Design and Evaluation of an Extended-release Matrix Tablet Formulation; the Combination of Hypromellose Acetate Succinate and Hydroxypropylcellulose

Overview

Journal Asian J Pharm Sci

Date 2020 Feb 28

PMID 32104324

Citations 5

Authors

Sachiko Fukui

Hideki Yano

Shuichi Yada

Tsuyoshi Mikkaichi

Hidemi Minami

Affiliations

Soon will be listed here.

Abstract

The purpose of this study was to develop an extended-release (ER) matrix tablet that shows robust dissolution properties able to account for the variability of pH and mechanical stress in the GI tract using a combination of enteric polymer and hydrophilic polymer. Hypromellose acetate succinate (HPMCAS) and hydroxypropylcellulose (HPC) were selected as ER polymers for the ER matrix tablet (HPMCAS/HPC ER matrix tablet). Oxycodone hydrochloride was employed as a model drug. Dissolution properties of the HPMCAS/HPC ER matrix tablets were evaluated and were not affected by the pH of the test medium or paddle rotating speed. In a USP apparatus 3 (bio-relevant dissolution method), dissolution profiles of the HPMCAS/HPC ER matrix tablets containing oxycodone hydrochloride were similar to that of the reference product (OxyContin). Moreover, performance after oral administration of the HPMCAS/HPC ER matrix tablets to humans was simulated by GastroPlus based on dissolution profiles from the USP apparatus 3. The plasma concentration-time profile simulated was similar to that of the reference product. These results suggest that the combination of HPMCAS and HPC shows a robust dissolution profile against pH and paddle rotating speed and indicates the appropriate extended-release profile in humans.

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