The aim of this research was to formulate effervescent floating drug delivery systems of theophylline using different release retarding polymers such as ethyl cellulose, Eudragit® L100, xanthan gum and polyethylene oxide (PEO) N12K. Sodium bicarbonate was used as a gas generating agent. Direct compression was used to formulate floating tablets and the tablets were evaluated for their physicochemical and dissolution characteristics. PEO based formulations produced better drug release properties than other formulations. Hence, it was further optimized by central composite design. Further subjects of research were the effect of formulation variables on floating lag time and the percentage of drug released at the seventh hour (D7h). The optimum quantities of PEO and sodium bicarbonate, which had the highest desirability close to 1.0, were chosen as the statistically optimized formulation. No interaction was found between theophylline and PEO by Fourier Transformation Infrared spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC) studies.
If the inline PDF is not rendering correctly, you can download the PDF file here.
1. M. V. Srikanth S. A. Sunil N. S. Rao B. J. Ram and K. V. R. Murthy Statistical design and evaluation of a propranolol HCl gastric floating tablet Acta Pharm. Sinica B.2 (2012) 60–69; DOI: http://dx.doi.org/10.1016/j.apsb.2011.12.008.
2. A. Nanda M. Ola R. Bhaskar C. K. Sharma and S. Nayak Formulation and evaluation of an effervescent gastroretentive drug delivery system Pharm. Tech. 10 (2010) 60–71; DOI: 10.4103/0253-7613.77344.
3. S. Arora J. Ali A. Ahuja R. K. Khar and S. Baboota Floating drug delivery systems: a review. AAPS PharmSciTech. 6 (2005) E372-90; DOI: 10.1208/pt060347.
4. V. S. Meka B. J. Ram S. A. Sunil N. S. Rao and K. Ramanamurthy Gastroretentive drug delivery systems: Novel approaches and its evaluation – a review Int. J. Pharm. Rev. Res.10 (2011) 203–216.
5. V. S. Meka H. W. L. Vanitha S. R. Dharmalingham R. Sheshala and A. Gorajana Preparation and in vitro characterization of non-effervescent floating drug delivery system of poorly soluble drug carvedilol phosphate Acta Pharm. 64 (2014) 485–494. DOI: 10.2478/acph-2014-0038.
6. B. N. Singh and K. H. Kim Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention J. Control. Release63 (2000) 235–259; DOI: 10.1016/S0168-3659(99)00204-7.
7. A. Chandel K. Chauhan B. Parashar H. Kumar and S. Arora Floating drug delivery systems: a better approach Int. Current. Pharm. J. 1 (2012) 110–118; DOI: http://dx.doi.org/10.3329/icpj.v1i5.10283.
8. S. Desai and S. Bolton A floating controlled release drug delivery system: in vitro-in vivo evaluation Pharm. Res. 10 (1993) 1321–1325; DOI: 10.1023/A:1018921830385.
9. J. Dubeh and N. Verma Floating Drug Delivery System: A Review Int. J. Pharm. Sci. Res.4 (2013) 2893–2899; DOI: 10.13040/IJPSR.0975-8232.4(8).2893-99.
10. P. J. Barnes Theophylline Am. J. Respir. Crit. Care Med. 188 (2013) 901–906; DOI: 10.1164/rccm.201302-0388PP.
11. Theophylline http://www.drugs.com/pro/theophylline.html; access date 15/10/2014.
12. V. S. Meka and V. R. M. Kolapalli Formulation of gastroretentive floating drug delivery system using hydrophilic polymers and its in vitro characterization Braz. J. Pharm. Sci. 50 (2014) 431–439; DOI: http://dx.doi.org/10.1590/S1984-82502014000200023.
13. V. S. Meka S. Pillai S. R. Dharmalingham R. Sheshala and A. Gorajana Preparation and in vitro characterization of a non-effervescent floating drug delivery system for poorly soluble drug glipizide Acta Pol. Pharm. Drug Res.72 (2015) 193–204.
