25.10.2017 change 25.10.2017

Scientists from the University of Silesia have patented an amorphous drug for people with cardiovascular disease

Amorphous double-action drug: reducing the level of "bad" cholesterol and lowering blood pressure - has been patented by scientists from the University of Silesia. Its ingredients include two active substances, which until now have been administered in separate tablets.

Amorphisation is one of the ways in which researchers improve the action of drugs. The amorphous bodies combine some of the properties of solids and liquids - the substance in the amorphous state is a solid, but the molecules that form it are arranged in a chaotic manner, more like a liquid. This, in turn, improves the solubility of the substance, thereby increasing its bioavailability.

As a result - according to assumptions - amorphous pharmaceuticals not only should work faster and more effectively, they are also expected to be safer for the body than drugs currently available on the pharmaceutical market.

These substances have been the subject of research of Prof. Marian Paluch from the Department of Biophysics and Molecular Physics, University of Silesia for over a dozen years. His team already has several patents in this field, including the recently patented method of obtaining a highly stable amorphous form of tadalafil - a drug used in men with erectile dysfunction.

Researchers have also developed drugs for people with cardiovascular disease.

According to the World Health Organization (WHO), cardiovascular disease is currently the leading cause of death in the world, and as one of the main treatments for cardiovascular disease is pharmacotherapy, innovative medicinal products containing active substance in the amorphous form could be a chance for patients.

One such amorphous dual-action medicine: lowering the level of "bad" cholesterol and lowering blood pressure has just been patented. Patent protection covers the amorphous pharmaceutical composition with high physical stability and its production method.

According to the university, the two active substances in the drug to combat the most common forms of cardiovascular disease are ezetimibe and indapamide.

"At present, these substances are sold as two separate tablets. Because the conditions for which these medicinal products are used often coexist, and there are no contraindications for the combined administration of these drugs, many patients are forced to take two tablets at the same time: one with ezetimibe and another with indapamide" - reads the release.

In addition, the active substance in these tablets is present only in its insoluble, crystalline form, poorly-absorbed by the body.

Researchers quoted by the University of Silesia press section emphasized that a real challenge in the process of amorphisation of these two substances was obtaining an amorphous composition of the two drugs, characterized by high physical stability.

"Amorphous drugs are by definition thermodynamically unstable, which means that they may return to their original, crystalline form during storage or production, thereby losing valuable properties. Each drug has a specific shelf life - it is also the minimum period during which the test substances must maintain their amorphous form - which is why the physical stability studies of the patented drug composition took three years" - reads the release.

The composition developed by the researchers has many advantages, according to its creators. As indicated - efficacy of ezetimibe and indapamide can be improved by transforming these drugs into their amorphous forms. This, in turn, allows to reduce the dose of the drug required to achieve the desired therapeutic effect, thus reducing the risk of side effects.

"In addition, the amorphous drugs are easier to bind, so significantly less binding substances are used to produce tablets containing amorphous pharmaceuticals. This results in a reduction in the size of the tablet" - the researchers emphasised.

In addition, including two active substances in one tablet improves patient comfort - fewer pills mean easier dosing. It also means one tablet instead of two different tablets, so one package.

According to the university, the authors of the invention are: Director of the Silesian Centre for Education and Interdisciplinary Research Prof. Marian Paluch and employees of the Department of Biophysics and Molecular Physics of the University of Silesia: Dr. Justyna Knapik-Kowalczuk, Dr. Żaneta Wojnarowska and Dr. Katarzyna Grzybowska (PAP)

author: Agnieszka Kliks-Pudlik

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