Effect of Different Meltable Binders on the Disintegration and Dissolution Behavior of Zolmitriptan Oromucosal Fast Melt Tablets
PDF

Keywords

 Melt granulation technique, fast release sublingual tablets, meltable binders, intragranular desintegrant, PEG4000, F68, F127.

How to Cite

Doaa Ahmed El-Setouhy, Emad B. Basalious, & Nevine Shawky Abdelmalak. (2017). Effect of Different Meltable Binders on the Disintegration and Dissolution Behavior of Zolmitriptan Oromucosal Fast Melt Tablets . Journal of Pharmacy and Nutrition Sciences, 7(1), 13–23. https://doi.org/10.6000/1927-5951.2017.07.01.3

Abstract

Objective: Fast melt tablets and sublingual route have been widely used for providing quick onset of action with the avoidance of first pass metabolism. The objective of this work was to compare the effect of different meltable binders namely; polyethylene glycol (PEG) 4000, pluronic F127 and pluronic F68 on the performance of fast release tablets of the model drug zolmitriptan prepared using the melt granulation technique regarding disintegration time (DT) and dissolution rate (DR) as criteria for rapid absorption and hence quick onset of action. Zolmitriptan is a potent antimigraine drug. Current oral zolmitriptan tablets suffer from slow onset of action, poor bioavailability and large inter-subject variability.

Methods: 33 factorial design was adopted. The effect of binder type, binder concentration and croscarmellose sodium (disintegrant) concentration were studied on DT and DR.

Results: The three factors were found to significantly affect the DR and the inverse square root of DT and significant interactions were elucidated.

Conclusion: Although satisfactory results were obtained regarding DR, modifications using different excipients and or preparation methods should be considered to comply with pharmacopoeia requirement for DT.

https://doi.org/10.6000/1927-5951.2017.07.01.3
PDF

References

Singh J, Philip AK, Pathak K. Optimization Studies on Design and Evaluation of Orodispersible Pediatric Formulation of Indomethacin. AAPS Pharm Sci Tech 2008; 9: 60-66. https://doi.org/10.1208/s12249-007-9018-4

Ibrahim HK, El-Setouhy DA. Valsartan Orodispersible Tablets: formulation and in-vitro/in-vivo Characterization. AAPS Pharm Sci Tech 2010; 11: 189-196. https://doi.org/10.1208/s12249-009-9354-7

Shoukri RA, Ahmed IS, Shamma RN. In vitro and in vivo evaluation of nimesulide lyophilized orally disintegrating tablets. Eur J Pharm Biopharm 2009; 73: 162-171. https://doi.org/10.1016/j.ejpb.2009.04.005

Tayel SA, El-Nabarawi MA, El-Setouhy DA, and Sleem A. Formulation, evaluation, anti-inflammatory activity and bioavailability of ketorolac tromethamine fast dissolving tablets prepared by three different techniques. Egypt J Biomed Sci 2006; 22: 41-65.

Sunada H, Bi Y. Preparation, evaluation and optimization of rapidly disintegrating tablets. Powder Tech 2002; 122: 188-198. https://doi.org/10.1016/S0032-5910(01)00415-6

Bi Y, Yonezawa Y, Sunada H. Rapidly disintegrating tablets prepared by wet compression method: mechanism and optimization. J Pharma Sci 1999; 1004-1110.

Fukami J, Yonemochi E, Yoshihashi Y, Terada K. Evaluation of rapidly disintegration tablets containing glycine and carboxymethylcellulose. Int J Pharm 2006; 310: 101-109. https://doi.org/10.1016/j.ijpharm.2005.11.041

Gohe MC, Jogani PD. Exploration of Melt Granulation Technique for the Development of Coprocessed Directly Compressible Adjuvant Containing Lactose and Microcry-stalline Cellulose. Pharm Dev Technol 2003; 8: 175-85. https://doi.org/10.1081/PDT-120018487

Perissutti B, Rubessa F, Moneghini M, Voinovich D. Formulation design of carbamazepine fast-release tablets prepared by melt granulation technique. Int J Pharm 2003; 256: 53-63. https://doi.org/10.1016/S0378-5173(03)00062-0

