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

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 beta-cyclodextrin (beta-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 beta-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.

Automated summary

Fluoxetine (FLX) has been formulated into orodispersible tablets (ODTs) with a fast release and acceptable taste through complexation with beta-cyclodextrin. Various super disintegrants were used in preparation, and the tablets met pharmacopeial requirements for content, weight, friability, and hardness. Accelerated stability testing and in vivo study confirmed the effectiveness of FLX ODTs in treating depression.