Novartis Pharma AG, Fabrikstrasse 2, CH-4056 Basel, Switzerland.
Technische Universität Braunschweig, Institut für Pharmazeutische Technologie und Biopharmazie, Mendelssohnstrasse 1, D-38106 Braunschweig, Germany; Technische Universität Braunschweig, Zentrum für Pharmaverfahrenstechnik - PVZ, Franz-Liszt-Strasse 35a, D-38106 Braunschweig, Germany.
Int J Pharm. 2021 Feb 15;595:120229. doi: 10.1016/j.ijpharm.2021.120229. Epub 2021 Jan 21.
Water uptake and swelling of tablets are processes occurring during active pharmaceutical ingredient (API) release. Thereby, disintegration is promoted and the enhanced exposure of API surface area to the release medium facilitates API dissolution. An experimental set-up for the simultaneous and time-resolved determination of water uptake and swelling of tablets has been developed. Water uptake was determined with a balance and swelling was determined with a camera. To validate the gravimetrical analysis, real-time water uptake measurements with inert test specimens were performed. The standard deviation of these measurements was considered to depict precision. A complementary gravimetrical analysis was employed to determine accuracy. For both, precision and accuracy, a maximum deviation of 6% was found. An algorithm for the symmetry-based 3D volume reconstruction was applied to obtain volumes of the tablets from 2D images. X-ray micro computed tomography was used to validate the accuracy and the determined volumes were in good accordance within 6% deviation. A case study with binary formulations of a filler and disintegrants confirmed reproducibility and demonstrated the ability of the method to discriminate formulation characteristics, such as disintegrant type, composition and porosity for water uptake and swelling with the necessary temporal resolution.
片剂的水分吸收和溶胀是在活性药物成分（API）释放过程中发生的过程。因此，促进了崩解，并增强了 API 表面与释放介质的接触，从而促进了 API 的溶解。已经开发出一种用于同时和时间分辨地测定片剂的水分吸收和溶胀的实验装置。通过天平测定水分吸收，通过相机测定溶胀。为了验证重量分析，对惰性测试样品进行了实时水分吸收测量。这些测量的标准偏差被认为可以描述精度。还采用了补充的重量分析来确定准确性。对于精度和准确性，发现最大偏差均为 6％。应用基于对称的 3D 体积重建算法，从 2D 图像中获得片剂的体积。使用 X 射线微计算机断层扫描来验证准确性，并且确定的体积在 6％的偏差内很好地一致。用填充剂和崩解剂的二元配方进行的案例研究证实了重现性，并证明了该方法能够以必要的时间分辨率区分水分吸收和溶胀的配方特征，例如崩解剂类型，组成和孔隙率。