Abdelbary G, Prinderre P, Eouani C, Joachim J, Reynier JP, Piccerelle P. The preparation of orally disintegrating tablets using a hydrophilic waxy binder. Int J Pharm 2004; 278: 423-433. https://doi.org/10.1016/j.ijpharm.2004.03.023

Passerini N, Albertini B, Gonzalez-Rodriguez ML, Cavallari C, Rodiguez L. Preparation and characterisation of ibuprofen poloxamer 188 granules obtained by melt granulation. Eur J Pharm Sci 2002; 15: 71-78. https://doi.org/10.1016/S0928-0987(01)00210-X

Schaefer T, Holm P, Kristensen HG. Melt granulation in a laboratory scale high shear mixer. Drug Dev Ind Pharm 1990; 16(8): 1249-77. https://doi.org/10.3109/03639049009115960

Abu Izza, Khawla A, Li Vincent H, Look LL, Parr GD, Schi-neller MK. Fast dissolving tablet. US patent 6733781; 2004.

Tayel S, Soliman I, Louis D. Formulation of Ketotifen Fumarate Fast-Melt Granulation Sublingual Tablet. AAPS Pharm Sci Tech 2010; 11: 679-685. https://doi.org/10.1208/s12249-010-9425-9

Malke S, Shidhaye S, Kadam V. Novel Melt Granulation Using Sugars for Metoclopromide Hydrochloride Orally Disintegrating Tablet. Asian Journal of Pharmaceutical and Clinical Research 2009; 2: 68-72.

Craig DQM. Polyethylene glycols and drug release. Drug Dev Ind Pharm 1990; 16: 2501-2526. https://doi.org/10.3109/03639049009058544

Kukec S, Dreu R, Vrbanec T, Sr?i? S, Vre?er F. Characterization of agglomerated carvedilol by hot-melt processes in a fluid bed and high shear granulator. Int J Pharm 2012; 430: 74-85. https://doi.org/10.1016/j.ijpharm.2012.03.041

Yang D, Kulkarni R, Behme RJ, Kotiyan PN. Effect of the melt granulation technique on the dissolution characteristics of griseofulvin. Int J Pharm 2007; 329: 72-80. https://doi.org/10.1016/j.ijpharm.2006.08.029

Wei Z, Hao J, Yuan S, Li Y, Juan W, Sha X, Fang X. Paclitaxel-loaded Pluronic P123/F127 mixed polymeric micelles: formulation, optimization and in vitro characterization. Int J Pharm 2009; 376: 176-85. https://doi.org/10.1016/j.ijpharm.2009.04.030

Kabanov AV, Batrakova EV, Alakhov VY. Pluronic block copolymers as novel polymer therapeutics for drug and gene delivery. J Contr Rel 82: 189-212.

Passerini N, Albertini B, Perissutti B, Rodriguez L. Evaluation of melt granulation and ultrasonic spray congealing as techniques to enhance the dissolution of praziquantel. Int J Pharm 2006; 318: 92-102. https://doi.org/10.1016/j.ijpharm.2006.03.028

El-Setouhy D, Basalious E, Abdelmalak NS. Bioenhanced sublingual tablet of drug with limited permeability using novel surfactant binder and microencapsulated polysorbate: In vitro/in vivo evaluation. European Journal of Pharmaceutics and Biopharmaceutics 2015; 94: 386-392. https://doi.org/10.1016/j.ejpb.2015.06.006

The British Pharmacopoeia. The Stationary Office, UK; 2007, pp. A 207,304, 208, 397- 405.

European Pharmacopoeia. 4th Edn, Council of Europe, Strasbourg, France 2002; pp. 1433-5.

Mahmoud A, Salah S. Fast relief from migraine attacks using fast-disintegrating sublingual zolmitriptan tablets Drug Development and Industrial Pharmacy 2011; 1-8.

Wells JI. Tablet testing. In: Swarbrick, J., Boylan, J.C. (Eds.), Encyclopaedia of Pharmaceutical Technology, Marcel Dekker, New York, 1997; vol. 141: pp. 401-418.

Pandya VM, Patel DJ, Pate lJK, Patel RP. Formulation, characterization, and optimization of fast-dissolving tablets containing celecoxib solid dispersion. Dissolution Tech 2009; 21-27.

