Kinetics of Zolpidem and Its Metabolite after Single Dose Oral Administration

Abstract

ABSTRACT. The present study aimed to describe the basic pharmacokinetics of zolpidem and its metabolite zolpidem phenyl-4-carboxylic acid after a single oral dose of 5 mg zolpidem. Six competing kinetic models were created in order to analyze the experimental data obtained from the 20 healthy volunteers enrolled in a clinical study. Based on rational model discrimination criteria (Akaike index value), the best one was chosen and further used for a better understanding of the kinetics of zolpidem and its metabolite in the body after administration. The kinetic model considers that zolpidem absorption process follows a first-order kinetics and during this stage it is partially metabolized (pre-systemic metabolism) to its main metabolite. The kinetics of both zolpidem and its metabolite is characterized by bicompartmental distribution and first order kinetics of both elimination and systemic metabolism.

Lack of kinetic interaction between zolpidem and duloxetine: results from a drug-drug interaction study in healthy volunteers

“…The chromatographic column used was a Zorbax SB-C18 (100 mm x 3.0 mm i.d., 3.5 μm) (Agilent Technologies). The same bioanalytical method was employed for quantification of zolpidem in other kinetic (PK) study and PK drug-drug interaction study [13,25,27].…”

Kinetics of Dapagliflozin after single dose oral administration of a 10 mg immediate release tablet

“…Compartmental pharmacokinetic analysis offers a better understanding of the relationship between the pharmacological effect and the administered dose. This mathematical approach deals with the quantitative analysis of the pharmacokinetic (PK) processes that occur in the human body after drug administration until its irreversible removal from the body, namely it describes the following processes: absorption, distribution, metabolism, and elimination (ADME) [7,8]. After the active drug substance/active pharmaceutical ingredient (API) is released from the pharmaceutical formulation, it is molecularly dispersed in the internal aqueous medium (or dissolved) and then is absorbed by crossing through various biological membranes, eventually reaching the blood stream [9].…”

“…It also gives a deeper insight of drug interactions with other drugs administered concomitantly or with food intake. Likewise, it permits a better calculation and choice of dosage regimen for a drug in particular situations, when the PK processes of absorption, distribution, metabolism and elimination are modified consequently to disease state or altered physiology [7,8].…”