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Thank you for registering for our webcast on The Use of Amorphous Solid Dispersions to Enhance Dissolution and Oral Bioavailability of Poorly Water-Soluble Pharmaceutical Compounds

Sponsored by Crystal Pharmatech

Slides can be downloaded here and a recording of the talk can be viewed here.

Wednesday June 20, 2012, 1-2 PM ET

The Use of Amorphous Solid Dispersions to Enhance Dissolution, and Oral Bioavailability of Poorly Water-Soluble Pharmaceutical Compounds

Presented by George Zografi, School of Pharmacy, University of Wisconsin-Madison, Madison, WIUSA

In recent years, the use of amorphous dispersions, consisting of polymers and API, has become a viable option for improving dissolution and bioavailability of poorly soluble pharmaceutical compounds. A number of factors need to be considered when developing these materials and this talk will cover

The structural, thermodynamic and dynamic properties of amorphous solids and how they relate to desired material properties for a dispersion
Analytical methods to determine if the dispersion is miscible or a physical mixture of amorphous drug and polymer
How to inhibit crystallization of API in the solid state during the time frame required for storage and handling
Factors that influence dissolution, supersaturation, and crystallization after administration of an amorphous solid dispersion

Bio: George Zografi ( Edward Kremers Professor Emeritus) received his B.S. in Pharmacy from Columbia University in 1956 and Ph.D. in Pharmaceutical Chemistry from the University of Michigan in 1960. After serving on the faculties of Columbia University and the University of Michigan, he joined the faculty of the University of Wisconsin, and assumed Emeritus status in 2002. His research interests have included: the properties of disordered solids; mechanisms of hygroscopicity; and the surface chemistry of lipids, polymers and proteins in monolayer and bilayer systems. He was the recipient of the APhA Ebert Prize in 1984 and 2001, the AAPS Dale E. Wurster Award for Pharmaceutics in 1990 and its Distinguished Scientist Award in 1995. In 1989, he was elected to the Institute of Medicine of the National Academy of Sciences.

Checkout the other talks in the Crystal Pharmatech Webcast Series on Using Solid Forms to Deal with Poorly Soluble APIs

Wednesday July 25, 2012, 1-2 PM ET

Polymorphism of Drugs - Can We Exploit Physical Form in the Development of Low Solubility Molecules?

Elizabeth Vadas, InSciTech Inc, Montreal Canada

The Holy Grail of drug discovery is to find the perfect molecule that can fulfill all requirements of specificity, potency, safety and efficacy resulting in a major breakthrough in targeting a specific disease. A newly discovered molecule must fulfill a number of other requirements before it can become a viable development candidate. These requirements include having the appropriate biopharmaceutical and pharmacokinetic properties, as well as physicochemical characteristics such as solubility, stability in the solid state and in solution to support the development of a scalable, commercially viable synthetic route and the development of a safe, efficacious and commercially viable dosage form(s).

Many drug molecules exhibit polymorphism and/or exist in various hydrated or solvated forms. The existence of these forms represents both a challenge and an opportunity to the process chemist and to the formulation scientist.

The pharmaceutical scientists must select a form that can be developed into a safe, bioavailable,stable and efficacious dosage form. This can be a formidable challenge, particularly in the case of poorly water soluble molecules. The first hurdle is to provide an appropriate dosing system for

animal toxicology to obtain sufficient exposure to meet regulatory expectations for safety margins. The second hurdle is to design a human dosage form that will support the clinical development program from first in man to late stage clinical studies and ultimately to commercial introduction. The presentation will provide definitions of the various forms, the pros and cons of their use, and illustrate, with some examples, how a challenge can be turned into an opportunity based on a thorough understanding of the physicochemical relationship among the forms.

Bio:Elizabeth B. Vadas received her Ph.D. in Physical Chemistry from McGill University in Montreal. She obtained her undergraduate degree in colloid and surface chemistry in Budapest, Hungary. She joined Merck Frosst, the Canadian subsidiary of Merck & Co. in 1980 as a senior research scientist in the department of Pharmaceutical Research and Development. Over the years she has been involved in the formulation development of many new chemical entities discovered at the Merck Frosst Centre for Therapeutic Research while taking on increasing management responsibilities. From 1991 to 2002 Dr. Vadas was head of Pharmaceutical Research and Development at Merck Frosst. The department, under her leadership, was responsible from early compound characterization to formulation and process development of new chemical entities including the supply of clinical trial materials from phase I through phase III and technical transfer to manufacturing. Notable accomplishments of her department were several products developed for worldwide market introduction. One of the most important of these products from the leukotriene program, leading to worldwide regulatory approval, was SINGULAIR®, Merck’s once a day oral asthma therapy. In mid-2002 Dr. Vadas decided to take early retirement to establish her own consulting company, InSciTech Inc. Currently she works with several drug discovery companies both in the US and Canada providing development expertise. Dr. Vadas has lectured and published widely. She is Past president of CSPS, has been elected Fellow of AAPS and Fellow of CSPS. She has been adjunct professor of pharmaceutics at the University of Montreal for several years. She is the recipient of a number of scientific and management awards.

Listen to the recording of the initial webcast here

Engineering Cocrystal Solubility and Streamlining Cocrystal Early Development

Presented by Naír Rodríguez-Hornedo, Dept. of Pharmaceutical Sciences, University of Michigan, Ann Arbor, MI, USA

Understanding how cocrystal solubility is influenced by cocrystal components and environmental conditions is essential to engineer cocrystals with customized solubility and streamline cocrystal development. This talk will present

Meaningful characterization methods to guide cocrystal and additive selection without the time and material consuming requirements of traditional methods
Key indicators of cocrystal solubility and thermodynamic stability
Overcoming the barriers in cocrystal stability by fine-tuning cocrystal/solution behavior
Critical analysis of cocrystal pHmax and cocrystal-surfactant interactions to highlight key issues on additive selection

Bio: Naír Rodríguez-Hornedo is Associate Professor of Pharmaceutical Sciences at the College of Pharmacy. She received her PhD from the University of Wisconsin Madison. Dr. Rodríguez has developed a research program based on molecular-mechanistic approaches, founded on the premise that the concepts of supramolecular chemistry and crystal engineering can be applied to: (i) design novel pharmaceutical materials with desirable composition, structure and properties, and (ii) understand crystallization pathways and phase transformations that are important in controlling pharmaceutical processes and outcomes. In 2005 Dr. Rodríguez was awarded the Ebert Prize for the best article published in the Journal of Pharmaceutical Sciences. Dr. Rodríguez has served on the FDA Advisory Committee for Pharmaceutical Sciences. She serves on the editorial boards of Crystal Growth and Design, Molecular Pharmaceutics and Journal of Pharmaceutical Sciences.

Listen to the webcast here

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