« Back
Improvement of dissolution properties of valsartan by co-crystallization with
Poster Title: Improvement of dissolution properties of valsartan by co-crystallization with
Submitted on 02 Jul 2015
Author(s): Liping Du, Alexander V. Dushkin and Weike Su
Affiliations: Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang
This poster was presented at Organizing committee of MedChem 2015
Poster Views: 1,597
View poster »

Poster Information
Abstract: Valsartan is a BCS class II angiotensin-II receptor antagonist. Its clinical application is limited by the poor solubility and low bioavailability.1 Pharmaceutical co-crystal is great potential value with modifying the unfavourable physicochemical properties, without changing the molecular structures of drugs.2 Thus in this study, a new pharmaceutical co-crystal of valsartan was synthesized with co-crystal former, vitamin C, to improve its water solubility by mechanochemical method. A high intensity oscillating mill was applied for producing valsartan-vitamin C co-crystal. Multi-instrumental characterizations confirmed the formation of the new co-crystal prepared by high mechanical process, as following: nuclear magnetic resonance, the optical activity test, Fourier transform infrared spectroscopy, differential scanning calorimetry and powder X-ray diffractometry. Meanwhile, the ratio of co-crystal components, which determined by quantitative nuclear magnetic resonance, was found to be 1:1 (valsartan to vitamin C). Eventually, dissolution test were carried in enzyme-free simulated fluid (pH 6.8). It showed that co-crystal of valsartan and vitamin C significantly increased the dissolution rate (nearly 18 times than free valsartan). It was concluded that valsartan-vitamin C co-crystal was successfully synthesized by mechanochemical method and behaved better in modifying physicochemical properties and pharmaceutical properties.Summary: Improve the solubility and dissolution properties of valsartan by co-crystallization with vitamin C via mechanochemical method References: 1. G. Flesch, M. P. Lloyd, Absolute bioavailability and pharmacokinetics of valsartan, an angiotensin II receptor antagonist in man, Eur. J. Clin. Pharmacol. 1997, 52, 115-120.
2 P. Mura, M. Cirri, M. T. Faucci, J. M. Gines-Dorado, G. P. Bettinetti, Investigation of effects of grinding and co-grinding on physicochemical properties of glisentide, J. Pharmaceut. Biomed. 2002, 30, 227-237.
Report abuse »
Ask the author a question about this poster.
Ask a Question »

Creative Commons

Related Posters

dragonfly® crystal: an ideal solution to problematic liquids in screening environments
Joby Jenkins, Gillian Lewis

strategies for high-throughput ligand screening -automated co-crystallisation and soaking
Paul Thaw1, David Hargreaves2, JörgBenz3, Joby Jenkins1

efficient crystallisation of a tuberculosis drug target using a dragonfly® crystal screen optimiser.
Joby Jenkins1, Gary Cochrane1, David Smith1, Michal Blaszczyk2

Optimized Expression of Membrane Proteins in the Expi293 and ExpiCHO Expression Systems: New Tools for Difficult to Express Proteins
Chao Yan Liu1, Jian Liu1, Wanhua Yan1, Sam Stepnowski1 ,Kyle Williston1, Katy Irvin1, Chetana Revankar2, Natasha Lucki2, Henry Chiou2, Jonathan Zmuda1. Thermo Fisher Scientific, 1Frederick, MD, U.S.A, 2Carlsbad, CA, U.S.A

In vitro selection & validation of synthetic single-domain antibodies & applications
Stéphanie Blachon1, Sandrine Moutel2, Selma Djander1&2, Vincent Collura1, Alexis Arrial1, Aurélien Olichon4, Franck Perez3, Jean-Christophe Rain1