Polymers in Medicine
2016, vol. 46, nr 2, July-December, p. 117–127
Publication type: original article
Investigation and Optimization of the Effect of Polymers on Drug Release of Norfloxacin from Floating Tablets
1 Shri Bhagwan College of Pharmacy, Aurangabad, India
2 Government College of Pharmacy, Osmanpura, Aurangabad, India
Background. Norfloxacin is fluoroquinolone anti-infective used in the treatment of urinary tract infections, prostatitis, gonorrhea and genital tract infections. It has plasma half life of 3 to 4 h requiring multiple dosing in the treatment. Releaseretarding polymers can be used to modulate the drug release of norfloxacin.
Objectives. The objective of this study was to investigate the effect of release-retarding polymers on the drug release of norfloxacin from floating tablets.
Material and Methods. Norfloxacin was procured as a gift sample from Concept Pharma Ltd. Aurangabad (India) and HPMC K100M was procured as a gift sample from Colorcon Asia Pvt. Ltd., Goa (India). The tablets were prepared by direct compression method and various pharmaceutical parameters were evaluated.
Results. It was observed that all tablet formulations F1–F9 retained the drug release up to 12 h with good floating property but only Batch-F4 complies with the USP dissolution limits with a minimum floating lag time. The drug release kinetics were evaluated by the model-dependent (curve fitting) method using PCP Disso v3 software shows Batch-F4 shows to best fit with Peppas model for which R2 value was 0.9921 and the release exponent value was 0.6892.
Conclusion. The drug release kinetics study indicates that the floating tablets release the drug by diffusion followed by erosion mechanism. Obtained in-vitro drug release data was analyzed by design expert software for drug release at first hour and at 12th h values and found that release the selected independent variables like HPMC K100M and sodium alginate concentration has a significant effect on drug release.
floating drug delivery systems, gastroretentive drug delivery systems, norfloxacin, drug dissolution
- Garg R., Gupta G.D.: Progress in controlled gastroretentive delivery systems. Tropical J. Pharm. Res. 2008, 7(3), 1055–1066.
- Uddin M., Rathi P.B., Siddiqui A.R., Sonawane A.R., Gadade D.D.: Recent development in floating delivery systems for gastric retention of drugs, an overview. Asian J. Biomed. Pharma. Sci. 2011, 1(3), 26–42.
- Goettsch W., Van Pelt W., Nagelkerke N. et al.: Increasing resistance to fluoroquinolones in Escherichia coli from urinary tract infections in the Netherlands. J. Antimicrob. Chemother. 2000, 46(2), 223–228.
- Nix D.E., Wilton J.H., Ronald B., Distlerath L., Williams V.C., Norman A.: Inhibition of norfloxacin absorption by antacids. Antimicrob. Agents Chemother. 1990, 34(3), 432–435.
- Clark D.E.: Rapid calculation of polar molecular surface area and its application to the prediction of transport phenomena. 1. Prediction of intestinal absorption. J. Pharm. Sci. 1999, 88(8), 807–814.
- Block J. Beale J.M.: Wilson and Gisvold’S Textbook of Organic Medicinal and Pharmaceutical Chemistry, London, Lippincott Williams & Wilkins, 2004.
- Shakya R., Thapa P., Saha R.N.: In vitro and in vivo evaluation of gastroretentive floating drug delivery system of ofloxacin. Asian J. Pharm. Sci. 2013, 8(3), 191–198.
- Deshpande A.A., Shah N.H., Rhodes C.T.: Development of a novel controlled-release system for gastric retention. Pharm. Res. 1997,14, 815–819.
- Aulton M.E.: Pharmaceutics, The Science of Dosage Form Design. Edinburgh, Churchill Livingstone 2005, 205–208.
- Madgulkar A., Kadam S., Pokharkar V.: Studies on formulation development of mucoadhesive sustained release itraconazole tablet using response surface methodology. AAPS PharmSciTech 2008,9(3),998–1005.
- Masareddy R., Kokate A., Shah V.: Development of orodispersible tizanidine HCl tablets using spray dried coprocessed exipient bases. Ind. J. Pharm. Sci. 2011, 73(4), 392–396.
