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本文引用的文献

1
Tucaresol increases oxygen affinity and reduces haemolysis in subjects with sickle cell anaemia.图卡雷索可增加镰状细胞贫血患者的氧亲和力并减少溶血。
Br J Haematol. 1996 Jun;93(4):817-21. doi: 10.1046/j.1365-2141.1996.d01-1744.x.
2
The pharmacokinetics, tolerability and pharmacodynamics of tucaresol (589C80; 4[2-formyl-3-hydroxyphenoxymethyl] benzoic acid), a potential anti-sickling agent, following oral administration to healthy subjects.图卡瑞索(589C80;4-[2-甲酰基-3-羟基苯氧基甲基]苯甲酸)作为一种潜在的抗镰状化药物,在健康受试者口服给药后的药代动力学、耐受性和药效学。
Br J Clin Pharmacol. 1993 Apr;35(4):419-25. doi: 10.1111/j.1365-2125.1993.tb04160.x.
3
Therapeutic potentiation of the immune system by costimulatory Schiff-base-forming drugs.共刺激席夫碱形成药物对免疫系统的治疗增强作用。
Nature. 1995 Sep 7;377(6544):71-5. doi: 10.1038/377071a0.
4
Pharmacokinetics and pharmacodynamics of tucaresol, an antisickling agent, in healthy volunteers.抗镰状化药物图卡索尔在健康志愿者体内的药代动力学和药效学。
Br J Clin Pharmacol. 1995 Apr;39(4):375-80. doi: 10.1111/j.1365-2125.1995.tb04465.x.
5
The use of non-parametric methods in the statistical analysis of the two-period change-over design.两阶段交叉设计统计分析中非参数方法的应用
Biometrics. 1972 Jun;28(2):577-84.

食物和性别对健康志愿者中土卡瑞醇药代动力学的影响。

Effect of food and gender on the pharmacokinetics of tucaresol in healthy volunteers.

作者信息

Peck R W, Wootton R, Wiggs R, Layton G, Posner J

机构信息

Glaxo Wellcome R & D Ltd, Greenford, Middlesex.

出版信息

Br J Clin Pharmacol. 1998 Jul;46(1):83-6. doi: 10.1046/j.1365-2125.1998.00047.x.

DOI:10.1046/j.1365-2125.1998.00047.x
PMID:9690954
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1873973/
Abstract

AIMS

The potential effects of food and gender on the pharmacokinetics of tucaresol were investigated in healthy volunteers.

METHODS

Ten males (mean weight 76.5 kg, age 27-42 years) and eight females (mean weight 58.9 kg, age 18-44 years) received a single oral dose of 200 mg tucaresol on two occasions in random order. On one occasion, tucaresol was given after an overnight fast and on the other, immediately after ingestion of a standard breakfast.

RESULTS

There were no significant differences in standard pharmacokinetic parameters between the two occasions but the rate of tucaresol absorption was faster after food intake. Female subjects had higher Cmax (ratio 1.25 with 95% CI 1.10-1.44) and AUC (ratio 1.25 with 95% CI 1.05-1.49) values than males but the differences were due to the higher body weights of the males; weight-adjusted apparent total clearance values (CL/F) were not different between genders (ratio 1.03 with 95% CI 0.87-1.21).

CONCLUSIONS

Food intake and gender have no significant effect on the exposure to orally administered tucaresol.

摘要

目的

在健康志愿者中研究食物和性别对土卡索(tucaresol)药代动力学的潜在影响。

方法

10名男性(平均体重76.5千克,年龄27 - 42岁)和8名女性(平均体重58.9千克,年龄18 - 44岁)以随机顺序接受两次单剂量口服200毫克土卡索。一次是在空腹过夜后给予土卡索,另一次是在摄入标准早餐后立即给予。

结果

两次给药之间标准药代动力学参数无显著差异,但进食后土卡索的吸收速率更快。女性受试者的Cmax(比值1.25,95%可信区间1.10 - 1.44)和AUC(比值1.25,95%可信区间1.05 - 1.49)值高于男性,但差异是由于男性体重较高;体重校正后的表观总清除率值(CL/F)在性别之间无差异(比值1.03,95%可信区间0.87 - 1.21)。

结论

食物摄入和性别对口服土卡索的暴露无显著影响。