Scientists at Kazan Federal University have developed a new method for preparing polymorphs (packages with a crystal structure) of medicinal substances. Chemists’ discoveries could significantly reduce the costs of developing and introducing new drugs. The Russian Ministry of Education and Science told socialbites.ca about this.
Polymorphs are different crystal packages of the same substance. The bioavailability of the drug, that is, its rate of dissolution in water and, in some cases, the organ on which the drug will act, depends on the crystal packaging. For example, the dissolution rate must be high for the treatment of mouth, throat and lung mucosa, and low for the stomach.
Therefore, drug manufacturers need to know all the polymorphs of the compounds they use in their drugs. The discovery of new polymorphs of already known substances may lead to additional costs for studying their pharmacological effects.
The search for polymorphs is complicated by the fact that it is not known in advance how many there may be. It is believed that the number of discovered polymorphs of a substance is related to the resources spent. There are devices for automatic screening of polymorphs that allow you to select a large number of crystallization conditions in a limited time. However, there is no complete guarantee that all possible crystal forms will be discovered.
One of the leading researchers, a professor at the Department of Physical Chemistry, explains to socialbites.ca: “If the developer cannot find the polymorph of a substance, the competitor may discover the polymorph and start selling the drug under its own brand, bypassing the copyright.” At the Research Laboratory “New methods of material processing and analysis for medicine under ultra-fast heating and cooling conditions” of the KFU Valery Gorbachuk Institute of Chemistry.
This opens up a wide field of possibilities for the creation of indigenous medicines.
“We have developed a method to search for and prepare polymorphs that allows us to minimize the chances of their discovery. Typically polymorphs are crystallized from solutions or melts. That is, the initial state is liquid. All our processes are solid phase. This means that crystalline forms are produced with the least dense packing, hence the most “That is, the solid phase process makes it possible to stabilize the state of the polymorph in a minimally stable manner. Before discovering a new method, the process was carried out from solutions and melts; apparently some forms of the best known and studied substances may remain undiscovered.” Research Laboratory “Novel processing and analysis of pharmaceutical materials under ultra-fast heating and cooling conditions” of the KFU Valery Gorbachuk Institute of Chemistry.
In particular, KFU scientists have prepared a polymorph of this substance, previously known only in mixture with a polymer solvent, as well as a new polymorph of indomethacin (a non-steroidal anti-inflammatory drug) with increased bioavailability. It should be understood that indomethacin has been studied for more than 50 years.
As KFU scientists expected, thanks to the new method of preparing polymorphs of medicinal substances, it will be possible to significantly reduce the costs of introducing new drugs into practice.
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