Carbamazepine dissolution properties

Figure 14.1 is an example of improved dissolution properties achieved via a co-crystal and shows the differences in properties between two co-crystals of the same API, carbamazepine. 

Carbamazepine (CBZ, 87) (Scheme 3.16), is an important antiepileptic agent in use for more than 30 years but suffers from low water solubility and oral bioavailability. Hickey and coworkers [129] prepared a cocrystal with saccharin (88) employing the peripheral hydrogen bonding capabilities of CBZ dimer. The cocrystal was found to possess favorable dissolution properties, suspension stability and pharmacokinetics using dog models. Similarly, Zaworotko, Shytle and CO workers [130] used cocrystallization to improve solubility and oral bioavailability of quercetin. 

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