title: Solid-phase column chromatographic and gas chromatographic-mass spectrometric determination of heptaminol in human urine and related pharmacokinetic profiles.
abstract: Heptaminol is an antihypotensive drug and is one of the stimulants banned in sport competitions. When heptaminol was fortified to a drug-free urine sample and subjected to solid-phase extraction, trifluroacetic anhydride derivatization, and gas chromatography-mass spectrometry analysis, the results indicated three chromatographic peaks, with one major peak [peak 1 (P1) as heptaminol-2TFA], appearing at retention time 7.17 min, and two minor peaks [peak 2 (P2) and peak 3 (P3) as heptaminol-TFA], appearing at RT 5.87 and 5.81 min, respectively. The characteristic ions of peak mass spectra were m/z 322, 224, and 140 for P1, m/z 223 (molecular ion), 208, 140, and 110 for P2, and m/z 208, 140, and 110 for P3. The urine samples collected from healthy male volunteers who orally ingested a single dose (100 mg) of heptaminol were similar to the analytical results shown in the heptaminol-spiked control urine samples. This result suggested that the unchanged heptaminol was the sole form found in urine. The unchanged parent compound was completely eliminated in urine within 24 h and an average of approximately 97% of the dose was excreted through the renal pathway.
authors.affiliation: Institute of Pharmacology and Toxicology and Doping Control Center, Tzu Chi University, Hualien, Taiwan. hing@mail.tcu.edu.tw
authors.forename: Ying Lung
authors.initials: YL
authors.lastname: Tseng
authors.forename: Chin-Hung
authors.initials: CH
authors.lastname: Liu
authors.forename: Fan-Hsin
authors.initials: FH
authors.lastname: Kuo
authors.forename: Min-Hua
authors.initials: MH
authors.lastname: Shieh
mesh_terms: D000089:Acetic Anhydrides; D000284:Administration, Oral; D000328:Adult; D002316:Cardiotonic Agents / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000652:urine*; D004300:Doping in Sports; D005463:Fluoroacetates; D008401:Gas Chromatography-Mass Spectrometry / Q000379:methods*; D006535:Heptaminol / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000652:urine*; D006801:Humans; D008297:Male; D008875:Middle Aged; D015203:Reproducibility of Results; D015813:Substance Abuse Detection / Q000379:methods*; D014269:Trifluoroacetic Acid / Q000737:chemistry
chemical_list: D000089:Acetic Anhydrides; D002316:Cardiotonic Agents; D005463:Fluoroacetates; D006535:Heptaminol; C017958:trifluoroacetic anhydride; D014269:Trifluoroacetic Acid