Kalinkova G N
Laboratory of Infrared Spectroscopy, Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Medical University, 24 Krakra Strasse, 1054, Sofia, Bulgaria.
Int J Pharm. 1999 Sep 30;187(1):1-15. doi: 10.1016/s0378-5173(99)00176-3.
A review of "up to date" research findings leading to new concepts of the pharmaceutical formulations and their interactions has been presented. The rational approaches to the excipients choice as well as to their interactions with medicaments have been shown as a basis for modern modelling of pharmaceutical formulations. The importance of complexation, hydrogen bonding, ion-dipole, dipole-dipole and van der Waals attractions as the tools which can modify the physicochemical, pharmacological or pharmacokinetical behaviour of the medicaments has been emphasised. In vivo studies (carried out in healthy human subjects-volunteers, in beagle dogs, in rats etc.) and in vitro studies (on excised human skin, hairless mouse skin etc.) as well as studies of chemical stability and bioavailability serve also as a proof of these interactions. Therefore, excipients are important components of pharmaceutical formulations and they can take an active part in the improvement of the characteristics of formulations (but they may also reduce the effectiveness of some preparations). In this context, the so called active and inactive ingredients in pharmaceutical formulations are inexact, old and "out-of date". Their further use is only conventional. In conclusion, among the various modern techniques applied the combination of infrared spectroscopy and X-ray diffraction has been estimated as the most successful in proving the interactions between drugs and excipients. Finally, pharmaceutical formulations and their interactions have constituted a diverse and rapidly expanding field of Pharmacy (Pharmaceutical Technology, Pharmaceutical Industry and Pharmaceutical Sciences) which covers a wide range of numerical topics within an unified framework.
本文综述了“最新”的研究成果,这些成果带来了药物制剂及其相互作用的新概念。已表明辅料选择及其与药物相互作用的合理方法是药物制剂现代建模的基础。强调了络合、氢键、离子偶极、偶极 - 偶极和范德华吸引力作为可改变药物物理化学、药理或药代动力学行为的工具的重要性。体内研究(在健康人类受试者 - 志愿者、比格犬、大鼠等中进行)、体外研究(在切除的人体皮肤、无毛小鼠皮肤等上进行)以及化学稳定性和生物利用度研究也证明了这些相互作用。因此,辅料是药物制剂的重要组成部分,它们可以积极参与改善制剂的特性(但它们也可能降低某些制剂的有效性)。在这种情况下,药物制剂中所谓的活性成分和非活性成分是不准确、陈旧且“过时”的。它们的进一步使用只是传统做法。总之,在所应用的各种现代技术中,红外光谱和X射线衍射的结合被认为是证明药物与辅料之间相互作用最成功的方法。最后,药物制剂及其相互作用构成了药学(制药技术、制药工业和药学科学)一个多样且迅速发展的领域,该领域在一个统一的框架内涵盖了广泛的数值主题。