Bioavailability of dextromethorphan (as dextrorphan) from sustained release formulations in the presence of guaifenesin in human volunteers. 1998

S Demirbas, and L Reyderman, and S Stavchansky
The University of Texas at Austin, College of Pharmacy, Pharmaceutics Division, 78712, USA.

A multiple dose bioavailability study with six healthy male human volunteers was conducted. The bioavailability of an experimental sustained release tablet containing dextromethorphan hydrobromide (DXP-HBr), was compared with a marketed sustained release DXP-HBr suspension in a three-way crossover study. Plasma samples, collected serially after oral drug administration, were analysed for the major metabolite of dextromethorphan (DXP), dextrorphan (DX), using a specific HPLC method with fluorescence detection. The bioavailability parameters; area under the concentration-time curve (AUC), maximum plasma concentration (Cmax), and time to peak (Tmax), were obtained from the plasma concentration-time data. Additionally, pharmacokinetic parameters such as mean residence time (MRT), accumulation factor (R), fluctuation index (Fi), total body clearance (Cl), and the average concentration (C) were estimated by using model independent kinetics approach. Analysis of variance of the data revealed that the presence of guaifenesin in the test formulation does not appear to have a statistically significant (p > 0.05) effect on the bioavailability of dextromethorphan as dextrorphan. The relative bioavailability of the tablet dosage form with respect to the suspension was found to be 113% on Day 1 and 110% on Day 6.

UI MeSH Term Description Entries
D008297 Male Males
D002851 Chromatography, High Pressure Liquid Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed. Chromatography, High Performance Liquid,Chromatography, High Speed Liquid,Chromatography, Liquid, High Pressure,HPLC,High Performance Liquid Chromatography,High-Performance Liquid Chromatography,UPLC,Ultra Performance Liquid Chromatography,Chromatography, High-Performance Liquid,High-Performance Liquid Chromatographies,Liquid Chromatography, High-Performance
D003692 Delayed-Action Preparations Dosage forms of a drug that act over a period of time by controlled-release processes or technology. Controlled Release Formulation,Controlled-Release Formulation,Controlled-Release Preparation,Delayed-Action Preparation,Depot Preparation,Depot Preparations,Extended Release Formulation,Extended Release Preparation,Prolonged-Action Preparation,Prolonged-Action Preparations,Sustained Release Formulation,Sustained-Release Preparation,Sustained-Release Preparations,Timed-Release Preparation,Timed-Release Preparations,Controlled-Release Formulations,Controlled-Release Preparations,Extended Release Formulations,Extended Release Preparations,Slow Release Formulation,Sustained Release Formulations,Controlled Release Formulations,Controlled Release Preparation,Controlled Release Preparations,Delayed Action Preparation,Delayed Action Preparations,Formulation, Controlled Release,Formulations, Controlled Release,Prolonged Action Preparation,Release Formulation, Controlled,Release Formulations, Controlled,Sustained Release Preparation,Timed Release Preparation,Timed Release Preparations
D003915 Dextromethorphan Methyl analog of DEXTRORPHAN that shows high affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist (RECEPTORS, N-METHYL-D-ASPARTATE) and acts as a non-competitive channel blocker. It is one of the widely used ANTITUSSIVES, and is also used to study the involvement of glutamate receptors in neurotoxicity. d-Methorphan,Delsym,Dextromethorphan Hydrobromide,Dextromethorphan Hydrobromide, (+-)-Isomer,Dextromethorphan Hydrobromide, Monohydrate,Dextromethorphan Hydrochloride,Dextromethorphan, (+-)-Isomer,Racemethorphan,Hydrobromide, Dextromethorphan,Hydrochloride, Dextromethorphan
D004347 Drug Interactions The action of a drug that may affect the activity, metabolism, or toxicity of another drug. Drug Interaction,Interaction, Drug,Interactions, Drug
D005100 Expectorants Agents that increase mucous excretion. Mucolytic agents, that is drugs that liquefy mucous secretions, are also included here. Expectorant,Mucolytic,Mucolytic Agent,Mucolytic Agents,Mucolytics,Agent, Mucolytic,Agents, Mucolytic
D006140 Guaifenesin An expectorant that also has some muscle relaxing action. It is used in many cough preparations. Guaiacol Glyceryl Ether,Guaiphenesin,Breonesin,Glycerol Guaiacolate,Guaiphenezine,Guiatuss,Humibid,Hytuss,My-301,Scott-Tussin,Ether, Guaiacol Glyceryl,Glyceryl Ether, Guaiacol,Guaiacolate, Glycerol,My 301,My301,Scott Tussin,ScottTussin
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000328 Adult A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available. Adults
D000996 Antitussive Agents Agents that suppress cough. They act centrally on the medullary cough center. EXPECTORANTS, also used in the treatment of cough, act locally. Antitussive,Antitussive Agent,Antitussive Drug,Cough Suppressant,Antitussive Drugs,Antitussives,Cough Suppressants,Agent, Antitussive,Agents, Antitussive,Drug, Antitussive,Drugs, Antitussive,Suppressant, Cough,Suppressants, Cough

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