Program 2018

September 10th - 11th, San Francisco, CA

7:30 AM - 8:20 AM

Registration & Refreshments

8:20 AM - 8:25 AM

8:25 AM - 9:00 AM - Keynote

Device Development

Challenges and Opportunities in Combination Product Design, Development and Use

Steve Bowman, Device Program Lead , Shire

  • Importance of coupling device design with drug formulation
  • Main challenges of designing user friendly devices

9:00 AM - 9:05 AM

Please Move to your Next Session

9:05 AM - 9:40 AM - Case Studies

Small Molecules

Artificial Gut Simulator: A Step Closer to In-Vitro In-Vivo Correlation?

Helen Hao Hou, Senior Scientist Small Molecule Pharmaceutical Sciences , Genentech

  • Conventional dissolution apparatus is often neither optimal nor satisfactory for differentiating the drug release performance of formulations and predicting oral bioavailability
  • The need to integrate dissolution and absorption has become increasing apparent
  • A novel apparatus to maintain absorptive sink conditions with a large surface area-to-volume ratio of absorptive surface was developed to conduct simultaneous dissolution and absorption testing
  • The system has been tested and optimized with a model drug, Ketoconazole, to obtain the biorelevant absorption rate constant, ka

Biologics

Characterization of Adsorbed Vaccine Formulation

Marina Kirkitadze, Head of Process Support & PAT Platform, Analytical Sciences, Sanofi Pasteur

  • Characterization of combination vaccines comprised of several antigens in a single formulation.
  • Scanning electron microscopy (SEM) and X-ray photoelectron spectroscopy are showcased to examine morphology and size
  • Use of nanoDSF and FTIR spectroscopy for lean material characterisation
  • Studying structure and stability of adsorbed vaccine formulation.

9:40 AM - 9:45 AM

Please Move to your Next Session

9:45 AM - 10:20 AM - Case Studies

Small Molecules

Physiologically Based Pharmacokinetic (PBPK) Modelling of Oral Absorption

Tao Zhang, Principal Scientist Drug Product Design- Molecular Pharmaceutics Pharmaceutical Sciences Small Molecules, Pfizer

  • Application in early pharmaceutical development
  • Role of physicochemical characterization
  • Relating physicochemical characterization to early pharmaceutical development

Device Development

Common Pitfalls in Developing Combination Products and Medical Devices

Scott Brown, Device Development Lead & Executive Director, Merck

  • Fundamental steps in development
  • How devices and combination products fail and steps to avoid failure
  • Project and people related issues

This presentation will go over the common sources of failure in delivery device and combination product development and how to systematically avoid them while optimizing the likelihood of a successful product approval and launch.  Emphasis is placed upon design integrity, simplicity and effectively meeting the needs of patients and healthcare professionals. The impact of parts count on reliability and the importance of good human factors engineering are also covered. A useful checklist is provided to provide guidance on what should be established before investing in capital equipment for manufacturing and assembly.

 

10:20 AM - 11:20 AM

iSolve & Networking Break

Please Proceed to Poster Competition Area and Vote Through the Mobile App

11:20 AM - 11:55 AM - Solution Spotlights

Small Molecules

How do I Develop Spray Dried Dispersions for Early Phase Clinical Trials and Beyond?

Nikki Whitfield, Vice President, CDMO Services, Quotient Sciences

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  • Benefits of spray-drying to address poor drug solubility
  • Fit-for-purpose systems in early clinical research & effectively transitioning to solid oral dosage forms
  • Adaptive manufacturing “tailored” to the clinical study and patient recruitment

Biologics

Rip Through Formulation Prep with a Junior, a Lunatic and an Uncle

Robin Sweeney, Automation Applications Scientist, Unchained Labs

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  • Identifying formulations for biologics is a painful process
  • Automated buffer exchange coupled with volume control can streamline the buffer exchange process
  • Lower volume analytic measurements provides a means to get to key formulations faster and more effectively
  • Combining automated buffer exchange with low sample volume analytics increases throughput and reduces sample burdens for discovery

11:55 AM - 12:00 PM

Please Move to your Next Session

12:00 PM - 12:35 PM - Case Studies

Small Molecules

Maximize the Potential of Discovery: Early Utilization of Enabling Technology

Richard Hu, Associate Director, CMC, Curis Inc.

