Department of Pharmaceutics, Semmelweis University, Hőgyes E. Str. 7, Budapest, 1092, Hungary.
Department of Electronics Technology, Budapest University of Technology and Economics, Egry J. Str. 18, Budapest, 1111, Hungary.
AAPS PharmSciTech. 2020 Dec 29;22(1):14. doi: 10.1208/s12249-020-01902-x.
Most of the commercially available pharmaceutical products for oral administration route are marketed in the tablet dosage forms. However, compression of multiparticulate systems is a challenge for the pharmaceutical research and industry, especially if the individual unit is a coated particle, as the release of the active ingredient depends on the integrity of the coating. In the present study, polymer-coated pellets tableted with different types of excipients (powder, granules, pellets) then were investigated by various tablet-destructive (microscopic) and tablet non-destructive (microfocus X-ray; microCT) imaging methods. The information obtained from the independent evaluation of the in vitro drug release profiles model is confirmed by the results obtained by image analysis, regardless of whether X-ray or stereomicroscopic images of the coated, tableted pellets were used for image analysis. The results of this study show that the novel easy-to-use, fast, and non-destructive MFX method is a good alternative to the already used microscopic image analysis methods regarding the characterization of particulates, compressed into tablets.
大多数市售的口服药物制剂以片剂形式销售。然而，多颗粒系统的压缩对制药研究和工业来说是一个挑战，特别是如果单个单元是包衣颗粒，因为活性成分的释放取决于包衣的完整性。在本研究中，用不同类型的赋形剂（粉末、颗粒、丸剂）对聚合物包衣丸剂进行压片，然后用各种片剂破坏性（显微镜）和片剂非破坏性（微焦点 X 射线；微计算机断层扫描）成像方法进行研究。通过对体外药物释放曲线模型的独立评估获得的信息，通过图像分析得到证实，无论是否使用 X 射线或立体显微镜图像进行图像分析。本研究的结果表明，新型易用、快速且非破坏性的 MFX 方法是一种很好的替代方法，可替代已经使用的微观图像分析方法，用于对压制成片剂的颗粒进行特征描述。
