PREPARATION AND EVALUATION OF ONCE DAILY FLOATING GMO-ALGINATE MICROSPHERES CONTAINING FAMOTIDINE

Authors

  • AMIR IBRAHIM MOHAMED Department Of Pharmaceutics And Industrial Pharmacy, Military Medical Academy, Cairo, Egypt https://orcid.org/0000-0002-2053-2050
  • MOHAMMED ISMAEL HERRY Department Of Pharmaceutics And Industrial Pharmacy, Military Medical Academy, Cairo, Egypt. https://orcid.org/0000-0003-3486-3659
  • MOHAMED A. KASSEM Department Of Pharmaceutics And Industrial Pharmacy, Faculty Of Pharmacy, Cairo University, Cairo, Egypt.
  • AHMED EL-NABARAWI Department Of Pharmaceutics And Industrial Pharmacy, Faculty Of Pharmacy, Cairo University, Cairo, Egypt.
  • MONA MOHAMED ABOELFOTOH EL KHATIB Department Of Pharmaceutics And Industrial Pharmacy, Faculty Of Pharmacy, Cairo University, Cairo, Egypt.

DOI:

https://doi.org/10.22159/ijap.2023v15i1.46503

Keywords:

Famotidine, ; Slightly-soluble drug, Water/Oil emulsion method, Glyceryl mono-oleate (GMO), Ca-alginate, Gastro-Retentive Floating microspheres

Abstract

Objective: In this work, a gastro-retentive floating microsphere delivery system composed of Drug/ Glyceryl mono-oleate (GMO) embedded in a Ca-alginate gas-generated matrix was designed to improve the bioavailability of a slightly-soluble model drug Famotidine.

Methods: The water/Oil emulsion method was used to prepare Famotidine floatable microspheres, and formulation variables such as Alginate: GMO ratio, gas-generated bicarbonates concentration, and loading drug concentration were investigated. Conventional techniques including DSC, XRD & FTIR were performed to confirm Famotidine compatibility with GMO and Alginate polymers. Real-Time X-ray Radiography was used for in-vivo imaging of Famotidine floatable microspheres using rabbits as an animal model. HPLC spectroscopic technique was used to determine Famotidine plasma concentration after oral administration of Alginate-GMO loaded microspheres.

Results:  Floating Famotidine Alginate-GMO microspheres (0.75:1:0.25) w/w/w showed a remarkable entrapment efficiency (>98%), good buoyancy (>84) and prolonged in-vitro drug release properties (>24hours). DSC, XRD, & FTIR techniques showed no evidence of interaction between Famotidine and Alginate or GMO. In-vivo Imaging of Famotidine floatable microspheres showed that capsules containing Famotidine-Alginate microspheres were not detected after 3hrs of administration, while capsules containing Famotidine-GMO-Alginate microspheres can be detected for more than 12hrs, indicating superior gastric retention properties. The pharmacokinetic parameters were calculated for Famotidine: GMO-Alginate, and Famotidine: alginate, and compared with the plain drug over 24 h period. Famotidine: GMO-Alginate microspheres exhibited controlled and prolonged absorption Tmax of 6.0 vs. 3.0 and 2.0 hrs; Cmax of 124.9±0.9 vs. 323.7±0.4and 458.6±0.5 ng/ml; AUC0-24 of 2153.025±6.7 vs. 1650.4±1.9 and 1110.725±2.1 ng/ml for Famotidine: alginate and plain drug, respectively, reflecting the increase in the bioavailability of the drug in the floating formulations compared to the free drug.

Conclusion: Prolonged gastric retention time and sustained release properties of floating GMO-alginate microsphere suggest that it could provide a valuable sustained release dosage form of slightly-soluble drugs.

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Published

09-11-2022

How to Cite

MOHAMED, A. I., HERRY, M. I., KASSEM, M. A., EL-NABARAWI, A., & EL KHATIB, M. M. A. (2022). PREPARATION AND EVALUATION OF ONCE DAILY FLOATING GMO-ALGINATE MICROSPHERES CONTAINING FAMOTIDINE. International Journal of Applied Pharmaceutics, 15(1). https://doi.org/10.22159/ijap.2023v15i1.46503

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