Broncel Mateusz, Juszczak Anna, Szczolko Wojciech, Silvestri Daniele, Białek-Dratwa Agnieszka, Wacławek Stanisław, Kowalski Oskar, Ramos Paweł
Department of Biophysics, Faculty of Pharmaceutical Sciences in Sosnowiec, Medical University of Silesia, Jedności 8, 41-200 Sosnowiec, Poland.
Doctoral School, Medical University of Silesia, Jedności 8, 41-200 Sosnowiec, Poland.
Pharmaceuticals (Basel). 2024 Oct 3;17(10):1323. doi: 10.3390/ph17101323.
Increasing drugs' stability and adequately protecting them against degradation will ensure a decrease in their price and broader availability of pharmaceutical substances. This is of great importance, especially for drugs used to treat the most common diseases in the population, such as hypertension. The study examined two newly synthesized substances from the angiotensin I-converting enzyme inhibitor (ACEI) group as potential drugs. ACEIs are among the leading drugs used in the treatment of hypertension in the world. The chemical modifications of the tested substances applied concerned the places most susceptible to degradation. The presented work analyzed the compatibility of new derivatives with selected excipients used in pharmacy. : Thermogravimetric (TGA) and differential thermal analyses (c-DTA) were used as the main methods. In addition, non-thermal methods such as colorimetry analysis, Fourier-transform infrared (FTIR) and UV spectroscopy were used. Results: Based on the conducted studies, it can be concluded that the incompatibility of IND-1 with glucose anhydrous and lactose monohydrate occurs only when the mixture is stored at higher temperatures. For the remaining IND-1 and IND-2 mixtures with excipients, compatibility was demonstrated. : The obtained results confirmed the usefulness of the applied thermal analyses (TGA and c-DTA) for assessing the compatibility of the tested potential drugs with excipients. However, in the case of incompatibility reactions of substances occurring under the influence of elevated temperatures, such as the Maillard reaction, it is necessary to use non-thermal methods to obtain the right result.
提高药物稳定性并充分保护其免受降解将确保药物价格降低以及药物物质更广泛的可及性。这非常重要,尤其是对于用于治疗人群中最常见疾病(如高血压)的药物。该研究检测了两种新合成的血管紧张素I转换酶抑制剂(ACEI)类物质作为潜在药物。ACEI是全球治疗高血压的主要药物之一。对受试物质进行的化学修饰涉及最易降解的部位。本研究分析了新衍生物与药学中使用的选定辅料的相容性。主要方法采用热重分析(TGA)和差示热分析(c-DTA)。此外,还使用了比色分析、傅里叶变换红外光谱(FTIR)和紫外光谱等非热方法。结果:基于所进行的研究,可以得出结论,仅当混合物在较高温度下储存时,IND-1与无水葡萄糖和一水乳糖才会发生不相容性。对于其余的IND-1和IND-2与辅料的混合物,证明了其相容性。所获得的结果证实了所应用的热分析(TGA和c-DTA)对于评估受试潜在药物与辅料相容性的有用性。然而,对于在高温影响下发生的物质不相容反应,如美拉德反应,有必要使用非热方法以获得正确结果。