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: | https://eprints.ugd.edu.mk/id/eprint/16864 |
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