共結晶は複数の成分からなる単一の結晶構造体であり、原薬単体よりも優れた特性を有する場合があります。Triclinic Labsはコクリスタル(共結晶)スクリーニングの豊富な経験とノウハウを用いて、御客様の御要望に対して御提案致します。Triclinic Labsコクリスタル(共結晶)スクリーニングのパイオニアです。

Cocrystals differ from salts in that cocrystal components are held together by non-ionic bonds. Cocrystals can be superior APIs when the active compound has poor physical properties and is either unable to form salts or whose salts also have inadequate physical properties. Cocrystals have been used to change the properties of active molecules, leading to enhanced bioavailability, lower hygroscopicity, and generation of crystalline from amorphous materials, among other things. In addition, cocrystals have been used to solve processing problems such as substitution of chromatographic purification methods with crystallization-based procedures. Triclinic Labs has extensive experience in finding and utilizing cocrystals. We carry out phase diagram-driven, solvent-based experiments in either manual mode or utilizing our custom, high-throughput reaction block system (Fig 1). The process was developed by testing with known cocrystals, and ultimately 75 cocrystals of 18 APIs were produced with a 100% success rate. The process has proven highly successful; we are currently finding cocrystals for >60% of the molecules tested.

cocrystals for >60% of the molecules

Figure 1. High Throughput Cocrystal Screens. Cocrystal screens can be carried out in specially designed reaction crystallization blocks suitable for 96 simultaneous reactions. These blocks are designed and milled multi-well plates (above) and are utilized to perform cocrystal screens.This approach applies phase diagram directed, solvent-based experimentation and can include ball-milling and other slurry techniques where kinetic energy is added to the system. The approach has a much higher degree of success (>60%) than conventional cocrystal screening systems.


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