Modern Concepts in Pharmaceutical Profiling & Preformulation - APV

seminars
Making
Science
Work
Modern Concepts in
Pharmaceutical Profiling
& Preformulation
From Compound Screening to
Candidate Selection
30 th
September to 1 st
October 2009
Berlin, Germany
Course No. 6246
Arbeitsgemeinschaft für Pharmazeutische
Verfahrenstechnik e.V.
Gemeinnütziger wissenschaftlicher Verein
International Association for
Pharmaceutical Technology
Kurfürstenstraße 59
55118 Mainz / Germany
Phone ++49/6131/9769-0
Telefax ++49/6131/9769-69
e-mail: apv@apv-mainz.de
http://www.apv-mainz.de
Target Group
This course is of interest for all
scientists involved into Pharmaceutical
Profiling and Preformulation
activities at the interface between
drug discovery and early development,
who want to broaden their
knowledge in the field. It is also of
relevance for scientists from Drug
Discovery, Pharmacokinetics and
Toxicology involved into the compound
selection process. Formulation
Scientists, Project Leaders and
Technical Managers will gain valuable
insights into this highly interdisciplinary
area.

seminars
Programme
Wednesday, 30 th September 2009
10.00-18.00 h
Course Introduction/Overview
Dr. Rainer Alex
F. Hoffmann-La Roche Ltd., Basle,
Switzerland
PD Dr. Stefanie D. Krämer
Federal Institute of Technology
Zurich (ETHZ), Zurich, Switzerland
Dr. Regina Moog
F. Hoffmann-La Roche Ltd., Basle
Switzerland
Part 1 – Physico-chemical Profiling-
Basics, Screening & Prediction tools
Physico-Chemical Characterization
– Basic Aspects
PD Dr. Han van de Waterbeemd
Perpignan, France
Tools for Optimization of Solid
State Properties: Pharmaceutical
Salts & Polymorphs
Dr. Christoph Saal
Merck-Serono, Darmstadt, Germany
Automated Salt and Polymorph
Screening
Dr. Kelly Swinney
Johnson & Johnson, Beerse, Belgium
Co-Crystals – A new Approach
Dr. Rolf Hilfiker
Solvias AG, Basle, Switzerland
Compound Solubility Testing
Dr. Alex Avdeef
pION Inc., Woburn, United States
HT Solubility and Dissolution Screening:
Key Elements and Strategies
Dr. Jochem Alsenz
F. Hoffmann-La Roche AG, Basle,
Switzerland
Lipophilicity: Its Calculation and
Application in ADMET Predictions
Prof. Dr. R. Mannhold
Heinrich Heine University Düsseldorf,
Düsseldorf, Germany
Thursday, 1 st October 2009
08.30-16.00 h
Part 2 - Biophamaceutical (PK)
Modeling & Simulation
In vitro Methods for Prediction of
Oral Absorption – for Compounds
and Formulations
Prof. Dr. Peter Langguth
University of Mainz, Mainz,
Germany
Metabolism and Transport Predictions:
in vitro and in silico Tools
PD Dr. Stefanie Krämer
PK Modelling & Simulation:
Tools
Dr. Neil Parrot
F. Hoffmann-La Roche Ltd.,
Basle, Switzerland
Part 3 – Formulation Strategies
Overview of Strategies for Formulation
of Poorly Water Soluble Drugs
Prof. Dr. Jennifer B. Dressman
Johann Wolfgang Goethe University
Frankfurt, Frankfurt, Germany
Formulation Development for Preclinical
Studies (Biology, DMPK and
Toxicology): Concepts and Points to
Consider
Dr. Regina Moog
Early Anticipation of Biopharmaceutical
and Technical Formulation
Issues
Prof. Dr. Martin Kuentz
University of Applied Sciences
Northwestern Switzerland, Basle,
Switzerland
From Preformulation Data to Entry
into Human Strategies
Dr. Jörg Berghausen
Novartis Pharma AG,
Basle, Switzerland
Course Leaders
Regina Moog is a pharmacist by training.
She did her PhD thesis at the
Tumor Biology Center in Freiburg
working on the entrapment of the
cytostatic drug Gemcitabine into
liposomal phospholipid gels and
received her PhD in Pharmaceutical
Technology at the University of Freiburg
(Germany) under the supervision
of Prof. Rolf Schubert in 1998.
Thereafter Regina joined the University
of Tromsø, Norway, first as a
Post-Doc and then as Associate Professor.
In 2000 she joined F. Hoffmann-La
Roche Ltd. (Basel, Switzerland)
starting as lab head in Pharmaceutical
and Analytical R&D in
the field of Pharmaceutical Profiling.
In this role she worked on the physicochemical
and biopharmaceutical
characterization of numerous challenging
compounds e. g. BCS 2/4 or
unstable molecules. She developed
exploratory formulations for pre-clinical
studies, supported the clinical
candidate selection and was responsible
for the EIH formulation strategy.
In 2004 Regina has been assigned
head of the preformulation
group being also responsible for the

