Tags

Type your tag names separated by a space and hit enter

Prediction of the Oral Pharmacokinetics and Food Effects of Gabapentin Enacarbil Extended-Release Tablets Using Biorelevant Dissolution Tests.
Biol Pharm Bull. 2018; 41(11):1708-1715.BP

Abstract

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 extended-release (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.

Authors+Show Affiliations

Pharmaceutical Research and Technology Labs., Astellas Pharma Inc. Department of Medical Biochemistry, School of Pharmaceutical Sciences, University of Shizuoka.Pharmaceutical Research and Technology Labs., Astellas Pharma Inc.Pharmaceutical Research and Technology Labs., Astellas Pharma Inc.Department of Medical Biochemistry, School of Pharmaceutical Sciences, University of Shizuoka.Department of Medical Biochemistry, School of Pharmaceutical Sciences, University of Shizuoka.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

30381671

Citation

Yamaguchi Ikeuchi, Satomi, et al. "Prediction of the Oral Pharmacokinetics and Food Effects of Gabapentin Enacarbil Extended-Release Tablets Using Biorelevant Dissolution Tests." Biological & Pharmaceutical Bulletin, vol. 41, no. 11, 2018, pp. 1708-1715.
Yamaguchi Ikeuchi S, Kambayashi A, Kojima H, et al. Prediction of the Oral Pharmacokinetics and Food Effects of Gabapentin Enacarbil Extended-Release Tablets Using Biorelevant Dissolution Tests. Biol Pharm Bull. 2018;41(11):1708-1715.
Yamaguchi Ikeuchi, S., Kambayashi, A., Kojima, H., Oku, N., & Asai, T. (2018). Prediction of the Oral Pharmacokinetics and Food Effects of Gabapentin Enacarbil Extended-Release Tablets Using Biorelevant Dissolution Tests. Biological & Pharmaceutical Bulletin, 41(11), 1708-1715. https://doi.org/10.1248/bpb.b18-00456
Yamaguchi Ikeuchi S, et al. Prediction of the Oral Pharmacokinetics and Food Effects of Gabapentin Enacarbil Extended-Release Tablets Using Biorelevant Dissolution Tests. Biol Pharm Bull. 2018;41(11):1708-1715. PubMed PMID: 30381671.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Prediction of the Oral Pharmacokinetics and Food Effects of Gabapentin Enacarbil Extended-Release Tablets Using Biorelevant Dissolution Tests. AU - Yamaguchi Ikeuchi,Satomi, AU - Kambayashi,Atsushi, AU - Kojima,Hiroyuki, AU - Oku,Naoto, AU - Asai,Tomohiro, PY - 2018/11/2/entrez PY - 2018/11/2/pubmed PY - 2019/2/15/medline KW - USP apparatus 4 (flow-through cell) KW - United States Pharmacopeia (USP) apparatus 3 (BioDis) KW - biorelevant dissolution testing KW - extended-release KW - oral administration KW - pharmacokinetics SP - 1708 EP - 1715 JF - Biological & pharmaceutical bulletin JO - Biol Pharm Bull VL - 41 IS - 11 N2 - 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 extended-release (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. SN - 1347-5215 UR - https://www.unboundmedicine.com/medline/citation/30381671/Prediction_of_the_Oral_Pharmacokinetics_and_Food_Effects_of_Gabapentin_Enacarbil_Extended_Release_Tablets_Using_Biorelevant_Dissolution_Tests_ L2 - https://dx.doi.org/10.1248/bpb.b18-00456 DB - PRIME DP - Unbound Medicine ER -