The role of cocrystallization screening for the assessment of structure-activity relationship in drug development

Cvetkovski, Aleksandar and Angelovska, Bistra (2016) The role of cocrystallization screening for the assessment of structure-activity relationship in drug development. Macedonian pharmaceutical bulletin. pp. 345-346. ISSN 1409 - 8695

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Abstract

The selection of the crystalline phases in a form of molecular co-crystals has become scientific challenge at the early stage of drug development of pharmaceutical formulations and in the late stage of synthesis and isolation of active pharmaceutical ingredients (APIs) in desirable defined crystalline forms. Optimal crystal form of API interactively interrelates and impacts its aqueous solubility and dissolution rate that are benchmark for drug delivery and absorption determining the extent of its bioavailability and pharmacokinetics profile. Determining the crystal structure and revealing the crystal packing forces and geometry of the API has impact its physicochemical properties. This approach is the criteria for assessment of the performance of the API. The range of crystal forms in which molecular co-crystals of APIs may exist is advantageous comparing to their polymorphs, salts, solvates and hydrates due to the vast number of potential co-formers which extend the limited counterions for salt formation implying the existence of more complex intermolecular interactions based on different H-bonding patterns with API that lead to conformational changes and flexibility for crystal packing in process of co-crystallization.

Item Type: Article
Subjects: Medical and Health Sciences > Other medical sciences
Divisions: Faculty of Medical Science
Depositing User: Bistra Angelovska
Date Deposited: 21 Dec 2016 10:59
Last Modified: 21 Dec 2016 10:59
URI: http://eprints.ugd.edu.mk/id/eprint/16864

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