Acivery has developed a new process for the production of pharmaceutical actives for pulmonary drug. Our technology leads to the precipitation of non-agglomerated crystalline powders with narrow particle size distributions
In Activery we believe that solid state modifications may lead to a critical changes in your active pharmaceutical, thus to a differentiated drug or to a brand new innovative medicine
Activery possess unrivalled specialist expertise about different crystallization techniques and expert knowledge in the field of solid state modulation.
In Activery, we design and produce particles for special uses where size matters such as nanoparticles for cancer treatment. Through our technology you would enable new administration routes or renewed performance of your drug formulation.
| Amorphization strategies |
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Amorphization: obtaining stable amorphous formsNowadays combinatorial chemistry is routinely used as method of choice for the discovery of new drugs. Despite its successes the technique frequently optimizes lead molecules which are poorly or completely insoluble in aqueous media.
This insolubility causes low total bioavailability and poses a significant challenge to formulators. Overcoming the solubility challenge has opened possibilities for new solid-state forms with enhanced solubility. Thermodynamically, the amorphous state shows the greatest solubility advantage, however it has also the largest propensity to revert to other, less soluble solid-state forms on storage. Further, the lack of a crystal lattice can cause increased degradation or even expose new parts of a molecule to chemical attack leading to additional stability storage problems. A challange for the pharmaceutical industryPreventing the transition into thermodynamically more stable forms is still a major challenge. Amorphous forms of pure drugs are often unstable and recrystallize easily. This problem is exacerbated with mixtures of drugs, which also have the possibility to demix in the solid state. In addition, not only one but several different amorphous states (by X-ray crystallography) can be envisaged, from microcrystalline composites to solid-state solutions in which all components are randomly distributed in a molecular dispersion. In trying to solve the physical stability challenge, polymers are usually employed to provide an amorphous matrix in which the drug can dissolve, whereby the viscosity of the matrix is usually high enough to prevent recrystallization on storage. Achieving chemical stability is an even greater challenge as the polymer matrix does not necessarily provide protection against degradation. Correspondingly, it is known that the polymeric material can lead to increased degradation. Further protective excipients are necessary, however many techniques generating amorphous states are not capable of adding further non-polymeric excipients. The Solution: Activery technologyThe ASP Process (Atmospheric Supercritical Precipitation) is capable of producing amorphous solid-states of pure drugs and combinations of drugs with or without polymers and excipients. Drug/excipient mixtures are recovered as fine dry powder in the form of a molecular dispersion, providing optimal contact between the components. Active, polymer and excipients are presented as a single solution, however it is possible to use suspensions or separate solute streams to provide flexibility in designing the right formulation. The drawback of low glass transition temperatures of amorphous mixtures is overcome in the ASP process through tuning of the operating temperature, which can be chosen to around or even below ambient.
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