Preparation and Evaluation of a Gas Formation-based Multiple-Unit Gastro-Retentive Floating Delivery System of Dipyridamole

DOI:

https://doi.org/10.37285/ijpsn.2012.5.1.3

Authors

  • Y. Madhusudan Rao
  • Katakam V V
  • S Reddy
  • J M Somagoni
  • P K Panakanti
  • Rallabandi R C

Abstract

The aim of this study was to prepare mini tablets to be filled into a capsule that is designed to float on the gastric contents based on gas formation technique. The drug-containing core mini-tablets were prepared by wet granulation method followed by a coating of the core units with seal coating, an effervescent layer and a gas-entrapping polymeric membrane (Eudragit RS30D, RL30D). Dipyridamole, which is predominantly absorbed in the upper part of GI tract and unabsorbed/insoluble at the lower intestine, was used as a model drug. The effect of the preparative parameters like amount of the effervescent agent layered onto the seal coated units, type and coating level of the gas-entrapping polymeric membrane, floating ability and drug release properties of the multiple-unit FDDS were evaluated. The formulations were evaluated for pharmacopoeial quality control tests. Physical parameters were found to be within the acceptable limits. The system using Eudragit® RL30D as a gas-entrapping polymeric membrane exhibited floating properties. The time to float decreased as amount of the effervescent agent increased and coating level of gas-entrapping polymeric membrane decreased. The optimum system exhibited complete floating within 3 minutes and maintained that buoyancy over a period of 8 hours. The drug release was sustained and linear with the square root of time. Increasing the coating level of the gas-entrapping polymeric membrane decreased drug release. Both the rapid-floating and sustained-release properties were achieved in the multiple-unit floating delivery system developed in this study. The in vivo gastric residence time was examined by radiograms and it was found that the units remained in the stomach for about 6 hours. The analysis of the dissolution data after storage at 40°C and 75% RH for 6 months showed no significant change indicating good stability.

Downloads

Download data is not yet available.

Metrics

Metrics Loading ...

Keywords:

Floating delivery system, mini-tablets, effervescent agent, polymeric membrane, controlled release

Downloads

Published

2012-05-31

How to Cite

1.
Rao YM, V V K, Reddy S, Somagoni JM, Panakanti PK, R C R. Preparation and Evaluation of a Gas Formation-based Multiple-Unit Gastro-Retentive Floating Delivery System of Dipyridamole . Scopus Indexed [Internet]. 2012 May 31 [cited 2024 Dec. 22];5(1):1607-16. Available from: https://ijpsnonline.com/index.php/ijpsn/article/view/561

Issue

Vol. 5 No. 1 (2012): April-June 2012

Section

Research Articles
Crossref
Scopus
Google Scholar
Europe PMC

References

Atyabi F, Sharma HL, Mohammad HAH, and Fell JT (1996). Controlled drug release from coated floating ion exchange resin beads. J Contr Release 42:25–28.

Bechgaard H and Ladefoged K (1978). Distribution of pellets in the gastrointestinal tract. The influence on transit time exerted by the density or diameter of pellets. J Pharm Pharmacol 30:690–692.

Chakrabarti S, Freedman JE (2008). Dipyridamole, cerebrovascular disease, and the vasculature. Vascul Pharmacol 48:143-9.

Choi BY, Park HJ, Hwang HS, and Park JB (2002). Preparation of alginate beads for floating drug delivery system: Effects of CO2 gas-forming agents. Int J Pharm 239:81–91.

Costa P and Sousa Lobo JM (2001). Modelling and comparison of dissolution profiles. Eur J Pharm Sci 13:123–133.

Kong SY, Lin R, and Chen GM (2003). Preparation of Dipyridamole Floating Tablets in Stomach. Chin J Pharm 34:395-397.

Malan CEP, Villers MM, and Lotter AP (1997). Application of differential scanning calorimetry and high performance liquid chromatography to determine the effects of mixture composition and preparation during the evaluation of niclosamide-excipient compatibility. J Pharm Biomed Anal 15:549–557.

Mathews BR (1999). Regulatory aspects of stability testing in Europe. Drug Dev Ind Pharm 25:831–856.

Moore JW and Flanner HH (1996). Mathematical comparison of curves with an emphasis on in-vitro dissolution profiles. Pharm Technol 20:64–74.

Mura P, Manderioli A, Bramanti G, Furlanetto S, and Pinzauti S (1995). Utilization of differential scanning calorimetry as a screening technique to determine the compatibility of ketoprofen with excipients. Int J Pharm 119:71–79.

Patel VF and Patel NM (2007). Statistical Evaluation of Influence of Xanthan Gum and Guar Gum Blends on Dipyridamole Release from Floating Matrix Tablets. Drug Development and Industrial Pharmacy. Vol. 33, No. 3, Pages 327-334.

Ritger PL and Peppas NA (1987). A simple equation for description of solute release. I. Fickian and non-Fickian release from nonswellable devices in the form of slabs, spheres, cylinders or discs. J Contr Release 5:23–36.

Sato Y, Kawashima Y, Takeuchi H, and Yamamoto H (2003). Physicochemical properties to determine the buoyancy of hollow microspheres (microballoons) prepared by the emulsion solvent diffusion method. Eur J Pharm Biopharm 55:297–304.

Soppimath KS, Kulkarni AR, Rudzinski WE, and Aminabhavi TM (2001). Microspheres as floating drug delivery system to increase the gastric residence of drugs. Drug Metab Rev 33:149-160.

Streubel A, Siepmann J, and Bodmeier R (2002). Floating microparticles based on low density foam powder. Int J Pharm 241:279–292.

Streubel A, Siepmann J, and Bodmeier R (2003). Multiple unit gastroretentive drug delivery systems: A new preparation method for low density microparticles. J Microencapsul 20:329–347.

Talukder R and Fassihi R (2004). Gastroretentive delivery systems: Hollow beads. Drug Dev Ind Pharm 30:405–412.

Vervaet C, Baert L, and Remon JJ (1995). Extrusion–spheronization: A literature review. Int J Pharm 116:131–146.