More than 60% drugs coming from synthesis and 40% drugs in the development are poorly soluble and create problem of poor water solubility in the pharmaceutical industry. So various techniques are tried to overcome this problem like solid dispersion, Co-Solvent, Co-amorphous Co-crystallization. Most promising one is Co-crystallization. In the present work Efavirenz co-crystallize with suitable Co-former such as Saccharine and Caffeine by solvent evaporation technique in 1:1 ratio. The prepared Co Crystal was characterized by DSC, IR, XRPD & other pharmaceutical properties like melting point, Solubility etc. Prepared Efavirenz Co-crystals exhibited excellent physicochemical properties when compared with pure drug. In FTIR analysis, there were no new peaks observed, indicating that no chemical reaction occurred during cocrystal preparation. DSC, SEM study confirms that the third product which was form after co-crystallization, they are co-crystal with change in Shape, Size, habit, Melting point. The X-Ray Powder Diffraction pattern shows peak reduced and confirm that the third product Co-crystal was formed. XRD shows that different peaks height in drug & more sharp peaks at 22.96,27.From solubility studies it was found that the co-crystal of Efavirenz with Saccharine in 1:1 stoichiometric ratio enhances the solubility up to 17 fold. So the Immediate release plain tablet of Efavirenz and its Saccharine co-crystal was prepared & evaluated for various post compression parameters such as thickness, hardness, friability, weight variation, drug content, disintegration. Faster disintegration and greater dissolution rate release 90.26% was observed with Cocrsytal compare to plain tablet of Efavirenz. Finally we concluded that Solubility enhancement & formulation development of Efavirenz successfully completed.
Keyword: Solubility, Cocrystal, Efavirenz, Saccharin, Caffine, Solvant Evaporation, Tablet
Publication date: 01/08/2020
https://ijbpas.com/pdf/2020/August/MS_IJBPAS_2020_5168.pdf
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https://doi.org/10.31032/IJBPAS/2020/9.8.5168
