Solid forms of ortataxel

摘要

The present invention relates to solid forms of 13-(N-Boc-β-isobutylserinyl)-14-β hydroxybaccatin III 1, 14-carbonate (Ortataxel). Amorphous Form A, crystalline Form B, mixtures thereof and processes for preparing them are disclosed. Amorphous Form A is prepared by fast precipitation of Ortataxel from a mixture of acetone and water. Form A transforms in Form B when suspended and stirred in a mixture of ethanol and water for 4-8 hours. If the suspension is stirred for less than 4 hours, mixtures of Form B and Form A are obtained. Form B or mixtures of Forms A and B can also be obtained dissolving Ortataxel in a protic organic solvent, followed by addition of water.

主权项

1. A process for preparing an amorphous solid Ortataxel, the process comprising the steps of dissolving Ortataxel in a ketone, an aprotic dipolar organic solvent, or mixtures thereof, followed by adding water containing 0.001% w/v to 0.003% w/v of an organic acid, thereby producing an amorphous solid Ortataxel.