报告题目：Pharmaceutical Cocrystals: Route of Molecules to Patient-Centric Medicine

报告人：德蒙福特大学李明忠教授

报告时间：2019年9月19日，14:30~16:30

报告地点：信息学馆228

邀请人：工业人工智能与自动化系常玉清教授

摘要

Oral solid dosage forms are the most popular and convenient methods for drug delivery. However, in current drug discovery on average only 5 out of every 5000 potential dugs are actually tested in clinical trials and of these only 1 will eventually be approved for use in patients. This poor turnaround is due to their toxicity, poor efficacy and in particular poor biopharmaceutical properties caused by their low solubility and slow dissolving rates. The cocrystal approach has emerged as a means to overcome the poor aqueous solubility of drug candidates, in particular for those the traditionally developed formulation approaches cannot be applied. By diversifying the number of crystal co-forms that exist for a particular drug, cocrystals can lead to improvements in solubility, dissolution rate, physical and chemical stability as well as in mechanical properties. However, limitations exist that a stable form of the parent drug tends to recrystallize during dissolution and subsequently lose its improved properties. Studies on phase transformation and release profiles gave evidence that various polymers could act as precipitation inhibitors during cocrystal dissolution. Meanwhile, it was suggested that interactions of the polymers with the surfaces of cocrystals might be the underlying mechanism. Unfortunately, evidence which could thoroughly explain such mechanisms at the molecular level is still largely lacking. The talkwill report a systematically study from Prof. Li’s research group at De Montfort University using combined experimental and molecular dynamic simulation approaches to reveal the dissolution and precipitation mechanisms of the cocrystals. The research provided insights into the mechanisms of cocrystal dissolution and how the polymeric excipients exhibited their inhibitory functions for precipitation, which were of great value to the development of novel cocrystal-based formulations.

报告人简介

Prof. Mingzhong LI is a Professor of Crystallisation Science and Drug Delivery in Leicester School of Pharmacy at De Montfort University (DMU). He gained his PhD in control and instrumentation engineering in 1998 from Northeastern University in China. After graduation, he worked at several world leading universities as a research fellow, i.e., the Hong Kong University of Science and Technology, Heriot-Watt University and University of Oxford. He took his first permanent academic post as a Senior Lecturer in the Leicester School of Pharmacy at DMU in 2006 and was promoted to a Professor in 2019. His research is largely interdisciplinary focusing broadly on the field of the crystallisation science and engineering, oral drug formulation design and delivery and pharmaceutical product manufacturing, including fundamental study of crystal/cocrystal thermodynamics and kinetics associated with nucleation and crystal growth, development and use of process analytical techniques for crystallisation/granulation monitoring and control, design of enabling formulation strategies for poorly water soluble drugs, development of in vitro dissolution testing for drug product design and quality assurance, and modelling techniques for reactor hydrodynamics and molecular interaction of drugs, excipients and/or solvents. He has published over 70 scientific peer reviewed journal papers in high quality journals.