Solid form selection
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The selection of a suitable solid form of the drug substance is a vital step in pharmaceutical development. Given that a drug substance can exist in multiple solid forms, including polymorphs, hydrates, solvates, salts, cocrystals, and amorphous, and that each of them have different properties that can affect bioavailability, solubility, dissolution rate, stability and manufacturability, the appropriate evaluation and comparison of the properties of the solid forms in a rigorous and effective manner requires extensive expertise, knowledge and a good methodology. Crystallics supports customers in their selection of the optimal crystal form for drug development with a series of preformulation studies. Preformulation studies include investigation of the key properties of the solid forms of a drug substance with the purpose to identify and select the optimal solid form for the desired formulation. The route of application and the intended daily dose play an important role within solid form selection. The requirements on the solid state properties can be completely different depending whether an oral, parenteral, transdermal or inhalation route is the desired way of application. Crystallics’ preformulation studies include, but are not limited to:

o   Solubility and dissolution rate in aqueous media and simulated body fluids at various pH values

o   Solubility in organic (pharmaceutically relevant) solvents

o   Hygroscopicity evaluation

o   Thermal characterization

o   Determination of partition coefficients

o   Determination of pKa

o   Drug-excipient compatibility

o   Particle size distribution

With the preformulation studies our customers are able to make informed decisions on how to proceed further in the development of their drug candidate.