Formulation and Evaluation of Sustained Release Tablets of Metformin Hydrochloride by Solid Dispersion Technique Using pH dependent and pH independent Eudragit Polymers

Authors

  • K Rajendra Baliram University Department of Pharmaceutical sciences. R.T.M. Nagpur University (India)
  • U Milind Janrao Department of Pharmaceutical Technology, Smt. Kishoritai Bhoyar College of Pharmacy, Kamptee. (India)
  • W Kamlesh Jayantilal Department of Pharmaceutical Technology, Smt. Kishoritai Bhoyar College of Pharmacy, Kamptee. (India);

Keywords:

Metformin hydrochloride, Sustained release, Matrix tablet, pH-independent polymers, pH-dependent polymers

Abstract

Objectives: The purpose of the present investigation was to evaluate the influence of solid dispersion of pH dependent and pH independent Eudragit polymers on the sustained release metformin hydrochloride matrix tablets.

Materials and methods: Matrix formulations were prepared by direct compression techniques. The excipients used in this study did not alter physicochemical properties of the drug, as tested by FTIR and DSC. All the batches were evaluated various physical parameters. The in vitro drug dissolution and SEM studies were also carried out. Mean dissolution time is used to characterize drug release rate from a dosage form.

Results and discussion: Among the different examined polymer blends, Eudragit RLPO with S100 and Ll00 matrix tablets based on solid dispersion showed highly sustained release pattern. Kinetic modeling of in vitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled to anomalous type.

Conclusions: Fitting the data to Korsmeyer equation indicated that diffusion along with erosion could be the mechanism of drug release.

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References

Qui Y, Zhang D. Research and Development Aspects of Oral controlled Release Systems, In: Handbook of Pharmaceutical Controlled Release Technology (Ed. D.L. Wise), Marcel Dekker Inc, New York 2000; p.465–503.

Colombo P, Bettini R , Santi P and Peppas NA. Swellable matrixes for controlled drug delivery: gel-layer behavior, mechanisms and optimal performance. Pharm Sci Technol Today. 2003;3:198–204.

Rodriguez L, Caputo O, Cini M , Cavallar C, R. Grecchi, In vitro release of theophylline from directly-compressed matrices containing methacrylic acid copolymers and/or dicalcium phosphate dehydrate. Farmaco.1993;48:1597–1604

Kidokoro M, Shah NH, Malick AW, Infel MH, McGinity JW. Properties of tablets containing granulations of ibuprofen and an acrylic copolymer prepared by thermal processes. Pharm Develop Technol. 2001;6:263–275.

Zhu Y, Shah NH, Malick AW, Infeld MH, McGinity JW. Influence of thermal processing on the properties of chlorpheniramine maleate tablets containing an acrylic polymer. Pharm Develop Technol, 2000;7:481–489.

Palmieri GE, Michelini S, Martino PD, Martelli S. Polymers with pH-dependent solubility: possibility of use in the formulation of gastroresistant and controlled-release matrix tablet. Drug Dev Ind Pharm. 2000;26:837–845.

Bruce LD, Shah NH, Malick AW, Infeld MH, McGinity JW. Properties of hot-melt extruded tablet formulations for the colonic delivery of 5-aminosalicylic acid. Eur J Pharm Biopharm. 2000;59:85–97.

Ashford M, Fell TJ, Attwood D, Woodhead PJ.An in vitro investigation into the suitability of pH-dependent polymers for colon targeting. Int J Pharm.1993;91:241–245.

Risbud MV, Hardikar AA, Bhat SV, Bhonde RR. PH sensitive freeze-dried chitosan-polyvinyl pyrrolidone hydrogels as controlled release system for antibiotic delivery. J Control Release. 2000;68:23–30.

Palmieri GE, Michelini S, Martino P, Martelli S. Polymers with pH-dependent solubility: possibility of use in the formulation of gastroresistant and controlled-release matrix tablets. Drug Dev Ind Pharm. 2000;26:837–845.

Gupta VK, Beckert TE, Price JC. A novel pH- and time based multi-unit potential colonic drug delivery system. I. Development. Int J Pharm. 2000;213:83–91.

Gurnasinghani ML, Bhatt HR, Lalla JK. Indomethacin delivery from matrix controlled release indomethacin tablets. J Control Release. 1989;8:211-222.