- Rao B.S., Seshasayana A., Himasankar K., Raju Y.P., Murthy K.R.: Design and evaluation of ethylene vinyl acetate sintered matrix tablets. Ind. J. Pharm. Sci. 2003, 65(5), 496–502.
- Adedokun M.O., Nkori A.M.: Preliminary investigation of mechanical properties of paracetamol tablets formulated with microcrystalline cellulose binder derived from Saccharum officinarum, L. Asian J. Biomed. Pharma. Sci. 2014, 4(38), 17.
- Jyothi G., Lakshmi P.K.: Comparative evaluation of natural and synthetic superdisintegrants with newer superdisintegrant Kyron T-314. Acta Pharm. Sci. 2011, 5(3), 35–44.
- Srivastava A.K., Ridhurkar D.N., Wadhwa S.: Floating microspheres of cimetidine, formulation, characterization and in vitro evaluation. Acta Pharm. 2005, 55(3), 277.
- Khan K.A.: The concept of dissolution efficiency. J. Pharm. Pharmacol. 1975, 27, 48–49.
- Modi A., Tayade P.: Enhancement of dissolution profile by solid dispersion (kneading) technique. AAPS PharmSciTech 2006, 7(3), E1–E6.
- Shahi S.R., Shinde S.B., Zadbuke N.S., Padalkar A.N.: Formulation developement and evaluation of floating matrix tablet of Verapamil HCl. Asian J. Pharm. 2013, 7(1), 27–35.
- Jasińska-Stroschein M., Kurczewska U., Orszulak-Michalak D.: Errors in reporting on dissolution research, methodological and statistical implications. Pharm. Dev. Tech. 2016, 1–8.
- Yoshida V.M., Granato E., Gremião M.P. et al.: A novel gastroretentive floating system for zidovudine, based on calciumsilicate beads. Afr. J. Pharm. Pharmacol. 2013, 2946–3946.
- Poonuru R.R., Gonugunta C.R.: Bimodal gastroretentive drug delivery systems of lamotrigine, formulation and evaluation. Ind. J. Pharm. Sci. 2014, 76(6), 476–482.
- Acharya S., Patra S., Pani N.R.: Optimization of HPMC and carbopol concentrations in non-effervescent floating tablet through factorial design. Carbohydr. Polym. 2014, 102, 360–368.
- Barse R., Kokare C., Tagalpallewar A.: Influence of hydroxypropylmethylcellulose and poloxamer composite on developed ophthalmic in situ gel, ex vivo and in vivo characterization. J. Drug Deliv. Sci. Tech. 2016, 33, 66–74.
- Nadaf S.J., Mali S.S., Salunkhe S.S., Kamble P.M.: Formulation and evaluation of ciprofloxacin suspension using natural suspending agent. Int. J. Pharm. Sci. Res. 2014, 5(3), 63–70.
- Shiledar R.R., Tagalpallewar A.A., Kokare C.R.: Formulation and in vitro evaluation of xanthan gum-based bilayered mucoadhesive buccal patches of zolmitriptan. Carbohydr. Polym. 2014, 101, 1234–1242.
- Wan Lucy S.C., Heng Paul W.S., Wong L.F.: Relationship between swelling and drug release in a hydrophilic matrix. Drug Dev. Ind. Pharm. 1993; 19(10), 1201–1200.
- Tiwari S.B., Rajabi-Siahboomi A.R.: Applications of complementary polymers in HPMC hydrophilic extended release matrices. Drug Dev. Tech. 2009, 9(7), 20–27.
- Thulluru A., Varma M.M., Setty C.M., Chintamaneni P.K., Samayamanthula S.: Effect of sodium alginate in combination with HPMC K100M in extending the release of metoprolol succinate from its gastro-retentive floating tablets. Ind. J. Pharm. Edu. Res. 2015, 49(4), 293–303.
- Dua K., Ramana M.V., Singh Sara U.V., Himaja M., Agrawal A., Garg V., Pabreja K.: Investigation of enhancement of solubility of norfloxacin β-cyclodextrin in presence of acidic solubilizing additives. Curr Drug Deliv. 2007, 4(1), 21–25.
- Foster K.A., Morgen M., Murri B. et al. Utility of in situ sodium alginate/karaya gum gels to facilitate gastric retention in rodents. Int J. Pharm. 2012, 434(1), 406–412.