      • Overview of enabling formulation technologies for poorly soluble compounds
      • Every compound/project is unique
      • Value appropriate, phase appropriate, adaptive formulation strategy

 

Biologics

Application of High Throughput and Automated Workflows to Large Molecule Formulation and Process Development

Nitin Rathore, Director of Formulation and Process Technologies, Amgen

  • As the design space for formulation design becomes more complex and the need for accelerated product development more urgent, traditional approaches do not provide a sustainable means to handle such challenges.
  • Modern development tools that minimize material requirements and maximize use of automation can help overcome these challenges and provide a differentiating capability to rapidly explore large formulation design spaces for novel modalities.
  • Case studies will be presented demonstrating application of these technologies to tackle various drug product development challenges. New approaches to data analysis and visualization leading to effective decision-making will also be covered.

12:35 PM - 12:40 PM

Please Move to your Next Session (6)

12:40 PM - 1:15 PM - Keynote

Small Molecules

Designing Excipients for Use in Enabling Technologies

Kevin O'Donnell, R&D Manager, DuPont Nutrition & Health

 

 

  • The need for enabling technologies for solubility enhancement is rapidly growing
  • Excipients can be designed not only for functional purposes, but to allow broader, simplified, or more effective use in these technologies

 

This presentation will provide a very brief background on amorphous systems and enabling technologies, and will discuss where excipients are limited in these processes. It will then focus on how excipients can be designed and modified to overcome the process challenges and allow effective use in amorphous solid dispersion formulation

1:15 PM - 2:15 PM

Networking Lunch

Lunch & Learn Round Table with Solvay USA

Ganesh Sanganwar, Principal Engineer R&I, Technology Center, Solvay USA

 

Docusate Sodium: A Multifunctional Excipient for Drug Bioavailability Improvement

Abstract:

Docusate sodium has been used as a pharmaceutical grade excipient for a long time thanks to its unique and versatile properties: wetting agent for poorly soluble APIs, tablet disintegration accelerator, dispersing agent for micro suspensions and emulsifier for creams and gels.

Continuous research is now also exposing its strong performance in advanced solubalization techniques. 

 

This presentation will highlight new applications of Docusate Sodium for drug bioavailability challenges

* Re-explore its wetting, dispersing, and emulsifying properties 

* Research and demonstrate new applications as an excipient for poorly soluble APIs

* Docusate as counter-ion for biopharmaceutical formulation development.

2:15 PM - 2:50 PM - Solution Spotlights

Small Molecules

Innovation in Manufacturing of Parenteral Packaging Components with First Line USA

Eugene Polini, Technical Key Account Manager , Datwyler Pharma Packaging, Inc.

 

      • World leader in parenteral packaging
      • Fluoropolymer coating to eliminate silicone oil and prevent interaction between drug product and elastomer
      • Manufacturing in controlled environment
      • Automation of industrial process to eliminate human intervention and contamination

Biologics

Formulation of Hard-to-Stabilize Biopharmaceuticals

Dr Phil Morton, Chief Technology Officer, Albumedix

  • Recombumin® for the formulation of next generation therapeutics: While in many cases the use of sugars, amino acids and detergents are sufficient there are a number of more challenging biologics where traditional approaches still fail or are suboptimal.
  • Recombumin® the importance of a controlled process:  The lack of endogenous ligands guarantees batch-to-batch consistency and consequently performance reproducibility. Depending on the mechanism of albumin stabilisation we would expect a different influence of excipients, buffer components and, in case of serum derived HSA by endogenous ligand present. 
  • An example is the cryopreservation of stem cells: the viability of the stem cells was kept above the set release criteria for longer using AlbIX compared to HSA.

