Micronization and Nanoization of Active Pharmaceutical Ingredients

• 作者: Stefan Mende
• 来源期刊: 物理科学与应用：英文版
• 学科: 物理学
• 关键词: APIS top DOWN process MICRONIZATION BIOAVAILABILITY scale-up GMP REPRODUCIBILITY IQ OQ FAT
• 年，卷（期）: 2018,（3）
• 页码范围: 1-9
• 页数: 9页
• 分类号: O4

摘要

More than 40%of newly discovered drugs have little or no water solubility which presents a serious challenge to the successful development and commercialization of new drugs in the pharmaceutical industry.Additionally,more than 90%of drugs approved since 1995 have poor solubility,poor permeability,or both.Therefore,it may be necessary to increase the dose of a poorly soluble drug to obtain the required efficacy which can lead to more side effects and higher cost to the patient.Performance of drugs can be improved by decreasing the particle size and,at the same time,increasing specific surface area,dissolution rate and the bioavailability of the drug in the human body.The routes of administration are different and listed as 60%for oral,5%for pulmonary,5%for ocular,5%for topical and 25%for injectable,approximately.The injectable drugs are the most interesting ones for nanoization,because smaller particles will increase performance,and will be useful when using micro needles.In a typical manufacturing process of APIs(active pharmaceutical ingredients)top down processes like high pressure homogenization and wet bead milling are used as standard methods to decrease the particle sizes down to a fineness range of 10 to 500 nanometers.