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Stiripentol Enteric Solid Dispersion-Loaded Effervescent Tablets: Enhanced Dissolution, Stability, and Absorption
Ying Wang1, Siyuan Xu1, Ziyue Xiao1
1Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, Nanjing, 211198, China.
AAPS Pharmscitech
|May 10, 2022
Summary
This study developed effervescent tablets with stiripentol (STP) solid dispersions to overcome poor solubility and acid stability issues. The new formulation significantly enhanced STP bioavailability and absorption, offering a promising oral drug delivery method.
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
- Materials Science
Background:
- Stiripentol (STP) exhibits poor solubility and stability in acidic conditions, hindering effective gastrointestinal administration.
- Developing stable and soluble oral formulations for acid-labile drugs like STP remains a significant pharmaceutical challenge.
Purpose of the Study:
- To investigate the use of effervescent tablets containing stiripentol-loaded enteric solid dispersions.
- To enhance the solubility, stability, and bioavailability of stiripentol for oral delivery.
Main Methods:
- Preparation of stiripentol-loaded solid dispersions (STP-SDs) via solvent evaporation.
- Formulation and optimization of effervescent tablets (STP-SD-ETs) using dry granulation technology.
- Characterization of STP-SDs for solid-state properties, in vitro release, and stability.
Main Results:
- Enterically coated amorphous STP-SDs were successfully prepared, significantly improving STP solubility and stability.
- STP-SD-ETs demonstrated a 138.71% bioavailability compared to STP suspensions.
- The effervescent tablets notably increased the intestinal absorption rate of stiripentol.
Conclusions:
- The combination of enteric solid dispersion and effervescent tablet technology offers an effective strategy for improving stiripentol's dissolution, stability, and absorption.
- This approach presents a promising method for enhancing the oral delivery of drugs with poor solubility and acid-labile characteristics.
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