INFLUENCE OF FREE-FLOW EXCIPIENTS ON FUNCTIONAL PERFORMANCE OF NOVEONAA1 IN CONTROLLED-RELEASE TABLETS

  • RubÉn Ramos Islas Department of Pharmacy, National School of Biological Sciences, National Polytechnic Institute of Mexico, D. F., Mexico.
  • Leopoldo Villafuerte Robles Department of Pharmacy, National School of Biological Sciences, National Polytechnic Institute of Mexico, D. F., Mexico

Abstract

Objective: The aim of this work is the assessment of an eventual improvement in flowability of free flowing excipients on formulations containing Noveon AA1 and their influence on compactibility and release profile.

Methods: Mixtures containing 20% Noveon AA1 and variable proportions of metronidazole and the free flowing excipients Prosolv EasyTab and GalenIQ 720 and 721were tested in their powder flow rate and the tablets compactibility and released profiles.

Results: The powder flowability obtained with GalenIQ is about 20% better than that obtained with EasyTab. However, it is lesser than that considered as acceptable for a high-speed tableting machine. EasyTab reduces the drug release up to a half along with a continuing flattening of the release profile. This is attributed to an increasing tortuosity of the drug release path as the proportion EasyTab increases. GalenIQ restricts drug release in about a third with a lesser change in the release mechanism. This is attributed to competition for the available water inside the tablet, between the hydrating Noveon AA1 and the dissolving GalenIQ. The compactibility of the metronidazole/Noveon AA1 mixtures increases after addition of EasyTab in about 3.5 N per unit percentage of the added excipient while GalenIQ does it in about 2.6 N.

Conclusion: The powder flowability of mixtures of metronidazole with Noveon AA1 was not suited for direct compression after addition of 40% of the free-flow excipient. The free-flow excipients reduce the metronidazole release rate and increase its compactibility. It was not observed a different clear functioning between both types of GalenIQ.

Keywords: Compactibility profiles, Powder flowability, Dissolution profiles, excipient functionality, Metronidazole, Controlled release, Noveon AA1, GalenIQ, EasyTab

