POROUS PLASTIC MATRIX TABLETS OF LEVETIRACETAM FOR ZERO-ORDER CONTROLLED RELEASE: DEVELOPMENT AND FORMULATION OPTIMIZATION

Authors

  • RAVI PARIMI University College of Pharmaceutical Sciences, Acharya Nagarjuna University, Nagarjuna Nagar, Guntur 522510, Andhra Pradesh, India
  • RAMA RAO VADAPALLI K. E. PRAVALLIKA
  • K. E. PRAVALLIKA University College of Pharmaceutical Sciences, Acharya Nagarjuna University, Nagarjuna Nagar, Guntur 522510, Andhra Pradesh, India

DOI:

https://doi.org/10.22159/ijap.2021v13i4.41172

Keywords:

Porous plastic matrix, Pore former, Highlysoluble drugs, Zero-order controlled release, Embedding

Abstract

Objective: The prior objective of the current research work was to develop once-daily levetiracetam extended/controlled-release tablets having zero-order release kinetics with the plastic matrix as the release retarding element. For a high water-soluble drug, the formulation of a dosage form so as to have an extended drug release has always been a difficult task.

Methods: In the current work, levetiracetam which is a highly soluble drug was taken as the model drug for which extended-release matrix tablets were developed using varied plastic polymers like Polyvinyl acetate (PVAc), Polyvinyl chloride (PVC), Eudragit RSPO and Eudragit RLPO. PVP was considered as a pore-forming agent and PEG 6000 was taken as a water regulating agent. The porous plastic matrix tablets were prepared by embedding the drug in solvent-activated polymer dispersion followed by drying, sieving, mixing with other excipients and finally compressed. Including physical characterization studies and drug release studies, the tablets were subjected to SEM studies before and after the dissolution studies to analyze the effect of the pore former.

Results: Pre-compression mixtures exhibited good packageability of 81-92% and hence the compressed tablets were strong enough with good tensile strength in the range of 0.78–0.90 N/mm2. Drug release study results showed that the drug release was controlled for a period of 12–24h. PVAc had shown better controlled-release among all the plastic polymers taken. PEG 6000 in combination with PVP produced the desired zero-order drug release.

Conclusion: The levetiracetam porous plastic matrix tablets were developed with zero-order drug release that was effectively controlled for 24hr.

Downloads

Download data is not yet available.

References

Mondal N. The role of matrix tablet in drug delivery system. Int J Appl Pharm 2018;10:1-6.

Patel H, Panchal DR, Patel U, Brahmbhatt T, Suthar M. Matrix type drug delivery system: a review. J Pharm Sci Bio-Sci Res 2011;1:143-51.

Reza MS, Quadi MA, Haider SS. Comparative evaluation of plastic, hydrophobic and hydrophilic polymers as matrices for controlled-release drug delivery. J Pharm Pharm Sci 2003;6:282-91.

Shammika P, Aneesh TP, Vidya Viswanad. Formulation and evaluation of synthesized quinazolinone derivative for colon specific drug delivery. Asian J Pharm Clin Res 2017;10:207-12.

Arafat M. Approaches to achieve an oral controlled release drug delivery system using polymers: a recent review. Int J Pharm Pharm Sci 2015;7:16-21.

Rajesh K, Deveswaran R, Bharath S, Basavaraj BV. Development of mesalazine microspheres for colon targeting. Int J Appl Pharm 2017;9:1-9.

Apu AS, Pathan AH, Shrestha D, Kibria G, Jalil R. Investigation of in vitro release kinetics of carbamazepine from Eudragit RSPO and RLPO matrix tablets. Trop J Pharm Res 2009;8:145.

Tabandeh H, Mortazavi SA, Guilani TB. Preparation of sustained-release matrix tablets of aspirin with ethylcellulose, Eudragit RS100 and Eudragit S100 and studying the release profiles and their sensitivity to tablet hardness. Iran J Pharm Sci 2003;2:201-6.

Pundir S, Badola A, Sharma D. Sustained release matrix technology and recent advance in matrix drug delivery system: a review. Int J Drug Res Tech 2013;3:12-20.

