Designing of Stable Co-crystals of Zoledronic Acid Using Suitable Coformers

Varma, Abhishek and Prasanna, Laxmi and Pai, Aravinda and Pai, Girish K and Vasantharaju, SG and Muddukrishna, BS (2019) Designing of Stable Co-crystals of Zoledronic Acid Using Suitable Coformers. Chemical and Pharmaceutical Bulletin, 67 (8). pp. 816-823. ISSN 0009-2363

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Abstract

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

Item Type: Article
Uncontrolled Keywords: Co-crystal; Solubility; Zoledronic acid; Biopharmaceutics Classification System (BCS) class III drug; Hydrogen bonding
Subjects: Pharmacy > MCOPS Manipal > Pharmaceutical Chemistry
Pharmacy > MCOPS Manipal > Pharmaceutical Quality Assurance
Pharmacy > MCOPS Manipal > Pharmaceutics
Depositing User: KMC Library
Date Deposited: 17 Aug 2019 04:23
Last Modified: 17 Aug 2019 04:23
URI: http://eprints.manipal.edu/id/eprint/154345

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