CONTROLLED-RELEASE EFFERVESCENT FLOATING MATRIX TABLETS OF METFORMIN USING COMBINATION OF POLYMERS
DOI:
https://doi.org/10.22159/ijpps.2016v8i11.13806Keywords:
Metformin, Gastro retentive, HPMC K15M, Kappa carrageenanAbstract
Objective: It is always challenging to prepare the floating gastro retentive formulation of the high dose drug. The present research was aimed to prepare gastro retentive controlled release, matrix tablets of metformin, using the combination of different ionic, anionic and polyanionic polymers with HPMC.
Methods: Formulations were prepared using sodium alginate, pullulan, kappa carrageenan, xanthan gum, poloxamer 68 in combination with HPMC K15M. All matrix tablets were prepared by direct compression method and evaluated for swelling, floating adhesive period and drug release.
Results: All the tablets showed acceptable physicochemical properties. Statistical analyses of data revealed that tablets prepared using HPMC K15M and kappa carrageenan, formulation F2, is best in terms of showing excellent floating properties, extended adhesion periods and sustained drug release characteristics with similarity factor as 92 on comparison with the theoretical release of the drug.
Conclusion: The combination of HPMC K15M and kappa carrageenan can be further optimized by applying the appropriate statistical design.
Downloads
References
Adikwu MU, Yoshikawa Y, Takada K. Pharmacodynamic–pharmacokinetic profiles of metformin hydrochloride from a mucoadhesive formulation of a polysaccharide with antidiabetic property in streptozotocin-induced diabetic rat models. Biomaterials 2004;25:3041-8.
Dunn CJ, Peters DH. Metformin: a review of its pharmacological properties and therapeutic use in non-insulin-dependent diabetes mellitus. Drugs 1995;49:721–49.
Basak SC, Rahman J, Ramalingam M. Design and in vitro testing of a floatable gastro retentive tablet of metformin hydrochloride. Die Pharmazie Int J Pharm Sci 2007;62:145-8.
Porta V, Schramm SG, Kano EK, Koono EE, Armando YP, et al. HPLC-UV determination of metformin in human plasma for application in pharmacokinetics and bioequivalence studies. J Pharm Biomed Anal 2008;46:143-7.
Corti G, Cirri M, Maestrelli F, Mennini N, Mura P. Sustained release matrix tablets of metformin hydrochloride in combination with triacetyl-β-cyclodextrin. Eur J Pharm Biopharm 2008;68:303-9.
Yadav A, Jain DK. Gastroretentive micro balloons of metformin: Formulation development and characterization. J Adv Pharm Tech Res 2011;2:51-5.
Stepensky D, Friedman M, Srour W, Raz I, Hoffman A. Preclinical evaluation of pharmacokinetic–pharmacodynamic rationale for oral CR metformin formulation. J Controlled Release 2001;7:107–15.
Colo GD, Falchi S, Zambito Y. In vitro evaluation of a system for pH-controlled peroral delivery of metformin. J Controlled Release 2002;80:119–28.
Ali J, Arora S, Ahuja A, Babbar AK, Sharma RK. Formulation and development of a hydrodynamically balanced system for metformin: in vitro and in vivo evaluation. Eur J Pharm Biopharm 2007;67:196-201.
Tack-Oon Oh, Ju-Young Kim, Jung-Myung Ha, Sang-Cheol Chi, Yun-Seok Rhee. Preparation and in vivo evaluation of highly porous gastro retentive metformin tablets using a sublimation method. Eur J Pharm Biopharm 2013;83 Suppl 3:460-7.
Anita KL, Emma L, McConnell LJ, Richard E, Christian S. Decoupling the role of image size and calorie intake on gastric retention of swelling-based gastric retentive formulations: pre-screening in dog model. Int J Pharm 2012;431:90-100.
Li H, Hardy RJ, Gu X. Effect of drug solubility on polymer hydration and drug dissolution from polyethylene oxide (PEO) matrix tablets. AAPS PharmSciTech 2008;9:437–43.
Colombo P, Bettini R, Massimo G, Catellani PL, Santi P. Drug diffusion front movement is important in drug release control from swellable matrix tablets. J Pharm Sci 1995;84:991–7.
Pillay V, Fassihi R. A novel approach for constant rate delivery of highly soluble bioactives from a simple monolithic system. J Controlled Release 2000;67:67–78.
