Advances in Clinical and Experimental Medicine

Adv Clin Exp Med
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Advances in Clinical and Experimental Medicine

2011, vol. 20, nr 3, May-June, p. 343–349

Publication type: original article

Language: English

Design and Evaluation of Modified Release Bilayer Tablets of Flurbiprofen

Projekt i ocena dwuwarstwowych tabletek flurbiprofenu o zmodyfikowanym uwalnianiu

Ali Sharif1,, Mahboob E-Rabbani2,, Muhammad Furqan Akhtar1,, Bushra Akhtar2,, Ammara Saleem2,, Kalsoom Farzana2,, Atif Usman2,, Ghulam Murtaza3,

1 Department of Pharmacy, the University of Lahore, Lahore, Pakistan

2 Faculty of Pharmacy, Bahauddin Zakariya University, Multan, Pakistan

3 Department of Pharmaceutical Sciences, COMSATS Institute of Information Technology, Abbottabad, Pakistan

Abstract

Objectives. To design and evaluate modified release bilayer tablets of flurbiprofen.
Material and Methods. In this study, bilayer modified release (MR) tablets of flurbiprofen were formulated using ethylcellulose (EC) and polyvinylpyrrolidone (PVP) in different ratios as release retardant materials using a wet granulation method. In vitro release studies were done in dissolution media of varying pH i.e. pH 1.2, 4.5, 7.0 and 7.5.
Results. All tablets exhibited good physical quality with respect to appearance, content uniformity, hardness, weight variation and friability. In vitro dissolution data showed that increasing proportions of EC retarded whereas increasing PVP enhanced the drug release rate. The bilayer MR tablets showed an initial release of approximately 35% (i.e. 100 mg drug) in about 1 h, then sustaining the release for 12 h, ending up with 89.56% and 96.12% for formulation MR1 and MR2, respectively. The kinetic analysis of dissolution data showed that zero order release was observed in these tablets. When data was fitted to the Korsmeyer-Peppas model, a non-Fickian transport was observed with the MR tablets. A model independent approach showed that as the release rate increases, the MDT decreases, showing the retarding behavior of the non-biodegradable polymers employed in formulation development.
Conclusion. Bilayer modified release tablets of flurbiprofen can be successfully formulated using ethylcellulose and polyvinylpyrrolidone in different ratios as release retardant materials employing a wet granulation method.

Streszczenie

Cel pracy. Zaprojektowanie i ocena dwuwarstwowych tabletek flurbiprofenu o zmodyfikowanym uwalnianiu.
Materiał i metody. W badaniu tym dwuwarstwowe tabletki flurbiprofenu o zmodyfikowanym uwalnianiu (MR) zostały stworzone z użyciem etylocelulozy (EC) i poliwinylopirolidonu (PVP) w różnych proporcjach jako środki opóźniające uwolnienie metodą mokrej granulacji. W badaniach uwalniania in vitro użyto środków rozpuszczających o różnym pH, tj. pH 1,2; 4,5; 7,0 i 7,5.
Wyniki. Wszystkie tabletki miały dobre fizyczne właściwości w odniesieniu do wyglądu, jednolitości zawartości, twardości, wahań wagi i kruszenia. W badaniach in vitro wykazano, że zwiększenie zawartości EC spowalniało, a zwiększenie zawartości PVP przyspieszało tempo uwalniania leku. Dwuwarstwowe tabletki MR wykazały początkowo uwalnianie ok. 35% (tj. 100 mg leku) w ciągu około 1 godz., a następnie utrzymanie rozpuszczenia przez 12 godz., kończąc na 89,56 i 96,12% dla preparatów MR1 i MR2. Analiza kinetyczna danych na temat rozpuszczania pokazała, że w tych tabletkach wystąpiło uwalnianie rzędu zerowego. Gdy dane dopasowano do modelu Korsmeyera-Peppasa, obserwowano transport masy tabletek MR niezgodny z prawem Ficka. Niezależne podejście wykazało, że w miarę wzrostu szybkości uwalniania, MDT zmniejsza się, co pokazuje opóźniające działanie nieulegających biodegradacji polimerów stosowanych w produkcji preparatu.
Wnioski. Dwuwarstwowe tabletki o zmodyfikowanym uwalnianiu flurbiprofenu z powodzeniem można produkować, stosując etylocelulozę i poliwinylopirolidon w różnych proporcjach jako środki opóźniające uwolnienie metodą mokrej granulacji.

