Micronization of drugs using supercritical carbon dioxide.
Particles from gas saturated solutions, a novel method for high pressure material processing, has been used for micronization of practically insoluble calcium-channel blockers nifedipine and felodipine and the hypolipidemic agent fenofibrate with the aim of increasing their dissolution rate and hence their bioavailability. Dependent on the pre-expansion conditions, a mean particle size of between 15 and 30 microm was achieved for micronized nifedipine and 42 microm for micronized felodipine. The particle size of processed fenofibrate, on the other hand, increased due to agglomeration. The highest dissolution rate was achieved by preparation of drug coprecipitates with PEG 4000.
Kerc
J
J
Lek Pharmaceutical and Chemical Company d.d., Research and Development Division, Celovska 135, 1526, Ljubljana, Slovenia.
Srcic
S
S
Knez
Z
Z
Sencar-Bozic
P
P
D001682:Biological Availability; D002121:Calcium Channel Blockers / Q000737:chemistry* / Q000493:pharmacokinetics; D002245:Carbon Dioxide / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000295:instrumentation / Q000379:methods*; D015736:Felodipine / Q000737:chemistry* / Q000493:pharmacokinetics; D011345:Fenofibrate / Q000737:chemistry* / Q000493:pharmacokinetics; D000960:Hypolipidemic Agents / Q000737:chemistry* / Q000493:pharmacokinetics; D009543:Nifedipine / Q000737:chemistry* / Q000493:pharmacokinetics; D010316:Particle Size; D012995:Solubility; D012996:Solutions
D002121:Calcium Channel Blockers; D000960:Hypolipidemic Agents; D012996:Solutions; D002245:Carbon Dioxide; D009543:Nifedipine; D015736:Felodipine; D011345:Fenofibrate