Faculty of Pharmacy, Pharmaceutics and Industrial Pharmacy Department, Al-Azhar University, Nasr City, Egypt.
Drug Dev Ind Pharm. 2021 Apr;47(4):645-653. doi: 10.1080/03639045.2021.1908336. Epub 2021 Apr 7.
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.
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 study with a marketed product.
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 -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 study proved the effectiveness of FLX ODTs as an antidepressant.
The results obtained showed a promising potential of the prepared FLX ODTs for treating depression effectively.
氟西汀（FLX）已成为治疗抑郁症患者的一线药物。然而，它有强烈的不愉快的苦味，导致治疗无法完成。在这项研究中，FLX 被制成口腔分散片（ODT），具有快速释放和可接受的口感。
FLX ODT 是通过 FLX 与β-环糊精（β-CD）的络合作用来掩盖味道，使用不同的超崩解剂，即交联聚维酮（CP）、交联羧甲基纤维素钠（Ccs）、交联羧甲基淀粉钠（SSG）和交聚维酮（indion）。对 FLX 粉末混合物进行压缩前后的参数估计。根据 40 秒内药物释放情况选择的片剂配方进行加速稳定性测试，并与市售产品进行比较研究。
发现所有 FLX 粉末混合物都具有良好的流动性能；所有制备的片剂都符合药典对含量、重量、脆碎度和硬度均一性的要求。此外，所有片剂在与β-CD 络合后都获得了可接受的口感。就使用的超崩解剂而言，药物释放的顺序如下：CP > Ccs > SSG > indion。对选定的配方 F2 和 F6 进行加速稳定性研究表明，物理性质、药物含量和药物释放百分比没有明显变化。此外，研究还证明了 FLX ODT 作为抗抑郁药的有效性。
研究结果表明，所制备的 FLX ODT 具有治疗抑郁症的良好前景。
