首页> 外文期刊>The Journal of Clinical Pharmacology: Official Journal of the American College of Clinical Pharmacology >A phase I/II evaluation of oral L-2-oxothiazolidine-4-carboxylic acid in asymptomatic patients infected with human immunodeficiency virus.
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A phase I/II evaluation of oral L-2-oxothiazolidine-4-carboxylic acid in asymptomatic patients infected with human immunodeficiency virus.

机译:对感染人免疫缺陷病毒的无症状患者口服L-2-氧噻唑烷-4-羧酸进行I / II期I / II期评估。

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摘要

A randomized double-blind, placebo-controlled study was conducted in 37 asymptomatic HIV-infected individuals (mean CD4 count 707 cells/mm3) to characterize the safety, pharmacokinetics, and effect on blood thiols of three dosage levels of a cysteine prodrug, L-2-oxothiazolidine-4-carboxylic acid (OTC; Procysteine; Clintec Technologies, Deerfield, IL). Single-dose administration of OTC resulted in measurable plasma levels at all dosages, with a mean peak plasma concentration of 734 +/- 234 nmol/mL at the highest dosage studied. After 4 weeks of administration three times daily, a statistically significant increase was seen in whole blood glutathione in the 1,500 mg and 3,000 mg dose groups compared with the placebo group. A significant increase in whole blood cysteine and peripheral blood mononuclear cell (PBMC) glutathione was not seen during the study period.
机译:在37个无症状HIV感染者中进行了一项随机双盲,安慰剂对照研究(平均CD4计数707细胞/ mm3),以表征三种剂量水平的半胱氨酸前药L的安全性,药代动力学和对血硫醇的影响-2-氧噻唑烷-4-羧酸(OTC;脯氨酸; Clintec Technologies,Deerfield,IL)。在所有剂量下,单剂量OTC均可产生可测量的血浆水平,在研究的最高剂量下,平均峰值血浆浓度为734 +/- 234 nmol / mL。每天3次给药4周后,与安慰剂组相比,在1500 mg和3,000 mg剂量组中,全血谷胱甘肽有统计学意义的增加。在研究期间未见全血半胱氨酸和外周血单核细胞(PBMC)谷胱甘肽的显着增加。

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