Key words

ethylcellulose, polyvinylpyrrolidone, wet granulation method, non-Fickian release.

Słowa kluczowe

etyloceluloza, poliwinylopirolidon, metoda mokrej granulacji, uwalnianie niezgodne z prawem Ficka.

References (14)

  1. Mullaichararm AR, Barish, Karthikeyan D: Comparative release studies of transdermal films of flurbiprofen across various diffusion barriers. The Ind Pharmacist 2004, 3, 56–58.
  2. Lafuente SC, Faucci TM, Arevalo FM, Fuentes AJ, Rabasco AM, Mura P: Development of sustained release matrix tablets of didanosine containing methacrylic and ethylcellulose polymers. Int J Pharm 2002, 234, 213–221.
  3. Abdelkader H, Abollah OY, Salem HS: Comparison of the effect of tromethomine and poilyvinylpyrrolidone on dissolution properties and analgesic effect of Nimesulide. AAPS PharmSciTech 2007, 8, 65–71.
  4. British Pharmacopoeia (BP), 2007. Appendix XII G. Uniformity of Weight (Mass). London: British Pharmacopoeia Commission. P 1.
  5. Cruz BA, Jordan D, Haza G, Aleman U, Caraballo AI: Statistical optimization of a sustained release tablet of lobenzarite disodium. Drug Dev Ind Pharm 2000, 26, 1303–1307.
  6. Murtaza G, Ahmad M, Asghar MW, Aamir MN: Salbutamol sulphate-ethylcellulose microparticles: formulation and in-vitro evaluation with emphasis on mathematical approaches. DARU 2009, 17, 209–216.
  7. Davidson AG: In Practical pharmaceutical chemistry. Eds.: Beckett AH, Stenlake JB, 4th Edition, CBS Publishers, New Dehli 2002, 275–337.
  8. Murtaza G, Ahmad M, Shehnaz G: Microencapsulation of diclofenac sodium by non-solvent addition technique: Use of toluene and petroleum benzin as solvent and non-solvent respectively. Trop J Pharm Res 2010, 09, 187–195.
  9. Rasool F, Ahmad M, Murtaza G, Khan HMS, Khan SA: Metoprolol tartrate-Ethylcellulose Tabletted Microparticles: Formulation and in-vitro Evaluation. Latin Am J Pharm 2010, 9, 984–990.
  10. Murtaza G, Ahmad M: Microencapsulation of tramadol hydrochloride and physicochemical evaluation of formulations. Pak J Chem Soc 2009, 31, 511–519.
  11. Murtaza G, Ahmad M, Khan SA: Release behavior of the ethylcellulose microcapsules containing model drugs of different physicochemical properties. J Pharm Bioal Sci 2010, 2, 153–153.
  12. Khan GM, Zhu JB: Ibuprofen release kinetics from controlled-release tablets granulated with aqueous polymeric dispersion of ethylcellulose. Influence of several parameters and co-excipients. J Control Rel 1998, 56, 127–134.
  13. Qudair MA, Chanda E, Haider SS, Reza MS, Datta BK: Evaluation of ethylcellulose as matrices for controlled release drug delivery. Pak J Pharm Sci 2005, 18, 29–34.
  14. Reza MS, Abdul-Quadir M, Haider SS: Comparative evaluation of plastic, hydrophobic and hydrophilic polymers as matrices for controlled-release drug delivery. J Pharm Pharm Sci 2003, 6, 282–291.