乙胺嘧啶和磺胺多辛的血浆浓度以及通过计算机曲线拟合对药代动力学数据的评估。
Plasma concentrations in pyrimethamine and sulfadoxine and evaluation of pharmacokinetic data by computerized curve fitting.
作者信息
Weidekamm E, Plozza-Nottebrock H, Forgo I, Dubach U C
出版信息
Bull World Health Organ. 1982;60(1):115-22.
Abstract
For the determination of the plasma concentration profiles of pyrimethamine and sulfadoxine after the administration of 1 tablet of Fansidar, highly specific analytical methods are needed as the pyrimethamine concentration is low (0.2 - 0.02 mg/litre) and the concentration ratio of the two components in the plasma is high (> 1: 500). The microbiological method described in this paper fulfils these requirements for high specificity and sensitivity (the sensitivity limit for sulfadoxine is 1 mg/litre and for pyrimethamine is 0.013 mg/litre).Pharmacokinetic data were evaluated for 14 volunteers after administration of 1 tablet of Fansidar, and a computer simulation of multiple dosing (1 tablet per week) was performed.
摘要
为了测定服用1片Fansidar后乙胺嘧啶和磺胺多辛的血浆浓度曲线，由于乙胺嘧啶浓度较低（0.2 - 0.02毫克/升）且血浆中两种成分的浓度比很高（> 1:500），因此需要高度特异性的分析方法。本文所述的微生物学方法满足了这些高特异性和高灵敏度的要求（磺胺多辛的灵敏度极限为1毫克/升，乙胺嘧啶为0.013毫克/升）。对14名志愿者服用1片Fansidar后的药代动力学数据进行了评估，并进行了多次给药（每周1片）的计算机模拟。
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本文引用的文献
1
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J Antibiot (Tokyo). 1970 May;23(5):250-1. doi: 10.7164/antibiotics.23.250.
2
Comparative toxicological, chemotherapeutic and pharmacokinetic studies with sulphormethoxine and other sulphonamides in animals and man.磺胺甲氧嗪与其他磺胺类药物在动物和人体中的比较毒理学、化疗学及药代动力学研究。
Chemotherapy. 1969;14(4):195-226. doi: 10.1159/000220630.
3
Pharmacokinetic rationale for a malarial suppressant administered once monthly.每月给药一次的疟疾抑制剂的药代动力学原理。
Ann Trop Med Parasitol. 1975 Jun;69(2):141-5. doi: 10.1080/00034983.1975.11686995.
4
The treatment of malaria.疟疾的治疗。
Br Med J. 1976 Feb 7;1(6005):323-8. doi: 10.1136/bmj.1.6005.323.
5
Determination of plasma concentrations of dapsone, monoacetyl dapsone and pyrimethamine in human subjects dosed with maloprim.测定服用复方磺胺多辛的人体受试者中氨苯砜、单乙酰氨苯砜和乙胺嘧啶的血浆浓度。
J Chromatogr. 1979 Jun 11;163(2):179-85. doi: 10.1016/s0378-4347(00)81461-9.
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