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; in vivo study; stability; super disintegrants; β-cyclodextrin.