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目的评价三药厂对乙酰氨基酚片(A、B、C)的生物等效性及体内吸收与体外释放的相关性,为评价口服制剂质量提供依据。方法试验为口服单剂量三周期三交叉设计,采用高效液相色谱法测定对乙酰氨基酚经时血浓度,DAS软件计算对乙酰氨基酚主要药代动力学参数,体外溶出试验方法计算口服制剂体外释放参数T50和Td,评价体外释放与体内吸收的相关性。结果对乙酰氨基酚A、B、C片口服给药后对乙酰氨基酚药代动力学参数t1/2为(2.41±0.51)、(2.85±0.55)和(7.79±0.54)h,Tm ax为(1.38±0.60)、(0.98±1.00)和(0.98±0.43)h,AUC0-15为(27.24±10.87)、(27.64±8.01)和(26.76±0.43)μg/mL.h,AUC0-∞为(27.68±10.94)、(28.36±8.16)和(27.46±7.29)μg/mL.h;T50为(33.34±4.81)、(3.33±0.38)和(2.54±0.32)m in,Td为(41.24±4.03)、(4.50±0.61)和(3.67±0.45)m in。结论三药厂对乙酰氨基酚片(A、B、C)体外溶出存在统计学差异,但生物等效,体内吸收与体外释放部分相关。
Objective To evaluate the bioequivalence of paracetamol tablets (A, B, C) and the correlation between in vivo absorption and in vitro release of acetaminophen tablets (A, B, C) in order to evaluate the quality of oral preparations. Methods The test was oral single-dose three-cycle three-crossover design. The concentration of paracetamol over time was determined by high performance liquid chromatography. The main pharmacokinetic parameters of paracetamol were calculated by DAS software. The in vitro dissolution test was used to calculate the oral formulation. The parameters T50 and Td were released to assess the correlation between in vitro release and in vivo absorption. Results After oral administration of acetaminophen tablets A, B and C, the pharmacokinetic parameters t1 / 2 of acetaminophen were (2.41 ± 0.51), (2.85 ± 0.55) and (7.79 ± 0.54) h, Tm ax was AUC0-15 was (27.24 ± 10.87), (27.64 ± 8.01) and (26.76 ± 0.43) μg / mL.h respectively, AUC0-∞ was (1.38 ± 0.60), (0.98 ± 1.00) and (27.68 ± 10.94), (28.36 ± 8.16) and (27.46 ± 7.29) μg / mL.h, T50 was (33.34 ± 4.81), (3.33 ± 0.38) and (2.54 ± 0.32) 4.03), (4.50 ± 0.61) and (3.67 ± 0.45) m in. Conclusions The dissolution of acetaminophen tablets (A, B, C) in three pharmaceutical companies is statistically different, but the bioequivalence and in vivo absorption are partly related to the release in vitro.