Hair Analysis for Pharmaceutical Drugs. II. Effective Extraction and Determination of Sildenafil(Viagra^<[○!R]>)and Its N-Desmethyl Metabolite in Rat and Human Hair by GC-MS^<1, 2)>

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概要

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• In order to study the incorporation of sildenafil(SDF)and its N-demethylated metabolite(norSDF)intohair, animal model experiments were carried out. After shaving the back hair, SDF was dosed to two sets of three male dark-agouti pigmented rats(5 weeks old)per each group at 25mg/kg once a day for 5 successive days with intraperitoneal(i.p.)(set1)and oral administration(set2). The regrown back hair was collected 14 d after the first administration. Three typical extraction methods, using methanol-5 M hydrochloric acid, methanol-trifluoroacetie acid and 1 M sodium hydroxide, were evaluated using the rat hair samples containing SDF and norSDF. Methanol-5 M hydrochloric acid was the best extraction method in terms of high efficiency and reproducibility. The extract was purified using Bond EIut Certify columns and was derivatized with trimethylsilylimidazole :N, O-bis(trimethylsilyltrifluoroacetamide):trimethylchlorosilane(3:3:2)at 90℃ for 30 min. The trimethylsilylated products were analyzed by GC-MS using selected ion monitoring. SDF and norSDF were simultaneously detected in the rat hair. The hair concentrations were 4.9.-6.3(av.5.8)ng/mg and 15.6-20.3(av.17.6)ng/mg for SDF and norSDF, respectively, with i.p. administration, and 2.6-4.1(av.3.6)ng/mg and 8.1-10.4(av.9.1)ng/mg with oral administration. The hair concentrations of norSDF were about three times higher than those of SDF, and the ratios of both compounds showed no significant difference between i.p.and oral administmtions. This method was applied to the scalp hair of two patients who orally took SDF at regular intervals for the treatment of penile erectile dysfunction. The hair concentrations of SDF and norSDF in the two patients were 19.8 and 55.9ng/mg, and 1.7 and 5.6ng/mg, respectively.

• 公益社団法人日本薬学会の論文
• 2001-12-01

著者

• Nakahara Yuji

  National Institute Of Health Sciences

• SAISHO Kazuhiro

  National Institute of Health Sciences

• SCOTT Karen

  National Institute of Health Sciences

• MORIMOTO Shigeyoshi

  Kishiwada City Hospital

関連論文

• Hair Analysis for Pharmaceutical Drugs.I.Effective Extraction and Determination of Phenobarbital, Phenytoin and Their Major Metabolites in Rat and Human Hair
• Hair analysis for abused and therapeutic drugs
• Hair Analysis for Pharmaceutical Drugs. II. Effective Extraction and Determination of Sildenafil(Viagra^)and Its N-Desmethyl Metabolite in Rat and Human Hair by GC-MS^
• Hair Analysis for Drugs of Abuse. XVIII. 3,4-Methylenedioxymethamphetamine (MDMA) Disposition in Hair Roots and Use in Identification of Acute MDMA Poisoning
• Hair analysis for drugs of abuse XIX. Determination of ephedrine and its homologs in rat hair and human hair
• Abuse of Smoking Methamphetamine Mixed with Tobacco. V.Plasma Metabolites of N-Cyanomethylmethamphetamine, a Pyrolysis Product Formed by Smoking Methamphetamine in Tobacco, and the Species Difference between Mouse and Rat
• Determination of a New Type of Phosphodiesterase-5 Inhibitor, Thioquinapiperifil, in a Dietary Supplement Promoted for Sexual Enhancement
• The disposition into hair of new designer drugs ; methylone, MBDB and methcathinone

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