In the present study a new co-crystal of Ticagrelor with L-Tartaric acid has been prepared with improved solubility. Ticagrelor is a class VI drug with poor solubility and permeability; hence an attempt has been made to improve its solubility by co-crystallization technology.A co-crystal is a structurally homogeneous crystalline material containing an API and the co-former in definite stoichiometric amounts. In this study the conformer selected was L-Tartaric acid based on ease of hydrogen bond formation. The co-crystal of Ticagrelor with L-Tartaric acid was prepared in different ratios (1:1, 2:1, 1:2). Ticagrelor formed stable co-crystals in the ratios 1:1and2:1. The formation of co-crystal was confirmed by FTIR, DSC and PXRD. The dynamic solubility of co-crystals in the ratios 1:1 and 2:1 was increased by approximately 2.7 and 2.6 fold respectively as compared to pure drug. The in-vitrodissolution study demonstrated a 1.5 fold increase in the solubility for selected TIC:L-TAR (1:1) as compared to its TIC active pharmaceutical ingredient and TIC physical mixture.
Co-crystal synthesis has become a field of high interest in the last decade. This category of solid forms has a variety of applications in industries such as textile, paper and electronics. For many purposes co-crystals will have superior properties in comparison to traditional salt crystals. This review article will focus on the application of co-crystals in pharmaceutical drugs. Co-crystals have opened doors to reintroduce previously poor performing bioactive ingredients in new and improved solid structures. They have also allowed for the introduction of a new range of compounds for pharmaceutical therapy. Most importantly, co-crystals can create new medicines with increased solubility and hence improve the efficiency and safety of the treatment.
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.
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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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