Aceves JM, Cruz R, Hernandez E. Preparation and characterization of furosemide-Eudragit controlled release systems. Int J Pharm. 2000;195:45-53.

Goracinova K, Klisarova LJ, Simov A. Physical characterisation and dissolution properties of verapamil HCl coprecipitates. Drug Dev Ind Pharm. 1995;21:383-391.

Pignatello R, Ferro M, De Guidi G, Salemi G, Vandelli MA, Guccione S, Geppi M, Forte C, Puglisi G. Preparation, Characterisation and photosensitivity studies of solid dispersions of diflunisal and Eudragit RS100 and RL100. Int J Pharm. 2001;218:27-42.

Yuasa H, Ozeki T, Kanaya Y, Oishi K, Oyake T. Application of the solid dispersion method to the controlled release of medicine. I. Controlled release of water soluble medicine by using solid dispersion. Chem Pharm Bull. 1991;39:465-467.

Yuasa H, Ozeki T, Kanaya Y, Oishi K. Application of the solid dispersion method to the controlled release of medicine. II. Sustained release tablet using solid dispersion granule and the medicine release mechanism. Chem Pharm Bull. 1992;40:1592-1696.

Ozeki T, Yuasa H, Kanaya Y, Oishi K. Application of the solid dispersion method to the controlled release of medicine. V. Suppression mechanism of the medicine release rate in the three-component solid dispersion system. Chem Pharm Bull. 1994;42:337-343.

Ozeki T, Yuasa H, Kanaya Y, Oishi K. Application of the solid dispersion method to the controlled release of medicine. VII. Release mechanism of a highly water-soluble medicine from solid dispersion with different molecular weight of polymer. Chem Pharm Bull. 1995;43:660-665.

Dunn CJ, Peters DH, Metformin: A review of its pharmacological properties and therapeutic use in non-insulin-dependent diabetes mellitus. Drugs. 1995;49:721-749.

Defang O, Shufang N, Wei L. In vitro and in vivo evaluation of two extended Release preparations of combination metformin and glipizide. Drug Dev Ind Pharm. 2005;31:677–685.

Martin A. Micromeritics. In: Physical Pharmacy. ed. Philadelphia, PA: Lippincott Williams & Wilkins; 2001. p. 423-454.

Wells J. Pharmaceutical preformulation: The physiochemical properties of drug substances. In: Aulton, ME. ed. Pharmaceutics the science of dosage form design London: Churchill Livingstone. 2002; 247 p.

Hiuchi T. Mechanism of sustained-action medication, Theoretical analysis of rate of release of solid drugs dispersed in solid matrices. J Pharm Sci. 1963;52:1145–1149.

Gibaldi M, Feldman S. Establishment of sink conditions in dissolution rate determinations—theoretical considerations and application to non disintegrating dosage forms. J Pharm Sci. 1967;56:1238–1242.

Korsmeyer RW, Gurny R, Doelker RE, Buri P, Peppas NA. Mechanism solute release from porus hydrophilic polymers. Int J Pharm. 1983;15:25–35.

Costa P, Sousa Lobo JM,.Modeling and comparison of dissolution profiles. Eur J Pharm Sci. 2001;13:123–133.

Rao VM, Engh K, Qiu Y. Design of pH-independent controlled release matrix tablets for acidic drugs. Int J Pharm. 2003;252:81–86.

Moore JW, Flanner HH. Mathematical comparison of dissolution profiles. Pharm. Tech. 1996;20:64–74.

Banker GS, Anderson. In: Lachman L, Liberman HA, Kanig JL. The theory and practice of industrial pharmacy. 3rd ed. Mumbai: Varghese publishing house; 1987. 383 p.

Published

2012-03-20

How to Cite

1.
Rajendra Baliram K, Milind Janrao U, Kamlesh Jayantilal W. Formulation and Evaluation of Sustained Release Tablets of Metformin Hydrochloride by Solid Dispersion Technique Using pH dependent and pH independent Eudragit Polymers. Ars Pharm [Internet]. 2012 Mar. 20 [cited 2024 Jul. 22];53(1):28-36. Available from: https://revistaseug.ugr.es/index.php/ars/article/view/4660

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