Fritz A K, Benziger D P, Peterson J E, Park G B, Edelson J
J Pharm Sci. 1984 Mar;73(3):326-31. doi: 10.1002/jps.2600730311.
The relative bioavailability and pharmacokinetics of a combination product containing pentazocine and acetaminophen were studied in 20 healthy human males. Each subject, in a single-dose three-way crossover design, received two different preparations containing 50 mg of pentazocine (as base) and 1300 mg of acetaminophen either as capsule-shaped tablets or as a solution. Plasma concentrations of pentazocine and acetaminophen were determined from 0.25 to 12 h following oral administration. The plasma data for both compounds in the tablet formulation were described by an open one-compartment body model with first-order absorption. The average (+/- SD) bioavailability of the tablet relative to that of the solution was 85.0 +/- 31.1 and 88.6 +/- 13.1% for pentazocine and acetaminophen, respectively. The apparent first-order regression-dependent elimination rate constants for pentazocine from the tablet and solution preparations were 0.19 +/- 0.08 and 0.20 +/- 0.06 h-1, respectively, while the rate constants for acetaminophen were 0.26 +/- 0.03 and 0.25 +/- 0.03 h-1 for the tablet and solution preparations, respectively. These rate constants correspond to terminal elimination half-lives of approximately 3.6 h for pentazocine and approximately 2.7 h for acetaminophen.
在20名健康男性中研究了含喷他佐辛和对乙酰氨基酚的复方制剂的相对生物利用度和药代动力学。在单剂量三交叉设计中，每位受试者分别接受两种不同制剂，分别为含50mg喷他佐辛（以碱计）和1300mg对乙酰氨基酚的胶囊形片剂或溶液。口服给药后0.25至12小时测定喷他佐辛和对乙酰氨基酚的血浆浓度。片剂制剂中两种化合物的血浆数据均用具有一级吸收的开放一室模型描述。片剂相对于溶液的平均（±标准差）生物利用度，喷他佐辛为85.0±31.1%，对乙酰氨基酚为88.6±13.1%。片剂和溶液制剂中喷他佐辛的表观一级回归依赖消除速率常数分别为0.19±0.08和0.20±0.06 h-1，而片剂和溶液制剂中对乙酰氨基酚的速率常数分别为0.26±0.03和0.25±0.03 h-1。这些速率常数对应的喷他佐辛终末消除半衰期约为3.6小时，对乙酰氨基酚约为2.7小时。
