Formulation and Evaluation of Gastro-Retentive Floating Extended Release Metoprolol Tablets using Sodium Alginate and HPMC K-100M Combination

DOI:

https://doi.org/10.37285/ijpsn.2015.8.3.9

Authors

  • Ashok Thulluru
  • M. Mohan Varma
  • C M Setty
  • Pavan Kumar Chintamaneni
  • S. Sriharsha vardhan

Abstract

The present study was aimed to convert Metoprolol Succinate convert into Gastro Retentive Floating Tablet (GRFT). The gas generating floating tablets of Metoprolol Succinate were prepared to increase the gastric retention and to extend the drug release up to 12 hr. and thereby enhancing its bioavailability. The floating tablets were formulated using HPMCK 100M alone and with the combination of sodium alginate to the polymer of varying concentrations. The tablets were prepared by non-aqueous wet granulation method. The formulated granules were evaluated for pre-compression studies, after the compression of tablets they were subjected to various post-compression studies: Average weight, thickness, density, hardness, % friability, % drug content, (In vitro buoyancy studies: floating time, total floating time and matrix integrity up to 12 hr) and the In vitro drug release studies. The optimized formulation (F4) was found to follow a near perfect zero order kinetics (regression coefficient,      r2 = 0.978). Higuchi plot for formulation, F4, showed r2 value of 0.978, suggesting that the diffusion and erosion plays an important role in the controlled release of the drug. The data was fitted to the Korsemeyer-Peppa’s equation; and the value of the diffusion component (n=0.654), for the formulation F4, indicated that the drug release follows non-Fickian diffusion.

 

Downloads

Download data is not yet available.

Metrics

Metrics Loading ...

Keywords:

Metoprolol, Gastro-retentive floating tablets, HPMC K100M, Sodium alginate

Downloads

Published

2015-08-30

How to Cite

1.
Thulluru A, Varma MM, Setty CM, Chintamaneni PK, vardhan SS. Formulation and Evaluation of Gastro-Retentive Floating Extended Release Metoprolol Tablets using Sodium Alginate and HPMC K-100M Combination. Scopus Indexed [Internet]. 2015 Aug. 30 [cited 2024 May 18];8(3):2947-54. Available from: http://www.ijpsnonline.com/index.php/ijpsn/article/view/798

Issue

Section

Research Articles

References

Aulton M.E and Wells T.I, (1988). Pharmaceutics: The Science of Dosage Form Design, London, England: Churchill Livingstone;.

Basak S.C (2004). Development And In Vitro Evaluation Of Oral Matrix Floating Tablets Formulation Of Ciprofloxacin. Ind. J Pharm Sci, 66: 313-316.

Choi B.Y. and Park H.J (2000). Preparation of Alginate Beads for Floating Drug Delivery System: Effect of CO2 Gas Forming Agent. J Cont Rel, 25: 488-491.

Cooper J and Gunn C (1986). Powder flow and compaction, In: Carter SJ, eds. Tutorial Pharmacy. New Delhi, India: CBS Publishers and Distributors. 211-233.

Dave BS, Amin AF and Patel M.M (2004). Gastro Retentive Drug Delivery System of Ranitidine Hydrochloride: Formulation and in-vitro Evaluation. AAPS Pharm Sci Tech, 5: 1-6.

Higuchi T. Mechanism of Sustained-action Medication (2004). Theoretical Analysis of Rate of Release of Solid Drugs Dispersed in Solid Matrices. J Pharm. Sci, 51: 1145-1149.

Hilton A.K. and Deasy B.P (1992). In vitro and in vivo evaluation of an oral sustained-release floating dosage form of Amoxycillintrihydrate. Int.J Pharm. 86: 79-88.

Himasankar K (2006). Design and Biopharmaceutical Evaluation of Gastric Floating Drug Delivery System of Metformin HCl. Ind. J Pharm Edu Res. 40: 369-382.

Ichikawa. M, Watanabe. S and Miyake Y. A (1991). New multiple-unit Oral Floating Dosage System: Preparation and in-vitro Evaluation of Floating and Sustained-release Characteristics. J Pharm Sci. 80:1062-1066.

J.R. Howard and Peter Timinis (1998). “Ph Dependent Polymer, Ph Independent Hydrocarbon Gelling Agent and Binder” US Patent 4792452.

Lakade S.H and Bhalekar MR (2008), Formulation and Evaluation of Sustained release Matrix Tablet of Anti-Anginal Drug, Influence of Combination of Hydrophobic and Hydrophilic Matrix Former, Research J. Pharm and Tech. 1: 410-413.

Libo Yang (1999). A New Intragastric Delivery System for the Treatment of H.Pylori associated with Gastric ulcers, J. Cont. Rel. 34: 215-222.

Menon A, Wolfgang A.R. and Saks. A (1994). Development and Evaluation of Monolithic Floating Dosage form for Furosemide, J.Pharm. Sci. 83: 239-245.

Nur O.A. and Zhang J.S. (2000). Captopril Floating and/or Bioadhesive Tablets: Design and Release kinetics. Drug Dev. Ind Pharm. 26:965-969.

Ozdemir N, Ordu S and Ozkan (2000). Studies of Floating Dosage Forms of Furosemide: in-vitro and in vivo Evaluations of Bilayer Tablet Formulations, Drug Dev. Ind Pharm, 26: 857-866.

Peppas N.A (1985). Analysis of Fickian and Non-Fickian Drug Release from Polymers. Pharma Aceta. Helv, 60: 110-111.

Rosa M., Zia H and Rhodes T., (1994). Dosing and Testing Invitro of A Bioadhesive and Floating Drug Delivery System for Oral Application. Int J. Pharm. 105: 65-70.

Rouge N and Allemann E (1998). Buoyancy and Drug release Patterns of Floating Mini Tablets containing Piretanide and Atenolol as model Drugs. Pharm Dev Technol, 3: 73-84.

Shah S, Quaqish R, Patel V and Amiji M. (1999) Evaluation of the Factors Influencing Stomach Specific Delivery of Antibacterial Agents for H.Pylori infections. J Pharm Pharmacol, 51: 667-672.

Shweta Arora (2005). Floating Drug Delivery: A Review, AAPS Pharm Sci Tech, 47: 268-272.

Singh B.N. and Kim (2000). H Floating Drug Delivery System an Approach to Control Delivery via Gastric Retention, J. Cont. Rel, 63:235-259.

Srivastava A.K. and Wadwa S (2005). Oral Sustain Delivery of Atenolol from Floating Matrix Tablets and In Vitro Evaluation. Drug Dev. Ind.Pharm, 31:367-374.

Streubel A, Siepmann J and Bodmeier R (2003). Floating Matrix Tablets Based on Low Density Foam Powder: Effects of Formulation and Processing Parameters on Drug Release. Eur J Pharm Sci. 18: 37-45.

Timmermans J and Moes AJ (2005). The Cut off Size for Gastric Emptying of Dosage Forms, J Pharm Sci, 82: 854.

Yeole P.G. Floating Drug Delivery System: Need and Development, Ind. J.Pharm Sci. 67: 265-272.