Detail of "99497-03-7"

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Pharmacokinetics and dose proportionality of domperidone in healthy volunteers

Pharmacokinetics and dose proportionality of domperidone in healthy volunteers. Huang, Yih Chain; Colaizzi, John L.; Bierman, Robert H.; Woestenborghs, Robert; Heykants, Joseph J. P. (Coll. Pharm., Rutgers State Univ., Piscataway, NJ 08854, USA). J. Clin. Pharmacol. 57808-66-9 and 99497-03-7 are cas registry numbers. These chemicals are also mentioned in this article., 26(8), 628-32 (English) 1986. CODEN: JCPCBR. ISSN: 0091-2700. DOCUMENT TYPE: Journal CA Section: 63 (Pharmaceuticals) Section cross-reference(s): 1 The bioequivalence of 20 mg of domperidone (I) [57808-66-9] given as free-base tablets and I maleate [99497-03-7] tablets, and the bioavailability of base and maleate tablets relative to a soln., were studied in 21 fasting men using a crossover design. The absorption of I was very rapid, with mean peak plasma concn. (Cmax) values of 18.8, 15.0, and 20.7 ng/mL attained at 0.9, 1.2, and 0.6 h after the administration of base tablet, maleate tablet, and soln., resp. The mean elimination half-life (t1/2) ranged from 12.6 to 16.0 h. The mean oral clearance (CL/F) after the soln. dose was 4.735-mL/min and the mean apparent vol. of distribution was 6.272 L, indicating an extensive distribution of I in the body. The area under the plasma concn.-time curve (AUC) data demonstrated bioequivalence of base and maleate tablets. The relative bioavailability for base tablet and maleate tablet was 107 and 116%, resp., of that of the soln. Dose proportionality of I was also studied in 12 subjects at soln. doses of 10, 20, and 40 mg. Linear correlations between the dose and Cmax and AUC values were obsd. Mean CL/F remained relatively const. after doses of 10, 20 and 40 mg indicating linear pharmacokinetics of I over the dose range studied. .