2:50 PM - 2:55 PM

Please Move to your Next Session

2:55 PM - 3:30 PM - Case Studies

Small Molecules

Impact of Method of Preparation on the Mechanical Properties of Amorphous Solid Dispersions

Karthik Nagapudi, Senior Scientist, Group Leader Solid State Characterization, , Genentech

  • Overview of methods used to make amorphous materials
  • How method of preparation impacts downstream processing of amorphous solids
  • Use of Resonant acoustic mixing in making amorphous dispersions
  • Mechanical characterization of amorphous solids

Biologics

Emerging Approaches for Patient-Centric Formulation and Therapy Delivery

Rahul Rajan Kaushik, Senior Director of Biologics CMC , Nektar Therapeutics

 

  • The next decade is poised to witness an explosion in new approaches  to treat grievous human illness, especially in oncology. 
  • These approaches include new modalities and combinations of existing therapies 
  • One aspect for the pharmaceutical industry to focus on would be on improving the experience of patients 
  • This talk will cover emerging therapeutic delivery approaches to enhance the patient experience, including decreasing injection pain, reducing visits to healthcare clinics and hospitals, as well as converting medicines to more tolerable routes of administration 

3:30 PM - 4:30 PM

iSolve & Networking Break

4:30 PM - 5:05 PM - Solution Spotlights

Small Molecules

Twin-Screw Melt Granulation of Thermally Labile Drug: Effect of Processing Conditions

Feng Zhang, Assistant Professor, University of Texas at Austin

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  • Processing temperature and reduction of GABA particle size during granulation are significant factors that can affect the chemical stability of GABA.
  • Small particle size of HPC can cause higher degradation due to higher surface area in contact with GABA particles.
  • Processing parameters (screw speed and feed rate) should be optimized to achieve the balance between improving compaction properties but still maintaining chemical stability of GABA.

Biologics

New Silicone-Free Option for Delivery of Sensitive Biologics in Bare Glass Pre-Filled Syringes

Russ Hornung, Business Development, W.L. Gore & Associates

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To ensure functionality of pre-filled syringe systems, the pharmaceutical industry has been utilizing silicone to ensure system functionality and performance. However, silicone poses many challenges not only to the drug product, but also to the manufacturing process. This talk will focus on some of the latest insights to highlight the challenges that silicone can introduce to the newer, more complex and sensitive biologics like aggregation, precipitation or immunogenicity issues.  Gore will then share how the removal of silicone can lead to more options for pharmaceutical manufacturers to have a robust product solution. 

5:05 PM - 5:10 PM

Please Move to your Next Session

5:10 PM - 5:45 PM - Keynote

Small Molecules

Challenges and Opportunities of Development of Salts of Weak Bases

Anand Sistla, Associate Research Fellow, Pfizer

Salts present a unique opportunity at fixing solubility/dissolution related exposure and/or solid form related challenges. However the drive to progress molecules with low basic pKa (to address safety concerns) in the discovery setting increases risks associated with the design of a robust solid dosage form (namely disproportionation to the base as drug substance or drug product).  Relationship between pKa, pHmax, and salt disproportionation will be discussed.  How to assess this risk and mitigation strategies will be presented

5:45 PM - 5:50 PM

Chair’s Closing Remarks and End of Day 1

Richard Hu, Associate Director, CMC, Curis Inc.

5:50 PM - 6:50 PM

Evening Drinks Reception

8:00 AM - 8:30 AM

Registration & Refreshments

8:30 AM - 8:35 AM

8:35 AM - 9:10 AM - Keynote

Technology & Innovation

In What Direction is the Drug Delivery Technology Space Moving?

