RESUMO
Pharmaceutical cocrystals are multicomponent systems in which at least one component is an active pharmaceutical ingredient and the others are pharmaceutically acceptable ingredients. Cocrystallization of a drug substance with a coformer is a promising and emerging approach to improve the performance of pharmaceuticals, such as solubility, dissolution profile, pharmacokinetics and stability. This review article presents a comprehensive overview of pharmaceutical cocrystals, including preparation methods, physicochemical properties, and applications. Furthermore, some examples of drug cocrystals are highlighted to illustrate the effect of crystal structures on the various aspects of active pharmaceutical ingredients, such as physical stability, chemical stability, mechanical properties, optical properties, bioavailability, sustained release and therapeutic effect. This review will provide guidance for more efficient design and manufacture of pharmaceutical cocrystals with desired physicochemical properties and applications.
RESUMO
Recently,the screening technologies of pharmaceutical cocrystals have become a research focus of improving drug solubility and stability. The technique changes medicine properties by intermolecular forces without changing the molecular structure , which provides new ways for the development of the insoluble drug. In addition,the formation of cocrystal gives new properties to drugs and intellectual property rights are effectively protected. This review focuses on screening technique ,which provides references for fur?ther studies of pharmaceutical cocrystal.
RESUMO
Co-crystal is a crystalline structure composed of at least two components, where the components may be active pharmaceutical ingredients (APIs) and co-formers in stoichiometric amounts. Co-crystal structure exhibits long range order and the components interact via non-covalent interaction such as hydrogen bonding, ionic interaction, vander-waals interaction, and π-π interaction. The intermolecular interaction and resulting crystal structure can generate physicochemical properties which differ from the properties of the individual components. Such properties include melting point, solubility, chemical stability, and mechanical properties. Meanwhile, co-crystal can break through patents protection of APIs. So co-crystal attracts more attention in pharmaceutical research and development field. With the development of pharmaceutical co-crystals, there may be an opportunity for improving the insoluble active ingredients of Chinese materia medica (CMM) in further development. This review has been organized around four categories: the co-crystals of flavonoids (I), alkaloids (II), terpenes (III), and polyphenols (IV) and their effects on physicochemical properties and bioavailability of those APIs, which provide a good reference for the application of pharmaceutical co-crystals in insoluble active ingredients of CMM.
RESUMO
Recently, the screening technologies of pharmaceutical cocrystals have become a research focus of improving drug solubility and stability. The technique changes medicine properties by intermolecular forces without changing the molecular structure,which provides new ways for the development of the insoluble drug. In addition,the formation of cocrystal gives new properties to drugs and intellectual property rights are effectively protected. This review focuses on screening technique, which provides references for further studies of pharmaceutical cocrystal.
RESUMO
@#Pharmaceutical cocrystals are formed from the active pharmaceutical ingredients and cocrystal formers through hydrogen bonding or other noncovalent bonds, which have attracted much attention in pharmaceutical field in recent years. From the analysis of patent application situation, patent applicant, legal status, and patent application techniques, guiding directions for the future research and development of the pharmaceutical cocrystals are proposed in this article.