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Practical Strategies for Developing Preclinical and Phase 1 Oral Drug Formulations
(Applied Drug Development Core Course)


October 4-8, 2010
Pyle Center, University of Wisconsin
702 Langdon Street
Madison, WI

On Campus Short Courses for the Pharmaceutical Industry


This program has been developed and will be presented in cooperation with the Lenor Zeeh Pharmaceutical Experiment Station in the School of Pharmacy at the University of Wisconsin-Madison.

More information about the Pharmaceutical Experimental Station

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Registration
Goals & Objectives
Special Offer for Academic Institutions
Short Course Program General Information
Who Should Attend
Contents
Instructors
More Information

Registration

Your registration options are as follows: $1995 ($1695 prior to 9/17/10)

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Register Online. Login in using your user account. If you don't have a user account creating one is free & easy.
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Download the registration form, complete & mail to:

Drug Development
Extension Services in Pharmacy
777 Highland Avenue
Madison, WI 53705

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By phone at 608.262.3130 or toll-free at 877-947-4255 using a credit card for payment.
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Download the registration form, complete & fax to 608.262.2431 using a credit card for payment.

Special Offer for Academic Institutions

Extension Services in Pharmacy at the University of Wisconsin School of Pharmacy has instituted a new policy for industrial professional development programs to encourage greater participation by faculty, graduate students and post doctoral students at academic institutions. Programs will be offered at a significantly reduced price, based on space availability. For information about any specific course please contact Dr. James E. De Muth by email.

Short Course Program General Information

Limited Enrollment

Enrollment is limited to 30 registrants.

Course Location

Courses are presented at the Pyle Center on the University of Wisconsin-Madison Campus. Summer time in Madison and the beauty of the on-campus location provide a relaxing atmosphere for learning. Evenings can be used to explore the University and the city. For more information about Madison, WI see www.visitmadison.com.

Accommodations

A block of rooms is available at the DoubleTree hotel which is next to the University of Wisconsin campus. The approximate cost per night is $130. Information hotels within walking distance will be sent to individuals when they receive their registration confirmation.

Registration Fee

Tuition for the 2010 program will be $1,995.00. Cancellations after September 17 are non-refundable. Cancellations prior to September 17 are subject to a $75 administration fee. In the event that an accepted applicant cannot attend, a substitute may be sent by the same company. Early bird rates ($1,995 - $300 = $1,695) are offered to individuals registering prior to September 17, 2010.

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2010 Goals & Objectives

This course covers practical aspects of dosage form development for preclinical and phase 1 formulations. The formulation approaches include solubilization and disperse phase systems (suspensions, emulsions, microemulsions, liposomes and micelles) for preclinical as well as powders for reconstitution, capsules and tablets for phase 1.

The course is a practical guide in that its focus is on major considerations in selecting and evaluating oral dosage forms for preclinical and phase 1 studies in pharmaceutical drug development by examining the excipients used, their typical level ranges and various preparation/processing procedures on small laboratory and pilot scales. The challenges in developing oral dosage forms at this early drug development stage will be examined in detail, including the major problems encountered and the common strategies that are used to overcome them.

In addition to its focus as a formulation guide, the course content includes key points in drug stability evaluation, such as excipient compatibility approaches and the ICH guidelines. The major physical tests used to assess formulations are an integral part of the course material and are covered in terms of their application to problem solving and in setting the product specification.

Upon completion of the course, the attendees should be able to describe:


View 2009 evaluation results.

See the full Program section for a detailed account of the course topics, problem sets and discussion sessions.

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Who Should Attend

The Practical Strategies for Developing Preclinical and Phase 1 Oral Drug Formulations course at the University of Wisconsin-Madison is intended for scientists and technical managers who work in early drug development and who are responsible for preclinical and/or phase 1 clinical formulations. Attendees at this professional development opportunity could include BS, MS and PhD graduates with less than 5 years of experience in the formulation discipline. Additional pharmaceutical scientists and managers who would benefit from the course include those working in analytical, preformulation, various biological sciences (toxicologists, pharmacokineticists, pharmacologists), and other groups interested in gaining a better understanding of principles and practices in the drug research and development process. Other individuals who would be well-suited to attend this short course are those who have previously completed the other core Applied Drug Development short courses: 1) Preclinical and Drug Development Design Strategies (CMC Track) and/or 2) Principles and Experimental Strategies in Physicochemical Characterization, Solubilization and Solid Form Screening for Candidate Selection.

2010 Contents

Monday, October 4

 

8:30am

Welcomes

James E. De Muth, Ph.D.
Professor, School of Pharmacy, University of Wisconsin-Madison

8:45am

Introduction and Overview of Course

9:00am

Solubilization Strategies and Formulations for Preclinical PK and Toxicology Studies
pH adjustment, cosolvents, complexation and oil/lipid-based formulations; small scale processing considerations; dosing small volumes; filling and dosing small capsules; comparing solution and suspension results

10:15am

Break

10:30am

Preclinical Animal Species
Animal species physiological differences related to absorption and metabolism; dose volume limitations for acute and chronic dosing; excipient toxicity considerations; excipient level restrictions; different routes of administration; allometric scaling

12:00pm

Lunch

1:00pm

Preclinical Formulation Problem Set
Given a compound with certain properties, provide a formulation strategy, including details of excipients used, their levels and dosing limitations for the animal specie

2:20pm

Break

2:35pm

Drug Substance Considerations
Salt forms; role of drug substance crystal form and particle size in capsule and tablet formulations; relevance to processing, drug product dissolution and oral bioavailability; ICH Q6A; literature review of crystal form solubility variability

