共结晶:通往更好药物治疗的创新途径

IF 0.7 Q4 PHARMACOLOGY & PHARMACY Journal of Reports in Pharmaceutical Sciences Pub Date : 2020-07-01 DOI:10.4103/jrptps.JRPTPS_103_19
Braham Dutt, M. Choudhary, Vikaas Budhwar
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引用次数: 1

摘要

如今,活性药物成分(API)的溶解性差、生物利用度低以及物理、化学和生物制药性能受到阻碍,成为制药科学家们讨论的一个非常重要的问题。对于制药研究人员和工业界来说,开发一种具有改进物理化学性质的合适配方是一项具有挑战性的任务。共结晶的过程是众所周知的;然而,近年来,这种方法作为一种相对较新的方法,在提高溶解度、生物利用度、稳定性、热性能、渗透性、片剂性能和其他相关物理化学性能方面,在药物中获得了巨大的重要性。共晶是多组分体系,其中API和共形成剂两种组分以化学计量比存在,并在晶格中通过非椭圆相互作用结合在一起。共结晶不仅能更好地优化原料药的理化性质,还能更好地优化其治疗反应和药理学性质。共结晶实验的设计基于稳健性、氢键规则和潜在的分子间相互作用。各种理论和实验方法增加了选择合适的共形成物的机会,这是共晶形成设计过程中最具挑战性的步骤。本文综述了共晶的分类、共晶的药物选择标准、共晶形成的化学、制备方法、表征以及在药物和生物医学领域的各种应用。
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Cocrystallization: An innovative route toward better medication
Nowadays, poor solubility, lower bioavailability, and hindered physical, chemical, and biopharmaceutical properties of active pharmaceutical ingredients (APIs) become a very important matter of discussion for pharmaceutical scientists. It is a challenging task for pharmaceutical researchers and industry to develop a suitable formulation with improved physicochemical properties. The process of cocrystallization is long known; however, in the recent times, this approach has gained enormous importance in pharmaceuticals as a relatively new method for enhancement of solubility, bioavailability, stability, thermal properties, permeability, tablet ability, and other related physicochemical properties. Cocrystals are multicomponent systems in which two components, an API and a coformer, were present in stoichiometric ratio and bonded together with non-covalent interactions in the crystal lattice. Cocrystallization offers better optimization of not only physicochemical properties but also therapeutic response and pharmacological properties of APIs. The design of a cocrystallization experiment is based on robustness, hydrogen bonding rules, and potential intermolecular interactions. Various theoretical and experimental approaches increase the chances for selection of a suitable coformer, the most challenging step during the design of cocrystal formation. The present review covers classification of cocrystals, drug selection criteria for cocrystals, chemistry involved in cocrystal formation, methods of preparation, their characterizations, and various applications in pharmaceutical and biomedical fields.
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来源期刊
Journal of Reports in Pharmaceutical Sciences
Journal of Reports in Pharmaceutical Sciences Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)
CiteScore
1.40
自引率
0.00%
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0
期刊介绍: The Journal of Reports in Pharmaceutical Sciences(JRPS) is a biannually peer-reviewed multi-disciplinary pharmaceutical publication to serve as a means for scientific information exchange in the international pharmaceutical forum. It accepts novel findings that contribute to advancement of scientific knowledge in pharmaceutical fields that not published or under consideration for publication anywhere else for publication in JRPS as original research article. all aspects of pharmaceutical sciences consist of medicinal chemistry, molecular modeling, drug design, pharmaceutics, biopharmacy, pharmaceutical nanotechnology, pharmacognosy, natural products, pharmaceutical biotechnology, pharmacology, toxicology and clinical pharmacy.
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