报告内容:
1．Enhancing the Elimination of Toxic Heavy Metals
报告人：Michael Jay
Fred N. Eshelman Distinguished Professor of Biomedical Engineering
Executive Vice Dean and Chief Academic Officer at University of North Carolina-Chapel Hill Eshelman School of Pharmacy
2. Amorphous Forms of Drugs for Improved Oral Bioavailability
报告人：Robin Bogner Professor of Pharmaceutics
Department of Pharmaceutical Sciences
School of Pharmacy
University of Connecticut
报告时间：2017年11月30日（周四）12:30-14:30
报告地点：8797威尼斯老品牌东十一楼楼顶平台（八楼楼顶）
报告人简介：
Dr. Michael Jay received his Ph.D. in Pharmaceutical Sciences in 1980 and began an academic career that included appointments at the University of Connecticut Health Center (Nuclear Medicine), the University of Kentucky (Medicinal Chemistry & Pharmaceutics) and the University of North Carolina (Pharmacoengineering & Molecular Pharmaceutics) where he currently serves as the Fred Eshelman Distinguished Professor and Chair. He has over 35 years of experience working at the interface of the pharmaceutical and imaging sciences. For nine years, he served as the director of the Center for Pharmaceutical Science & Technology at the University of Kentucky which housed an FDA-registered cGMP manufacturing facility and operated as a fully-integrated pharmaceutical development organization. He has received several honors including the Berson-Yalow Award from the Society of Nuclear Medicine and the Distinguished Teaching Award at University of North Carolina, and was elected as a Fellow of the American Association of Pharmaceutical Scientists. He has published 145 peer-reviewed scientific manuscripts, 10 patents and received in excess of $20 million in research support.
Title: Enhancing the Elimination of Toxic Heavy Metals
Abstract: Heavy metal poisoning is an increasing concern of industrialized societies. The metals that have recently been gaining public attention include lead (Pb) (e.g., water supply in Flint, Michigan USA), cadmium (Cd) (contaminated soil, Hunan Province, China), gadolinium (Gd) from MRI procedures (USA, Japan, Europe) and radioactive metals such as americium (Am) and plutonium (Pu) following a nuclear terrorism event (worldwide). The urinary excretion of many of these heavy metals can be enhanced by the administration of multi-valent chelating agents like diethylene-triamine-penta-acetic acid (DTPA). However, because these chelating agents are highly charged, their bioavailability after oral administration is very low; thus, they must be administered intravenously. This is not very convenient for patients who require chelation therapy over a period of weeks to month. We have developed an analog of DTPA called C2E2 that is orally bioavailable and capable of binding several heavy metals. We demonstrated that it was effective in removing the body burden of Gd and Am in contaminated animals. The drug has undergone extensive safety-toxicology tests, and a cGMP manufacturing method has been developed. An Investigational New Drug (IND) application was submitted to the US FDA which is now active. In this seminar, we will present data on the competitive binding of C2E2 and various blood elements for Gd and Am, and will demonstrate that an appropriate dosing regimen based on the pharmacokinetics of C2E2 and the toxicokinetics of heavy metals reduces the tissue burden of these metals, thereby reducing their toxicity.
2. Dr. Bogner is Professor of Pharmaceutics in the Department of Pharmaceutical Science at the University of Connecticut where she is also a member of the Institute of Materials Science. She received her B.S. in Pharmacy from Rutgers University, M.S. from the University of Iowa, and Ph.D. from Rutgers University after which she joined the faculty of the University of Connecticut. Dr. Bogner’s research interests are focused on the characterization and dissolution of pharmaceutical solids, both freeze-dried parenterals and oral dosage forms. The amorphous form of drugs and the implications of partially crystalline systems are a more recent interest. Dr. Bogner has a patent and many publications. She has served on several editorial boards, a USP committee, an FDA advisory committee and in various leadership roles in American Association of Pharmaceutical Scientists. Dr. Bogner is a Teaching Fellow at the University of Connecticut, and Fellow of the AAPS.
Title: Amorphous Forms of Drugs for Improved Oral Bioavailability
Abstract: Many therapeutic drug candidates are poorly soluble, which can limit the oral dose that can be absorbed. There are several approaches to improve the oral bioavailability of poorly water-soluble drugs. One approach that provides a large increase in bioavailability is amorphization. The amorphous (or non-crystalline solid) form dissolves to form a supersaturated solution. However, supersaturated solutions are not stable and precipitation can occur before the maximum theoretical concentration can be reached. Predictions of the maximum theoretical concentration have been refined to provide a tool for deciding whether to pursue the amorphous approach for improving oral bioavailability. Two predictive models will be discussed. During dissolution of the amorphous form, the concentration of the metastable supersaturated solution declines toward equilibrium with the lower energy state crystalline form. The time course of the decline in concentration can affect the bioavailability. Processing and the composition of the dissolution fluid can alter the time course of the solution mediated phase transformation to the poorly soluble form of the drug, which can affect oral bioavailability.
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