ATORVASTATIN ADSORPTION STUDIES ON CHITOSANS IN AN in vitro PHARMACEUTICAL MODEL
Journal Title: Progress on Chemistry and Application of Chitin and its Derivatives - Year 2018, Vol 0, Issue
Abstract
During the pharmacological therapy of specific diseases, drugs are used which, with other preparations or foods, can create connections, in many cases changing or even blocking their action. On the other hand, the use of unsuitable polymers as excipients may result in drug-polymer incompatibilities. Interactions consisting mainly of the occurrence of the adsorption phenomenon and on the formation of complex bonds that reduce the effect of the drugs are of particular importance. The aim of the study was to investigate whether the active substance atorvastatin is incompatible with dietary supplements containing chitosan. The phenomenon of the adsorption of the drug was examined using a static model of a pharmaceutical gastrointestinal tract, in the concentration range generally ingested in a single dose. Measurement results of the amount of bound drug were used to determine the average percentage of adsorbed drug dose. The results of the study prove that the anticholinesterase drug is adsorbed on chitosan in the pH ranges used, and that the binding capacity depends on the chitosan variety, which indirectly affects the reaction of the environment. It was observed that the average size of sorption depending on the chitosan variety ranged from 38% to 86%. The fact that the lowest value of adsorption was at pH 6.4 can be explained by the chemical properties of chitosan, which shows a charge only at pH >6.7. Under such conditions, the phenomenon of electrostatic adsorption may occur in relation to the healing substances of weak acids. At a pH above 7.6, corresponding to the intestinal fluid-filled intestine, the mean sorption for the highest dose of chitosan was from 38–86%. The increase in the adsorbed amount of anticholinesterase drugs on the polymer along with the increase in pH from 7.6 to 8.0 can be explained by the chitosan swelling properties, which increase with an increase in the pH. As a result, the specific surface area of the polymer and its sorption capacity increase. Based on the above considerations, it can be concluded that there is an antagonistic interaction between the drug and the polymer studied, which involves the adsorption of a drug from this group on the polymer (chitosan) and a decrease in its bioavailability.
Authors and Affiliations
Jan Meler, Bożena Grimling, Maria Szcześniak, Paweł Biernat
Keywords
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- EP ID EP537271
- DOI 10.15259/PCACD.23.14
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