|Solid form screen: salt, polymorph, cocrystal & amorphous solid dispersions|
Solid form screening, including salt, polymorph, cocrystal and amorphous solid dispersions, is vitial for successful pharmaceutical development. With an increase in the size and complexity of the molecules that enter into drug development, companies face a larger number of compounds that are either poorly soluble, difficult to crystallize or problematic with respect to desired physical chemical properties hindering successful drug development. Crystallics has an extensive track record in executing solid state research studies and its research team has a broad expertise in identifying new crystal forms as well as in solving problems related to polymorphism and crystallization.
Physicochemical properties of drug substances, such as solubility, dissolution rate, and physicochemical stability can be altered significantly by salt formation. Consequently, important properties of the drug product such as bioavailability or shelve life can be radically influenced. Crystallics' technology platform for crystallization screening accommodates salt screening studies using only minimal amounts of drug substance while still performing a large number of experiments. High-throughput salt screening is used for both early phase salt selection studies and broad patent protection.
Cocrystals provide additional opportunities to alter the physicochemical properties of the drug substance or to crystallize compounds that fail to do so by applying more conventional approaches. For non-ionizable APIs, cocrystallization is the alternative to salt formation for altering the physicochemical properties.
The pharmaceutical industry is often confronted with the phenomenon of multiple polymorphs of the same crystalline chemical entity. Polymorphism is often characterized as the ability of a drug substance to exist as two or more crystalline phases that have different arrangements and/or conformations of the molecules in the crystal lattices giving the crystals different physicochemical properties. The ability to be able to manufacture the selected polymorphic form reliably is a key factor in determining the success of the drug product.
Amorphous solid dispersion screening
Using the amorphous form of a drug substance offers several advantages with respect to dissolution rate and solubility of the substance. However, reduced chemical stability, increased hygroscopicity and, most important, physical instability are the major drawbacks of using the amorphous phase in the final drug product. These drawbacks can be overcome by stabilizing the amorphous phase of the API in a polymer matrix, e.q. an amorphous solid dispersion. Amorphous phases dissolve more rapidly than crystalline forms, and can significantly increase bioavailability of poorly water soluble drugs substances. However, the use of amorphous materials requires confidence that crystallization will not occur during the product lifespan. For a material that has never been obtained in a crystalline form, focus should be put on attempting to crystallize it. Crystallics has extensive experience of obtaining crystalline phases from amorphous materials.
Increased costs for drug development, weak product pipelines and particularly, increased competition, are forcing the pharmaceutical industry to explore the true potential of existing molecules in order to maintain or extend patent protection. The quest to stretch a molecule's patent protected life has become at least as important as the discovery and development of new drug candidates. Lifecycle management is a strategic exercise for the pharmaceutical industry for which solid state research provides new insights and techniques.
High potent substances
Crystallics is one of the few companies worldwide that is able to work with high potent substances. The set up of our laboratory is in line with international and national regulatory authorities and we hold the necessary certificates to work on high potent substances. Crystallics can perform all solid state experiments required to bring your project with high potent drugs to the next stage.
Crystallics is also one of the few companies worldwide that hold the necessary certification to work with controlled substances. The permits allow us to import controlled substances and work with them in our laboratories, performing all solid state experiments required to bring your project to the next stage.