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

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.

Automated summary

This study aimed to improve the solubility and stability of stiripentol (STP), an insoluble and acid-labile drug, through the preparation of enteric solid dispersions and effervescent tablets. Results showed that the enteric amorphous STP-SDs significantly improved the solubility and stability of STP. The bioavailability of STP-SD-ETs was as high as 138.71% and the intestinal absorption rate of STP was increased. This oral preparation combining enteric solid dispersion and effervescent tablet technology provides a promising method to enhance the delivery of drugs with poor solubility and acid-labile stability.