Preparation and Solid State Characterisation of Co-Crystals of Etravirine Engineered by Fabricating with Flavonoids as Possible Conformers

Azzouz, Mohammed E and Chen, Yuan and Hassan, Hasnaa M and Agarwal, Shivangi and Pai, Aravind and Muddukrishna, BS (2018) Preparation and Solid State Characterisation of Co-Crystals of Etravirine Engineered by Fabricating with Flavonoids as Possible Conformers. Latin American Journal of Pharmacy, 37 (9). pp. 1784-1790. ISSN 0326 2383

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Abstract

The following study was done to establish that etravirine, which is an anti-human immuno deficiency virus drug, when produced as co-crystals helps in improving its solubility. The produced cocrystals were also characterized. According to the Biopharmaceutical Classification System, etravirine is categorised in class IV category; that is; a drug having low permeability and solubility. Structurally, pharmaceutical co-crystals are homogeneous crystalline materials involving an active pharmaceutical ingredient and the conformer in precise stoichiometric amounts. Physicochemically stable co-rystals of etravirine were formed with rutin and piperine when prepared in 1:1 and 1:2 molar ratio by solvent evaporation method. Analytical techniques like X-ray diffraction, DSC and Fourier transform infrared spectroscopy were utilised to confirm the co-crystal formation. The dynamic solubility of etravirine in the cocrystal of ratio 1:1 and 1:2 was improved by approximately 2-3 fold as compared to pure etravirine This study helps in demonstrating the capability of co-crystalization method to enhance the solubility of etravirine.

Item Type: Article
Uncontrolled Keywords: Co-crystal; Etravirine; Piperine; Rutin; Solubility
Subjects: Pharmacy > MCOPS Manipal > Pharmaceutical Chemistry
Pharmacy > MCOPS Manipal > Pharmaceutical Quality Assurance
Depositing User: KMC Library
Date Deposited: 25 Sep 2018 10:09
Last Modified: 25 Sep 2018 10:09
URI: http://eprints.manipal.edu/id/eprint/152018

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