Bettini R, Catellani PL, Santi P, Massimo G, Peppas NA. Translocation of drug particles in HPMC matrix gel layer: effect of drug solubility and influence on release rate. J Controlled Release 2001;70:383–91.
Dorozynski P, Kulinowski P, Mendyk A, Jachowicz R. Gastroretentive drug delivery systems with l-dopa based on carrageenans and hydroxypropylmethylcellulose. Int J Pharm 2011;404:169–75.
Kshirsagar RV, Jain V, Wattamwar S. Effect of different viscocity grade HPMC polymers on gastro retentive drug delivery of metformin HCL. Int J Appl Pharm 2009;1 Suppl 1:44-50.
Mandal U, Pal TK. Formulation and in vitro studies of a fixed-dose combination of a bilayer matrix tablet containing metformin HCl as sustained release and glipizide as an immediate release. Drug Dev Ind Pharm 2008;34:305–13.
Rawlins EA. Bentley’s textbook of pharmaceutics. London, England: Cassell and Collier Macmillan; 1977.
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;31:677–85.
The Indian Pharmacopoeia, Indian Pharmacopoeia Commission, Ministry of Health and family welfare, Government of India; 2007. p. 193.
Dorozynski P, Jachowicz R, Kuligowski P, Kwiecinski S, Szybinski K. The polymers for the preparation of hydrodynamically balanced systems–methods of evaluation. Drug Dev Ind Pharm 2004;30 Suppl 9:947–57.
Patel A, Modasiya M, Shah D, Patel V. Development and in vivo floating behaviour of verapamil HCl intragastric floating tablets. AAPS PharmSciTech 2009;10 Suppl 1:310–5.
Rosa M, Zia H, Rhodes T. Dosing and testing in vitro of a bioadhesive and floating drug delivery system for oral application. Int J Pharm 1994;105:65–70.
Nakamura F, Ohta R, Machida Y, Nagai T. In vitro and in vivo nasal mucoadhesion of some water-soluble polymers. Int J Pharm 1996;134:173–81.
Perioli L, Ambrogi V, Paganoa C, Scuota S, Rossi C. FG90 chitosan as a new polymer for metronidazole mucoadhesive tablets for vaginal administration. Int J Pharm 2009;377:120–7.
Yuksel N, Kanik AE, Baykara T. Comparison of in vitro dissolution profiles by ANOVA-based, model-dependent and-independent methods. Int J Pharm 2000;209:57-67.
Costa P, Jose MSL. Modeling and comparison of dissolution profiles. Eur J Pharm Sci 2001;13:123-33.
Rao MRP, Sonar GS, Mandsaurwale RR, Vanshiv SD. Evaluation of effervescent floating matrix tablet formulations of salbutamol sulfate using full factorial design. Asian J Pharm 2009;3:43-9.
Puthori H, Murthy T, Kaushik A, Murthy K. Formulation and evaluation of floating tablets of niacin for sustained release. Asian J Pharm 2012;6 Suppl 1:31-7.
Timmins P, Delargy AM, Howard JR. Optimization and characterization of a pH independent extended-release hydrophilic matrix tablet. Pharm Dev Technol 1997;2 Suppl 1:25-31.
Campo VL, Kawano DF, da Silva, Jr DB, Carvalho I. Carrageenans: biological properties, chemical modifications, and structural analysis a review. Carbohydr Polym 2009;77:167–80.
Tatavarti AS, Mehta KA, Augsburger LL, Hoag SW. Influence of methacrylic and acrylic acid polymers on the release performance of weakly basic drugs from sustained release hydrophilic matrices. J Pharm Sci 2004;93 Suppl 9:2319-31.
Singh A, Sharma PK, Malviya R. Release behavior of drugs from various natural gums and polymers. Polim Med 2011;41 Suppl 4:73-80.
Nayak A, Maji R, Das B. Gastroretentive drug delivery systems: a review. Asian J Pharm Clin Res 2010;3:1-10.
Tatavarti AS, Hoag SW. Microenvironmental pH modulation based release enhancement of a weakly basic drug from hydrophilic matrices. J Pharm Sci 2006;95 Suppl 7:1459-68.
Izutsu Y, Sogo K, Okamoto S, Tanaka T. Pullulan and sugar coated pharmaceutical composition. US Patent; 1987.
Published
How to Cite
Issue
Section
