Kummer M, Mehlhaus N
Fortschr Med. 1984 Feb 16;102(7):173-8.
The plasma concentrations of acetaminophen (paracetamol) and codeine were determined in a cross-over study in twelve healthy volunteers after oral and rectal application of a compound preparation. The relative bioavailability from the two forms of application was also computed. The two active substances showed almost parallel plasma concentration paths, and thus were systemically available at the same time. The maximum levels in plasma were already reached after one to two hours. In both active substances the suppositories displayed a classical retardation effect. In contrast to acetaminophen the rectal absorption of codeine was almost as effective as the oral absorption. Thus this application form shows almost bioequivalency vis-à-vis the capsule form. Based on these results the rectal form of administration of codeine as well as the combination of this substance with acetaminophen can be regarded, from the pharmacokinetic point of view, as a rational enhancement of the treatment of various forms of pain.
在一项交叉研究中,对12名健康志愿者口服和直肠给予复方制剂后,测定了对乙酰氨基酚(扑热息痛)和可待因的血浆浓度。还计算了两种给药方式的相对生物利用度。两种活性物质显示出几乎平行的血浆浓度变化轨迹,因此它们在体内的起效时间相同。血浆中的最高浓度在1至2小时后即可达到。两种活性物质的栓剂均显示出典型的缓释作用。与对乙酰氨基酚不同,可待因的直肠吸收几乎与口服吸收一样有效。因此,这种给药形式与胶囊形式几乎具有生物等效性。基于这些结果,从药代动力学角度来看,可待因的直肠给药形式以及该物质与对乙酰氨基酚的组合可被视为合理增强各种疼痛治疗效果的方法。