471422 Particle Characterization Technique to Enable Rapid Pharmaceutical Formulation and Process Optimization

Friday, November 18, 2016: 9:14 AM
Continental 4 (Hilton San Francisco Union Square)
Mark Menning, Nucleo Life Sciences, San Francisco, CA

Pharmaceutical processing consists of several unit operations that transform active ingredients and excipients to improve the processing and handling characteristics for downstream processing into the desired solid dosage form. These same processes can impart physical changes to an active an ingredient that can potentially affect the in vivo performance of the formulated product.

The current in vitro analytical methodology used by industry to predict in vivo absorption is often times poorly correlated to true product performance. The standard USP/Ph Eur in vitro dissolution methods do not allow for a complete understanding of dissolution kinetics and underlying particle-engineering principles that may be at the root cause of a potential processing issue.

Understanding the performance of the drug product is of utmost importance to establish the fundamental mechanisms of drug release. The drug release is governed by the formulation composition and to a larger extent the processing conditions for a given formulation. If a drug substance has low solubility, for example, then the particle size will be a governing factor of drug absorption.

The focused beam reflectance measurement (FBRM) probe is an integral tool for formulation and process development at Nucleo Life Sciences. The FBRM is implemented in formulation optimization, qualification of API particle size, evaluation of formulation performance, and scale-up qualification. The measurements are simple and quick to analyze and provide a wealth of information on the particulate system.

Evaluating formulations using the FBRM particle size characterization provides valuable insight to formulation development. The ability to monitor tablet and granule disintegration behavior allows for an understanding of the underlying mechanisms of product performance. All of these dynamic events can be monitored in situ. Our goal is to assist companies with implementing the data generated by FBRM into regulatory submissions to support the selection of the in vitro dissolution method development or even use the FBRM methodology as a routine in process release test.

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