Pund S, Joshi A, Vasu K, Nivsarkar M, Shishoo C. Multivariate optimization of formulation and process variables influencing physico mechanical characteristics of site-specific release isoniazid pellets. Int J Pharm 2010; 388: 64-72. https://doi.org/10.1016/j.ijpharm.2009.12.034

Abd Elbary A, Ibrahim HK, Hazaa BS. Understanding the formulation variables of orodispersible tablets containing simvastatin solid dispersion using Box-Behnken design. Drugs and Therapy Studies 2012; 2: 29-35. https://doi.org/10.4081/dts.2012.e7

Iwao Y, Tanaka S, Uchimoto T, Noguchi S, Itai S. An easy-to-use approach for determining the disintegration ability of disintegrants by analysis of available surface area. Int J Pharm 2013; 448: 1-8. https://doi.org/10.1016/j.ijpharm.2013.03.012

Batrakova EV, Li S, Li YL, Alakhov VY, Elmquist WF, Kabanov AV. Distribution kinetics of a micelle-forming block copolymer Pluronic P85. J Control Release 2004; 100: 389-397. https://doi.org/10.1016/j.jconrel.2004.09.002

Kolašinac N, Kachrimanis K, Homšek I, Gruji? B, Ðuri? Z, Ibri? S. Solubility enhancement of desloratadine by solid dispersion in poloxamers. Int J Pharm 2012; 436: 161-70. https://doi.org/10.1016/j.ijpharm.2012.06.060

Zhai H, Li S, Jones DS, Walker GM, Andrews GP. The effect of the binder size and viscosity on agglomerate growth in fluidised hot melt granulation. Chemical Engineering Journal 2010; 164: 275-284. https://doi.org/10.1016/j.cej.2010.08.056

Yadav VB, Yadav AV. Enhancement of solubility and dissolution rate of Fenofibrate by melt granulation techniques. Int J PharmTech Res 2009; 1: 256.

Abdelbary G, Makhlouf A. Adoption of polymeric micelles to enhance the oral bioavailability of dexibuprofen: formulation, in-vitro evaluation and in-vivo pharmacokinetic study in healthy human volunteers. Pharm Dev Technol 2014; 6: 717-27. https://doi.org/10.3109/10837450.2013.823994

Chandrasekhar R, Hassan Z, Alhusban F, Smith AM, Mohammed AR. The role of formulation excipients in the development of lyophilized fast-disintegrating tablets. Eur J Pharm Biopharm 2009; 72: 119-129. https://doi.org/10.1016/j.ejpb.2008.11.011

Kanig JL, Rudnic EM. The mechanism of disintegrant action. Pharm Technol 1984; 8: 50-62.

Van Kamp HV, Bolhuis GK, De Boer AH, Lerk CF, Lie-A-Huen L. The role of water uptake on tablet disintegration. Pharm. Acta Helv 1986; 61: 22-29.

Caramella C, Colombo P, Conte U, Ferrari F, La Manna A, Van Kamp HV, Bolhuis GK. Water uptake and disintegrating force measurements: towards a general understanding of disintegration mechanisms. Drug Dev Ind Pharm 1986; 12: 1749-1766. https://doi.org/10.3109/03639048609042607

Ford JL, Rubinstein MH. Formulation and ageing of tablets prepared from indomethacin-polyethylene glycol 6000 solid dispersions. Pharm Acta Helv 1980; 55: 1-7.

Ford JL. The preparation and properties of tablets containing indomethacin and polyethylene glycol 6000. Pharm Acta Helv 1983; 58: 101-108.

Haware RV, Chaudhari PD, Parakh SR, Bauer-Brandl A. Development of a melting tablet containing promethazine HCl against motion sickness. AAPS Pharm Sci Tech 2008; 9(3): 1006-15. https://doi.org/10.1208/s12249-008-9133-x

Kaul G, Huang J, Chatlapalli R, Ghosh K, Nagi A. Quality-by-Design Case Study: Investigation of the Role of Poloxamer in Immediate-Release Tablets by Experimental Design and Multivariate Data Analysis. AAPS Pharm Sci Tech 2011; 12: 1064-1076. https://doi.org/10.1208/s12249-011-9676-0

Creative Commons License

This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.

Copyright (c) 2017 Doaa Ahmed El-Setouhy, Emad B. Basalious, Nevine Shawky Abdelmalak