Abstract

This study establishes that etraverine, an anti human immuno deficiency virus drug, is produced as cocrystals to improve the solubility of the same by cocrystallisation methods and characterization of the cocrystals formed. Etraverine belongs to the class IV category as per the Biopharmaceutical Classification System which are basically classified as a drug with low solubility and low permeability. Pharmaceutical cocrystals are structurally homogeneous crystalline materials containing an API and the conformer in definite stoichiometric amounts. Etraverine formed physicochemically stable cocrystal with tartaric acid when prepared in 1:1 molar ratio by slurry method.The formation of the cocrystals was confirmed by analytical techniques such as X-ray diffraction, differencial scaning calorimetry and Fourier transform infrared spectroscopy. The dynamic solubility of etraverine in the cocrystal of ratio 1:1 was improved by approximately 3.6 fold as compared to pure etaverine. The percentage of drug release at 180 min was also four times higher for etraverine cocrystal of ratio 1:1 as compared to pure etraverine. This study demonstrates the capability of co-crystalization technique to improve the solubility of etraverine.

Original languageEnglish
Pages (from-to)972-979
Number of pages8
JournalLatin American Journal of Pharmacy
Volume36
Issue number5
Publication statusPublished - 2017

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Solubility
Pharmaceutical Preparations
Calorimetry
Fourier Transform Infrared Spectroscopy
X-Ray Diffraction
Permeability
Viruses

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science
  • Drug Discovery

Cite this

@article{368e0bf8bc9046a2a9d048871661e826,
title = "Preparation, solid state characterization of etraverine co-crystals with improved solubility",
abstract = "This study establishes that etraverine, an anti human immuno deficiency virus drug, is produced as cocrystals to improve the solubility of the same by cocrystallisation methods and characterization of the cocrystals formed. Etraverine belongs to the class IV category as per the Biopharmaceutical Classification System which are basically classified as a drug with low solubility and low permeability. Pharmaceutical cocrystals are structurally homogeneous crystalline materials containing an API and the conformer in definite stoichiometric amounts. Etraverine formed physicochemically stable cocrystal with tartaric acid when prepared in 1:1 molar ratio by slurry method.The formation of the cocrystals was confirmed by analytical techniques such as X-ray diffraction, differencial scaning calorimetry and Fourier transform infrared spectroscopy. The dynamic solubility of etraverine in the cocrystal of ratio 1:1 was improved by approximately 3.6 fold as compared to pure etaverine. The percentage of drug release at 180 min was also four times higher for etraverine cocrystal of ratio 1:1 as compared to pure etraverine. This study demonstrates the capability of co-crystalization technique to improve the solubility of etraverine.",
author = "Karthik Aithal and Aravind Pai and Girish Pai and Sathyanarayana, {Muddukrishna B.}",
year = "2017",
language = "English",
volume = "36",
pages = "972--979",
journal = "Latin American Journal of Pharmacy",
issn = "0326-2383",
publisher = "Colegio de Farmaceuticos de la Provincia de Buenos Aires",
number = "5",

}

TY - JOUR

T1 - Preparation, solid state characterization of etraverine co-crystals with improved solubility

AU - Aithal, Karthik

AU - Pai, Aravind

AU - Pai, Girish

AU - Sathyanarayana, Muddukrishna B.

PY - 2017

Y1 - 2017

N2 - This study establishes that etraverine, an anti human immuno deficiency virus drug, is produced as cocrystals to improve the solubility of the same by cocrystallisation methods and characterization of the cocrystals formed. Etraverine belongs to the class IV category as per the Biopharmaceutical Classification System which are basically classified as a drug with low solubility and low permeability. Pharmaceutical cocrystals are structurally homogeneous crystalline materials containing an API and the conformer in definite stoichiometric amounts. Etraverine formed physicochemically stable cocrystal with tartaric acid when prepared in 1:1 molar ratio by slurry method.The formation of the cocrystals was confirmed by analytical techniques such as X-ray diffraction, differencial scaning calorimetry and Fourier transform infrared spectroscopy. The dynamic solubility of etraverine in the cocrystal of ratio 1:1 was improved by approximately 3.6 fold as compared to pure etaverine. The percentage of drug release at 180 min was also four times higher for etraverine cocrystal of ratio 1:1 as compared to pure etraverine. This study demonstrates the capability of co-crystalization technique to improve the solubility of etraverine.

AB - This study establishes that etraverine, an anti human immuno deficiency virus drug, is produced as cocrystals to improve the solubility of the same by cocrystallisation methods and characterization of the cocrystals formed. Etraverine belongs to the class IV category as per the Biopharmaceutical Classification System which are basically classified as a drug with low solubility and low permeability. Pharmaceutical cocrystals are structurally homogeneous crystalline materials containing an API and the conformer in definite stoichiometric amounts. Etraverine formed physicochemically stable cocrystal with tartaric acid when prepared in 1:1 molar ratio by slurry method.The formation of the cocrystals was confirmed by analytical techniques such as X-ray diffraction, differencial scaning calorimetry and Fourier transform infrared spectroscopy. The dynamic solubility of etraverine in the cocrystal of ratio 1:1 was improved by approximately 3.6 fold as compared to pure etaverine. The percentage of drug release at 180 min was also four times higher for etraverine cocrystal of ratio 1:1 as compared to pure etraverine. This study demonstrates the capability of co-crystalization technique to improve the solubility of etraverine.

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VL - 36

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JO - Latin American Journal of Pharmacy

JF - Latin American Journal of Pharmacy

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