Development And Characterization Of Gastroretentive Floating Drug Famotidine

Authors

  • Rakhi Thareja
  • Yogesh Tiwari
  • Lokesh Premchand Kothari
  • Jeevanandham Somasundaram
  • Yash Srivastav
  • Dinesh Prabhakar Borkar
  • Ajay Chouhan
  • Ritesh Kumar

Keywords:

Famotidine, microballoons, gastroretentive, Korsmeyer-Peppas, HPMC K4M, peptic ulcer.

Abstract

In this study, gastroretentive famotidine microballoons were designed and studied with the purpose of improving the treatment of peptic ulcers by extending the duration of stomach retention and regulating the release of the medicine. With a systematic modification in polymer-drug ratios ranging from 1:1 to 1:3, and stirring speeds ranging from 900 to 1500 revolutions per minute, nine different formulations (F1-F9) were created with HPMC K4M through the process of emulsion solvent diffusion. Excellent micromeritic qualities were demonstrated by the microballoons, as evidenced by appropriate flow characteristics (angle of repose: 22.14°-27.19%; Carr's index: 7.93-13.11%) and sustained buoyancy (>12 hours, 64.17-83.21%), all of which are essential for stomach retention. In order to ensure efficient drug loading, a high drug encapsulation efficiency (63.47-70.34%) was utilised. While FTIR and DSC tests demonstrated that there were no interactions between the medication and the excipient, scanning electron microscopy (SEM) revealed porous spherical structures that made flotation easier. In vitro release experiments demonstrated that the kinetics of the formulation were dependent on the formulation. The formulations F1, F4-F5, and F7-F9 adhered to the Korsmeyer-Peppas model, while F2 and F6 adhered to the Higuchi kinetics. F3 displayed optimal zero-order release (R2=0.9954). Through the maintenance of prolonged therapeutic drug levels in the stomach, this gastroretentive system is able to successfully address the pharmacokinetic limitations of famotidine, particularly its short elimination half-life (2.5-4 hours). Famotidine's therapeutic potential for acid-related illnesses is considerably enhanced by the combination of extended buoyancy and controlled release profile. This combination has the potential to improve treatment efficacy while simultaneously reducing the frequency of dose to minimise adverse effects. Based on these data, it appears that microballoons based on HPMC K4M could be a promising method for the targeted delivery of famotidine to the stomach

Downloads

Download data is not yet available.

References

Chawla, G., Gupta, P., Koradia, V., & Bansal, A. K. (2003). Gastroretention: A means to address regional variability in intestinal drug absorption. Pharmaceutical Technology, 27(3), 50-68.

Deshpande, A. A., Shah, N. H., Rhodes, C. T., & Malick, W. (1997). Development of a novel controlled-release system for gastric retention. Pharmaceutical Research, 14(6), 815-819. https://doi.org/10.1023/A:1012100421849

Garg, S., & Sharma, S. (2003). Gastroretentive drug delivery systems. Business Briefing: Pharmatech, 5(1), 160-166.

Gohel, M. C., & Mehta, P. R. (2004). Formulation and optimization of controlled-release microballoons of diclofenac sodium. Drug Development and Industrial Pharmacy, 30(3), 307-312. https://doi.org/10.1081/DDC-120030930

Hoffman, A., Stepensky, D., Lavy, E., Eyal, S., Klausner, E., & Friedman, M. (2004). Pharmacokinetic and pharmacodynamic aspects of gastroretentive dosage forms. International Journal of Pharmaceutics, 277(1-2), 141-153. https://doi.org/10.1016/j.ijpharm.2003.09.047

Jain, S. K., Awasthi, A. M., Jain, N. K., & Agrawal, G. P. (2005). Calcium silicate-based microspheres of repaglinide for gastroretentive floating drug delivery: Preparation and in vitro characterization. Journal of Controlled Release, 107(2), 300-309. https://doi.org/10.1016/j.jconrel.2005.06.019

Klausner, E. A., Lavy, E., Friedman, M., & Hoffman, A. (2003). Expandable gastroretentive dosage forms. Journal of Controlled Release, 90(2), 143-162. https://doi.org/10.1016/S0168-3659(03)00203-7

Korsmeyer, R. W., Gurny, R., Doelker, E., Buri, P., & Peppas, N. A. (1983). Mechanisms of solute release from porous hydrophilic polymers. International Journal of Pharmaceutics, 15(1), 25-35. https://doi.org/10.1016/0378-5173(83)90064-9

Lachman, L., Lieberman, H. A., & Kanig, J. L. (2009). The theory and practice of industrial pharmacy (4th ed.). CBS Publishers & Distributors.

