Kerc J, Srcic S, Knez Z, Sencar-Bozic P
Lek Pharmaceutical and Chemical Company d.d., Research and Development Division, Celovska 135, 1526, Ljubljana, Slovenia.
Int J Pharm. 1999 May 10;182(1):33-9. doi: 10.1016/s0378-5173(99)00063-0.
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.
来自气体饱和溶液的颗粒,一种用于高压材料加工的新方法,已被用于将实际不溶性的钙通道阻滞剂硝苯地平和非洛地平和降血脂药物非诺贝特微粉化,目的是提高它们的溶解速率,从而提高它们的生物利用度。根据预膨胀条件,微粉化硝苯地平的平均粒径在15至30微米之间,微粉化非洛地平的平均粒径为42微米。另一方面,加工后的非诺贝特由于团聚而粒径增大。通过制备与聚乙二醇4000的药物共沉淀物实现了最高的溶解速率。