Preliminary Program - American Association of Pharmaceutical ...

60
2009 AAPS Annual Meeting and Exposition
Physical Pharmacy and Biopharmaceutics (PPB) Programming
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Sunday, November 8, 2009
8:00 am – 4:00 pm
Rational Design and Development of
Solid Dispersions with Amorphous Drug
for Improving Oral Bioavailability
Short Course #6
An additional fee is required to attend this short course
It has been estimated that over 50% of the new
chemical entities (NCEs) are too insoluble for
efficient oral absorption. Increasing dissolution
rate and in vivo exposure of poorly soluble drugs
by the use of high energy solids (e.g., amorphous
state) and the application of polymer matrices for
delivery purpose have been broadly employed. In
recent years, there has been a large increase in the
number of scientific publications and patents in
this area of research. Reports in the literature have
shown remarkable enhancement in dissolution
rates and enhanced oral absorption of high energy
solids generated by spray drying, antisolvent
precipitation, and hot-melt extrusions. The advances
in fundamental understanding of high energy solids
as well as development of practical approaches
to overcome inherent limitations with high energy
solids have made the field highly attractive for
pharmaceutical scientists. However, discussions on
recent exploration of high energy solids and related
technical challenges at national and international
forums have been limited. Although some aspects
of amorphous systems, solid dispersions, crystal
engineering, etc., were presented in different
meetings, there was no general discussion of
various aspects of amorphous solids in one forum.
This short course will focus on all aspects of high
energy, amorphous solids and related drug product
development, including generating amorphous
materials via different manufacturing processes,
selecting polymer to stabilize the amorphous state,
making appropriate formulations intended for oral
administration, characterizing and understanding
solid state physical stability, applying appropriate
analytical methodologies, etc. All of these
aspects will profoundly influence the scientific
community of formulation scientists and analytical
scientists for exploration of amorphous solids and
facilitating technical breakthroughs in this field.
Numerous challenges exist in consistently and
reproducibly generating amorphous solid materials,
characterizing of amorphous solids regarding its
in vitro performance, selecting and optimizing
the appropriate polymeric matrices for achieving
physical stability, selecting desired manufacturing
process (e.g., spray drying, hot-melt extrusion, etc.)
with optimal conditions, and achieving improved in
vivo exposure, and developing formulation products
intended for oral use. This short course will focus on
all aspects of amorphous solids towards successful
oral delivery of insoluble compounds.
Moderators
Ping Gao, Ph.D.
Abbott Laboratories
Jiansheng Tang, Ph.D.
Mylan Pharmaceuticals, Inc.
Eric Munson, Ph.D.
University of Kansas
Crystallization and Stabilization of
Amorphous Solids
Lian Yu, Ph.D.
University of Wisconsin-Madison
Enablement of Drug Discovery through
Supersaturation and Amorphous Solids
Michael J. Hageman, Ph.D.
Bristol-Myers Squibb
Crystallization from Amorphous Systems
Lynne Taylor, Ph.D.
Purdue University
Assessing and Optimizing Supersaturation
in Amorphous Solids and Dispersions
Marcus Brewster, Ph.D.
Johnson & Johnson
Predicting Amorphous Drug Stability in Drug
Formulations
Eric Munson, Ph.D.
University of Kansas
Characterization of In Vitro Release Attributes
of Amorphous Solids and their Relevance to
In Vivo Absorption
Ping Gao, Ph.D.
Abbott Laboratories
Turning Challenges into Opportunities:
Formulation Development for Poorly Soluble
Drugs — The Meltrex Approach
Ulrich Westedt, Ph.D.
Abbott Laboratories
Enhancing Bioavailability of Low Solubility
Compounds: Amorphous Dispersion Delivery
Platforms
David Vodak, Ph.D.
Bend Research Inc.
Monday, November 9, 2009
MONDAY MORNING ROUNDTABLES
Funded by a Grant from
8:00 am – 10:00 am
Optimization of Systemic Exposure in
Preclinical and Clinical Development:
“Success Stories” of Proven Methods for
Challenging Drug Candidates — What
You Did Not Already Know!
Roundtable
The identification and development of new drug
candidates with a desirable systemic exposure
that is both efficacious and safe in humans
with “developable” formulations based on
preclinical data remains a major challenge in the
pharmaceutical sciences. One reason is that oral
systemic exposure is determined by a variety of
physicochemical and metabolic factors including
drug solubility, permeability, dissolution, dosage
forms, as well as, first-pass, transporter effects,
and varying gastrointestinal physiology. Another
reason is that multidisciplinary teams often cannot
reach consensus which formulation and modeling
approaches can be used with confidence to select
a dosage form for first in human studies. Thus,
science driven strategies to determine the systemic
exposure rate limits will be presented based on
new compounds and new data to correct analysis
of factors controlling exposure for drugs of all
BCS classes. When low exposure is seen, there
can be the incorrect perception that formulation
improvement works for every compound. In other
cases, controlled release formulations should be
attempted to optimize the PK profiles. Modeling and
simulation are also meaningful tools in designing
PK/formulation/ADME/TK studies, as well as,
species scaling to human. Specific formulation
strategies, and proven modeling approaches that
can be used when facing different BCS classification
compounds will be shared. In addition, the role
of transporters in drug disposition with a focus
on BCS Class II-IV drugs will be discussed, as well
as, science-driven optimization of formulation
selection studies for clinical trials and final
marketing formulations.
Moderators
Tycho Heimbach, Ph.D., M.S.
Novartis
Hyo-Kyung Han, Ph.D.
Chosun University