Martin, A. (1999). Physical pharmacy (4th ed.). Lippincott Williams & Wilkins.

Merck & Co. (1996). The Merck Index (12th ed.). Merck & Co., Inc.

Mojaverian, P., Vlasses, P. H., Kellner, P. E., & Rocci, M. L. (1988). Effects of gender, posture, and age on gastric residence time of an indigestible solid: Pharmaceutical considerations. Pharmaceutical Research, 5(10), 639-644. https://doi.org/10.1023/A:1015928702898

Patel, A., Modasiya, M., Shah, D., & Patel, V. (2009). Development and in vivo floating behavior of verapamil HCl intragastric floating tablets. AAPS PharmSciTech, 10(1), 310-315. https://doi.org/10.1208/s12249-009-9210-9

Peppas, N. A., & Sahlin, J. J. (1989). A simple equation for the description of solute release. III. Coupling of diffusion and relaxation. International Journal of Pharmaceutics, 57(2), 169-172. https://doi.org/10.1016/0378-5173(89)90306-2

Rouge, N., Buri, P., & Doelker, E. (1996). Drug absorption sites in the gastrointestinal tract and dosage forms for site-specific delivery. International Journal of Pharmaceutics, 136(1-2), 117-139. https://doi.org/10.1016/0378-5173(96)85200-8

Singh, B. N., & Kim, K. H. (2000). Floating drug delivery systems: An approach to oral controlled drug delivery via gastric retention. Journal of Controlled Release, 63(3), 235-259. https://doi.org/10.1016/S0168-3659(99)00204-7

Streubel, A., Siepmann, J., & Bodmeier, R. (2006). Gastroretentive drug delivery systems. Expert Opinion on Drug Delivery, 3(2), 217-233. https://doi.org/10.1517/17425247.3.2.217

Talukder, R., & Fassihi, R. (2004). Gastroretentive delivery systems: A mini review. Drug Development and Industrial Pharmacy, 30(10), 1019-1028. https://doi.org/10.1081/DDC-200040239

Whitehead, L., Fell, J. T., & Collett, J. H. (1998). Development of a gastroretentive dosage form. European Journal of Pharmaceutical Sciences, 6(1), 71-77. https://doi.org/10.1016/S0928-0987(97)00072-4

Yang, L., Eshraghi, J., & Fassihi, R. (1999). A new intragastric delivery system for the treatment of Helicobacter pylori associated gastric ulcer: In vitro evaluation. Journal of Controlled Release, 57(3), 215-222. https://doi.org/10.1016/S0168-3659(98)00117-2.

Downloads

Published

2025-07-17

How to Cite

1.
Thareja R, Tiwari Y, Kothari LP, Somasundaram J, Srivastav Y, Borkar DP, Chouhan A, Kumar R. Development And Characterization Of Gastroretentive Floating Drug Famotidine. J Neonatal Surg [Internet]. 2025Jul.17 [cited 2025Oct.13];14(32S):5632-41. Available from: https://www.jneonatalsurg.com/index.php/jns/article/view/8348

Issue

Vol. 14 No. 32S (2025): Journal of Neonatal Surgery

Section

Original Article

License

Creative Commons License

This work is licensed under a Creative Commons Attribution 4.0 International License.

You are free to:

  • Adapt — remix, transform, and build upon the material for any purpose, even commercially.

Terms:

  • Attribution — You must give appropriate credit, provide a link to the license, and indicate if changes were made. You may do so in any reasonable manner, but not in any way that suggests the licensor endorses you or your use.
  • No additional restrictions — You may not apply legal terms or technological measures that legally restrict others from doing anything the license permits.