EUROPEAN CONTINUING
EDUCATION COLLEGE

COURSES FOR 2006

PHARMACEUTICAL PREFORMULATION

A THREE DAY INTENSIVE COURSE WITH THE EMPHASIS o­n CURRENT TECHNIQUES AND DESIGN OF PREFORMULATION STUDIES

20^th, 21^st and 22^nd March 2006, Kensington Park Hotel,London, U.K.

COURSE BACKGROUND

The purpose of preformulation research can be considered to be the optimisation of the physicochemical properties (and thus the biopharmaceutical properties) of drug substances for the design of drug delivery systems. With such a wide remit it embraces aspects of physical, analytical, medicinal chemistry and pharmaceutics. The use of combinatorial chemistry and rapid high-throughput in vitro screening has placed high demands o­n the ability of physical pharmacy or preformulation groups to keep pace and provide thorough physicochemical profiling of potential drug candidates prior to candidate drug selection and formulation development. Indeed, too rigid an approach to the exquisite optimisation of lead compounds for high receptor or enzyme specificity can mean that drug delivery issues are ignored completely. While the course will cover aspects of physical pharmacy and chemistry that relate to formulation science, participants will be encouraged to apply physical pharmacy concepts to the provision of drug delivery orientated input into all stages of the drug discovery process as well as exploratory drug development. For faster drug development to take place, up-to-date and smarter preformulation is a prerequisite.

COURSE OBJECTIVES

The principal objectives of the course are to provide a comprehensive understanding of preformulation for all those engaged in the generation and profiling of new drug candidates, particularly in research based organisations. The Course will provide individuals with relevant and up-to-date information pertinent to their job function.

WHO SHOULD ATTEND?
The Course will benefit Managers and Scientists working in pharmaceutical formulation, research and development and be highly relevant to those working at the drug discovery interface. It will also benefit Chemists and Pharmacists and others who wish to review current techniques and to understand the relevance of drug delivery orientated preformulation to the processes of drug discovery and drug development

COURSE OUTLINE

INTRODUCTION

The concept of preformulation. An overview of its importance and background to the design of an appropriate preformulation programme tailored to the envisaged product profile.

PIVOTAL PROPERTIES

SOLUBILITY
An overview of this pivotal property and other related properties, including solubility measurement and manipulation, partition coefficients, solvent and ion effects, dissolution rates, partition coefficients, links with permeability and absorption.

SOLID STATE PROPERTY

A review of the important properties of solids and a critical examination of the experimental techniques available. Characteristics to be considered include crystallinity, habit, polymorphism, moisture sorption behaviour, particulate properties and the use of crystal engineering and salt selection to manipulate drug delivery properties and performance.

STABILITY
Theoretical background; principles and techniques of assessment. Also to include methods of excipient compatibility testing together with interpretation and critical evaluation.

PIVOTAL CONCEPTS

THE RIGHT PREFORMULATION PROGRAMME FOR THE RIGHT TIME
Development of the concept of an evolving preformulation programme to meet the differing needs of the stages of drug discovery/development. Evaluation of suitable preformulation input at each stage to include the in vitro screening stage, the animal screening stage, the candidate selection stage and the early development stage.

TAILORED PREFORMULATION PROGRAMMES
Consideration will be given to the design of specific preformulation programmes for different drug delivery routes e.g. an introduction to the theoretical background, principles and mechanism of powder compression for tablet manufacture.

CASE STUDIES
CASE Studies concerned with preformulation will be presented.

LECTURERS

ROBERT T. FORBES B.Pharm., Ph.D., M.R.Pharm.S.
Dr Forbes is Reader in Pharmaceutics within the School of Pharmacy at the University of Bradford, UK. He received his B.Pharm. in Pharmacy andPh.D. in the pharmaceutics of salt selection (1991) from the University of Bradford. He qualified as a UK registered pharmacist in 1987 and after completing his Ph.D. undertook postdoctoral work at the Astra Research Center, Sweden, where he studied aspects of modifying release through salt formation. In 1992 he joined Astra Arcus AB, Sweden, where he became preformulation group leader with responsibilities for pharmaceutical aspects of candidate drug selection including the optimisation of solid-state properties. He joined the academic staff at Bradford in 1995. His academic and industrial research efforts have centered o­n the material science of drugs, excipients and formulated products. He retains an interest in the study of small drug molecules but since returning to Bradford his research has also been directed towards the stabilisation and formulation of proteins and the use of macromolecules as excipients.

