<p>Diclofenac is an anti-inflammatory drug with poor water solubility and ulcerogenic properties. In the present study, co-crystals of diclofenac and glycine were developed by microwave irradiation to improve solubility and minimize the ulcerogenicity of diclofenac. FTIR, DSC, and PXRD studies confirmed the formation of a new crystalline phase. The developed co-crystals showed increased solubility and intestinal permeability. The co-crystals were significantly (<i>P</i> &lt; 0.05) effective against inflammation in the rat model compared with diclofenac. Also, the <i>in vivo</i> studies on rats revealed that the developed co-crystals were non-ulcerogenic. These findings suggest that the diclofenac and glycine co-crystal might have increased the efficacy of diclofenac and decreased its gastro-toxicity.</p>

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Co-Crystallization with Glycine Enhances the Solubility and Permeability of Diclofenac While Reducing Ulcerogenicity and Increasing Efficacy against Acute Inflammation

  • A. Sahoo,
  • V. R. Regu,
  • S. Routray,
  • D. Mishra,
  • D. Behera,
  • R. P. Swain,
  • B. B. Subudhi

摘要

Diclofenac is an anti-inflammatory drug with poor water solubility and ulcerogenic properties. In the present study, co-crystals of diclofenac and glycine were developed by microwave irradiation to improve solubility and minimize the ulcerogenicity of diclofenac. FTIR, DSC, and PXRD studies confirmed the formation of a new crystalline phase. The developed co-crystals showed increased solubility and intestinal permeability. The co-crystals were significantly (P < 0.05) effective against inflammation in the rat model compared with diclofenac. Also, the in vivo studies on rats revealed that the developed co-crystals were non-ulcerogenic. These findings suggest that the diclofenac and glycine co-crystal might have increased the efficacy of diclofenac and decreased its gastro-toxicity.