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References

1. www.micromeritics.com.Expanding the material characterization “Toolbox” for excipient and active pharmaceutical ingredient (API) vendor qualification. Applications note # 163. 4356 Communications Dr. Norcross, GA; 2016. p. 2.
2. Lubrizol. Guidance document for processing carbopol polymers in solid dosage. Available from: http://www.lubrizol.com/life-Science/Documents/Pharmaceutical/Brochures/Guidance-Document-on-Processing-Carbopol-Polymers-in-Oral-Solid-Dosage-Forms.pdf. [Last accessed on 10 Nov 2015].
3. Laguna-López S, Villafuerte-Robles L. Noveon AA1 as an enhancer of HPMC as a direct compression matrix for controlled release. J Appl Pharm Sci 2014;4:62-8.
4. Laguna-López SM, Angulo-Delgado CR, Villafuerte-Robles L. Effect of insoluble excipients on the performance of direct compression controlled release matrices. Lat Am J Pharm 2015;34:552-61.
5. Angulo-Delgado CR, Villafuerte-Robles L. Noveon AA1 as a matrix for controlled release of direct compression tablets. Lat Am J Pharm 2016;35:156-65.
6. Fuentes-González KI, Villafuerte-Robles L. Powder flowability as a functionality parameter of the excipient GalenIQ 720. Int J Pharm Pharm Sci 2014;6:66-74.
7. Rashid I, Al Omari MMH, Badwan AA. From native to multifunctional starch-based excipients designed for direct compression formulation. Starch/Stärke 2013;65:552–71.
8. Ruppel J, Müller AK, Althaus G, Drexel CP, Zimmerman I. The modified outflow funnel-A device to assess the flow characteristics of powders. Powder Technol 2009;193:87–92.
9. Arce-Fernández E, Villafuerte-Robles L. Características tecnológicas de mezclas de senósidos A+B con excipientes para la formulación de tabletas. Rev Cubana Farm 2008;42. Available from: http://scielo.sld.cu/scielo. php?script= sci_arttextandpid=S0034-75152008000300002andlng=e). [Last accessed on 10 Nov 2015].
10. GalenIQ 720. Available from: http://www.higuchi-inc.co.jp/pharma/excipient/isomalt/pdf/detail_galenIQ720.pdf. [Last accessed on 05 Nov 2015].
11. Ndindayino F, Henrist D, Kiekens F, Van den Mooter G, Vervaet C, Remon JP. Direct compression properties of melt extruded isomalt. Int J Pharm 2002;235:149–57.
12. Bolhuis GK, Engelhart JJP, Eissens AC. Compaction properties of isomalt. Eur J Pharm Biopharm 2009;72:621–5.
13. Galen IQ. Beneo-Palatinit. Available from: http://www. galeniq.com/galenIQ_Grades/galenIQ721/. [Last accessed on 05 Nov 2015].
14. Samayoa-Sandoval L, Villafuerte-Robles L. Compactibility as a functionality parameter of the excipient GalenIQ 720. Rev Mex Cienc Farm 2013;44:34-45.
15. Physical properties of GalenIQ 721. Available from: http://www.galeniq.com/galenIQ_Grades/galenIQ721/Technical_data_galenIQ_720-810_small.jpeg. [Last accessed on 05 Nov 2015].
16. Barrios-Vazquez SC, Villafuerte-Robles L. Functionality of GalenIQ 721 as excipient for direct compression tablets. J Appl Pharm Sci 2013;3:8-19.
17. Pharmaceutical Powder Compaction Technology. 2nd Edition. Edited by Metin Çelik. Chapter 8/compaction properties of directly compressible materials. GK Bolhuis, H de Waard. Informa Healthcare. CRC Press; 2011. p. 176-7.
18. Vollmer R, Stoyanov E. An all-around excipient for direct compression. Pharm Technol Eur 2010;22:34.
19. Prosolv Easy Tab. Prosolv Family of high functionality excipients. Wall chart. JRS Pharma GmbH+Co. KG. 73494. Rosenberg (Germany). 2010. Available from: www.jrspharma.de. [Last accessed on 03 Nov 2015].
20. Prosolv EasyTab SP. JRS Pharma; 2015. Available from: http://www.jrspharma.com/pharma_en/products-services/excipients/hfe/prosolv-easytab-sp.php. [Last accessed on 03 Nov 2015].
21. Patel MA, Pingale PL. Comparative effect of different high functionality excipients on various characteristics of Vardenafil. HCl tablets (BCS II drug). Int J Pharm Sci Res 2014;5:5447-51.
22. Williams HD, Ward R, Cully A, Hardy IJ, Melia D. Designing HPMC matrices with improved resistance to dissolved sugar. Int J Pharm 2010;401:51-9.
23. Vaidya MP, Avachat AM. Investigation of the impact of insoluble diluents on the compression and release properties of matrix based sustained release tablets. Powder Technol 2011; 214:375-81.
24. Kàllai N, Luhn O, Dreedán J, Kovács K, Lengyel M, Antal I. Evaluation of drug release from coated pellets based on isomalt, sugar, and microcrystalline cellulose inert cores. AAPS PharmSciTech 2010;11:383-91.
25. López-Solís J, Villafuerte-Robles L. Effect of disintegrants with different hygroscopicity on the dissolution of Norfloxacin/ Pharmatose DCL 11 tablets. Int J Pharm 2001;216:127–35.
26. Castillo S, Villafuerte L. Compactibility of binary mixtures of pharmaceutical powders. Eur J Pharm Biopharm 1995;41:309-14.
27. Castillo S, Villafuerte L. Compactibility of ternary mixtures of pharmaceutical powders. Pharm Acta Helv 1995;70:329-37.
28. Muzíková J, Pavlasová V. Energy evaluation of the compaction process of directly compressible isomalt. Ceska Slov Farm 2011;60:11-6.
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Islas, R. R., and L. V. Robles. “INFLUENCE OF FREE-FLOW EXCIPIENTS ON FUNCTIONAL PERFORMANCE OF NOVEONAA1 IN CONTROLLED-RELEASE TABLETS”. International Journal of Pharmacy and Pharmaceutical Sciences, Vol. 8, no. 9, Sept. 2016, pp. 6-13, doi:10.22159//ijpps.2016.v8i9.10193.
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