Drug Applied Research Center, Research Committee and Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
Biotechnology Research Center, and Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
Pharm Dev Technol. 2024 Apr;29(4):353-358. doi: 10.1080/10837450.2024.2334754. Epub 2024 Apr 8.
One of the widely used approaches for improving the dissolution of poorly water-soluble drugs is particle size reduction. Ball milling is a mechanical, top-down technique used to reduce particle size. The effect of ball number, ball size, and milling speed on the properties of milled Aprepitant is evaluated. A full factorial design was employed to investigate the influence of affecting factors on particle size reduction. The initial suspension was made by suspending the drug in distilled water using excipients followed by milling in a planetary ball mill. Ball size, ball number, and milling speed modulated particle size distribution of Aprepitant. Increasing the number of balls from minimum to maximum for each ball size led to approximately a 28% reduction in mean particle size, a 37% decrease in , and a 25% decrease in the ratio of volume mean particle diameter to numeric mean particle diameter. On average, using 10 mm balls instead of 30 mm balls reduced mean particle size by 1.689 µm. As a result, ball size, ball number, and milling speed are three effective factors in the process of ball milling. By increasing the ball number and decreasing the ball size, efficient micronization of drug particles takes place and the particle size is more uniform.
一种广泛应用于提高难溶性药物溶解性能的方法是减小粒径。球磨是一种机械的自上而下的技术，用于减小粒径。研究了球的数量、球的大小和研磨速度对研磨阿瑞匹坦性能的影响。采用完全析因设计研究了影响因素对粒径减小的影响。初始悬浮液是通过将药物在赋形剂存在的情况下悬浮在蒸馏水中，然后在行星式球磨机中研磨制得。球的大小、球的数量和研磨速度调节了阿瑞匹坦的粒径分布。对于每种球的大小，将球的数量从最小增加到最大，导致平均粒径减小约 28%， 减小 37%，体积平均粒径与数字平均粒径的比值减小 25%。平均而言，使用 10mm 球代替 30mm 球可使平均粒径减小 1.689μm。因此，球的大小、球的数量和研磨速度是球磨过程中的三个有效因素。通过增加球的数量和减小球的大小，可以实现药物颗粒的高效微细化，并且粒径更加均匀。
