Enhancement of dissolution rate and oral bioavailability of poorly soluble drug florfenicol by using solid dispersion and effervescent disintegration technology

Abstract

Objective

Florfenicol(FF) is an excellent veterinary antibiotic, limited by poor solubility and poor bioavailability.

Significance

Here in, we aimed to explore the applicability of fast disintegrating tablets compressed from Florfenicol-loaded solid dispersions (FF-SD-FDTs) to improve the dissolution rate and oral bioavailability of Florfenicol.

Methods

Utilizing selecting appropriate preparation methods and carriers, the solid dispersions of Florfenicol (FF-SDs) were prepared by solvent evaporation and the fast disintegrating tablets (FF-SD-FDTs) were prepared by the direct compression (DC) method.

Results

The tablet properties including hardness, friability, disintegration time, weight variation, etc. all met the specifications of Chinese Veterinary Pharmacopeia(CVP). FF-SD-FDTs significantly improved drug dissolution and dispersion of FF in vitro compared to florfenicol conventional tablets (FF-CTs). A pharmacokinetics study in German shepherd dogs proved the AUC_0-∞ and C_max values of FF-SD-FDTs are 1.38 and 1.38 times more than FF-CTs, respectively.

Conclusions

Overall, it can be concluded that FF-SD-FDTs with excellent disintegration and dissolution properties were successfully produced, which greatly improved the oral bioavailability of the poorly soluble drug FF, and the study provided a new idea for a broader role of FF in pet clinics.

Graphical Abstract

Keywords:

• Florfenicol
• Solid dispersions
• Effervescent tablets
• Fast disintegrating tablets
• Pharmacokinetics

Acknowledgements

This work was supported by the College of Veterinary Medicine of Sichuan Agricultural University.

Disclosure statement

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

Additional information

Funding

The author(s) reported there is no funding associated with the work featured in this article.