22Jul 2018


Crossref Cited-by Linking logo
  • Abstract
  • Keywords
  • References
  • Cite This Article as
  • Corresponding Author

Modulated carbamazepine prolonged release dosage forms, microspheres have been prepared by the emulsion solvent evaporation method using Methocel K4M, PEG 4000 and Eudragit RLPO. A 22 factorial design was made by central composite design where the amount of Methocel K4M and PEG 4000 were selected as independent variables. Thirteen formulations were prepared with MDT, T50%, T80%, and swelling index as dependent variables. Data’s were analyzed statistically using linear regression model by IBM SPSS version 22. Effect of varying amount of Methocel K4M and PEG 4000 on the drug content, entrapment efficiency, swelling index, surface morphology (SEM), and in-vitro drug release rate were evaluated. Formulations with high amount of Methocel K4M showed good swelling properties. In SEM studies microspheres appeared rough and spherical in shape. Increasing amount of PEG produced pores on the surface of the microspheres due to the diffusion of polymers towards the external phase thus showing better drug release (B1, B3 & B8). Further clarification on release mechanism from spherical particles were studied using the Kopcha kinetics, Weibull model and Baker-Lonsdale model. In Kopcha kinetics all the formulations had ratio of A/B greater than 1 where release was primarily controlled by a Fickian diffusion. Weibull Model has parameters that are more sensitive to release kinetic data, the value of ? was <1 and Td value was low showing enhance drug release. In Baker-Lonsdale model most spherical matrix had uniformly distributed drugs with consistent drug release by diffusion mechanism which was seen as linear graphs.

  1. Asif, M. (2016): A review on antiepileptic drug and their uses, mechanism of actions, adverse effects and drug interaction. Curr. Sci. Perspectives., 2(2): 19-38.
  2. Mukhopadhyay, H.K., Das, S.K., Bhowmik, M., Ray, S., Rajabalaya, R., Ghosh, L. and Gupta, B.K. (2014): Preparation and characterization of polymethacrylate-based matrix microspheres of carbamazapine using solvent evaporation method. Farmacia., 62(1): 137-157.
  3. Mitra, A. and Dey, B. (2011): Chitosan microspheres in novel drug delivery systems. J. Pharm. Sci., 73(4): 355-366.
  4. Soni, M.L., Kumar, M. and Namdeo, K.P. (2010): Sodium alginate microspheres for extending drug release: formulation and in-vitro Int. J. Drug. Deliv., 2(1): 64-68.
  5. Mamun, M.A.R.A., Bagchi, M., Amin, M.L., Sutradhar, K.B. and Huda, H. (2014): Development of natural gum based glipizide mucoadhesive microsphere. J. App. Pharma. Sci., 4(1): 66-69.
  6. Rahman, M., Khalipha, A.B.R., Azad, M.A., Faruki, M.Z., Chaurasiya, A.K. and Hossain, H. (2013): Effect of natural and synthetic polymer on release of ketotifen fumarate matrix tablets: a sustained release dosage form. J. Pharm. Sci. and Res., 4(4): 1401-1408.
  7. Gupta, S., Munjal, T., Bhatia, P. and Kaur, I. (2014): Fabrication and evaluation of fluvastatin sodium loaded sustained release microspheres using polymer blends. J. Pharm. PharmSci., 6(5): 365-71.
  8. Khidr, S.H., Niazy, E.M. and Sayed, Y.M.E. (1998): Development andin-vitro?evaluation of sustained-release meclofenamic acid microspheres. J. Microencap. Micro. Nano. Carr., 15(2): 153-162.
  9. Higuchi, T. (1963): Mechanism of sustained medication, theoretical analysis of rate of release of solid drugs dispersed in solid matrices. J. Pharm. Sci., 52(12): 1464-77.
  10. Hixson, A.W. and Crowell, J.H. (1931): Dependence of reaction velocity upon surface and agitation: theoretical considerations. Eng. Chem., 23(8): 923?931.
  11. Korsmeyer, R.W., Gurny, R., Doelker, E., Buri, P. and Peppas, N.A. (1983): Machanisms of solute release from porous hydrophilic polymers. Int. J. Pharm., 15(1): 25-35.
  12. Kopcha, M., Lordi, N.G. and Tojo, K.J. (1991): Evaluation of release from selected thermo softening vehicles. Pharm. Pharmacol., 43(6): 382-387.
  13. Biswas, G. and Majee, S.B. (2015): Modeling of drug-diffusion kinetics of amoxicillin trihydrate from buccal tablets. J. Pharm. Bio. Sci., 6(2): 859 ? 866.
  14. Langenbucher, F. (1972): Linearization of dissolution curves by the Weibull distribution. J. Pharm. Pharmacol., 24(12): 979?81.
  15. Patel, N., Chotai, N., Patel, J., Soni, T., Desai, J. and Patel, R. (2008): Comparison of in-vitro dissolution profiles of oxcarbazepine-HP β-CD tablet formulations with marketed oxcarbazepine tablets. Diss. Tech., 28-33.
  16. Baker, R.W. and Lonsdale, H.S. (1974): Controlled release: mechanism and rates. In: Tanquary, A.C. and Lacey, R.E. (eds.) Controlled release of biologically active agents, New York, Plenum Press: pp. 15-71.
  17. Ramos, B.Z., Soldi, M., Soldi, V. and Senna, E.L. (2006): The effect of polyethylene glycol on drug content, particle morphology, and carbamazepine release profiles of sustained release microspheres prepared from cellulose acetate butyrate. Acta. Farm. Bonaerense., 25(2): 177- 83.
  18. Hasan, I., Paul, S., Akhter, S., Ayon, N.J. and Reza, M.S. (2013): Evaluation and optimization of influence of permeability property and concentration of polymethacrylic polymers on microspheres of metformin HCl. Dhaka. Univ. J. Pharm. Sci., 12(2): 131-141.
  19. Saha, N., Hasan, I., Nazmi, M. and Reza, M.S. (2013): Design and development of sustained release microspheres of Ibuprofen by emulsification solvent evaporation method using polymeric blend. Bangladesh. Pharma. J., 16(1): 39-44.

[Nasreen Sultana, Nusrat Ahmed, Ikramul Hasan and Selim Reza. (2018); PREPARATION AND CHARACTERIZATION OF METHOCEL K4M, EUDRAGIT RLPO AND PEG 4000 LOADED CARBAMAZEPINE MICROSPHERES. Int. J. of Adv. Res. 6 (Jul). 731-742] (ISSN 2320-5407). www.journalijar.com

Nusrat Ahmed
Department of Pharmacy, University of Asia Pacific, 74/A, Green Road, Dhaka-1215, Bangladesh.


Article DOI: 10.21474/IJAR01/7419      
DOI URL: http://dx.doi.org/10.21474/IJAR01/7419