A theoretical approach to evaluate the release rate of acetaminophen from erosive wax matrix dosage forms

Agata, Yasuyoshi; Iwao, Yasunori; Shiino, Kai; Miyagishima, Atsuo; Itai, Shigeru

doi:10.1016/j.ijpharm.2011.05.015

Cited by 7 publications

(1 citation statement)

References 6 publications

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“…4a. In contrast, the predicted C max and AUC 0-inf with BioDis were close to the observed values with their %PE values of within 15%, which is generally considered to be high prediction accuracy, 29) for both PK parameters. The simulated T max was 0.83 h earlier than the observed mean value, suggesting that some subjects in clinical studies might exhibit slower gastric emptying of the gabapentin enacarbil ER tablet than the assumed 1 h in the in vitro dissolution test under the simulated fasted state.…”

Section: Resultssupporting

confidence: 50%

Prediction of the Oral Pharmacokinetics and Food Effects of Gabapentin Enacarbil Extended-Release Tablets Using Biorelevant Dissolution Tests

Ikeuchi

Kambayashi

Kojima

et al. 2018

Biological & Pharmaceutical Bulletin

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The purpose of this research was to establish an in vitro dissolution testing method to predict the oral pharmacokinetic (PK) profiles and food effects of gabapentin enacarbil formulated as wax matrix extendedrelease (ER) tablets in humans. We adopted various biorelevant dissolution methods using the United States Pharmacopeia (USP) apparatus 2, 3 and 4 under simulated fasted and fed states. Simulated PK profiles using the convolution approach were compared to published in vivo human PK data. USP apparatus 2 and 4 underestimated the in vivo performance due to slow in vitro dissolution behaviors. In contrast, biorelevant dissolution using USP apparatus 3 coupled with the convolution approach successfully predicted the oral PK profile of gabapentin enacarbil after oral administration of a Regnite ® tablet under fasted state. This approach might be useful for predicting the oral PK profiles of other drugs formulated as wax matrix-type ER tablets under fasted state.

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Section: Resultssupporting

confidence: 50%