GASTRO-FLOATING TABLETS OF REPAGLINIDE: PREPARATION AND IN VIVO EVALUATION
DOI:
https://doi.org/10.22159/ajpcr.2018.v11i7.25776Keywords:
Repaglinide, Floating tablets, Hydroxypropyl methylcellulose K1500 PH PRM, Diabetes mellitus, Bioavailability studiesAbstract
Objective: Current research concerns the expansion of repaglinide matrix floating tablets, which are designed to prolong the gastric residence time, increase the drug bioavailability, and diminish the side effects.
Methods: Different formulations of repaglinide floating tablets were prepared with different grades of hydroxypropyl methylcellulose (HPMC) and other agents. Evaluation parameters and in vivo bioavailability studies were conducted in the suitable model.
Results: Among all the formulations, F21 containing HPMC K1500 PH PRM, Polyox WSR 303, and sodium bicarbonate, as gas generating agent was selected as optimized formulation based on physicochemical properties, floating lag time (36 s), and total floating time (>24 h). From in vitro dissolution studies, the optimized formulation F21 showed drug release of 98.92±5.19% within 24 h whereas 95.09±5.01% of the drug was released from the marketed product within 1 h.
Conclusion: From in vitro and in vivo bioavailability studies repaglinide floating tablets expected to give a new choice for safe, economical, and increased bioavailability for effective management of diabetes mellitus.
Downloads
References
Deshpande AA, Rhodes CT, Shah NH. Controlled release drug delivery system for prolonged gastric residence an overview. Drug Dev Ind Pharm 1996;22:531-9.
Hibaezzathamed, Kamal BA. Preparation and in-vitro evaluation of desloratadine floating tablet. Int J Pharm Pharm Sci 2015;6:154-9.
Whiteheadz L, Fell JT, Collett JH. Development of a gastroretentive dosage form. Eur J Pharma Sci 1996;4:182.
Mojaverian P, Vlasses PH, Kellner PE, Rocci M. Effects of gender, posture and age on gastric residence time of an indigestible solid pharmaceutical considerations. Pharm Res 1988;10:639-44.
Hwang SK, Park H, Park K. Gastric retentive drug delivery systems.Crit Rev Ther Drug Carrier Syst 1998;15:243-84.
Siepmann J, Kranz H, Bodmeier R, Peppas NA. HPMC-matrices for controlled drug delivery a new model combining diffusion, swelling, and dissolution mechanisms and predicting the release kinetics. Pharm Res 1999;16:1748-56.
Chokshi MM, Gupta MM, Gupta M. Formulation development and evaluation of gastroretentive Floating tablet of Ciprofloxacin Hydrochloride. Int J Pharm Pharm Sci 2016;8:148-52.
Desai S, Bolton S. A floating controlled release drug delivery system in vitro-in vivo evaluation. Pharma Res 1993;10:1321-5.
Culy C, Jarvis B. Repaglinide a review of its therapeutic use in type 2 diabetes mellitus. Drugs 2001;61:1625-60.
Li S, Lin S, Chien TW, Daggy BP, Mirchandani HL. Statistical optimization of gastric floating system for oral controlled delivery of calcium. AAPS Pharm Sci Tech 2001;2:783-93.
Martindale. The Complete Drug Reference 1996;35:766-79.
Rao TR, Krishna KB, Hussain MA, Anjum M, Rahman MA. Formulation and evaluation of gastroretentive floating tablets of quetiapine fumarate. Res J Pharm Biol Chem Sci 2014;5:975-8585.
Peppas NA. Analysis of fickian and non-fickian drug release from polymers. Pharm Acta Helv 1985;60:110-1.
Nasrin N, Zaman MA, Mowla R, Rizwan F, Alam A. A comparative study of physical parameters of selected ketorolac tromethamine tablets available in the pharma market of Bangladesh. J Appl Pharm Sci 2008;1:101-3.
Penners G, Lustig K, Jorg PV. Inventors. Expandable Pharmaceutical Forms. US Patent No. 5. 1997. p. 651-985.
Phuapradit W, Bolton S. Influence of tablet density on oral absorption of sustained release acetaminophen matrix tablets. Drug Dev Ind Pharm 1991;17:1097-107.
Phuapradit W. Influence of tablet buoyancy on oral absorption of sustained release acetaminophen matrix tablets. Jamaica, NY: St John’s University; 1989.
Tyagi LK, Kori ML. Stability study and in-vivo evaluation of lornoxicam loaded ethyl cellulose microspheres. Int J Pharm Sci Drug Res 2014;6:26-30.
Kadivar A, Kamalidehghan B, Javar HA, Davoudi ET, Zaharuddin ND, Sabeti B, et al. Formulation and In vitro, in vivo evaluation of effervescent floating sustained-release imatinib mesylate tablet. PLoS One 2015;10:e0126874.
Published
How to Cite
Issue
Section
The publication is licensed under CC By and is open access. Copyright is with author and allowed to retain publishing rights without restrictions.