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Related Experiment Video

Updated: May 12, 2026

Formation of Dispersible Taohong Siwu Tablets

Formation of Dispersible Taohong Siwu Tablets

Published on: February 3, 2023

Coamorphous repaglinide-saccharin with enhanced dissolution.

Yuan Gao¹, Jiao Liao, Xuan Qi

¹School of Pharmacy, China Pharmaceutical University, Nanjing 210009, PR China.

International Journal of Pharmaceutics

|April 25, 2013

Summary

This study developed a coamorphous repaglinide-saccharin system to enhance the solubility and dissolution of the anti-diabetic drug repaglinide. The new formulation demonstrated improved bioavailability and a stabilized amorphous state.

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Area of Science:

Pharmaceutical Sciences
Materials Science

Background:

Coamorphous systems offer advantages over traditional solid dispersions for drug formulation.
Repaglinide (REP) is a BCS class II anti-diabetic drug with poor aqueous solubility.

Purpose of the Study:

To create and characterize a coamorphous repaglinide-saccharin (REP-SAC) system.
To evaluate the solubility, dissolution, and stability of the REP-SAC coamorphous form.

Main Methods:

Solution crystallization was used to prepare the REP-SAC coamorphous system.
High-performance liquid chromatography (HPLC) was employed for simultaneous drug quantification.
Characterization included thermal analysis, Fourier-transform infrared spectroscopy (FTIR), and X-ray diffraction (XRD).

Main Results:

A 1:1 stoichiometric coamorphous REP-SAC was successfully formed, confirmed by unique thermal behavior, FTIR shifts, and absence of sharp XRD peaks.
The coamorphous system exhibited significantly improved solubility and dissolution rates compared to crystalline repaglinide.
REP-SAC demonstrated enhanced supersaturation and prolonged drug retention in a metastable state in distilled water.

Conclusions:

Coamorphous REP-SAC formation was confirmed through physical characterization and indicated hydrogen bonding interactions.
The developed coamorphous system effectively enhances repaglinide's dissolution and stabilizes its amorphous state, potentially improving bioavailability.
This approach offers a viable strategy for formulating poorly soluble drugs with improved pharmaceutical properties.