Effect of insoluble matrixformers on trimetazidine dihydrochloride in vitro release from matrix tablets

  • V. V. Mohylyuk Shupyk National Medical Academy of Post-graduate Education, Kyiv
  • L. L. Davtian Shupyk National Medical Academy of Post-graduate Education, Kyiv
Keywords: matrix former, matrix tablets, drug release, Eudragit RSPO, Kollidon SR, Precirol ATO 5, Ethocel 10

Abstract

Oral matrix tablet is a modern dosage form using which could be achieved desirable in vitro dissolution profile of API and correspondent in vivo API concentration level. Therefore, the study of factors that affect in vitro dissolution profile of API is the actual task.

The aim of this work was study of insoluble matrix formers with different molecular structure and physicochemical properties effect on in vitro dissolution profile of API.

The object of this study were the matrix tablets with Eudragit RSPO, Kollidon SR, Precirol ATO 5, Ethocel 10 matrix formers and trimetazidine dihydrochloride (TMZ•2HCl) as model substance.

Laser light scattering method‎ for particles size measurement and direct compression method for tablets preparation, Dissolution method for determination of TMZ•2HCl in vitro release kinetic, tablets drying to constant weight at 105 °С and gravimetric weighting for lost of dry determination, diameter and height measurement using caliper for tablet’s volume determination, there used. Polyvinyl acetate films were prepared for Kollidon SR matrix former behavior investigation: the film from Kollicoat SR 30D was prepared using film casting method and followed by drying at 70 °С, the film from Kollidon SR only was prepared using hydraulic hand press.

The study showed that the ability of matrix formers to slow down of TMZ•2HCl release from matrix tablets in pH 1 and pH 6.8 medium is arranged in the same sequence: Ethocel 10 > Precirol ATO 5 > Kollidon SR > Eudragit RSPO. Was established that the matrix tablets with Kollidon SR and Eudragit RSPO are swell considerably in comparison with Ethocel 10 and Precirol ATO 5 which is consistent with their chemical structure. The specific moisture content decreasing of matrix tablets during the "dissolution" test in accordance with their matrix formers is arranged in the follow sequence: Kollidon SR > Eudragit RSPO > Precirol ATO 5 > Ethocel St. 10 FP. In contrast to Kollicoat SR film swelling was found that Kollidon SR matrix system swelling occurs due to the Kollidon SR particles elastic recovery of spherical shape and size increasing during polyvinyl acetate hydration.

References

1. Aulton M.E. Pharmaceutics: the science of dosage form design. 2 nd Ed. - Edinburgh, UK: Churchill & Livingston, 2002. - P. 297-302.

2. Li X., Jasti B. R., Design of Controlled Release Drug Delivery Systems. - New York, USA: Mc-Graw-Hill, 2006. - P. 115-120.

3. Bawa R., Siegel R. A., Marasca B. et. al. An explanation for controlled release of macromolecules from polymers // J. Controlled Release. - 1985. - Vol. 1 - P. 259-267.

4. Frenning G. Modeling drug release from inert matrix systems: From moving-bound to continuous-field descriptions // Int. J. Pharmaceutics. - 2011. - V. 418. - P. 88-99.

5. Bühler V. Kollidon - Plyvinylpyrrolidone excipients for the pharmaceutical industry. 9th ed. - Ludwigshafen: BASF SE Pharma Ingredients and Services, 2008. - R. 17-134.

6. Bühler V. Kollicoat grades - Functional polymers for the pharmaceutical industry - Ludwigshafen: BASF SE Pharma Ingredients and Services, 2007. - P. 101-110.

7. Pasynsky AG Hydration / The Great Medical Encyclopedia: In 30 volumes, ed. 3 [AMS of the USSR] / Ch. Ed. B.V. Petrovsky. - M .: Sov. Encyclopedia, 1977. - T. 5. - XVI. - P. 365-366.

8. Hamdani J., Moes A. J., Amighi K. Physical and thermal characterization of Precirol & Compritol as lipophilic glycerides used for the preparation of controlled release matrix pellets // Int J. Pharm. - 2003. - V. 260. - P. 47-57.

Ethocel - Ethylcellulose Polymers Technical Handbook - USA: Dow Cellulosics, 2005. - P. 1-27.

10. Rowe R. C., Sheskey P. J., Quinn M. E. Handbook of Pharmaceutical Excipients. 6th ed. - London, Chicago: Pharmaceutical Press, 2009. - P. 525-533.
Published
2018-09-04
How to Cite
Mohylyuk, V. V., & Davtian, L. L. (2018). Effect of insoluble matrixformers on trimetazidine dihydrochloride in vitro release from matrix tablets. Farmatsevtychnyi Zhurnal, (3), 26-33. Retrieved from https://pharmj.org.ua/index.php/journal/article/view/213
Section
Pharmaceutical technology