3:55pm

Dosage Form Selection for Phase 1
3:55 Dosage Form Selection for Phase 1 Drug-in-bottle approach, reconstitution (solutions and suspensions), advantages and disadvantages, when and when not to use; time, resource and drug substance requirement comparison with capsules and tablets; excipient compatibility and stability considerations

4:30pm

Adjournment

6:00pm

Reception: Hilton Monona Terrace

Sponsor:

Cetero Research
Cary, NC

7:00pm

Dinner

Tuesday, October 5

8:30am

Excipient Compatibility
Traditional and statistical design approaches vs. the miniformulation strategy

9:30am

Placebo Considerations for Capsules and Tablets
Matching; controls for stability

10:15am

Break

10:3am

Excipient Compatibility Problem Set
Given a compound with certain properties, design an excipient compatibility study; a dataset will be provided and groups will review results to determine next steps and select the optimum ingredients for a formulation

12:00pm

Lunch

1:00pm

Considerations for Capsule Formulation Development
Advantages and when to use capsules; excipients used, functionality and levels; capsule filling process, manual vs. automated; gelatin and nongelatin capsules, gelatin specific issues; processing formulations at lab and pilot scales

2:30pm

Break

2:45pm

Assessment of Capsules and Tablets (Part 1)
Physical characterization of powders (api and blends) and granules; crystal form identification, size, morphology, density, porosity, flowability, hardness, water content

4:15pm

Discussion Session
Questions and answers session on the day’s topics in a group discussion format; communication of experiences from course members

4:30pm

Adjournment
Evening Free to Explore Madison

Wednesday, October 6

8:30am

Considerations for Tablet Formulation Development
Advantages and when to use tablets; excipients used, functionality and levels; tablet compaction process, manual vs. automated; direct compression, wet granulation, dry granulation, film coating; processing formulations at lab and pilot scales

10:05am

Break

10:25am

Assessment of Capsules and Tablets (Part 2)
Properties of tablets (thickness, weight, porosity, hardness/tensile strength, friability, water content); disintegration test; dissolution test and in vitro-in vivo correlation; other tests (identification, weight variation, content uniformity); the product specification

12:00pm

Lunch

1:00pm

Capsule and Tablet Formulation Issues
Opportunity for participants to highlight capsule and tablet formulation, processing and stability problems that they have encountered; causes and problem solving approaches

3:00pm

Break

3:20pm

Formal Stability Assessment of Solid Oral Dosage Forms
ICH guideline; stability protocols; common stability problems for capsules and tablets (e.g., decrease in dissolution); problem solving strategies

4:00pm

Adjournment

Tour of School of Pharmacy and Pharmaceutical Experiment Station Labs

Evening Free to Explore Madison

Thursday, October 7

 

8:30am

Capsule or Tablet Problem Set
Given a drug with certain properties, anticipate potential problems and devise a formulation strategy, inlcuding excipients and processing detailss

10:15am

Break

10:30am

Drug Substance Processsing Considerations for Enhancing Oral Bioavailability
Assessing dissolution rate limited oral bioavailability; milling, micronization and wet milling at lab and pilot scales; key methods for physicochemical characterization of processed drug substance and small particles

12:00pm

Lunch

1:00pm

Solid Dispersion Approach to Enhancing Oral Bioavailability of Capsules and Tablets
When to and not to consider solid dispersions; eutectics and amorphous solid dispersions; excipients used; methods of manufacture at lab and pilot scales; importance of physicochemical characterization; physical and chemical stability

2:30pm

Break

2:50pm

Solid Dispersion Formulation Problem Set
Given a compound with certain properties, devise a formulation strategy, including excipient choices, levels considered and stability assessment

4:00pm

Discussion Session
Questions and answers session on the day’s topics in a group discussion format; communication of experiences from course members

4:30pm

Adjournment

6:00pm

Reception: Alumni Lounge, Pyle Center

Sponsor:

PPD
Wilmington, NC and Middleton, WI

7:00pm

Dinner

Friday, October 8

 

8:30am

Liquid Filled Capsule Formulations for Enhancing Oral Bioavailability
Assessing solubility limited absorption; when to and not to consider liquid filled capsules; excipients used and their functionality; excipient levels and capsule shell compatibility; liquid fill process considerations for hard shell capsules (e.g., temperature and banding); soft gel capsule filling process

10:00am

Break

10:15am

Liquid Filled Capsule Formulation Problem Set
Given a compound with certain properties, devise a formulation strategy, including excipient choices, levels considered and stability assessment

10:30am

Discussion Session
Questions and answers session on the day’s topics in a group discussion format; communication of experiences from course members

11:00am

Course Assessment

11:30pm

Adjournment

 

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2010 Instructors

Mark Sacchetti, Ph.D.
Scientific Director, Zeeh Pharmaceutical Experiment Station
School of Pharmacy, University of Wisconsin–Madison
Madison, WI

Edmund (Ed) Elder, Jr., R.Ph., Ph.D.
Director, Zeeh Pharmaceutical Experiment Station
School of Pharmacy, University of Wisconsin–Madison
Madison, WI

Peter J. Sausen, Ph.D., DABT
Executive Director
Program Management Services
Covance Laboratories
Madison, WI

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For More Information

James E. De Muth, Ph.D., Course Coordinator
Extension Services in Pharmacy
777 Highland Avenue
Madison, WI 53705
(608) 262-3130
FAX (608) 262-2431
Send Email

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