Compact and Integrated Approach for Advanced End-to-End Production, Purification, and Aqueous Formulation of Lidocaine Hydrochloride

详细信息    查看全文

• 作者：Jean-Christophe M. Monbaliu ; Torsten Stelzer ; Eve Revalor ; Nopphon Weeranoppanant ; Klavs F. Jensen ; Allan S. Myerson
• 刊名：Organic Process Research & Development
• 出版年：2016
• 出版时间：July 15, 2016
• 年：2016
• 卷：20
• 期：7
• 页码：1347-1353
• 全文大小：407K
• 年卷期：0
• ISSN：1520-586X

文摘

A compact, fully integrated, and automated system is developed for end-to-end production, purification, and formulation of the active pharmaceutical ingredient (API) lidocaine hydrochloride, a widely used local anesthetic. The purification strategy includes appropriate combination of extraction, reactive crystallization, and antisolvent cooling crystallization that enables the production of lidocaine hydrochloride formulated solution, for topical application meeting US Pharmacopeia (USP) standards. On the basis of the optimal yield observed in each step, the system sustains a daily production of 810 doses (dosage strength = 20 mg mL^–1, i.e., 2% formulation in commercial denomination).