Many existing drug compounds as well as those coming out of discovery are poorly soluble which need special efforts to be formulated into drug products. The second annual conference on Formulation and Drug Delivery will discuss effective formulation and delivery technologies for enhancing solubility and bioavailability. We invite you to join the leading formulation experts from around the world in this key discussion on formulation and delivery, and see how experts like you are developing poorly soluble drugs into scientifically sound, patient-centric formulations, and reducing their product development timelines.
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Wednesday, May 21
7:00 am Registration and Morning Coffee
8:00 Chairperson’s Opening Remarks
Geeti Gangal, Ph.D., Principal Scientist, Chemical and Pharmaceutical Profiling, Novartis Institutes for Biomedical Research, Inc.
8:05 FEATURED PRESENTATION: Solithromycin, a Fourth Generation Macrolide, the First Fluoroketolide in Development for Use in Oral and Intravenous Dosing Formulations for Adult and Pediatric Use
Prabhavathi Fernandes, Ph.D., President and CEO, Cempra, Inc. - Biography
In the last two decades there has been a focus on developing i.v. antibiotics. Hospitalization is expensive and exposes patients to hospital acquired infections. In many cases, a potent oral antibiotic can allow a patient to be treated as an outpatient. Solithromycin is in Phase 3 clinical development in oral and i.v. dosing formulations. If approved, solithromycin would be the first antibiotic in a generation to be available in oral capsule and suspension and as i.v. formulation to be able to treat all age groups, including young children.
8:35 Impact of BDDCS Compound Classification on Oral Absorption and the Need for Influx Intestinal Transporter: Statins/ACE Inhibitors as a Case Study
Ayman El-Kattan, Ph.D., Associate Research Fellow, Pharmacokinetic Dynamics & Metabolism, Pfizer, Inc. - Biography
Some statins/ACE inhibitors have low intestinal permeability with usually poor fraction of absorption (fa<<80%). Based on BDDCS classification, these compounds are class III and IV. In this presentation, we discuss: 1) The influx intestinal transporters that facilitate the absorption of statins/ACEi including review of structure, SAR/clinical relevance; 2) The impact of food and pharmacogenomics on statins/ACEi absorption; and 3) The use of prodrug as an effective approach to overcome poor oral absorption.
9:05 Simulating the Gastro-Intestinal Tract to Understand Drug Behavior – How Close Do We Need to Go?
Anette Müllertz, Ph.D., Associate Professor, Pharmaceutical Design and Drug Delivery, Department of Pharmacy, University of Copenhagen - Biography
Depending on the drug and the dosage form in question, different conditions or events encountered during transit of the gastro-intestinal tract will be determining the absorption of the drug. Therefore one should carefully consider how to develop an in vitro assay that will predict the behavior of specific dosage forms. In some cases simulations of the stomach will be of utmost importance, whereas this is not important in other cases. Likewise the digestion processes have to be taken into account for some dosages forms. These factors should be considered when developing an in vitro model for development of oral drug products.
9:35 Coffee Break in the Exhibit Hall with Poster Viewing
10:20 Risk-Based Approach to Exploratory Drug Product Development
Madhushree Gokhale, Ph.D., Senior Research Investigator, Drug Product Science &Technology, Bristol-Myers Squibb Co. - Biography
An integrated risk-based approach to understand material (form) risks, chemical stability risks, delivery risks and processing risks during early stages of drug product development not only provide a robust design space but also lead to focused drug product development and risk mitigation plans. This talk will highlight use of high-throughput screening techniques, in vitro, in silico, in vivo tools and mini-piloting tools, as well as case studies to showcase integrated risk-based approach in early drug product development.
10:50 What You See May NOT be What You Get— Why Dissolution Testing May be an Unreliable Predictor of in vivo Success
Robert A. Bellantone, Ph.D., Associate Professor, Division of Pharmaceutical Sciences, Arnold & Marie Schwartz College of Pharmacy and Health Sciences, Long Island University; President, Physical Pharmaceutical LLC - Biography
For poorly soluble drugs and new oral drug delivery strategies, compendial in vitro dissolution methods may not provide data relevant for predicting whether a formulation will work successfully in vivo. This talk will discuss dissolution-absorption and excipient-solubility relationships, which in vitro data aremost relevant for different situations, and why existing methods may not provide the needed data. In addition, some new methods to obtain relevant in vitro data will be discussed.
11:20 Disadvantaged Drugs Turned into Super APIs with Expanded Clinical Utility
Gabor Heltovics, CEO, DRGT - Biography
The continuous flow Super-API technology delivers significant pharmacological improvements for compounds where earlier tmax, higher Cmax and higher exposure can lead to clinically meaningful benefit. Disadvantageous food effect can also be reduced or eliminated by the technology due to the novel structure of the developed Super-APIs.