Anand Subramony, Vice President Novel Product Technologies, MedImmune

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  • Evaluating how fast the delivery technology field has evolved until now – are there limiting factors to its continued development?
  • What is the potential of less-traditional delivery routes such as nasal and ocular delivery?
  • Discussing the future of evolving areas including polymer technologies, auto injectors, microneedles etc.
  • Looking retrospectively, has the industry done all it can until now to maintain the R&D paradigm?

9:15 AM - 9:50 AM - Keynote

Device Development

Understanding the Changing needs for Combination Products and Digital Health

Andrew M. Ratz, Senior Director, Delivery, Device and Connected Solutions, Eli Lilly and Company

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Over the past several years, development of novel subcutaneous delivery technologies has undergone significant growth fuelled to a great extent by the increasing importance of protein based combination products as treatments for acute and chronic diseases.  Likewise, investments in digital health through the integration of connectivity with drug delivery has continued to grow in the med tech and pharma industries. While the emerging landscape has great potential to yield new compelling solutions for patients and caregivers, it does present the drug delivery and device community with some unique challenges.  A number of these challenges and potential areas of opportunity for future development will be highlighted, as well as critical enablers that drive and integrate continued evolution and rapid innovation in these important areas.

9:50 AM - 9:55 AM

Please Move to your Next Session

9:55 AM - 10:30 AM - Solution Spotlights

Small Molecules

Improved Safety Profile of Docetaxel Injection

William Zhao, Chief Executive Officer, Meridian Lab

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  • Meridian Docetaxel Injection regulatory path
  • Safety benefit of removing Polysorbate-80 and replacing with Captisol
  • Product proven Bioequivalent

Biologics

Hydroxypropyl-ß-Cyclodextrins Kleptose® HPB & HP: Novel Tools for Protein Stabilization

Sofiya Yashchuk, Global Technical Application Specialist - BioPharma Applications, Roquette

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  • Review on cyclodextrins and their historic use in small molecule formulations
  • Reported applications and benefits in biopharma formulations
  • Roquette case study on two proteins: stabilization effects on the Human Growth Hormone hGH and the mAb Infiximab

10:30 AM - 11:30 AM

iSolve & Networking Break

 

Please Proceed to Poster Competition Area and Vote Through the Mobile App

11:30 AM - 12:05 PM - Case Studies

Biologics

Developing Novel Nanocarriers for Improved Drug Targeting

Seungpyo Hong, Professor Pharmaceutical Sciences and Principal Investigator at the Hong Research Group, University of Wisconsin-Madison

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  • Controlling biological interactions of polymers with cells at the nano-scale
  • Targeting drugs at cancer cells

Device Development

Electronically-Controlled Meshless Pocket-Size Ultrasonic Inhalers

Chen S. Tsai, Chancellor’s Professor Department of Electrical Engineering and Computer Science, University of California, Irvine

  • First, we describe: (1) the architecture of our silicon-based MFH nozzle and its excitation of megahertz (MHz) Faraday waves in the liquid (medicine) layer sitting on the nozzle end face, and (2) the requisite drive power for droplet ejection and drive frequency for desired droplet diameter.
  • Second, we present data demonstrating the realization of low-drive power pocket-size prototype inhalers and their uses for nebulization of a variety of common and experimental pulmonary drugs with desirable aerosol characteristics.
  • Finally, we discuss the new inhaler’s additional unique capabilities, including simultaneous aerosolization of multiple drugs for combination therapy and the potential for incorporation of IOT technology for enhanced functionality.

