Microfluidics platform for polymorph screening directly from powder

Guillem Peybernès (1) , Romain Grossier (1) , Frédéric Villard (2) , Philippe Letellier (2) , Nadine Candoni (1) , Stéphane Veesler (1)

1 CINaM - Centre Interdisciplinaire de Nanoscience de Marseille
2 Technologies Servier

We describe a microfluidic platform for solid phase screening using extremely small quantities of raw materials. Based on our previous setup for solubility measurement that generates saturated solutions directly from powder, the platform requires no solution in excess of that used for the droplet-crystallization experiment. The setup is compatible with most solvents and molecules without using surfactant. Using this microfluidic platform, we first measured the solubility of Sulfathiazole in water, isopropanol, and acetonitrile. Second, we performed a polymorph screening of Sulfathiazole using as little as 30 mg of raw material, for numerous identical cooling crystallization experiments from 80 to 10°C. In the experiments presented, we obtained the 3 usual polymorphs of Sulfathiazole. We show that this economical approach yields reliable information on the probability of nucleation of a given polymorph, useful in pharmaceutical development.

Mots clés: screening; microfluidic; polymorphism; solubility

Domaines: Science des matériaux [cond-mat.mtrl-sci]; Génie chimique

Guillem Peybernès, Romain Grossier, Frédéric Villard, Philippe Letellier, Nadine Candoni, et al.. Microfluidics platform for polymorph screening directly from powder. Crystal Growth & Design, 2020, 20, pp.3882-3887. ⟨hal-02477923v2⟩