EVALUATION OF PHYSICOCHEMICAL PROPERTIES OF SOLID DISPERSIONS OF BCS CLASS II SUBSTANCES WITH CHITOSAN

• Authors: Bożena Grimling , Agata Górniak , Jan Meler , Janusz Pluta
• Languages of publication: EN

Abstracts

EN

The BCS class II includes drugs with low solubility and high permeability. The substances require modification to increase their solubility in the upper part of the digestive system. Fenofibrate is an example of this class drugs. The aim of the study was to investigate the effect of chitosan on the solubility of fenofibrate incorporated into this polymer carrier. The study investigated fenofibrate in solid dispersions using a method of the solvent evaporation by means of freeze-drying at the drug to polymer ratio of 3:7,5:5,7:3. The study revealed a multi-fold increase (from 33 to 57 times) in fenofibrat solubility in the presence of chitosan, which increased with duration of the study and with increasing percentage of the polymer in formulations. DSC examination revealed a possible physical interaction between the drug and the polymer. The degree of lowering of temperature and increased heat effects is correlated with increased solubility of the drug in all the formulations. DSC studies confirmed that fenofibrate is present in solid dispersions in a crystalline form.

Keywords

EN

DSC studies; chitosan; dissolution; fenofibrate; solid state lyophilisation

• Publisher: Sieć Badawcza Łukasiewicz - Polskie Towarzystwo Chitynowe
• Journal: Progress on Chemistry and Application of Chitin and its Derivatives
• Year: 2012
• Volume: 17
• Pages: 87 - 94

Contributors

author

Bożena Grimling

• Faculty of Pharmacy The “Silesian Piast” memorial Medical University of Wroclaw

author

Agata Górniak

• Department Inorganic Chemistry, Medical University of Wrocław

author

Jan Meler

• Faculty of Pharmacy The “Silesian Piast” memorial Medical University of Wroclaw

author

Janusz Pluta

• Faculty of Pharmacy The “Silesian Piast” memorial Medical University of Wroclaw

References

• Amidon G.L., Lennernäs H., Shah V.P., Crison J.R..;(1995) A Theoretical Basis for a Biopharmaceutic Drug Classification: The Correlation of in Vitro Drug Product Dissolution and in Vivo Bioavailability. Pharm. Res. 12, pp. 413-420.
• Yasir M., Asif M., Kumar A., Aggarval A.;(2010) Biopharmaceutical Classification System: An Account; Int. J. of Pharm. Tech. Res. 2, pp. 1681-1690.
• Woskowicz M.;(2008) Biofarmaceutyczny system klasyfikacji (BCS) jako nowoczesna metoda oceny właściwości fizykochemicznych i farmakokinetycznych środków leczniczych. Farmacja Polska 64, pp. 191-195.
• Vogt M., Kunath K., Dressman J.B.;(2008) Dissolution enhancement of fenofibrate by micronization, cogrinding and spray-drying: Comparison with commercial preparations; Eur. J. of Pharm. and Biopharm. 68, pp.283–288.
• Guyot M., Fawaz F., Bildet J., Bonini F., Lagueny A.M.;(1995) Physicochemical characterization and dissolution of norfloxacin/cyclodextrin inclusion compounds and PEG solid dispersions. Int. J. Pharm.123,pp.53-63.
• Patel A.R., Vavia P.R.;(2006) Effect of hydrophilic polymer on solubilization of fenofibrate by cyclodextrin complexation; J. of Inc. Phen.And Macr.Chem. 56, pp. 247-251.
• Saharan V.A., Kukkar V., Kataria M., Gera M., Choudhury P.K.;(2009) Dissolution Enhancement of Drugs. Part I: Technologies and Effect of Carriers.; Int. J. Health Res.2, pp.107-124.
• Farmakopea Polska VIII, Warszawa: URPL i WB 2008, tom I, str. 1434-1435.
• Vippagunta S.R.;(2006) Factors affecting the formation of eutectic solid dispersions and their dissolution behavior;)J. Pharm. Sci, 96,pp. 294-304.

• Document Type: article