Product Development Strategies for Poorly Soluble Compounds: Adding Value with Spray Dried Dispersion

Data Driven Formulation Development

As NCEs coming out of discovery present solubility challenges, often companies do not have the expertise to identify the most appropriate formulations to support toxicology and clinical studies. Regrettably, very rarely does the first solubility-enabling formulation solve dosing requirements. Fortunately, there are several key compound characteristics that can help direct formulation develop and formulation selection. Pharmatek recommends taking an agnostic approach therefore relying on relevant data and formulation expertise to make these key unbiased decisions. A compound’s physiochemical characteristics as well as dosing requirements should be carefully assessed while multiple formulation types are considered, including API-in-a-capsule, simple blends, liquids, spray-dried dispersions and melt granulations, to determine the best path forward. This presentation will cover multiple dosing strategies and methods to determine which technology is best suited for your needs. Topics include:

• What Data is Necessary to Make Confident Development Decisions
• How to Design a Data-Driven Formulation Development Program
• Options for Difficult to Formulate Molecules

Spray Dried Dispersions Formulation Development for Early Phase Clinical Studies

Current estimates indicate that more than 70% of new chemical entities require solubility enhancement to achieve plasma exposure. Amorphous dispersion technology is a growing approach to improve solubility and in vitro dissolution rate of these insoluble compounds by providing a supersaturated concentration of drug, which often translates to rapid in vivo solubility and improved bioavailability. A common technology for preparing these amorphous dispersions is spray drying. This presentation will focus on the fundamentals of developing and handling spray-dried dispersions, including stability assessment, in-vitro performance, and downstream manufacturability. Topics will include:

• Parameters that indicate amorphous dispersions and spray dried dispersions are an optimal formulation approach
• Best practices for formulation screening and evaluation of stability, performance, and manufacturability of spray dried dispersions
  • Pre-Formulation solvent solubility screening and stability assessment
  • Rapid polymer screening for solubility enhancement
  • Screening of selected polymers and drug loads for physical and chemical stability
  • Excipient compatibility testing
  • In-vitro and in-vivo formulation screening

Speakers

Bryan Knox, Senior Director of Pharmaceutics, Pharmatek

Bryan Knox is a Senior Director of Pharmaceutics at Pharmatek, a contract dosage form development and GMP manufacturing organization. He has a broad background in preclinical and clinical drug development and manufacturing of small molecules and peptides. Mr. Knox’ nineteen years of Pharmaceutical industry experience include managing hundreds of oral formulation and analytical development projects, controlled release and amorphous dispersion formulations development, process scale up and technology transfer. He earned his MBA from the University of California San Diego’s Rady School of Management and his bachelor of science in biochemistry from the University of California, San Diego.

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Nathan Barksdale , Senior Scientist, Pharmatek

Nathan Barksdale is a Scientist at Pharmatek. Mr. Barksdale has over 10 years of experience in the Pharmaceutical development and manufacturing industry working with Small Molecules & Peptides. He has broad background in preclinical through clinical drug development and GMP manufacturing. He possesses a strong knowledge base in oral formulation development and manufacturing, complex process trains, and highly-potent & cytotoxic compounds. Nathan received his Bachelor of Science in Pharmacological Chemistry from the University of California, San Diego.

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