Supercritical Antisolvent Micronization of Minocycline Hydrochloride
Sustainable process-product development & green chemistry
SCF as Solvent Substitutes (T1-8)
Keywords: Supercritical antisolvent, Micronization, Minocycline, Carbon Dioxide, Antibiotic
Minocycline is a second-generation, long-acting tetracycline that penetrates well into the central nervous system (CNS) via blood-brain barrier. In addition to its actions as antibiotic, Mcc has other biologic effects, recently researched, affecting inflammation, proteolysis, angiogenesis, apoptosis, metal chelation, ionophoresis and bone metabolism.
Micronization of minocycline hydrochloride (Mcc) solubilized in ethanol and with supercritical carbon dioxide as antisolvent has been successfully performed using a recently built SAS apparatus. Amorphous particles, in the form of wrinkled shells (balloons), of Mcc ranging from 100 to 1000 nm have been obtained. The mean particle size and the particle size distribution were determined by Scanning Electron Microscope (SEM) and by Dynamic Light Scattering. The quality of the micronized Mcc was analyzed by HPLC to verify if it was acceptable according with the United States Pharmacopeia. The experiments were carried out in order to study the effects of the pressure, temperature, concentration of the liquid solution and the antisolvent/solvent flow ratio on the mean particle size, particle size distribution and quality of the obtained final product.
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Presented Monday 17, 15:40 to 16:00, in session SCF as Solvent Substitutes (T1-8).