DESIGN AND DEVELOPMENT OF LOSARTAN POTASSIUM FLOATING DRUG DELIVERY SYSTEMS
Objective: The current study was projected to prepare a losartan potassium gastroretentive drug delivery system (GRDDS) of floating tablets was planned to enhance the gastric residence time, thus prolong the drug release.
Methods: Effervescent floating matrix tablets of losartan potassium were prepared by direct compression technique using polymers like HPMC k4m, guar gum, and gum karaya, with lubricants magnesium stearate and talc. In the present study, sodium bicarbonate was incorporated as a gas generating agent. Total nine formulations were designed and evaluated for pre-compression parameters known as the angle of repose, bulk density, tapped density, Hausnerâ€™s ratio, compressibility index, and post-compression parameters are uniformity of weight, hardness, and drug content percentage, variability, in vitro buoyancy, dissolution studies, and Fourier transform infrared spectroscopy (FTIR).
Results: An in vitro dissolution study was carried out by using buffer pH 1.2. From in vitro dissolution studies, it has been found that an increase in polymer concentration diminishes the drug release profile. The in vitro drug release percentage from F4-F9 formulations ranged from 60.28%-98.66% at the closing of 12 h and buoyancy found over 12 h.
Conclusion: The in vitro drug release from F1-F3 and F7-F9 followed zero-order, F4 followed Higuchi order, F5 and F6 followed Hixon-Crowell release kinetics. The drug release mechanism was set up to be F1-F8 non-Fickian (anomalous behavior) and F9 having Fickian diffusion type.
2. Bardonnet PL, Faivre V, Pugh WJ, Piffaretti JC, Falson F. Gastro retentive dosage forms: overview and the special case of helicobacter pylori. J Controlled Release 2006;111:1-18.
3. Timmermans J, Moes AJ. How well do floating dosage forms float? Int J Pharm 1990;62:207-16.
4. Streubel A, Siepmann J, Bodmeier R. Floating matrix tablets based on low-density foam powder: effects of formulation and processing parameters on drug release. Eur J Pharm Sci 2003;18:37-45.
5. Nayak AK, Malakar J, Sen KK. Gastroretentive drug delivery technologies: current approaches and future potential. J Pharm Educ Res 2010;1:1-10.
6. Kothari Abhaykumar H, Manish J. Gastroretentive drug delivery system and its approaches: a review. Int J Pharm Res Development 2013;4:7-18.
7. Rouge N, Buri P, Doelker E. Drug absorption sites in the gastrointestinal tract and dosage form for site-specific delivery. Int J Pharm 1996;136:117-39.
8. Fell JT, Whitehead L, Collet H. Prolonged gastric retention using floating dosage forms. Pharm Technol 2000;24:82-90.
9. Streubel A, Siepmann J, Bodmeier R. Gastroretentive drug delivery system. Expert Opin Drug Delivery 2006;3:217-33.
10. Bramhankar DM, Jaiswal SB. Controlled release medication. Jain MK. editor. Design of controlled drug delivery systems. 1st ed. Delhi: Vallabh Prakashan; 2002. p. 335-7.
11. Minami H, McCallum RW. The physiology and pathophysiology of gastric emptying in humans. Gastroenterology 1984; 86:1592-610.
12. Patel VF, Patel NM, Yeole PG. Studies on the formulation and evaluation of ranitidine floating tablets. Indian J Pharm Sci 2005;67:703-9.
13. Banker GS, Rhodes CT. Target-oriented drug delivery systems and packaging of pharmaceutical dosage forms. Banker GS, Rhodes CT. editors. 3rd ed. New York: Marcel Dekker; 1996. p. 678-721.
14. Samyuktha M, Vasanth PM, Suresh K, Ramesh T, Ramesh M. Formulation and evaluation of gastroretentive floating tablets of losartan potassium. Int J Biopharm 2013;4:18-26.
15. Sandhyarani S, Ramesh A, Krishna KVM. Formulation and evaluation of stable floating tablet of losartan potassium for oral controlled drug delivery system. J Pharm Sci Res 2015;7:946-51.
16. Audumbar DM, Ritesh SB. Development and evaluation of gastroretentive floating tablets of a quinapril HCL by direct compression technique. Int J Pharm Pharm Sci 2017;9:35-46.
17. Ahmed AA, Wedad KA, Al-saady FA. Formulation and evaluation of prochlorperazine maleate sustained floating release tablet. Int J Pharm Pharm Sci 2017;9:89-98.
18. Manojkumar SP, Vidyasagar G, Patil VB. Formulation, optimization and evaluation of floating tablets clarithromycin. Int J Pharm Pharm Sci 2015;7:320-6.
19. Radhika PR, Nishala N, Kiruthika M, Iswarya S. Design and evaluation of intragastric buoyant tablets of venlafaxine hydrochloride. Asian J Pharm Clin Res 2017;10:166-70.
20. Sreejan M, Jayasri K, Kancherla RA, Lakshmi KK. Alginate-based gastro-retentive raft forming tablets for enhanced bioavailability of tinidazole. Int J Appl Pharm 2017;9:16-21.
21. Bharat WT, Umesh TJ, Shruti GP, Vijay RP. Formulation and in vitro evaluation of floating tablets of cefpodoxime proxetil. Int J Curr Pharm Res 2017;9:18-22.
22. Shah HP, Prajapati ST, Patel CN. Gastroretentive drug delivery systems: from conception to commercial success. J Crit Rev 2017;4:10-21.