SOLID DOSAGE FORM DEVELOPMENT OF GLIBENCLAMIDE WITH INCREASING THE SOLUBILITY AND DISSOLUTION RATE USING COCRYSTALLIZATION


Arif Budiman, Sandra Megantara, Putri Raraswati, Tazyinul Qoriah

Abstract


Objective: The aim of this study was to develop a solid dosage form of glibenclamide with increasing the solubility properties of glibenclamide with cocrystallization method.

Methods: Virtual screening was performed to investigate the interaction between glibenclamide and a co-former. Saccharin, the selected co-former, then co-crystallized with glibenclamide with equimolar ratios of 1:1 and 1:2 using the solvent evaporation method. Further characterization was performed using an infra-red (IR) spectrophotometer, differential scanning calorimetry (DSC), and powder x-ray diffraction (PXRD).

Results: Co-crystals of 1:2 equimolar ratio were more highly soluble compared to pure glibenclamide (30-fold for 12 h and 24-fold for 24 h). The dissolution rate had also increased from 46.838% of pure glibenclamide to 77.655% of glibenclamide co-crystal in 60 min. There was no chemical reaction observed during the co-crystallization process based on the IR spectrum. However, there was a new peak in the X-Ray diffractogram and a reduction of melting point in the DSC curve, indicating the formation of co-crystals.

Conclusion: The optimal co-crystal ratio of glibenclamide-saccharin was found to be 1:2, which was successful in improving the solubility of glibenclamide.


Keywords


Glibenclamide, Co-crystal, Saccharin, Dissolution

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About this article

Title

SOLID DOSAGE FORM DEVELOPMENT OF GLIBENCLAMIDE WITH INCREASING THE SOLUBILITY AND DISSOLUTION RATE USING COCRYSTALLIZATION

Keywords

Glibenclamide, Co-crystal, Saccharin, Dissolution

DOI

10.22159/ijap.2018v10i6.29257

Date

12-09-2018

Additional Links

Manuscript Submission

Journal

International Journal of Applied Pharmaceutics
Articles In Press [Scheduled in Nov-Dec 2018] Page: 181-186

Online ISSN

0975-7058

Authors & Affiliations

Arif Budiman
Department of Pharmaceutic and Technology of Pharmacy, Faculty of Pharmacy, Universitas Padjadjaran
Indonesia

Sandra Megantara
bDepartment of Pharmaceutical Analysis and Medicinal Chemistry, Faculty of Pharmacy, Universitas Padjadjaran

Putri Raraswati
Department of Pharmaceutic and Technology of Pharmacy, Faculty of Pharmacy, Universitas Padjadjaran
Indonesia

Tazyinul Qoriah
Department of Pharmaceutic and Technology of Pharmacy, Faculty of Pharmacy, Universitas Padjadjaran


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