title: [The pharmacokinetics and bioequivalence of various dosage forms of ambroxol].
abstract: An intraindividual comparative single-dose study was carried out under carefully controlled conditions on 12 healthy volunteers in order to establish the bioavailability of trans-4-(2-amino-3,5-dibromobenzyl)-amino-cyclohexanol (ambroxol) the active principle of newly developed tablets and drops, in comparison to a commercial i.v. preparation. In an additional single-dose, cross-over study on 12 healthy volunteers the bioequivalence of ambroxol was investigated after administration of a newly developed vs. a commercial dose-equivalent, sustained-release dosage form. Following off-line derivatisation using formaldehyde to the corresponding tetrahydroquinazoline compound, ambroxol was assayed from plasma by high-performance liquid chromatography. A 2-compartment model was taken as a basis for the calculation of the plasma concentration curves and the pharmacokinetic parameters following intravenous injection of the drug. After i.v. administration, the terminal elimination half-life, the apparent volume of distribution and the total plasma clearance were determined to be 3.72 h, 1.52 l/kg and 565 ml/min, respectively. From the tablet and drop formulations the systemic availabilities were calculated to 73 and 81%, respectively; the mean transit times were determined to be 6.8 and 5.4 h, respectively. Both sustained-release dosage forms investigated are bioequivalent.
mesh_terms: D000328:Adult; D000551:Ambroxol / Q000008:administration & dosage / Q000378:metabolism*; D001964:Bromhexine / Q000031:analogs & derivatives*; D002214:Capsules; D002851:Chromatography, High Pressure Liquid; D003692:Delayed-Action Preparations; D005260:Female; D006801:Humans; D007700:Kinetics; D008297:Male; D012996:Solutions; D013607:Tablets; D013810:Therapeutic Equivalency
chemical_list: D002214:Capsules; D003692:Delayed-Action Preparations; D012996:Solutions; D013607:Tablets; D000551:Ambroxol; D001964:Bromhexine
vernacular_title: Untersuchungen zur Pharmakokinetik und Bioäquivalenz unterschiedlicher Darreichungsformen von Ambroxol.