmax生物等效有差异,泡腾片剂型较普通片吸收快,Tmax小。

Objective To compare the pharmacokinetics and bioequivalence of between effervescent tablet and general tablet of paracetamol. Methods 18 Chinese healthy male volunteers in a randomized 2-way crossover study were given a single oral dose 660 mg effervescent tablet (sample) and 500 mg general tablet (control) respectively. The plasma concentrations of paracetamol was measured by high performance liquid chromatography. Results The serum concentration-time curves appeared one-compartment open model. The results of the effervescent tablet and the general tablet of paracetamol showed that Tmax (0.29±0.10) and 0.68 ±0.46h Cmax (16.87±3.81) and (8.69±3.25)μg.ml-1 T1/2 (10.56±1.75) and 10.16±1.65 h AUC (36.33±8.70) and (26.22±8.33) μg.ml-1.h. Conclusion No significant difference appears in the pharmacokinetic parameters between the two formulations except for Tmax and Cmax (P<0.01). The relative bioavailability of paracetamol effervescent tablet is 109.81%±11.44%. The AUC between the two formulations is bioequivalent but the Tmax and Cmax are non-bioequivalent. The absorption of effervescent tablet is faster than of general tablet and the former Tmax is smaller .