Particle design of poorly water-soluble drug substances using supercritical fluid technologies.
In order to improve the dissolution properties of poorly water-soluble drugs, some drugs were subjected to micronization or prepared as composite particles using supercritical fluid (SCF) technology with carbon dioxide (CO(2)). Solubility in CO(2) is the key when using this method. Solubility affects the supersaturation of the materials in the solvent as well as the mass transfer of that solvent, which are both critical to the micronization of the materials and the formation of the composite particles. Some useful techniques that can be used to avoid the problems posed by the characteristics of the drug itself are combining SC-CO(2) with other technologies, such as the formation of coacervates or emulsions, and other equipment types, such as milling or ultrasound fields. Another advantage of SCF technology is that it is considered to be green chemistry. SC-CO(2) can improve the solubility of poorly water-soluble drug substances using few or no organic solvents and with little or no heating.
Yasuji
Takehiko
T
Pharmaceutical Research and Technology Labs, Astellas Pharma Inc., 180 Ozumi, Yaizu, Shizuoka 425-0072, Japan.
Takeuchi
Hirofumi
H
Kawashima
Yoshiaki
Y
D002245:Carbon Dioxide / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D025924:Chromatography, Supercritical Fluid / Q000379:methods*; D010316:Particle Size; D010592:Pharmaceutic Aids / Q000737:chemistry; D004364:Pharmaceutical Preparations / Q000737:chemistry*; D012995:Solubility; D013678:Technology, Pharmaceutical / Q000379:methods*
D010592:Pharmaceutic Aids; D004364:Pharmaceutical Preparations; D002245:Carbon Dioxide