Preparation and solid state characterisation of co-crystals of etravirine engineered by fabricating with flavonoids as possible conformers

Mohammed E. Azzouz, Yuan Chen, Hasnaa M. Hassan, Shivangi Agarwal, Aravind Pai, Muddukrishna B. Sathyanarayana

Research output: Contribution to journalArticle

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-crystals 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 co-crystal 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.

Original languageEnglish
Pages (from-to)1784-1790
Number of pages7
JournalLatin American Journal of Pharmacy
Volume37
Issue number9
Publication statusPublished - 01-01-2018

Fingerprint

etravirine
Flavonoids
Solubility
piperine
Pharmaceutical Preparations
Rutin
Fourier Transform Infrared Spectroscopy
X-Ray Diffraction
Permeability
Viruses

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science
  • Drug Discovery

Cite this

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title = "Preparation and solid state characterisation of co-crystals of etravirine engineered by fabricating with flavonoids as possible conformers",
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-crystals 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 co-crystal 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.",
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Preparation and solid state characterisation of co-crystals of etravirine engineered by fabricating with flavonoids as possible conformers. / Azzouz, Mohammed E.; Chen, Yuan; Hassan, Hasnaa M.; Agarwal, Shivangi; Pai, Aravind; Sathyanarayana, Muddukrishna B.

In: Latin American Journal of Pharmacy, Vol. 37, No. 9, 01.01.2018, p. 1784-1790.

Research output: Contribution to journalArticle

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AU - Azzouz, Mohammed E.

AU - Chen, Yuan

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AU - Agarwal, Shivangi

AU - Pai, Aravind

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