Objectives: This current research work aimed for improvement of the solubility and permeability of poorly permeable Doxorubicin HCl through generating co-crystals. The main goal for the preparation of oral drugs is to decrease the overall cost of healthcare and route of administration is made easy. Methodology: In this study co-crystals of Doxorubicin HCl with Quercetin hydrate and Naringin has been prepared based on ease of hydrogen bond formation. The co-crystal batches of Doxorubicin HCl-Quercetin hydrate in ratio 1:1, 1:2, 2:1 and Doxorubicin HCl-Naringin in ratio 1:1 are prepared by slow solvent evaporation technique. Results and Discussion: The formation of co-crystal was confirmed by PXRD, DSC and FTIR. Doxorubicin HCl with Naringen crystal batch show improved solubility. The dynamic solubility of Doxorubicin HCl-Naringin co-crystal in the ratios 1:1 increased by approximately 9.2-fold as compared to pure drug and Doxorubicin HCl-Quercetin hydrate cocrystal batches.
In this present study a new co-crystals of zoledronic acid with DL-tartaric acid and nicotinamide has been developed with improved solubility. Zoledronic acid is a class III drug with poor oral bioavailability due to its poor permeability and low aqueous solubility; hence an attempt has been made to improve its solubility by co-crystallization technology. Pharmaceutical cocrystals are multi-component crystals with a stoichiometric ratio of active pharmaceutical ingredients (APIs) and cocrystal coformers (CCFs) that are assembled by noncovalent interactions such as hydrogen bonds, π-π packing, and Vander Waals forces. In this study the coformers selected were DL-tartaric acid and nicotinamide based on ease of hydrogen bond formation. The co-crystal of zoledronic acid with DL-tartaric acid were prepared in three ratios (1 : 1, 1 : 2 and 2 : 1) by slow solvent evaporation method and with nicotinamide in 1 : 1 ratio by dry grinding method. The formation of co-crystal was confirmed by powder X-ray diffractometry (PXRD), differential scanning calorimetry (DSC) and Fourier transform (FT)IR. The dynamic solubility of co-crystals with DL-tartaric acid in the ratios 1 : 1, 1 : 2 and 2 : 1 increased by fold as compared to pure drug.
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