11:35 Sponsored Presentation (Opportunity Available)
11:50 How HIGH Can You Get? – The Use of in vitro Data to Reduce Animal Experiments
Geeti Gangal, Ph.D., Principal Scientist, Chemical and Pharmaceutical Profiling, Novartis Institutes for Biomedical Research, Inc. - Biography
Cocrystals, nanosuspension, microemulsion and amorphous Solid dispersion are the various techniques that are commonly utilized to manage solubility issues of the poorly water soluble drugs. In vitro tools like pBDDCS, Q-plus and Gastroplus have been used in the literature for the compound classification and assessing the risk associated in the development. However, together these in vitro tools can be used as powerful guidance to pick the best formulation that would work for your compound and can lead to reducing animal experiments.
12:20 pm Is it Crystal Clear? Stability and Performance Prediction for Amorphous Pharmaceuticals
Sunny P. Bhardwaj, Ph.D., Senior Scientist, Discovery Pharmaceutical Sciences, Merck & Co. - Biography
Majority of new drug candidates under development are poorly water-soluble. The amorphous state is of considerable interest since it confers higher apparent solubility and faster dissolution than its crystalline counterpart. However, being the thermodynamically unstable form, it runs the risk of crystallization leading to the loss of solubility advantage. In this presentation, we will discuss different approaches to predict the solid-state and solution state physical stability of the amorphous state with case studies.
12:50 Luncheon Presentation (Sponsorship Opportunity Available) or Lunch on Your Own
1:30 Session Break
2:00 Chairperson’s Remarks
Rajesh N. Davé, Ph.D., Distinguished Professor of Chemical, Biological and Pharmaceutical Engineering; Site Director, NSF-ERC on Structured Organic Particulate Systems, New Jersey Institute of Technology
2:05 Novel Approach of IV Formulation Development of Solithromycin, a Fourth Generation Macrolide Antibiotic
Sara Wu, Ph.D., Director, Product Development, Cempra, Inc. - Biography
Solithromycin is a fourth generation macrolide, the first fluoroketolide antibiotic in Phase III clinical trials for Community Acquired Bacterial Pneumonia. The challenges faced during the development of the intravenous formulation of solithromycin will be presented. Optimization of the intravenous formulation to achieve the dosing goal while providing acceptable solubility and local site tolerance relied on an in vitro dynamic precipitation model, rabbit ear-vein irritation model and the Phase I clinical results on local tolerance.
2:35 Microfluidics: A New Platform for Early Stage Formulation Development
Sabiruddin Mirza, Ph.D., Sr. Research Associate, School of Engineering & Applied Science, Harvard University- Biography
Early formulation development is a significant challenge for the pharmaceutical industry, primarily because of the lack of drug materials available at this stage. Microfluidics, an advanced technology that combines the use of tiny volumes of materials with precisely controlled experimental conditions, opens new perspectives in screening and development of clinical trials materials. This talk will highlight the utility of microfluidic platforms in aiding formulation optimization of difficult-to-deliver APIs at the early stage of development.
3:05 Nano Suspension: Why, How & the “Golden Syringe”
Lieyu (Richard) Hu, Ph.D., Scientist, Pharmaceutical Sciences, Cubist Pharmaceuticals, Inc. - Biography
A major challenge hindering the development of new chemical entities is low aqueous solubility, limiting formulation and delivery options, in particular intravenous administration. Nanosuspensions, which consist of pure crystalline drug particles stabilized with surface modifier(s) in aqueous media, offer an attractive means of addressing such development challenges. Nanosuspensions can be tailored to enable drug release in a controlled fashion to meet the needs of patients. This talk describes the preparation, characterization, and applications of such nanosuspensions.
3:35 Selected Poster Presentation: A Fast and Reliable Empirical Approach for Estimating Solubility of Crystalline Drugs in Polymers for Hot Melt Extrusion Formulations
Samuel Kyeremateng, Ph.D., Formulation Scientist, Global Pharmaceutical Sciences, AbbVie Deutschland GmbH & Co. KG
Data on solubility of crystalline drug in polymers play a crucial role in formulation and process development of amorphous solid dispersion (ASD). Currently this data is not widely utilized within the pharmaceutical industry because generating such data is very challenging and time consuming. Our work introduces a novel and fast analytical approach for generating solubility data based on an empirical algorithm which can be applied in designing ASD for maximum drug load and physical stability.
4:05 Refreshment Break in the Exhibit Hall with Poster Viewing
5:00 Plenary Keynote Presentation:
Catalyzing Translational Innovation
Christopher P. Austin, M.D., Director, National Center for Advancing, Translational Sciences, National Institutes of Health
6:00 Welcome Reception in the Exhibit Hall with Poster Viewing
7:00 Close of Day
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