Department of Pharmaceutics, London School of Pharmacy, London, UK.
Obes Facts. 2010 Aug;3(4):231-7. doi: 10.1159/000319450. Epub 2010 Aug 9.
To compare the pharmaceutical quality of Xenical (chemically produced orlistat) with nine generic products, each produced by fermentation processes.
Xenical 120 mg capsules (Roche, Basel, Switzerland) were used as reference material. Generic products were from India, Malaysia, Argentina, Philippines, Uruguay, and Taiwan. Colour, melting temperature, crystalline form, particle size, capsule fill mass, active pharmaceutical ingredient content, amount of impurities, and dissolution were compared. Standard physical and chemical laboratory tests were those developed by Roche for Xenical.
All nine generic products failed the Xenical specifications in four or more tests, and two generic products failed in seven tests. A failure common to all generic products was the amount of impurities present, mostly due to different by-products, including side-chain homologues not present in Xenical. Some impurities were unidentified. Two generic products tested failed the dissolution test, one product formed a capsule-shaped agglomerate on storage and resulted in poor (</=15%) dissolution. Six generic products were powder formulations.
All tested generic orlistat products were pharmaceutically inferior to Xenical. The high levels of impurities in generic orlistat products are a major safety and tolerability concern.
比较罗氏公司（瑞士巴塞尔）生产的化学合成奥利司他（商品名：赛尼可）与 9 种采用发酵工艺生产的仿制药的药品质量。
以罗氏公司生产的赛尼可 120mg 胶囊作为参比制剂，仿制药分别来自印度、马来西亚、阿根廷、菲律宾、乌拉圭和中国台湾地区。比较了颜色、熔点、晶体形态、粒径、胶囊填充质量、主药含量、杂质含量和溶出度。采用罗氏公司为赛尼可开发的标准理化实验室检测方法进行检测。
9 种仿制药在 4 项或更多检测项目中不符合赛尼可的标准，有 2 种仿制药在 7 项检测中不合格。所有仿制药都存在共同的缺陷，即杂质含量较高，主要是由于不同的副产物，包括赛尼可中不存在的侧链同系物。一些杂质尚未鉴定。有 2 种仿制药的溶出度检测不合格，有 1 种产品在储存过程中形成胶囊状团聚，导致溶出度较差（</=15%）。6 种仿制药为粉末制剂。
所有检测的仿制药奥利司他在药品质量上均劣于赛尼可。仿制药奥利司他中存在的大量杂质是一个严重的安全性和耐受性问题。
