In Vitro/in vivo relationship of gabapentin from a sustained-release tablet formulation: a pharmacokinetic study in the beagle dog.
The aim of this study was to examine the in vitro/in vivo relationship of the drug release behavior of a sustained-release formulation of gabapentin. The immediate-release formulation was used as the reference formulation. The dissolution test was employed using pH 1.2, 4.0, or 6.8 buffer solution, or water, to determine the in vitro release behaviors of gabapentin tablets. Gabapentin was released completely within 1 h from the immediate-release tablet and released for 12 h from the sustained-release tablet. A single dose (600 mg) of each formulation was orally administered to four beagle dogs under fasted conditions, and the pharmacokinetic parameters were calculated. Although the sustained-release tablet did not disintegrate and had slow drug release characteristics, it showed similar pharmacokinetic parameters to the immediate-release tablet, which rapidly disintegrated and showed fast drug release. Thus, the in vivo release of gabapentin did not correlate with in vitro release of drug.
Rhee
Yun-Seok
YS
College of Pharmacy, Sungkyunkwan University, Suwon, Korea.
Park
Seok
S
Lee
Tae-Won
TW
Park
Chun-Woong
CW
Nam
Tae-Young
TY
Oh
Tack-Oon
TO
Jeon
Ji-Woong
JW
Han
Sang Beom
SB
Lee
Dong-Soo
DS
Park
Eun-Seok
ES
D000588:Amines / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D000818:Animals; D000927:Anticonvulsants / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D019540:Area Under Curve; D002138:Calibration; D002851:Chromatography, High Pressure Liquid; D003509:Cyclohexanecarboxylic Acids / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D003692:Delayed-Action Preparations; D004285:Dogs; D000077206:Gabapentin; D006207:Half-Life; D008297:Male; D011786:Quality Control; D015203:Reproducibility of Results; D012995:Solubility; D005680:gamma-Aminobutyric Acid / Q000008:administration & dosage* / Q000493:pharmacokinetics*
D000588:Amines; D000927:Anticonvulsants; D003509:Cyclohexanecarboxylic Acids; D003692:Delayed-Action Preparations; D005680:gamma-Aminobutyric Acid; D000077206:Gabapentin