Premium
Pharmacokinetics of Gabapentin in a Novel Gastric‐Retentive Extended‐Release Formulation: Comparison With an Immediate‐Release Formulation and Effect of Dose Escalation and Food
Author(s) -
Chen Cuiping,
Cowles Verne E.,
Hou Eddie
Publication year - 2011
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/0091270010368411
Subject(s) - pharmacokinetics , gabapentin , bioavailability , plasma concentration , pharmacology , dosing , immediate release , dosage form , medicine , chemistry , pathology , alternative medicine
The objectives of the 3 phase I studies described herein were (1) to compare the pharmacokinetics of gabapentin delivered from a novel gastric‐retentive dosage form vs an immediate‐release formulation, (2) to assess the dose proportionality of the gastric‐retentive extended‐release formulation, and (3) to determine the effect of food on the pharmacokinetics of gabapentin delivered from this formulation. The time to reach maximum plasma concentration (t max ) was extended for gabapentin delivered from the gastric‐retentive extended‐release formulation compared with the immediate‐release formulation. A dose‐related increase in both the maximum plasma concentration (C max ) and the area under the plasma concentration‐time curve (AUC) was observed as the gabapentin dose increased from 600 to 2400 mg. Fed status and increased fat content delayed t max and enhanced C max and AUC in proportion to the fat content. The pharmacokinetics of gabapentin delivered from this extended‐release formulation allows a reduced dosing frequency while maintaining bioavailability and possibly diminishing the occurrence of adverse events attributable to a slower increase to the peak concentration compared with the immediate‐release dosage form.