High-throughput crystallization: polymorphs, salts, co-crystals and solvates of pharmaceutical solids

Morissette, Sherry L.; Almarsson, Ӧrn; Peterson, Matthew L.; Remenar, Julius F.; Read, Michael J.; Lemmo, Anthony V.; Ellis, Steve; Cima, Michael J.; Gardner, Colin

doi:10.1016/j.addr.2003.10.020

Cited by 641 publications

(425 citation statements)

References 72 publications

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“…By the cocrystallization of antifungal drug itraconazole with 1,4-dicarboxylic acids (succinic acid, L-tartaric acid or L-malic acid) a modification of the dissolution profile is achieved compared to the amorphous form of itraconazole (Sporanox, Janssen-Cilag) 7 . A 1:1 carbamazepine/saccharin cocrystal compared to polymorph III of carbamazepine (anticonvulsant Tegretol, Novartis) shows no polymorphous behaviour and is not prone to hydration 8 .…”

Section: Productionmentioning

confidence: 99%

Pharmaceutical Cocrystals

深水¹

2017

Solid State Properties of Pharmaceutical Materials

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Cocrystals are very interesting and useful product. In this paper the main information about cocrystals is presented. It is shown that cocrystals are solid substances, which consist of few components mixed together. There are a lot of ways of cocrystals production and application. It is shown that cocrystals can be applied in medicine and pharmaceutical industry for improving different properties such as dissolution rate, melting point, solubility, chemical stability etc. Another way of cocrystals application is drug pharmacological action modification.

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Section: Productionmentioning

confidence: 99%

Pharmaceutical Cocrystals

深水¹

2017

Solid State Properties of Pharmaceutical Materials

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“…In an example from pharmaceutical crystallization, exposure of immobilized polymer monolayers to supersaturated solutions can lead to the selective, heterogeneous nucleation of stable polymorphs (Morissette et al 2004). This enables exploration of the polymorph space in a high throughput manner.…”

Section: Mineralization and Crowding In Quasi-2 Dimensionsmentioning

confidence: 99%

Mineralization and non-ideality: on nature’s foundry

Rao¹,

Cölfen

2016

Biophys Rev

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Understanding how ions, ion-clusters and particles behave in non-ideal environments is a fundamental question concerning planetary to atomic scales. For biomineralization phenomena wherein diverse inorganic and organic ingredients are present in biological media, attributing biomaterial composition and structure to the chemistry of singular additives may not provide a holistic view of the underlying mechanisms. Therefore, in this review, we specifically address the consequences of physico-chemical non-ideality on mineral formation. Influences of different forms of non-ideality such as macromolecular crowding, confinement and liquid-like organic phases on mineral nucleation and crystallization in biological environments are presented. Novel prospects for the additive-controlled nucleation and crystallization are accessible from this biophysical view. In this manner, we show that non-ideal conditions significantly affect the form, structure and composition of biogenic and biomimetic minerals.

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“…The compounds which are liquid at room temperature are called as solvates whereas those compounds which are solid at room temperature are called as cocrystals. If the solvates contain water as a solvent in their crystal lattice then they are known as hydrates [21] . Solvates/hydrates are commonly formed during the cocrystallization via solution or liquid assisted grinding [9] and they can alter physicochemical properties of API's.…”

Section: Difference Between Cocrystals Salt Solvates and Hydratesmentioning

confidence: 99%

“…Among all these, the cocrystals should have the advantages that they will exist in stable crystalline form and no need of other excipients and additives in formulations [21] . The factors which play important role in affecting the physicochemical properties are the properties of APIs and coformers, the nature of molecular interaction between them and the employed synthetic procedures.…”

Section: Advantages Of Cocrystalsmentioning

confidence: 99%