
The old jokes about women using headaches as an excuse to resist the amorous intentions of partners may be revived by a recent review on cocrystals (Drug Discovery Today, 2008, 13, 440-446).
The review reports that a number of drug substances currently on the market form useful co-crystals with novel properties. Among these is a cocrystal of sildenafil, the active ingredient of Viagra®, with acetyl salicylic acid (Aspirin) (normally sildenafil is sold in the citrate salt form). The new cocrystal exhibits an intrinsic dissolution rate of 11.75 mg/min/cm2 vs 6.64 for the citrate salt and is also stable up to 165oC, even though it melts at 143oC. The new cocrystal therefore, may have advantages for oral administration, but the presence of the “aspirin” may also mean that additional testing may be necessary.
The review reports that a number of drug substances currently on the market form useful co-crystals with novel properties. Among these is a cocrystal of sildenafil, the active ingredient of Viagra®, with acetyl salicylic acid (Aspirin) (normally sildenafil is sold in the citrate salt form). The new cocrystal exhibits an intrinsic dissolution rate of 11.75 mg/min/cm2 vs 6.64 for the citrate salt and is also stable up to 165oC, even though it melts at 143oC. The new cocrystal therefore, may have advantages for oral administration, but the presence of the “aspirin” may also mean that additional testing may be necessary.















