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疱疹样皮炎中氨苯砜的药代动力学观察。

Pharmacokinetic observations on dapsone in dermatitis herpetiformis.

作者信息

Swain A F, Ahmad R A, Rogers H J, Leonard J N, Fry L

出版信息

Br J Dermatol. 1983 Jan;108(1):91-8. doi: 10.1111/j.1365-2133.1983.tb04583.x.

Abstract

The pharmacokinetics of dapsone (DDS) and monoacetyldapsone (MADDS) following an oral dose of 150 mg DDS were studied in sixteen patients with dermatitis herpetiformis and seven normal subjects. No differences in DDS disposition were observed between the two groups. The maintenance dose of DDS for individual patients was not significantly correlated with jejunal biopsy morphology, DDS or MADDS half-lives, or the area under the plasma concentration-time curves for DDS or MADDS. DDS plasma protein binding was normal in patients and did not apparently determine the concentration of DDS in skin biopsies, for which the skin/plasma DDS concentration ratio was approximately unity. There was no undue representation of acetylator phenotype in the patient group and no correlation between maintenance dose and MADDS/DDS ratio was noted. The determinants of the maintenance DDS dose have not been found. This may relate to pharmacodynamic differences, but alternatively the concentration of oxidative metabolites rather than DDS or MADDS could be responsible for the therapeutic activity in dermatitis herpetiformis.

摘要

对16例疱疹样皮炎患者和7名正常受试者口服150mg氨苯砜(DDS)后的氨苯砜(DDS)和单乙酰氨苯砜(MADDS)的药代动力学进行了研究。两组之间未观察到DDS处置的差异。个体患者的DDS维持剂量与空肠活检形态、DDS或MADDS半衰期、或DDS或MADDS的血浆浓度-时间曲线下面积均无显著相关性。患者的DDS血浆蛋白结合正常,且显然不决定皮肤活检中DDS的浓度,皮肤/血浆DDS浓度比约为1。患者组中乙酰化表型没有过度表现,且未观察到维持剂量与MADDS/DDS比值之间的相关性。尚未发现维持DDS剂量的决定因素。这可能与药效学差异有关,但氧化代谢物的浓度而非DDS或MADDS可能是疱疹样皮炎治疗活性的原因。

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