Sotiropoulus J B, Deutsch T, Plakogiannis F M
J Pharm Sci. 1981 Apr;70(4):422-5. doi: 10.1002/jps.2600700420.
Four different acetaminophen products (three tablets and one liquid) were evaluated for their in vitro properties and in vivo comparative bioavailability. The in vivo properties included assay, hardness, thickness, friability, weight variation, content uniformity, disintegration, and dissolution. A statistically significant variation was observed in friability, disintegration, and dissolution. The dissolution rates were determined in 0.1 N HCl under sink conditions, and the T50% value for Brand A was 50 min while the values for Brands B and C were 1 min. The in vivo evaluation was completed in four subjects with a urinary excretion experiment using a crossover design. The calculated elimination half-lives were 4.12, 2.77, 3.14. amd 2 h for Brands A, B, and C and the standard, respectively. The relative bioavailabilities (with respect to solution) were 82, 87, and 92% for Brands A, B, and C, respectively. The mean amount excreted with Brand A was less than the reference at all time points, although it was not significant. Comparison of the in vitro and in vivo data for the three tablets indicated that the rate and amount of acetaminophen excreted may be related to the dissolution rate.
对四种不同的对乙酰氨基酚产品（三种片剂和一种液体制剂）进行了体外性质和体内相对生物利用度的评估。体内性质包括含量测定、硬度、厚度、脆碎度、重量差异、含量均匀度、崩解和溶出。观察到脆碎度、崩解和溶出存在统计学上的显著差异。在0.1N盐酸下沉条件下测定溶出速率，A品牌的T50%值为50分钟，而B品牌和C品牌的值为1分钟。体内评估在四名受试者中采用交叉设计通过尿液排泄实验完成。计算得出的A、B、C品牌以及标准品的消除半衰期分别为4.12、2.77、3.14和2小时。A、B、C品牌的相对生物利用度（相对于溶液）分别为82%、87%和92%。尽管不显著，但在所有时间点，A品牌的平均排泄量均低于参比制剂。对三种片剂的体外和体内数据比较表明，对乙酰氨基酚的排泄速率和量可能与溶出速率有关。