14. Evonik Industries. EUDRAGIT® L100 http://eudragit.evonik.com/product/eudragit/en/prod-uctsservices/eudragit-products/enteric-formulations/l-100/pages/default.aspx; access date 24/11/2015.
15. A. Becker F. Katzen and L. Lelpi Xanthan gum biosynthesis and application: a biochemical/genetic perspective Appl. Microbiol. Biotechnol. 50 (1998) 145–152; DOI: 10.1007/s002530051269.
16. S. Kumar R. K. Sahu S. Sharma and R. Jangde Design and evaluation of an oral floating matrix tablet of salbutamol sulphate Trop. J. Pharm. Res. 11 (2012) 569–576; DOI: http://dx.doi.org/10.4314/tjpr.v11i4.7.
17. B. Y. Choia H. J. Park S. J. Hwangb and J. B. Parkc Preparation of alginate beads for floating drug delivery system: Effects of CO2 gas-forming agents Int. J. Pharm. 239 (2002) 81–91; DOI: 10.1016/S0378-5173(02)00054-6.
18. V. S. Meka N. S. Rao S. A. Sunil B. J. Ram and K. V. R. Murthy Statistical optimization of a novel excipient (CMEC) based gastroretentive floating tablet of propranolol HCl and its in vivo buoyancy characterization in healthy human volunteers DARU J. Pharm. Sci. 20 (2012) 1–12; DOI: 10.1186/1560-8115-20-4.
19. M. Grassi and G. Grassi Mathematical modeling and controlled drug delivery: matrix systems Curr. Drug. Deliv.2 (2005) 97–116; DOI: 10.2174/1567201052772906.
20. F. Khan M. S. M. Razzak and M. S. Reza Preparation and in vitro evaluation of theophylline loaded gastroretentive floating tablets of METHOCEL K4M Dhaka Univ. J. Pharm. Sci. 7 (2008) 65–69; DOI: 10.3329/dujps.v7i1.1220.
21. C. Narendra M. S. Srinath and A. Moin The study on the effect of formulation variables on in vitro floating time and the release properties of floating drug delivery system by a statistical optimization technique Chem. Ind. Chem. Engin. Quart.14 (2008) 17–26; DOI: 10.2298/ciceq0801017n.
22. K. K. Satish K. P. Santhosh K. N. Nishanth and B. P. Bharghav Formulation and in vitro evaluation of ofloxacin tablets J. Pharm. Res. 4 (2011) 3007.
23. R. H. Myers D. C. Montgomery and C. M. A. Cook Response Surface Methodology: Process and Product Optimization Using Designed Experiments 3rd ed. Wiley New York 2009 pp. 15–29.
24. V. S. Meka N. S. Rao S. A. Sunil B. J. Ram and K. V. R. Murthy Thermal sintering: a novel technique used in the design optimization and biopharmaceutical evaluation of propranolol HCl gastric floating tablets Drug. Dev. Ind. Pharm.40 (2014) 33–45; DOI: 10.3109/03639045.2012.744416.
25. United States Pharmacopeia 29 NF 24 Pharmacopeial Forum. 30 (2006) p. 1474.
26. United States Pharmacopeia 29 NF 25 Tablet friability. Chapter 1216. USP30–NF25 Pharmacopeial Forum. 31 (2007) p. 1735.
27. M. Yasir M. Asif A. Bhattacharya and M. Bajpai Development and evaluation of gastroretentive drug delivery system for theophylline using psyllium husk Int. J. Chem. Tech. Res. 2 (2010) 792–799.
28. C. Rajveer B. S. Rathinaraj M. Fareedullah G. S. Bangale and G. Shinde Design and evaluation of ketorolac tromethamine sustained release matrix tablets Deccan. J. Pharm. Cosmet.1 (2010) 57–71.