Challenges in the development of hydrate phases as active pharmaceutical ingredients--an example.

The challenges during pilot plant scale-up of the SAR474832 API (active pharmaceutical ingredient) production in view of crystallization, isolation, drying and micronization are reported. A variety of different solid-state analytical and spectroscopic techniques (also coupled methods) were applied in order to understand the complex phase transition behaviour of the crystallographic phase (form 1) chosen for development: a partially non-stoichiometric channel-hydrate (x (1+1.25) H(2)O) crystallizing from pure water in the crystal habit of fine needles, which tend to agglomerate upon isolation and drying.

Changes in the carotenoid content of apricot (Prunus armeniaca, var Bergeron) during enzymatic browning: β-carotene inhibition of chlorogenic acid degradation.

Considering the numerous beneficial effects in human health ascribed to carotenoids, studies were performed to investigate the modification of carotenoid amount and composition during apricot enzymatic browning. First works on bruised apricot purees have shown a trans-β-carotene isomerisation (20%) induced by enzymatic browning. To clarify this isomerisation, oxidation of chlorogenic acid in presence of trans-β-carotene, catalysed by purified apricot polyphenoloxidase (PPO), was followed by HPLC and polarography.