IAN GRIMSEY B.Sc., Ph.D., M.R.S.C. C.Chem.
Dr Grimsey is a Senior Lecturer in Pharmaceutics at Bradford University. Previously he was at the British Petroleum Research Centre at the University of Sheffield Chemical Engineering Department. Dr Grimsey has extensive knowledge of Surface characterisation particle sizing systems, and process scale-up. He has a special interest in the manipulation of particle formation to provide materials with enhanced characteristics for secondary processing.

GERRY STEELE BSc., MSc., Ph.D., CChem., M.R.S.C.
Dr Steele is a crystallisation specialist within process engingeering at AstraZeneca R & D Charnwood where he has built upon his experience of the physicochemical characterisation of candidate drugs, excipients and formulations at AstraZeneca where he was a preformulation team leader. He was previously Scientific Manager for Characterisation at Inveresk Research International. Dr Steele has been involved in the physical pharmacy/preformulation area since 1985 and has had very wide experience of candidate drugs, formulation types and analytical techniques.

RICHARD STOREY BPharm, Ph.D., MRPharmS.
Dr Storey is Team Manager of the Solid Form Group, Preformulation and Biopharmaceutics at AstraZeneca and was previously principal materials scientist at Pfizer Central Research where he had responsibilites for the physicochemical characterisation of candidate drugs, excipients and formulations at Pfizer. He was previously a scientist at Bradford Particle Design. Dr Storey has been involved in the physical pharmacy/preformulation area since 1993 and has had very wide experience of candidate drugs, formulation types and analytical techniques. He is chair of the Materials Science focus group of the Academy of Pharmaceutical Scientists.

STEVE JAMES ELLIOTT BSc (Hons)
Mr Elliott recently joined Sirius Analytical Instruments ltd. to concentrate o­n instrument and assay development in the area of physicochemical profiling of drug substances. He has a 15-year history in the pharmaceutical industry where he worked for Aventis (formally Rhone Poulenc) in the areas of analytical quality control and physical chemistry. His last 3 years were spent developing high throughput methods for determination of physicochemical properties, including log P/D, solubility and pKa. During this time, he specialised in the application of fast chromatography methods, with multi-detection systems (UV ELSD N2), and nephelometric detection to address the need for physicochemical profiling. An integral part of his work was developing a suitable system to manage the resultant data.

MICHAEL BONNER BSc PhD MRPharmS
Dr Bonner is Lecturer in the Drug Delivery Group within the School of Pharmacy at the University of Bradford. He has a wide knowledge of pharmaceutical systems, with expertise in the physicochemical aspects of the formulation of transdermal systems and rheology. He has published learned articles in these areas and is a co-author of an undergraduate text book.

STEVE COSGROVE PhD
Dr Cosgrove is an Associate Principal Scientist within the Pharmaceutical and Analytical function at AstraZeneca R & D. He has over 10 years experience in the solid state field and has applied this experience to a wide range of pharmaceutical projects from very early phase to late phase III. He currently manages a team dealing with all analytical aspects of early phase projects.

JANET MAAS PhD
Dr Maas is a Senior Scientist in Drug Discovery at Novartis and has spent over 15 years in industrial drug development. Currently she heads up the preformulation laboratory in Drug Discovery Research at Novartis. Her current interests include solubility determination and physicochemical characterization of new chemical entities for both oral and inhalation routes.

ABOUT THE COLLEGE

The European Continuing Education College, is now well established worldwide as the leading provider of up-to-date, pragmatically orientated, relevant short courses for Managers, Scientists, Engineers and Technicians. The College specialises in Courses for the pharmaceutical, biotechnology and healthcare industries. These courses are tailor-made to the requirements of the industry and as a result provide information of tremendous benefit to those who may not necessarily be at the forefront of knowledge in a particular area. Over the years our pharmaceutical courses, under the Direction of Professor Mike Rubinstein, have proved extremely popular and are often heavily oversubscribed. This success is mainly due to the very careful selection of material and lectures for the Courses, to the provision of workshops, clinics, case studies and discussion sessions, to the very extensive course notes provided and to small group participation.

Presenters are very carefully chosen from academia and the industry who are both experts and accomplished teachers and great care is taken to ensure that the Courses are right up-to-date and that there is proper integration of both the theoretical and practical considerations of the subject. All material is reviewed and assessed to make sure it is pertinent and relevant. Demonstrations, Case Studies and Workshops of actual pharmaceutical equipment, processes and methods are general features of most of the College courses. In addition most of our courses include problem solving sessions and recently the College has introduced E.C.E.C. Technical Clinics. Participants o­n our courses can let us know beforehand or bring with them, a particular problem or problems pertinent to the subject area of the course, which they would like advice about. This advice will be given either confidentially or more usually at a special open discussion session during the course, at which other participants can offer their advice and experience as well.

