Development and In Vitro – In Vivo Evaluation of Gastro-retentive Floating Tablets Containing Repaglinide

DOI:

https://doi.org/10.37285/ijpsn.2018.11.2.4

Authors

  • Poornima P
  • Abbulu K
  • Mukkanti K

Abstract

The present investigation concerns the development of the repaglinide floating matrix tablets, which after oral administration are designed to prolong the gastric residence time, increase the drug bioavailability and diminish the side effects of irritating drugs. FTIR studies revealed that there is no interaction between the drug and polymers used for the formulation. 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 physico chemical properties, floating lag time (36 sec) and total floating time (>24 h). From in vitro dissolution studies, the optimized formulation F21 showed drug release of 98.92±5.19% within 24h whereas 95.09±5.01% of the drug was released from the marketed product within 1h. The major mechanism of drug release follows zero order kinetics and non-Fickian transport by coupled diffusion and erosion. In vivo experiments supported the expectations in prolonging the gastric residence time in the fasted state in beagle dogs. The mean gastric residence time for the tested tablets was 270 min±60. This result is encouraging, because a longer gastric residence time is an important condition for higher bioavailability of the drugs included in the prolonged or controlled release dosage forms.

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Keywords:

Repaglinide, Floating tablets, Drug delivery., HPMC K1500 PH PRM

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Published

2018-03-31

How to Cite

1.
P P, K A, K M. Development and In Vitro – In Vivo Evaluation of Gastro-retentive Floating Tablets Containing Repaglinide. Scopus Indexed [Internet]. 2018 Mar. 31 [cited 2024 Nov. 19];11(2):4026-3. Available from: https://ijpsnonline.com/index.php/ijpsn/article/view/360

Issue

Vol. 11 No. 2 (2018): March-April 2018

Section

Research Articles
Crossref
Scopus
Google Scholar
Europe PMC

References

Baumgartner S, Julijana Kristl, Franc Vrecer, Polona Vodopivec, and Bojan Zorko (2000). Optimization of floating matrix tablets and evaluation of their gastric residence time. International Journal of Pharmaceutics 195:125-135.
Culy C and Jarvis B (2001). Repaglinide a review of its therapeutic use in type 2 diabetes mellitus. Drugs 61: 1625-1660.
Desai and S. Bolton (1993). A Floating Controlled Release Drug Delivery System In vitro – In vivo Evaluation. Pharma. Res 10 (9): 1321-325.
Deshpande, C.T. Rhodes and N.H. Shah (1996). Controlled release drug delivery system for prolonged gastric residence an overview. Drug Dev.Ind. Pharm 22: 531- 539.
Fell WJT and Collett JH (1996). Development of a Gastroretentive Dosage Form. Eur. J. Pharma. Sci. 4(1): 182.
Hwang SK, Park H and Park K (1998). Gastric retentive drug delivery systems.Crit. Rev. Ther.Drug Carrier Syst 15: 243-284.
Janssen M, Ufuk Tan Timur and Nina Woike (2016). Celecoxib-loaded PEA microspheres as an auto regulatory drug-delivery system after intra-articular injection. Journal of Controlled Release 244: 30-40.
Li S, Lin S, Chien TW, Daggy BP and Mirchandani HL (2001). Statistical optimization of gastric floating system for oral controlled delivery of calcium. AAPS Pharm Sci Tech. 2: 783-793.
Małgorzata W, Marcin Z and Aleksandra A (2016). Tasting cetirizine-based microspheres with an electronic tongue. Sensors and Actuators B Chemical 238: 1190-1198.
Martindale (1996). The Complete Drug Reference 35: 766-779.
Mojaverian PH, Vlasses, P. E. Kellner and M. Rocci (1988). Effects of gender, posture and age on gastric residence time of an indigestible solid pharmaceutical considerations. Pharm. Res 10: 639-644.
Nasrin N, Muhammad Asaduzzaman, Rumana Mowla, Farhana Rizwan and Ashiqul Alam (2008). A Comparative Study of Physical Parameters of Selected Ketorolac tromethamine tablets available in the Pharma Market of Bangladesh. Journal of Applied Pharmaceutial Science 1(08): 101-103.
Penners G, Lustig K and Jorg PVG inventors (1997). Expandable pharmaceutical forms. US patent 5: 651-985.
Peppas NA (1985) Analysis of Fickian and non-Fickian drug release from polymers. Pharm Acta Helv 60: 110-111.
Phuapradit W (1989). Influence of Tablet Buoyancy on Oral Absorption of Sustained Release Acetaminophen Matrix Tablets. Jamaica, NY. St John’s University.
Phuapradit W and Bolton S (1991). Influence of tablet density on oral absorption of sustained release acetaminophen matrix tablets. Drug Dev Ind Pharm 17: 1097-1107.
Rama Rao T, Bala Krishna K, Hussain M A, Anjum M and Azizurrahman M. (2014). Formulation and Evaluation of Gastroretentive Floating Tablets of Quetiapine Fumarate. RJPBCS. 5(5): 0975-8585.
Siepmann J, Kranz H, Bodmeier R and Peppas NA (1999) HPMC-matrices for controlled drug delivery a new model combining diffusion, swelling, and dissolution mechanisms and predicting the release kinetics. Pharm Res 16: 1748-1756.
Singh K, Kumar A, Langyan N and Ahuja M (2009). Evaluation of mimosa pudica seed mucilage as sustained-release excipient. AAPS Pharm Sci Tech. 10: 1121-1127.
Tyagi LK and Kori ML (2014). Stability Study and In-vivo Evaluation of Lornoxicam Loaded Ethyl Cellulose Microspheres. International Journal of Pharmaceutical Sciences and Drug Research 6(1): 26-30.