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, 62. pp. 345-346. ISSN 1409 - 8695

[thumbnail of Mac.Pharm.Bull-Vol_62_201611.pdf]

Download (1MB) | Preview


The selection of the crystalline phases in a form of molecular cocrystals 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. Hence, determining the crystal structure and revealing the crystal packing forces and geometry of the API impact upon its physicochemical properties what it is a threshold for controlling the performance of the API. The range of crystal forms in which molecular cocrystals of APIs may exist are advantageous comparing to its polymorphs, salts, solvates and hydrates due to the vast number of potential coformers 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 cocrystallization.
This paper refer to structures analyses for “drug-drug” type of PCCs where both API and CF exhibit pharmacological effect. This approach of designing “drug-drug” type of PCC aligned to the strategy for drug repositioning, the idea for use of a drug for treating diseases other than the drug-specified. This concept was prompted in 2012 through the Discovering New Uses for Existing Molecules program, initiated by US’s National Institute of Health (NIH).

Item Type: Article
Subjects: Medical and Health Sciences > Basic medicine
Engineering and Technology > Chemical engineering
Engineering and Technology > Materials engineering
Engineering and Technology > Nano-technology
Divisions: Faculty of Medical Science
Depositing User: Aleksandar Cvetkovski
Date Deposited: 27 Jan 2017 11:13
Last Modified: 27 Jan 2017 11:13

Actions (login required)

View Item View Item