Stiripentol Enteric Solid Dispersion-Loaded Effervescent Tablets: Enhanced Dissolution, Stability, and Absorption

Overview

Journal AAPS PharmSciTech

Publisher Springer

Specialty Pharmacology

Date 2022 May 10

PMID 35538376

Authors

Ying Wang

Siyuan Xu

Ziyue Xiao

Yuxin Jiang

Qi Jiang

Jun Li

Wei He

Affiliations

Soon will be listed here.

Abstract

Due to poor solubility and stability in acid conditions, the gastrointestinal administration of stiripentol (STP) is still a significant challenge. This study aimed to explore the applicability of effervescent tablets compressed from STP-loaded enteric solid dispersions to improve the solubility and stability of the insoluble and acid-labile drug. STP-loaded solid dispersions (STP-SDs) and the effervescent tablets (STP-SD-ETs) were prepared using solvent evaporation and dry granulation technology, respectively, and their formulations were optimized. Then, STP-SDs were characterized regarding solid state, in vitro release, stability, etc. Results showed that enteric amorphous STP-SDs were successfully prepared and significantly improved the solubility and stability of STP. Moreover, compared with STP suspensions, the bioavailability of STP-SD-ETs was as high as 138.71%. Concomitantly, STP-SD-ETs significantly increased the intestinal absorption rate of STP. Overall, the oral preparation encompassing enteric solid dispersion combined with effervescent tablet technology possesses excellent performance in enhancing dissolution, anti-acid hydrolysis stability, and absorption of STP. Our work provides a promising method to improve the delivery of drugs with poor solubility and acid-labile stability.

Citing Articles

Solubilization techniques used for poorly water-soluble drugs.

Xie B, Liu Y, Li X, Yang P, He W Acta Pharm Sin B. 2024; 14(11):4683-4716.

PMID: 39664427 PMC: 11628819. DOI: 10.1016/j.apsb.2024.08.027.

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