Cvetkovski, Aleksandar and Gjorgieva Ackova, Darinka and Smilkov, Katarina (2018) Preliminary study on screening the intermolecular interactions of organic cation drugs from BSC Class III (case study Metformin). In: CA16205, F2F meeting, UNGAP WGs, 8-9 March 2018, Leuven, Belgium.
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Abstract
Among the orally administered drugs, about 40% share the properties of organic cations (protonated bases) or neutral bases at physiological pH, which indicates one important point for studying their transport mechanisms [1]. Antineoplastic platinum compounds [2,3], the histamine H2 receptor antagonist cimetidine [4], the antiviral drugs (acyclovir, gancyclovir, lamivudine and zalcitabine) [5-7], the antidiabetic drug metformin [8,9], and the antiarrhythmic drug quinidine [10], are the identified to be transported by the organic cation transporters OCT1, OCT2 and OCT3 (membrane transporters) [2]. The case study of drug model (DM) metformin (MET), that according to Biopharmaceutical Classification System (BCS) belongs to the class III drugs (high solubility, low permeability) [11], emphasizes the importance of non-covalent interactions of this dication drug with range of ligands selected from the GRAS (Generally Recognized as Safe by FDA for food additives list) [12].Comparable study on predicting ligands for OTC1 by docking, applying High-Throughput Screening (HTS) and in silico modeling [15], offer an opportunity for growing the molecular crystals of MET with drugs, that are uses in combo- therapy with MET, as well with excipients and food ingredients, thus by generating the crystallographic, thermodynamic and spectroscopy data MET-ligand interactions, contributes the development of delivery systems with enhanced permeability of BSC class III drug models.
| Item Type: | Conference or Workshop Item (Poster) |
|---|---|
| Subjects: | Medical and Health Sciences > Other medical sciences Natural sciences > Other natural sciences |
| Divisions: | Faculty of Medical Science |
| Depositing User: | Darinka Gorgieva Ackova |
| Date Deposited: | 16 Oct 2018 10:01 |
| Last Modified: | 16 Oct 2018 10:01 |
| URI: | https://eprints.ugd.edu.mk/id/eprint/20566 |
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