MANUFACTURE OF SPHERICAL GRANULES OF ISOSORBIDE DINITRATE WITH MODIFIED RELEASE

Yıl 2020, Cilt: 44 Sayı: 3, 481 - 493, 30.09.2020

Dmytro Olıınykov Andrii Kaplaushenko Svetlana Trehub Katerina Kovalyova

https://doi.org/10.33483/jfpau.736331

Cited By: 2

Öz

Objective: This study was aimed to obtain spherical matrix pellets of isosorbide dinitrate with different dissolution kinetics to create a multidosage medicinal form with controlled release of the active substance.

Material and Method: Spherical matrix granules were obtained by extrusion-spherinization and coated with different amounts of polymer shell. Dissolution profiles of the obtained spheroids were compared with reference drug tablets.

Result and Discussion: The results showed that the combination of spherical granules provides an isosorbide dinitrate release profile similar to the dissolution of Cardicet Retard tablets. The target dissolution profile is achieved using a combination of uncoated spherical granules and spheroids with a 10% film coating. The similarity coefficient (f2) is 73.6.

Anahtar Kelimeler

Isosorbide dinitrate, release profile, spherical matrix pellets

Destekleyen Kurum

RPF "MICROKHIM", Ukraine

MODİFİYE SALIMLI İSOSORBİT DİNİTRAT KÜRESEL GRANÜLLERİNİN ÜRETİMİ

Öz

Amaç: Bu çalışma, etkin maddenin kontrollü salımını yapan çok dozlu bir tıbbi form oluşturmak için farklı çözünme kinetiklerine sahip izosorbit dinitratın küresel matris pelletlerini elde etmeyi amaçlamıştır.

Gereç ve Yöntem: Küresel matris granüller ekstrüder-sferonizer yöntemi ile elde edilmiş ve farklı miktarlarda polimer kabuk ile kaplanmıştır. Elde edilen kürelerin çözünme profilleri, referans ilaç tabletleri ile karşılaştırılmıştır.

Sonuç ve Tartışma: Sonuçlar, küresel granüllerin kombinasyonunun, Cardicet Retard tabletlerinin çözünmesine benzer bir izosorbit dinitrat salım profili sağladığını göstermiştir. Hedef çözünme profili, kaplanmamış küresel granüller ve % 10'luk film kaplı kürelerin bir kombinasyonu kullanılarak elde edilmiştir. Benzerlik katsayısı (f2) 73.6'dır.

Anahtar Kelimeler

İsosorbit dinitrat, salım profili, küresel matriks pelletler

Kaynakça

• 1. Kovalenko, V.M., Lutaj, M.I., Bratus’, V.V. et. al.; Kovalenkao, V.M. (Ed.) (2008). Rukovodstvo po kardiologii’ [Guide for cardiology]. Kyiv: МОRІОN, 1424. http://snsk.az/snsk/file/2013-06-20_09-52-44.pdf
• 2. Soman, B., Vijayaraghavan, G. (2017). The role of organic nitrates in the optimal medical management of angina. European Society of Cardiology 15 (2)
• 3. Kumar, S., Jeet, K., Baldi, A. (2015). Recent technological advancements in multiparticulate formulations: The smart drug delivery systems. Asian Journal of Pharmaceutic 9 (4): 13-25. https://www.researchgate.net/publication/28891779
• 4. Roy, P., Shahiwala, A. (2009). Multiparticulate formulation approach to pulsatile drug delivery: current perspectives. J Control Release 134: 74–80. https://doi.org/10.1016/j.jconrel.2008.11.011
• 5. Shah, S., Shah, B.P., Patel,M., Patel, M.R. (2015) A review on extended release drug delivery system and multiparticulate system. World Journal of Pharmaceutical Research 4 (8):724-747. https://www.researchgate.net/publication/281098252
• 6. Jadhav, N., Irny, P., Mokashi, A., Souche, P., Paradkar, A. (2012). Pelletization by Extrusion Spheronization Technique: An Excipient Review. Drug Delivery Letters. 2. 132-145. https://www.researchgate.net/publication/284590372
• 7. Sagar, M., Tanaji, N., Sushilkumar, P. (2016). Extrusion–spheronization a promising pelletization technique: In-depth review. Asian Journal of Pharmaceutical Sciences II: 684–699. http://dx.doi.org/10.1016/j.ajps.2016.08.001
• 8. Oliinykov, D.S., Kaplaushenko, A.G. (2019a). Substantiation of manufacture technology development for the tablets of isosorbide dinitrate with modified release. Current issues in pharmacy and medicine: science and practice 12 (2): 160–165. https://doi.org/10.14739/2409-2932.2019.2.170982
• 9. European Directorate for the Quality of Medicines et al. & HealthCare: European Pharmacopoeia 9.0.[Internet]. 2019.
• 10. Oliinykov, D.S., Kaplaushenko, A.G. (2019b). Development and validation of the HPLC-procedure for the quantitative determination of isosorbide dinitrate in matrix granules. Journal of Organic and Pharmaceutical Chemistry 17 (3): 51-58. https://doi.org/10.24959/ophcj.19.174771
• 11. CPMP/QWP/EWP/1401/98 Rev.1/Corr** «Guideline on the Investigation of Bioequivalence»
• 12. Access mode: https://healthcare.evonik.com/sites/lists/NC/DocumentsHC/Evonik-Eudragit_brochure.pdf
• 13. Bhaskaran, S., Lakshmi, P.K. (2010). Extrusion Spheronization –A Review. Int.J. PharmTech Res 2(4): 2429-2433.