Modern Concepts in Pharmaceutical
Profiling & Preformulation
a seminar organised by the APV focus group
Biopharmacy and Pharmacokinetics
development and the supply of formulations
used in all preclinical and
toxicological studies up to launch.
Rainer Alex studied Pharmacy at the
University of Tübingen, Germany,
and received his PhD in Pharmaceutical
Technology from the University
of Munich, Germany. After a postdoctoral
fellowship at the University
of Texas at Austin, USA, he joined
F. Hoffmann - La Roche Ltd. in Basel,
Switzerland in 1989 as a lab leader in
Pharmaceutical R&D, where he got
involved into preformulation activities.
Later on he was heading the
Pharmaceutical and Analytical R&D
department at Roche in Basel. In
2005 he joined the Global Technical
Sciences Organization in Pharma
Research, where he is in charge of
strategic coordination in Pharmaceutical
and Analytical R&D. Dr. Alex
is also a lecturer in Life Science
Engineering at the University of
Karlsruhe, Germany.
Stefanie D. Krämer is a Senior Lecturer
(Privatdozentin) in Biopharmacy
at the Institute of Pharmaceutical
Sciences at the ETH Zürich
(Switzerland). She is a pharmacist by
training (ETH Zürich) and has received
her PhD degree in the Biopharmacy
group of Heidi Wunderli-
Allenspach at the ETH. She accomplished
two post-docs, one at Sanofi-Recherche
in Montpellier (F) on
the characterization of physicochemical
properties of compounds, the
other one in London at King’s College
with David J. Begley and N. Joan
Abbott where the focus was on
blood-brain barrier models. Since
the year 2000 she is back at the ETH
where she completed her habilitation
on “drug interactions with lipid
bilayers and P-glycoprotein” in 2007.
Current research in Biopharmacy
focuses on drug-interactions with
lipid bilayers, including bilayer permeation,
on P-glycoprotein and on
the influence of the lipid environment
on the processing of amyloidprecursor
protein. Since 2008 she is
also a member of the group of
Radiopharmaceutical Science at the
ETH where she is involved in the in
vitro characterization of potential
new PET tracers. Stefanie teaches
“Biopharmacy” at the Bachelor level
and “Biotransformation of Drugs
and Xenobiotics” on the Master
level.
Objectives
Pharmaceutical Preformulation
plays a key role in rational formulation
design and drug development.
While focusing mostly on physicochemical
characterization of preselected
drug candidates in the past,
pharmaceutical preformulation
strategies nowadays include a broader
range of activities and play a role
in the candidate screening and selection
process. In addition, preformulation
activities support initial
formulation screening and provide
valuable input for early formulation
concepts for preclinical and clinical
testing. This course will address the
various aspects of modern pharmaceutical
profiling and preformulation.
The first part will provide an introduction
into the basic aspects of
physico-chemical profiling and will
review recent developments related
to automation, high throughput
techniques and parallel testing.
Miniaturisation of assays and automation
technologies have enabled
profiling activities not only at earlier
stages with smaller compound
quantities but also allow the characterization
of a higher number of
compounds or parallel testing of
different experimental conditions.
In the second part in vitro and in
silico tools for the biopharmaceutical
and pharmacokinetic evaluation
of drug candidates will be addressed.
This includes prediction of
single ADMET processes including
drug absorption, efflux transport
and metabolism as well as modelling
of complex pharmacokinetic
behaviour.
As early formulation ideas and concepts
are developed and tested in
the preformulation phase, the third
part of the course will discuss relevant
aspects related to solubility
improvement of poorly water
soluble compounds, options for
increasing compound exposure in
tox studies and the application of
preformulation information to devise
the formulation strategy for entry
into human studies.
Programme is subject to change

Date
Course No. 6246
from 30 th Sept. 2009 10.00 h
to 1 st Oct. 2009 16.00 h
Location
Golden Tulip
Berlin - Hotel Hamburg
Landgrafenstr. 4
10787 Berlin, Germany
Phone: ++49/30/26477-0
Telefax: ++49/30/262-9394
seminars
Organisation
Registration
Registration fee
APV member 1360 EUR
Non-member 1490 EUR
(free of VAT according § 4,22
UStG)
Coffee breaks, lunch, dinner
and proceedings included.
Members of authorities pay
half of the APV member’s and
non-member’s registration fee
respectively.
Accounts
Dresdner Bank AG Mainz
Konto Nr. 2 325 159 00
BLZ 550 800 65
Postbank Frankfurt/M.
Konto Nr. 127 35-606
BLZ 500 100 60
Registration
APV-Geschäftsstelle
Kurfürstenstraße 59
55118 Mainz / Germany
Phone ++49/6131/9769-0
Telefax ++49/6131/9769-69
e-mail: apv@apv-mainz.de
You will receive a confirmation
of your registration with the
invoice.
Seminaranmeldung / Registration
per Telefax ++49/6131/9769-69
oder per Post an/or by postal service to:
APV Arbeitsgemeinschaft für
Pharmazeutische Verfahrenstechnik e.V.
Kurfürstenstraße 59
D-55118 Mainz
Hotel reservation
Golden Tulip
Berlin - Hotel Hamburg
Landgrafenstr. 4
10787 Berlin, Germany
Phone: ++49/30/26477-0
Telefax: ++49/30/262-9394
Participants should make their
own hotel reservation referring
to the APV seminar.
Deadline for the special
conference rate:
2 nd September 2009
Special rate:
Single room incl. breakfast
buffet from EUR 124,00 per
night.
Mainz, April 2009
Veranstaltung/Course No. 6246
Titel/Title: Modern Concepts in Pharmaceutical Profiling
& Preformulation
in Berlin, Germany, 30 th September to 1 st October 2009
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