12:05 PM - 12:10 PM

Please Move to your Next Session

12:10 PM - 12:45 PM - Solution Spotlights

Small Molecules

Designing Amorphous Formulations and Manufacturing Processes for Challenging Compounds

Michael Grass, Principal Scientist Product Development, Lonza Bend

Lonza provides design, development and manufacturing services for active pharmaceutical ingredients, drug product intermediates and finished dosage forms.  Specialized capabilities are in place for improving low solubility / bioavailability (BA) and modulating pharmacokinetics (PK) to meet target product profiles.  Dr. Michael Grass will provide the following overview with representative case studies:

  • The range of enabling technologies utilized to improve solubility and BA
  • Key criteria for matching enabling technologies to API / formulation problem statements
  • Case study #1 - Improving the BA of Itraconazole over the amorphous reference listed drug utilizing a dissolution-permeation in vitro test
  • Case study #2 - Manufacturing amorphous dispersions with methacrylic acid/methyl methacrylate copolymer for improved performance and stability
  • Summary and Q&A

Technology & Innovation

OralogiK™ - A Versatile Timed Release Technology for Optimal Drug Delivery

Carol Thomson, Chief Executive Officer, BDD Pharma

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  • Achieving Complex Drug Delivery Profiles with intelligent formulation design
  • Understand regional absorption for optimisation in combination with gamma scintigraphy
  • Use of Lean Clinical strategies to drive compound development strategy

 

12:45 PM - 1:45 AM

Networking Lunch

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1:45 PM - 2:20 PM - Case Studies

Small Molecules

Enabling Dry Powder Inhalation Discovery Compounds for Lung Delivery

Ajit Narang, Senior Scientist, Genentech

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  • Material properties and their influence on particle agglomeration in powder mixtures

  •  Dry powder aerosol generation, characterization, and controlling/preventing particle agglomeration during toxicology testing

  • Mechanistic drivers and balancing priorities for phase appropriate clinical formulation development

Device Development

Nanostructured Devices for Therapeutic Delivery

Tejal Desai, Professor & Chair, Department of Bioengineering and Therapeutic Sciences, University of California San Francisco

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Therapeutic peptides, proteins, and macromolecular drugs represent highly efficacious approaches for the pharmacologic treatment of human diseases.  However, current administration of such drugs continues to be bolus injection which is inconvenient, painful, and can lead to variable dosing.  In this talk, I will discuss nanoporous materials that can be used to deliver proteins to the eye as well as  nanostructured surfaces that enhance the permeability of macromolecules across epithelial cells in response to direct contact. New systems that can deliver proteins and peptides in a stable and controlled manner will have great potential to impact therapeutic development in the future.

2:20 PM - 2:25 PM

Please Move to your Next Session

2:25 PM - 3:05 PM - Solution Spotlights

Small Molecules

An Innovative Approach to Solubility Enhancement – Quadrant 2®

Jason M. Vaughn, Vice President, Process and Technology Development, Patheon, Part of Thermo Fisher Scientific

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  • Computational modeling of drug properties as means to identify suitable solubilization techniques
  • Computational modeling of drug and polymer interactions to predict suitable formulations and drug levels
  • Case studies in the use of Quadrant 2 in early pharmaceutical development. 

Small Molecules

In Vivo Predictive Dissolution – Flux Measurements

Konstantin Tsinman, Chief Scientific Officer, Pion

 

Amount and the rate of absorption for the active pharmaceutical ingredient (API) to the blood circulation from the orally administered drug products is determined by the flux of API through epithelial lining of the small intestine. The flux values would depend on the amount of the dissolved API available at the site of permeation as well as on the rate with which drug penetrates the membranes separating GIT from blood capillaries. The former quantity is governed by dissolution and solubility of API in the corresponding medium at biorelevant load while the latter is determined by effective permeability of the compound through the biological membranes.

Establishing meaningful correlations between in vivo absorption and in vitro measurements have been presenting a significant challenge for pharmaceutical researchers especially when dealing with low soluble compounds. One of the reason is that in many cases the effect of solubilizing formulations was studied through USP-type dissolution measurements without taking into account biorelevant dissolution medium/volume parameters and interconnection between formulation additives and dissolution/solubility/permeability values.

