Department of Pharmaceutical Technology, Faculty of Pharmacy, Gazi University, Ankara, Turkey.
Zoleant Pharmaceuticals International, Istanbul, Turkey.
AAPS PharmSciTech. 2020 Apr 15;21(3):115. doi: 10.1208/s12249-020-01653-9.
The objective of the current study was to develop ziprasidone hydrochloride monohydrate (ZHM) nanocrystal-based orally dispersible tablet (ODT) formulations. Design of experiment approach was used to develop ODTs. The tablets were compressed using direct compression method and characterized with quality control tests. In vitro dissolution studies and Caco-2 cell permeability tests were executed. The hardness and friability values of nanocrystal-based ODTs were found 31.2 N and 1.05%, respectively. The disintegration time was below 10 s. Dissolution profile in pH 7.4 phosphate buffer showed that nanocrystal-based ODTs and commercial product were dissolved in 120 min 58.98% and 16%, respectively. In pH 7.4 phosphate buffer with SLS, sample groups dissolved above 85% at the end of the study. Permeability value and cumulative ZHM amount on the cells were improved with nanocrystals. In conclusion, the novel formulation of ZHM nanocrystal-based ODTs was successfully developed for alternative dosage form.
本研究旨在开发盐酸齐拉西酮一水合物（ZHM）纳米晶口服分散片（ODT）制剂。采用实验设计方法开发 ODT。采用直接压片法对片剂进行压缩，并进行质量控制试验。进行了体外溶出度研究和 Caco-2 细胞渗透性试验。纳米晶 ODT 的硬度和脆碎度值分别为 31.2 N 和 1.05%。崩解时间低于 10 s。在 pH 7.4 磷酸盐缓冲液中的溶出曲线表明，纳米晶 ODT 和商业产品在 120 分钟内分别溶解了 58.98%和 16%。在含 SLS 的 pH 7.4 磷酸盐缓冲液中，研究结束时各实验组的溶解率均超过 85%。纳米晶体提高了药物的渗透值和细胞累积 ZHM 量。总之，成功开发了 ZHM 纳米晶 ODT 的新型制剂，作为替代剂型。
