Design and Development of Metformin HCl Floating Microcapsules using Two Polymers of Different Permeability Characteristics
DOI:
https://doi.org/10.37285/ijpsn.2009.2.3.6Abstract
The objective of the present investigation was to design a sustained release floating microcapsules of Metformin HCl using two polymers of different permeability characteristics Cellulose acetate butyrate (MW of 16,000) and Eudragit RL100 (MW of 150,000) using the oil-in-oil emulsion solvent evaporation method. Polymers were used separately and in combination (1:1) to prepare different microcapsules using acetone as organic phase. In all batches of microcapsules, the total polymer concentration was kept constant (10%w/w). No significant differences in drug loading in microcapsules made from different polymer were noted. Drug loaded microcapsules were found to float on 0.1M HCl for more than 8 hour. FT-IR study showed no drug polymer interaction. SEM study clearly revealed the smoothness of the spherically shaped particles. All the prepared microcapsules showed higher amount of drug release in phosphate buffer (pH 6.8) as compared to the release in 0.1M HCl (pH 1.2). Evaluation of the release data reveals that microcapsules prepared from RL100, Cellulose acetate butyrate and combination of both the polymers exhibit Higuchi spherical matrix release, followed by first order and zero-order release kinetics. Finally, the drug loaded floating microcapsules were found to be safe, economical and will overcome the drawbacks associated with the drug in conventional tablet form, by reducing plasma drug fluctuations.
Downloads
Metrics
Downloads
Published
How to Cite
Issue
Section
References
Ali javed, Khar RK , Ahuja alka and Sharma KR. Formulation and development of hydro dynamically balanced system for Metformin HCl: Invitro and invivo evaluation. Eu .J Pharm. Biopharm. 28: 46-53 (2006).
Bodmeier R and Chen H. Preparation and characterization of microspheres containing the anti-inflammatory agents, Indomethacin, ibuprofen and kitoprofen. J. Control. Release. 10: 167-175 (1989).
Costa P and Sousa LJM. Modeling and comparison of dissolution profiles. Eu. J. Pharm. Sci. 13: 123-133 (2001).
El-Gibaly I. Development and in vitro evaluation of novel floating chitosan microcapsules for oral use: comparison with non-floating chitosan microspheres. Int. J. Pharm. 249: 7-21 (2002).
El-Kamel AH, Sokar MS, Al Gamal SS and Naggar VF. Preparation and evaluation of ketoprofen floating oral drug delivery system. Int. J. Pharm. 220:13-21(2001).
Goodman and Gilman. The Pharmacological Basis of Therapeutics. 10th edition, edited by Joel G. Hardman, McGraw Hill, medical publishers Div, New Delhi, (2000).
Higuchi T. Mechanism of sustained action medication theoretical analysis of rate of release of solid drugs dispersed in solid matrices. J. Pharm. Sci. 52: 1145-1149 (1963).
Jain SK, Awasthi AM and Jain NK. Calcium silicate based microspheres of repaglinide for gastro retentive floating drug delivery: Preparation and in vitro characterization. J. Control. Release. 8: 58-64 (2005).
Kawashima Y, Niwa T and Takeuchi H. Preparation of multiple unit hollow microspheres (micro balloons) with acrylic resin containing tranilast and their drug release characteristics (in vitro) and floating behavior (in vitro). J. Control. Rel. 16:279-290 (1991).
Kim Kook-Chong’s, Kim Mi-jung and Oh. Hee Kyong. Preparation and evaluation of sustained release microcapsules of terbutaline sulphate. Int. J. Pharm. 106: 213-219 (1994).
Klausner EA, Lavy E and Friedmon M. Expandable gastro retentive dosage forms. J. Control. Release. 90:143-162 (2003).
Korsemeyer RW, Gunny R and Peppas NA. Mechanism of solute release from porous hydrophilic polymers. Int. J. Pharm. 15:25-35 (1983).
Marathe PH, Wen Y, Norton J and Wilding IR. Effect of altered gastric emptying and gastrointestinal motility on bioavailability of metformin, in: AAPS Annual Meeting, New Orleans, LA, 1999.
Menon A, Wolfgang A, Ritschel A and Sakr A. Development and evaluation of monolithic floating dosage form for furosemide. J. Pharm. Sci. 83:239-245 (1994).
O’Donnell P B and McGinity J.W. Preparation of microspheres by the solvent evaporation technique. Advanced Drug Delivery Reviews. 28:25–42 (1997).
Obeidat MW and Price JC. Preparation and invitro evaluation of Propylthiouracil microspheres made of CAB and eudragit RL100 by emulsion solvent evaporation method. J. Microencap. 22:(3):281-289 (2005).
Rao V.K and Nair Subhash. Design and biopharmaceutical evaluation of gastric floating drug delivery system of Metformin HCl by using various hydrophilic polymers. Ind. J. Pharm. Edu. 5:23-27 (2006).
Ray Subhabrata, Patel Asha and Thakur SR. Invitro evaluation and optimization of Controlled release Floating Drug Delivery System of Metformin HCl. DARU. Pharm. 14: (2): 137-141 (2003).
Singh BN and Kim KH. Floating drug delivery system: approach to oral controlled drug delivery via gastro-retention. J. Control. Release. 63:235-259 (2000).
Srivastava AK, Ridhurkar Rao and Waodha Saurabh. Floating microspheres of Cimetidine: Formulation, Characterization and In vitro evaluation. Acta. Pharma. 55: 277-285 (2005).
Stepensky D, Friedman M, Sour W and Hoffmann A. Preclinical evaluation of pharmacokinetic-pharmacodynamic rationale for oral CR metformin formulation. J. Control. Release. 71:107-15 (2001).
Stithit S, Chen W and Price JC. Development and characterization of buoyant theophylline microspheres with near zero order release kinetics. J. Microencap. 15: (6): 725-37 (1998).
Streubel A, Siepmann J and Bodmeier R. Floating microparticles based on low density foam powder. Int. J. Pharm. 241: 279-292 (2002).
Talukdar R and Fassinir R. Gastroretentive Delivery System: Hollow beads. Drug. Dev. Ind. Pharm. 4:405-412 (2004).
Thanoo BC, Sunny MC and Jayakrishna A. Oral sustained –release drug delivery system using polycarbonate microspheres capable of floating on the gastric fluid. J. Pharm. Pharmacol. 45:21-24 (1993).
Vidon N, Chaussade S and Noel M. Metformin in the digestive tract. Diabetes. Res. Clin. Pract. 4: 223-29 (1988).