This presentation introduces principles and devices that can be utilized for flux measurements in a systematic and reproducible manner. Measuring flux and its dependence on formulations allows assessment of complex interplay between solubility, permeability and dissolution rate in formulation development. The case will be made that flux measurements can be used for early prediction of fraction absorbed, formulation ranking, bioequivalence study risks, drug-drug interactions from pH modifying agents and other biorelevant in vitro studies.

3:05 PM - 3:10 PM

Please Move to your Next Session

3:10 PM - 3:45 PM - Case Studies

Small Molecules

Designing Robust Tablet Formulas through DOE (Design of Experiment)

Tian Hao, Principal Scientist, Pharmavite LLC

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  • Resiliance to raw material variation
  • Resiliance to production variations

Technology & Innovation

Clinical Translation of Nanotherapeutics: Beyond Simple Drug Delivery

Andrew Wang, Associate Professor, University of North Carolina

  • Bench to bed story of utilizing nanotherapeutics in cancer chemoradiotherapy for the curative management of cancer
  • Utilizing nanotechnology to improve cancer immunotherapy

3:45 PM - 4:20 PM - Case Studies

Small Molecules

Solubilization of a Poorly Soluble Drug with Combination of In-Vitro Dynamic Flow and In-Vivo Rabbit Ear to Identify Parenteral Formulation

Yingqing Ran, Senior Scientist, Genentech

Phlebitis of a parental formulation is one of the main concerns for patient compliance.  It has two major causes, one is the physical precipitation of the compound in blood stream after administration, and another one is chemically irritation due to the compound chemical entity.

In this study, the phlebitis issue of phase I formulation of compound A was due to its poor solubility. Physical precipitation occurred after formulation intravenous injection. In order to minimize precipitation induced phlebitis, pH combination with cosolvents, surfactants, and Cyclodextrins were used to screen the formulation.  L-lactic acid and D-Glucuronic acid are the two counter ions show better solubility of compound A. Both hydroxyl- β-cyclodextrin (HP-β-CD) and sulfobutylether- β-cyclodextrin (SBE- β-CD) have shown further enhancement of the solubility combining with either lactic acid or glucuronic acid. An in vitro dynamic precipitation and an in vivo rabbit ear models have been used to investigate the potential of precipitation and phlebitis of the promising new formulations, there is a correlation between in vitro and in vivo findings. Based on both in vitro and in vivo data, the formulation composed of 40% SBE--β-CD, 50mM Glucuronic acid, and 13mg/ml compounds A has shown significant improvement of phlebitis compared to phase 1 formulation.

Biologics

Intradermal Delivery of Vaccines: A clinical study with ZOSTAVAX®

Brian K. Meyer, Principal Scientist New Technologies, Vaccine Drug Product Development, Bioprocess Research and Development, Merck

 

  • Introduction to intradermal vaccines
  • History of intradermal vaccines
  • ZOSTAVAX® delivered intradermally

An experimental medicine study to evaluate delivering ZOSTAVAX® via the intradermal (ID) route will be discussed.  The goal was to evaluate the impact of ID delivery using the MicronJet™ device compared to the standard subcutaneous (SC) route on immunogenicity.  Immunogenicity results (both antibody and T-cell responses) between ID and SC were comparable, indicating that ID delivery may be a beneficial way to administer attenuated live virus vaccines in the future.  This talk will highlight some of the potential risks (e.g. reactogenicity) as well as benefits (e.g. dose sparing) associated with the use of alternate delivery of vaccines, along with progress made on vaccine delivery approaches and potential novel delivery devices.

4:20 PM - 4:55 PM - Keynote

Device Development

How Will the Future Look for Next Generation Devices?

Ravi Gopalakrishnan, Head of Mobility, Chief Technology Officer Office, AstraZeneca

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  • New materials
  • Improved human factor engineering
  • Connectivity and integration into wider healthcare system

4:55 PM - 5:00 PM

Chair’s Closing Remarks and End of Conference

DDF Poster 2018 Winner Announcement and Award Presentation