NDLI: Population pharmacokinetics of S(−)-carvedilol in healthy volunteers after administration of the immediate-release (IR) and the new controlled-release (CR) dosage forms of the racemate

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Population pharmacokinetics of S(−)-carvedilol in healthy volunteers after administration of the immediate-release (IR) and the new controlled-release (CR) dosage forms of the racemate

Content Provider	Springer Nature Link
Author	Othman, Ahmed A. Tenero, David M. Boyle, Duane A. Eddington, Natalie D. Fossler, Michael J.
Copyright Year	2007
Abstract	Carvedilol is a β$_{1}$-, β$_{1}$-, and α$_{1}$-adrenoreceptor blocker indicated for treatment of hypertension and mild-tosevere congestive heart failure. The objective of this study was to develop and evaluate a single population model that describesS(−)-carvedilol pharmacokinetics from both the immediate-release (IR) and the new controlled-release dosage forms of the racemate. Carvedilol IR data (1270 measurements) were obtained from 2 open-label studies (50 mg/25 mg Q12 hours for 2 doses). Carvedilol CR data (2058 measurements) were obtained from an open-label, nonrandomized, dose-rising (10, 20, 40, and 80 mg), 4-period balanced crossover study. All data were simultaneously analyzed using NONMEM V. Leverage analysis and internal evaluations were conducted for the final model. A 2-compartment model with first-order absorption and elimination provided the best fit. The model included different absorption rates (KAs) for the CR and IR morning (IR$_{AM}$) and evening (IR$_{PM}$) doses; incorporating change-points at certain times. Estimates of KAs indicated that the absorption was slower at equivalent times and extended for CR relative to IR carvedilol. Oral clearance ofS(−)-carvedilol was 149 L/h. The IR$_{PM}$ and the CR doses had bioavailability (F$_{rel}$) of 0.80 and 0.76, respectively, relative to the IR$_{AM}$ dose. The inter-subject variability in KAs was lower for the CR dosage form than the original IR dosage form. Estimation of interoccasion variability on KAs and F$_{rel}$ for the CR dosage form improved the fit. The model performed well in simulation and leverage analysis indicated its robustness. The model will be a useful tool for future simulation studies.
Starting Page	E208
Ending Page	E218
File Format	PDF
ISSN	12341234
Journal	The AAPS Journal
Volume Number	9
Issue Number	2
e-ISSN	15507416
Language	English
Publisher	Springer-Verlag
Publisher Date	2007-01-01
Publisher Institution	American Association of Pharmaceutical Scientists
Publisher Place	New York
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Carvedilol controlled-release NONMEM relative bioavailability population analysis Pharmacy Pharmacology/Toxicology Biotechnology
Content Type	Text
Resource Type	Article

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Corrigendum: Population pharmacokinetics of S(-)-carvedilol in healthy volunteers after administration of the immediate-release (IR) and the new controlled-release (CR) dosage forms of the racemate

Corrigendum: Population pharmacokinetics of S(-)-carvedilol in healthy volunteers after administration of the immediate-release (IR) and the new controlled-release (CR) dosage forms of the racemate

Population pharmacokinetics of S(−)-carvedilol in healthy volunteers after administration of the immediate-release (IR) and the new controlled-release (CR) dosage forms of the racemate

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