• RAJESH PAWAR MAEER’s Maharashtra Institute of Pharmacy, MIT Campus, Kothrud, Pune, India.
  • SWATI JAGDALE School of Pharmacy, Dr. Vishwanath Karad MIT World Peace University, MIT Campus, Kothrud, Pune, India
  • DHEERAJ RANDIVE Rajarambapu College of Pharmacy, Sangli, India



Novel excipient, Drug release, Floating drug delivery system, Mixture design, HPMC, PEO, Total floating time, Floating lag time, FDDS


Objective: The present study aimed to develop a new SR metformin hydrochloride (MH) gastroretentive formulation with novel excipient (NE), which has better floatation and can be prepared with more simple pharmaceutical techniques for the treatment of diabetes Mellitus.

Methods: A gastro-retentive floating matrix tablet (GFT) formulation of MH was prepared using various concentrations of PEO (Polyox WSR-303) and hydroxypropyl methylcellulose K100M (HPMC K100 M) and Floating agent (novel excipient) to achieve desirable TFT, FLT and drug release. The wet granulation method was selected using isopropyl alcohol as a binder for the preparation of tablets. D-optimal non-simplex mixture design was used for the selection of suitable polymer concentrations and floating agents. Release kinetics was used to determine the mechanism of drug release.

Results: It was observed that GFT with optimum quantities of PEO, HPMC K100M, and the floating agent showed 100 % of drug release in 24h with FT up to 24h and minimum FLT of less than 2 min. Formulation with an in vitro release profile slower to the marketed sample was prepared.

Conclusion: A sustained-release (GFT) of MH tablets using PEO, HPMC K100M, and an effervescent system was successfully prepared. A GFT formulation with an in vitro release profile slower to the marketed sample that releases MH for 24h may suitable for once-daily dosing can be prepared.


Download data is not yet available.


Gupta BP, Thakur N, Jain NP, Banweer J, Jain S. Osmotically controlled drug delivery system with associated drugs. J Pharm Pharm Sci 2010;13:571–88.

Prausnitz MR, Mitragotri S, Langer R. Current status and future potential of transdermal drug delivery. Nat Rev Drug Discovery 2004;3:115–24.

Wei H, Yongji L, Rao Z, Zhannan W, Lifang Y. Gastro-floating bilayer tablets for the sustained release of metformin and immediate release of pioglitazone: preparation and in vitro and in vivo evaluation. Int J Pharm 2014;476:223–31.

Faria S, Syed M, Juliana J, Uttam M. Design and in-vitro evaluation of sustained-release floating tablets of metformin HCl based on effervescence and swelling. Iranian J Pharm Res 2016;15:53-70.

Yun Y, Cho YW, Park K. Nanoparticles for oral delivery: Targeted nanoparticles with peptidic ligands for oral protein delivery. Adv Drug Delivery Rev 2013;65:822–32.

Palaksha M, Mani TT, Manjunatha E, Kumar GPS. Comparative study of in vivo effects of glipizide and metformin HCl on plasma concentration of aminophylline in healthy rabbits. Asian J Pharm Res 2020;10:62–6.

Mathews R, Prakash Rao B, Konde A, Sudarshan S, Taha NA, Suresh C. Statistical design and development of a liquid oral floating in situ gel of metformin hydrochloride for sustained release: pharmacodynamic and toxicity (histopathology) studies. Int J Appl Pharm 2019;11:96–104.

Lamos EM, Stein SA, Davis SN. Combination of glibenclamide-metformin HCl for the treatment of type 2 diabetes mellitus. Expert Opin Pharmacother 2012;52:862–7.

Umapathi P, Ayyappan J, Darlin Quine S. Quantitative determination of metformin hydrochloride in tablet formulation containing croscarmellose sodium as disintegrant by HPLC and UV spectrophotometry. Trop J Pharm Res 2012;11:107–16.

Sambol NC, Chiang J, O’Conner M, Liu CY, Lin ET, Goodman AM, et al. Pharmacokinetics and pharmacodynamics of metformin in healthy subjects and patients with noninsulin-dependent diabetes mellitus. J Clin Pharmacol 1996;36:1012–21.

Chaudhari SP, Patil PS. Pharmaceutical excipients: a review. Int J Adv Pharm Biol Chem 2012;1:21–34.

Katdare A, Chaubal MV. Excipient development for pharmaceutical, biotechnology, and drug delivery systems. Excip Dev Pharm Biotechnol Drug Delivery Syst 2006;1:1–436.

Gharti KP, Thapa P, Budhathoki U, Bhargava a: formulation and in vitro evaluation of floating tablets of hydroxypropyl methylcellulose and polyethylene oxide using ranitidine hydrochloride as a model drug. J Young Pharm 2012;4:201-8.

