In vitro and in vivo evaluation of taste-masked orodispersible tablets of fluoxetine hydrochloride for the treatment of depression

Abstract

Aim

Fluoxetine (FLX) has become the first-line drug in the pharmacotherapy of patients with depression. However, it has a strong unpleasant bitter taste, leading to the failure to complete the therapy. In this study, FLX is formulated into orodispersible tablets (ODTs) characterized by a fast release with an acceptable taste.

Method

FLX ODTs were prepared by the complexation of FLX with β-cyclodextrin (β-CD) for taste-masking, using different super disintegrants, namely crospovidone (CP), croscarmellose sodium (Ccs), sodium starch glycolate (SSG), and indion. The FLX powder blend is estimated for pre-and post-compression parameters. The selected tablet formulations based upon drug release at 40 s with acceptable release patterns are investigated for accelerated stability testing and comparative in vivo study with a marketed product.

Results

It was found that all FLX-powder blends have good flow properties; all the prepared tablets complied with the pharmacopeial requirements for the unity of content, weight, friability, and hardness. Moreover, all the tablets obtained acceptable taste after complexation with β-CD. The order of release of the drug, regarding super disintegrants used, was as in the following descending order: CP > Ccs > SSG > indion. Accelerated stability study of selected formulation F2 and F6 showed that; there were no considerable changes in physical properties, drug content, and percentage drug release. Furthermore, also the in vivo study proved the effectiveness of FLX ODTs as an antidepressant.

Conclusion

The results obtained showed a promising potential of the prepared FLX ODTs for treating depression effectively.

Keywords:

• Fluoxetine HCl
• β-cyclodextrin
• super disintegrants
• stability
• in vivo study

Acknowledgments

I would like to thank Dr. Karima Mohammed Abu-Elfotouh (Lecturer of Pharmacology and Toxicology Department, Faculty of Pharmacy, Al-Azhar University) for providing support and facilities during the in vivo research work.

Disclosure statement

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