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Development of non-covalent derivative of sulfasalazine with  theobromine for its properties optimization

Volume No : (2017) Volume: 05 Issue : 27 Year : 2017 Page No: 154-158

Authors : Madhu Bala, Manoj K. Gautam, Renu Chadha

Abstract :

To customize the biopharmaceutical parameters of a poorly soluble, disease modifying anti-rheumatic drug, sulfasalazine (SSZ) by preparing its novel non-covalent derivative (NCD). For this theobromine (TBR) was used as coformer. The novel solid form prepared by liquid assisted grinding of SSZ with TBR using catalytic amount of solvent and termed as SSZ-TBR. The ground product (SSZ-TBR) was characterized with various techniques such as differential scanning calorimetry, powder X-ray diffraction (PXRD), and spectrometric methods involving Fourier transform infrared and solid state nuclear magnetic resonance. The structure of the SSZ-TBR was determined from its PXRD pattern using Material Studio® by BIOVIA. The crystal structure also helped to understand the nature of complex and type of interactions involved in its formation and stabilization. The SSZ-TBR was further evaluated for in vitro solubility and intrinsic dissolution rate (IDR) profile. This NCD was characterized to be cocrystal of SSZ with TBR in 1:1 stoichiometry. Its crystal packing as well as nature of interactions was established by crystal structure determination. Further, the fulfillment of objective was witnessed byE increased solubility as well as IDR in comparison to the pure SSZ. The evaluation of this novel cocrystal of SSZ a poorly soluble drug with TBR exhibit potential to enhance the option of material phase in comparison to pure active pharmaceutical ingredient without disturbing its chemical structure.

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