The E.C.E.C.also provides tailor-made ‘in-house’ courses for Pharmaceutical, Biotechnology and Healthcare companies.

If you would like further details of our forthcoming Courses, please ask our Office to put you o­n our mailing list. If you require details of our ‘in house’ course service, please contact our Office for more information.

FEES AND REGISTRATION
The participation fee is £1115.00 (exclusive of VAT). Places are strictly limited and therefore applications will be accepted o­n a first come basis. Under UK law all applications are subject to Value Added Tax (VAT) irrespective of the country of origin of participants. Most VAT registered companies/organisations can reclaim this tax. The fee includes full personal participation, extensive bound course notes, luncheons and light refreshments, o­n all days of the Course. Dinner at night is not included. Cancellations cannot be accepted less than 14 days prior to the start of the Course, but substitutions may be made at any time. The Course language will be English. An approved Certificate of Attendance will be given to each participant at the end of the Course.

TIMING OF THE COURSE
Registration will be at 8.45am o­n Monday 20th March and the Course will commence promptly at 9.00am. The Course will finish at about 17.00 o­n Wednesday 22nd March. The Course will end at about 19.00 o­n each of the first two days.

‘E.C.E.C. TECHNICAL CLINIC’

The College recognises that participants may have a particular problem or problems that they would like advice about. o­n this course participants are invited to send in beforehand (or bring with them) details of their technical problems, which will be considered by the lecturers. A special open discussion session has been timetabled o­n this course at which participants’ problems will be discussed and advice given. At this session other course participants can offer their advice and experiences as well. If you would like advice to be given confidentially, please advise the College beforehand.

ACCOMMODATION

A special room rate of £138.00 (normal rate £190.00) per night single with bathroom, inclusive of breakfast (£172.00 twin/double (normal rate £207.00)), exclusive of VAT, has been negotiated for participants o­n this Course at the superb 4 star luxury Kensington Park Hotel in fashionable Kensington. The Hotel is opposite Kensington Palace and is peacefully situated in De Vere Gardens, just off Kensington High Street. The Hotel is close to Hyde Park, the stylish shops of Knightsbridge (Harrods) and Kensington and the Royal Albert Hall. The West End, Buckingham Palace, Piccadilly Circus, Trafalgar Square and the Houses of Parliament, in fact almost every major attraction, is within easy reach. Nightlife is no problem with cinemas, restaurants, clubs and theatres all in the vicinity. The Hotel has numerous restaurants and bars. High Street Kensington Underground Station is a couple of minutes walk from the Hotel.

DIRECTIONS

BY AIR: From Heathrow Airport the ‘Heathrow Express’ should be taken to Paddington Station. This express train service operates every 15 minutes and the journey time is 15 minutes. o­nce at Paddington Station in central London a short taxi ride can be taken to the Kensington Park Hotel off Kensington High Street. Alternatively the underground ‘tube’ can be taken from Paddington directly to High Street Kensington (4 stops o­n the Circle or District line). o­nce at High Street Kensington Underground Station the Hotel is a couple of minutes walk away. From Gatwick Airport take the train to Victoria and then either a taxi or the Underground (Circle or District Lines) 4 stops, directly to High Street Kensington.

BY TRAIN: All the main line stations connect with the London Underground and participants can get the Underground to High Street Kensington.

BY ROAD: Car parking facilities in Young Street are available nearby but it is expensive.

HOW TO REGISTER-

To register please complete the registration form and forward with your payment to the:

EUROPEAN CONTINUING EDUCATION COLLEGE

24 Menlove Gardens North,

Liverpool L18 2EJ, U.K.

Telephone:+44 (0)151 737 1993 Fax: +44 (0) 151 737 1070

E-MAIL: REGISTER@ECEC.CO.UKWEBSITE: WWW.ECEC.CO.UK

All applications will be acknowledged and a formal V.A.T. receiptissued. Telephone reservations (+44 (0) 151 737 1993) or better Fax (+44 (0) 151 737 1070) or E-Mail (REGISTER@ECEC.CO.UK) to the Courses’ Secretary will be provisionally accepted and confirmed o­n receipt of the form.

REGISTRATION FORM – PHARMACEUTICAL PREFORMULATION

20^th, 21^st and 22^nd March 2006, The Kensington Park Hotel, Kensington, London, U.K.

Please charge to my q VISA q Mastercard/Eurocard q American Express

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EUROPEAN CONTINUING EDUCATION COLLEGE

24 Menlove Gardens North

Liverpool L18 2EJ, U.K.

Tel: +44 (0) 151 737 1993Fax: +44(0) 151 737 1070

E-Mail: register@ecec.co.uk

www.ecec.co.uk