Department of Pharmacy, University of Patras, GR-26504 Rio Achaias, Greece.
Institute of Chemical Engineering Sciences, Foundation of Research and Technology-Hellas (ICE-HT/FORTH), GR-26504 Platani Achaias, Greece.
Molecules. 2022 Apr 18;27(8):2602. doi: 10.3390/molecules27082602.
The assessment of active pharmaceutical ingredient (API) particle size and morphology is of great importance for the pharmaceutical industry since it is expected to significantly affect physicochemical properties. However, very few methods are published for the determination of API morphology and particle size of film-coated (FC) tablets. In the current study we provide a methodology for the measurement of API particle size and morphology which could be applied in several final products. Bismuth Oxide 120 mg FC Tabs were used for our method development, which contain bismuth oxide (as tripotassium dicitratobismuthate (bismuth subcitrate)) as the active substance. The sample preparation consists of partial excipient dissolution in different solvents. Following this procedure, the API particles were successfully extracted from the granules. Particle size and morphology identification in Bismuth Oxide 120 mg FC Tabs was conducted using micro-Raman mapping spectroscopy and ImageJ software. The proposed methodology was repeated for the raw API material and against a reference listed drug (RLD) for comparative purposes. The API particle size was found to have decreased compared to the raw API, while the API morphology was also affected from the formulation manufacturing process. Comparison with the RLD product also revealed differences, mainly in the API particle size and secondarily in the crystal morphology.
药物活性成分(API)粒度和形态的评估对制药行业非常重要,因为它预计会显著影响物理化学性质。然而,用于测定薄膜包衣(FC)片剂的 API 形态和粒度的方法却非常少。在本研究中,我们提供了一种可应用于多种最终产品的 API 粒度和形态测量方法。我们使用 120 毫克 FC 铋 tabs 进行方法开发,其中包含作为活性物质的氧化铋(作为三钾二柠檬酸铋(次柠檬酸铋))。样品制备包括在不同溶剂中部分溶解赋形剂。按照该程序,API 颗粒从颗粒中成功提取。使用微拉曼映射光谱和 ImageJ 软件对 120 毫克 FC 铋 tabs 中的铋氧化物的粒度和形态进行鉴定。为了进行比较,对原始 API 材料和参比药物(RLD)重复了该方法。与原始 API 相比,API 粒径减小,而 API 形态也受到制剂制造工艺的影响。与 RLD 产品的比较也显示出差异,主要在 API 粒径上,其次在晶体形态上。