Bharate SS, Bharate SB, Bajaj AN. Interactions and incompatibilities of pharmaceutical excipients with active pharmaceutical ingredients: a comprehensive review. J Excipients Food Chem 2010;1:3–26.

Lundstedt T, Seifert E, Abramo L, Thelin B, Nyström A, Pettersen J, et al. Experimental design and optimization. Chemom Intell Lab Syst 1998;42:3–40.

Dejaegher B, Vander Heyden Y. Experimental designs and their recent advances in set-up, data interpretation, and analytical applications. J Pharm Biomed Anal 2011;56:141–58.

Baumgartner S, Kristl J, Vrecer F, Vodopivec P, Zorko B. Optimization of floating matrix tablets and evaluation of their gastric residence time. Int J Pharm 2000;195:125–35.

Putra WA, Kusumawati IGAW. The use of clinoptilolites as carrier of metformin hydrochloride in drug delivery system: in vitro drug release study. Asian J Pharm Clin Res 2018;11:285–9.

Nanjwade BK, Mhase SR, Manvi FV. Formulation of extended-release metformin hydrochloride matrix tablets. Trop J Pharm Res 2011;10:375–83.

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.

Veronika E, Joachim S, Patrick AC Gane, Rainer A, Jorg H, Maxim P. Floating gastroretentive drug delivery systems: comparison of experimental and simulated dissolution profiles and floatation behavior. Euro J Pharm Sci 2014;58:34–43.

Mage I, Næs T. Split-plot design for mixture experiments with process variables: a comparison of design strategies. Chemom Intell Lab Syst 2005;78:81–95.

Ng LY, Andiappan V, Chemmangattuvalappil NG, Ng DKS. A systematic methodology for optimal mixture design in an integrated biorefinery. Comput Chem Eng 2015;81:288–309.

Chouhan P, Saini TR. D-optimal design and development of microemulsion based transungual drug delivery formulation of ciclopirox olamine for treatment of onychomycosis. Indian J Pharm Sci 2016;78:498–511.

Roy P, Shahiwala A. Statistical optimization of ranitidine HCl floating pulsatile delivery system for chronotherapy of the nocturnal acid breakthrough. Eur J Pharm Sci 2009;37:363–9.

Hooda A, Nanda A, Jain M, Kumar V, Rathee P. Optimization and evaluation of gastroretentive ranitidine HCl microspheres by using design expert software. Int J Biol Macromol 2012;51:691–700.

Onsekizoglu P, Savas Bahceci K, Acar J. The use of factorial design for modeling membrane distillation. J Memb Sci 2010;349:225–30.

Eastwood DC, Mead A, Sergeant MJ, Burton KS. Statistical modeling of transcript profiles of differentially regulated genes. BMC Mol Biol 2008;9:1–16.

Aggarwal N, Goindi S, Khurana R. Formulation, characterization and evaluation of an optimized microemulsion formulation of griseofulvin for topical application. Colloids Surf B 2013;105:158–66.

Jannin V, Musakhanian J, Marchaud D. Approaches for the development of solid and semi-solid lipid-based formulations. Adv Drug Delivery Rev 2008;60:734–46.

Baumgartner S, Kristl J, Vrecer F, Vodopivec P, Zorko B. Optimisation of floating matrix tablets and evaluation of their gastric residence time. Int J Pharm 2000;195:125–35.

Nama M, Gonugunta CSR, Reddy Veerareddy P. Formulation and evaluation of gastroretentive dosage forms of clarithromycin. AAPS PharmSciTech 2008;9:231–7.

Jaimini M, Rana A, Tanwar Y. Formulation and evaluation of famotidine floating tablets. Curr Drug Delivery 2006;4:51–5.

Ali J, Arora S, Ahuja A, Babbar AK, Sharma RK, Khar RK, et al. Formulation and development of the hydrodynamically balanced system for metformin: in vitro and in vivo evaluation. Eur J Pharm Biopharm 2007;67:196–201.

Singhvi G, Singh M. In vitro drug release characterization models. Int J Pharm Stud Res 2011;2:77–84.

Mehta G, Hsiao AY, Ingram M, Luker GD, Takayama S. Opportunities and challenges for use of tumor spheroids as models to test drug delivery and efficacy J Controlled Release 2012;164:192–204.

Costa P, Sousa Lobo JM. Modeling and comparison of dissolution profiles. Eur J Pharm Sci 2001;13:123–33.



How to Cite

PAWAR, R., S. JAGDALE, and D. RANDIVE. “DEVELOPMENT OF FLOATING GASTRORETENTIVE DRUG DELIVERY SYSTEM BASED ON A NOVEL EXCIPIENT FOR METFORMIN HYDROCHLORIDE USING MIXTURE DESIGN”. International Journal of Pharmacy and Pharmaceutical Sciences, vol. 12, no. 10, Oct. 2020, pp. 62-71, doi:10.22159/ijpps.2020v12i10.38678.



Original Article(s)