TY - JOUR
T1 - Crystallization of microparticulate pure polymorphs of active pharmaceutical ingredients using CO 2-expanded solvents
AU - Sala, Santiago
AU - Córdoba, Alba
AU - Moreno-Calvo, Evelyn
AU - Elizondo, Elisa
AU - Muntó, Maria
AU - Rojas, Paula Elena
AU - Larrayoz, Maria Àngels
AU - Ventosa, Nora
AU - Veciana, Jaume
PY - 2012/4/4
Y1 - 2012/4/4
N2 - The feasibility of the Depressurization of an Expanded Liquid Organic Solution (DELOS) method to process different active pharmaceutical ingredients (APIs) as finely divided powders with narrow particle size distribution, high crystallinity degree, high polymorphic purity, and free from residual solvent has been demonstrated. Cholesterol, acetylsalicylic acid (aspirin), naproxen, acetaminophen, and ibuprofen were chosen as model drugs. It has been demonstrated that the supersaturation ratio attained during crystallization from CO 2-expanded solvents can be modulated through appropriate variations of process parameters - CO 2 content and concentration of the initial solution. In view of the potential application that compressed fluids-based technologies have in the pharmaceutical industry, a preliminary scalability study of the process in compliance with the constraints imposed by the Good Manufacturing Practices (GMP) specifications is presented herein. © 2012 American Chemical Society.
AB - The feasibility of the Depressurization of an Expanded Liquid Organic Solution (DELOS) method to process different active pharmaceutical ingredients (APIs) as finely divided powders with narrow particle size distribution, high crystallinity degree, high polymorphic purity, and free from residual solvent has been demonstrated. Cholesterol, acetylsalicylic acid (aspirin), naproxen, acetaminophen, and ibuprofen were chosen as model drugs. It has been demonstrated that the supersaturation ratio attained during crystallization from CO 2-expanded solvents can be modulated through appropriate variations of process parameters - CO 2 content and concentration of the initial solution. In view of the potential application that compressed fluids-based technologies have in the pharmaceutical industry, a preliminary scalability study of the process in compliance with the constraints imposed by the Good Manufacturing Practices (GMP) specifications is presented herein. © 2012 American Chemical Society.
U2 - 10.1021/cg200356x
DO - 10.1021/cg200356x
M3 - Article
VL - 12
SP - 1717
EP - 1726
JO - Crystal Growth and Design
JF - Crystal Growth and Design
SN - 1528-7483
IS - 4
ER -