Fabrication of gastro-floating sustained-release etoricoxib and famotidine tablets: design, optimization, in-vitro, and in-vivo evaluation

Abstract

In this study, a new gastro-floating sustained-release tablet (GFT) with a combination of Etoricoxib (ET) and Famotidine (FM) was successfully developed. GFTs were prepared by using a combination of hydrophilic swellable natural/semi-synthetic polymers as a controlled-release layer. Through a 2⁴ full factorial statistical experimental design, the effects of formulation factors on the release of GFTs were conducted. The ideal floating tablet (FT) comprised konjac-gum (150 mg), guar-gum (26.57 mg), xanthan-gum (54.17 mg), and HPMC-K15-M (69.25 mg). The ideal FT exhibited a high swelling index (SI) (297.7%) and rapid FLT (around 50 s) in 0.1 N HCl as well as controlled release of ET (22.43% in 1 h and 77.47% in 8 h) and FM (24.89% in 1 h and 93.82% in 8 h) with the absence of any drug-excipient interactions. The AUC_0∼72 (ng h/mL) of ET and FM in the GFTs were approximately double-fold of the market, respectively. The relative bioavailability was (207.48 ± 12.02% and 208.51 ± 13.11%) compared with commercial tablets. The X-ray imaging showed a promising buoyancy ability for approximately 8 h. These findings revealed the successful preparation of the sustained-release floating tablet with improved dual drug delivery.

Keywords:

• Etoricoxib
• famotidine
• floating sustained-release
• x-ray imaging
• GRDDS
• bioavailability

Ethical approval statement

The Research Ethics Committee (REC) for experimental and clinical studies at the Faculty of Pharmacy Cairo University approved this research protocol PI (3014).

Participation consent

Informed consent was obtained from all individual participants included in the study.

Publication consent

The authors affirm that human research participants provided informed consent for the publication of the images in Figure 7.

Authors contribution

All authors have contributed equally

Disclosure statement

No potential conflict of interest was reported by the author(s).

Data availability statement

The data supporting the findings of the article are available from the corresponding author upon request. The data are not publicly available due to restrictions of their containing information that could compromise the privacy of research participants.

Additional information

Funding

The authors declare no funding.