Preformulation characterization studies generally include accelerated stability (stress) studies, stability-indicating analytical method development, and other physiochemical characterizations designed to pinpoint potential product candidate stability problems and enable formulation opimization. The following table shows examples of preformulation studies.
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Characterizations
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Examples
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Stress Studies
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Accelerated stability studies
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Heat, Freezing, pH, Light, Agitation, Oxidation, Dehydration, Surfaces, Shear, etc.
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Key Degradation products
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Aggregation, Oxidation, Deamidation, Cleavage, Surface adsorption, surface denaturation, etc.
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Stability-indicating assays
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HPLC, electrophoresis, spectrometry, particle count, turbidity, recovery, biological activity, etc.
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Physical characterizations
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Structural analyses, thermal denaturation, solubility, viscosity, syringeability, etc.
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Biological Characterizations
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Substrate or receptor affinity, in vitro bioassay (information typically provided by customers)
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The objectives of the pre-formulation research will include:
- Understanding the pharmaceutically significant physicochemical properties
- Estimating product's stability when exposed to various common stresses
- Developing stability-indicating assays for major degradation products
- Deciding upon a lyophilized or liquid formulation for initial clinical studies
- Finalizing a formulation development research protocol (matrix of buffer, pH, stabilizer, tonicity modifier; analytical methods; etc.)
Example of Integrity Bio's preformulation study Package (2-3 months)
A preformulation study will perform systematic research designed to examine the physicochemical properties of product candidate that may be important in formulation development. During such a study, the product candidate will be exposed to various stresses, key degradation products will be identified, and appropriate stability-indicating assays will be developed. The product candidates will be prepared in well defined formulation matrix, exposed to relevant stresses, and analyzed by stability indicating assays.
Stability indicating analytical methods, either developed by Integrity Bio or transferred from clients, will be used to determine the degradation products. We recommend using orthogonal methods to assess comprehensive stability profile of each product.