FORMULATION AND EVALUATION OF FLOATING ORAL IN SITU GEL OF DILTIAZEM HYDROCHLORIDE
Objective: The objective of the present study was to formulate and evaluate the floating in-situ gelling system of diltiazem hydrochloride.
Methods: Sodium alginate based diltiazem hydrochloride floating in situ gelling systems were prepared by dissolving hydroxyl propyl methyl cellulose (HPMC) in 25% of water, to which calcium carbonate and diltiazem hydrochloride were added with stirring to form, a proper and a homogenous dispersion of diltiazem hydrochloride. Meanwhile, 30% of water was heated to 60 ËšC on a hot plate to dissolve sodium alginate and cooled to 40 ËšC. The resulting solution was added to HPMC solution and mixed well. To 5% of water at 60 ËšC, sodium methyl paraben was added and dissolved and cooled to 40 ËšC and was added to the above mixture and mixed well. The volume was adjusted finally to 100% with distilled water. Prepared formulae were evaluated for physicochemical properties, drug content, pH, in vitro gelling capacity, in vitro buoyancy, viscosity, water uptake and in vitro drug release.
Results: Formulation variables such as type and concentration of viscosity enhancing polymer (sodium alginate) and HPMC affected the formulation viscosity, gelling properties, floating behavior, and in vitro drug release. Formulation F5 and F6 showed the floating time of 5 min and more than 20 h respectively. A significant decrease in the rate and extent of the drug release was observed with the increase in polymer concentration in in-situ gelling preparation. Formulation F4, F5, F6 were shown to have extended drug release until the end of 7 h.
Conclusion: The prepared in situ gelling formulations of diltiazem hydrochloride could float in the gastric conditions and released the drug in a sustained manner. The present formulation was non-irritant, easy to administer along with good retention properties, better patient compliant and with greater efficacy of the drug.
2. Pande SD, Vaidya KP, Gulhane KP. Floating drug delivery system (fdds): a new way for oral drug delivery system. Int J Pharm Clin Sci 2013;3:1-13.
3. Nidhi D. In-situ gel: a novel approach of gastro retentive drug delivery. Asian J Pharm Sci Res 2013;3:1-14.
4. Plourde F, Motulsky A, Couffin-Hoarau AC, Hoarau D, Ong H, Lerour JC. The first report on the efficacy of l-alanine based In-situ-forming implants foe the long-term parenteral delivery of drugs. J Controlled Release 2005;108:433-41.
5. Khan AD, Meenakshi B. Floating drug delivery system: an overview. Int J PharmTech Res 2010;2:2497-505.
6. Miyazaki S, Endo K, Kawasaki N, Kubo W, Watanale H, Attwood D. Oral sustained delivery of paracetamol from in situ gelling xyloglucan formulations. Drug Dev Ind Pharm 2003;29:113-9.
7. Modi SA, Gaikwad PD, Bankar VH, Pawar SP. Sustained release drug delivery system: a review. Int J Pharm Res Dev 2011;2:147-60.
8. Moin Afrasim, Shiva kumar HG. Formulation of sustained release Diltiazem matrix tablet using hydrophilic gum blends. Top J Pharm Res 2010;9:283-91.
9. Nayak Amitkumar, Maji Ruma, Das Biswarup. Gastroretentive drug delivery system: a review. Asian J Pharm Clin Res 2010;3:1-10.
10. Madan M, Bajaj A, Lewis S, Udapa N, Baig JA. In-situ forming polymeric drug delivery. Indian J Pharm Sci 2009;71:242-51.
11. Moin A, Reddy MM, Reddy DJ, Shivakumar HG. Formulation of sustained release matrix tablet using chitosan/ghatti. gum. poly electrode complex Sch. Res Lib 2011;3:119-28.
12. Thomas LM. Formulation and evaluation of floating oral in-situ gel of metronidazole. Int J Pharm Pharm Sci 2014;6:265-9.
13. Hasan MJ, Kamal BA. Formulation and evaluation of ranitidine hydrochloride are floating In situ gel. Int J Pharm Pharm Sci 2014;6(Suppl 2):401-5.
14. Shivaraju, Parthiban S, Senthilkumar SK. Preparation and evaluation of ornidazole in situ gelling system for gastro retentive drug delivery. Int J Pharm 2013;3:62-9.
15. Al-Mamun MA, Rahman MR, Biswas S, Kundu SK, Rayhan J. Formulation and bioequivalence evaluation of an extended release solid drug delivery system for metronidazole using using eudragit nm30d and methocel premium K4m as retardant material. Am J Adv Drug Delivery 2014;2:39-51.
16. Patel DM, Patel CN. Formulation and evaluation of floating oral in-situ gelling system of amoxicillin. ISRN Pharm 2011;1:1-8.
17. Patel JK, Chavda JR, Modasiya Mk. Floating in-situ gel based on alginate as a carrier for stomach specific drug delivery of famotidine. Int J Pharm Sci Nanotech 2010;3:1092-104.
18. Choi BY, Park HJ, Hwang SJ, Park JB. Preparation of alginate boads for floating drug delivery system: effects of CO2 gas-forming agents. Int J Pharm 2002;239:81-91.
19. Google J, Vandrbist F, Amighi K. Development and evaluation of new multiple-unit levodopa sustainedâ€“release floating dosage forms. Int J Pharm 2007;334:35-41.
20. Rajinikanth PS, Mishra B. Floating in-situ gelling system for stomach site-specific delivery of clarithromycin to eradicate Helicobacter pyroli. J Controlled Release 2008;125:33-41.