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Related Experiment Video

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Surface Properties of Synthesized Nanoporous Carbon and Silica Matrices

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Published on: March 27, 2019

Revaprazan-loaded surface-modified solid dispersion: physicochemical characterization and in vivo evaluation.

Jong Hyuck Park¹, Jung Hyun Cho¹, Dong Shik Kim¹

¹a College of Pharmacy & Institute of Pharmaceutical Science and Technology, Hanyang University , Ansan , South Korea.

Pharmaceutical Development and Technology

|March 20, 2019

Summary

A novel revaprazan-loaded surface-modified solid dispersion (SMSD) significantly enhances drug solubility and oral bioavailability. This water-based formulation offers an eco-friendly pharmaceutical alternative with improved drug delivery.

Keywords:

Revaprazan drug solubility oral bioavailability surface-modified solid dispersion unchanged crystalline

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Area of Science:

Pharmaceutical Science
Drug Delivery Systems
Materials Science

Background:

Revaprazan solubility and bioavailability challenges necessitate advanced drug delivery systems.
Surface modification of solid dispersions can improve drug physicochemical properties.
Hydrophilic polymers and surfactants are key excipients for enhancing drug solubility.

Purpose of the Study:

To develop a novel revaprazan-loaded surface-modified solid dispersion (SMSD).
To enhance revaprazan's aqueous solubility and oral bioavailability.
To evaluate an environmentally friendly, water-based formulation approach.

Main Methods:

Investigated the impact of hydroxypropyl methylcellulose (HPMC) and Cremophor A25 on revaprazan solubility.
Prepared numerous SMSDs using varying carrier concentrations in distilled water.
Assessed physicochemical properties, dissolution, and pharmacokinetics in rats.

Main Results:

Identified an optimal revaprazan/HPMC/Cremophor A25 SMSD (1:0.28:1.12 ratio) with ~6000-fold solubility enhancement.
Characterized SMSD particles showing carrier attachment to crystalline revaprazan.
Achieved a 5.3-fold improvement in oral bioavailability with faster Tmax and increased AUC and Cmax.

Conclusions:

The developed SMSD system significantly improves revaprazan solubility and oral bioavailability.
The water-based, solvent-free preparation method is environmentally advantageous.
This SMSD represents a promising oral pharmaceutical alternative for revaprazan delivery.