Singh S, Bhavesh S, Sanjaykumar N, Sunil B. Formulation and evaluation of levetiracetam extended-release tablets. Int J Pharm Sci Nanotech 2003;6:1958-65.

Eerike M, Konda VGR, Arunachalam R, Dawood U. Evaluation of antiepileptic activity of ethanolic extract of Azimatetracantha root in mice. Int J Curr Pharm Res 2016;8:76-9.

Alhalmi A, Altowairi M, Saeed O, Alzubaidi N, Almoiliqy M, Abdulmalik W. Sustained release matrix system: an overview. World J Pharm Pharm Sci 2018;7:1470-86.

Srikar G, Avula P, Koreddi S. Embedment technique: an alternative to wet granulation for bettercontrol of release of highly water-soluble drugs–a case study with diltiazem HCl. IntJ Pharm Pharm Sci 2015;7:270-6.

Karvekar M, Khan AB. A brief review on sustained-release matrix-type drug delivery system. J Pharm Res 2017;16:282-9.

Mohammed SS. Preparation, characterization and preformulation studies of diltiazem sustain release tablet. Asian J Res Pharm Sci Biotechnol 2014;2:16-22.

Chavan PM, Ughade S. Preparation, characterization and evaluation of tablet for colonic delivery. Int J Pharm Sci Res 2018;9:2027-33.

Eichie FE, Kudehinbu AO. Effect of particle size of granules on some mechanical properties of paracetamol tablets. Afr J Biotechnol 2009;8:5913-6.

Zaid AN, Al-Ramahi RJ, Ghoush AA, Qaddumi A, Zaroor YA. Weight and content uniformity of lorazepam half tablets: a study of correlation of low drug content product. Saudi Pharm J 2013;21:71-5.

Vijaya Durga K, Ashok Kumar P, Kulkarni SV. Influence of natural, synthetic polymers and fillers on sustained release matrix tablets of pregabalin. Int J Drug Dev Res 2013;5:252-67.

S Sivaneswari, E Karthikeyan, PJ Chandana. Novel expandable gastro retentive system by unfolding mechanism of levetiracetam using simple lattice design–formulation optimization and in vitro evaluation. Bull Fac Pharm Cairo Univ 2017;55:63-72.

Row RC, Shesky PJ, Owen SC. editors. Handbook of pharmaceutical excipients. London: Pharmaceutical Press; 2006.

Keller PE, Kouzes R. Water vapor permeation in plastics. Pacific Northwest National Laboratory: Washington; 2007.

Maskova E, Naiserova M, Kubova K, Masek J, Pavlokovs S, Urbanova M, et al. Highly soluble drugs directly granulated by water dispersions of insoluble Eudragit polymers as a part of hypromellose K100M matrix systems. BioMed Res Int 2019. https://doi.org/10.1155/2019/8043415

D’souza AA, Shegokar R. Polyethylene glycol (PEG): a versatile polymer for pharmaceutical applications. Expert Opin Drug Delivery 2016;13:1257-75.

Robinson JR, Lee VHL. editors. Controlled drug delivery–fundamentals and applications. New York: Informa Healthcare; 2011.

Yang M, Xie S, Li Q, Wang Y, Chang X, Shan L, et al. Effects of polyvinylpyrrolidone both as a binder and pore-former on the release of sparingly water-soluble topiramate from ethylcellulose coated pellets. Int J Pharm 2014;465:187-96.

Hwang JR, Sefton MV. The effects of polymer concentration and a pore-forming agent (PVP) on HEMA-MMA microcapsule structure and permeability. J Membr Sci 1995;108:257-68.

Published

07-07-2021

How to Cite

PARIMI, R., VADAPALLI, R. R., & PRAVALLIKA, K. E. (2021). POROUS PLASTIC MATRIX TABLETS OF LEVETIRACETAM FOR ZERO-ORDER CONTROLLED RELEASE: DEVELOPMENT AND FORMULATION OPTIMIZATION. International Journal of Applied Pharmaceutics, 13(4), 135–141. https://doi.org/10.22159/ijap.2021v13i4.41172

Issue

Section

Original Article(s)