Nanosizing of Poorly Water Soluble Compounds UsingRotation/Revolution Mixer

摘要

In this study, nanoparticles of various poorly water soluble compounds were prepared by wet milling thatwas carried out using a rotation/revolution mixer and zirconia balls. To be compared with Beads mill,rotation/revolution mixer has superior in very quick process (5 min) and needs very few amounts of zirconia balls(2.4 g) for pulverizing drugs to nanometer range. Phenytoin, indomethacin, nifedipine, danazol, and naproxenwere selected as the standard poorly water soluble compounds. Various parameters of the rotation/revolutionmixer were studied to decide the optimal pulverization conditions for the production of nanoparticles of theabovementioned compounds. The rotation/revolution speed, shape of the mixing vessel, amount of zirconia balls,and volume of the vehicle (methylcellulose solution) mainly affected the pulverization of the compounds. Usingthe mixer, phenytoin could be pulverized to nanoparticles within a few minutes. The particle size was confirmedby using a scanning electron microscope and a particle size analyzer. The crystallinity of the pulverized pheny-toin particles was confirmed by X-ray diffractometry (XRD) and differential scanning calorimetry (DSC). It wasobserved that the pulverized phenytoin particles retained their crystallinity, and amorphous phenytoin was notdetected. Particles of other poorly water soluble compounds were also reduced to the nanometer range by usingthis method.