Designing of Stable Co-crystals of Zoledronic Acid Using Suitable Coformers.
Chem Pharm Bull (Tokyo)
; 67(8): 816-823, 2019.
Article
in En
| MEDLINE
| ID: mdl-31366831
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.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Tartrates
/
Drug Design
/
Niacinamide
/
Zoledronic Acid
Language:
En
Journal:
Chem Pharm Bull (Tokyo)
Year:
2019
Document type:
Article