For many years, researchers have been searching for methods to make the lively ingredient acetylsalicylic acid (ASA)—the lively ingredient of aspirin—extra water-soluble. It is used not solely as ache reduction, but additionally to stop the formation of life-threatening blood clots in coronary heart assaults and strokes. The sooner the drug works, the higher.

A crew from the Inorganic Chemistry Division at Ruhr College Bochum, Germany, headed by Dr. Klaus Merz has now succeeded in combining the lively ingredient with an ineffective excipient to type a co-crystal that makes it extra water-soluble and thus more practical. Ruhr College Bochum has utilized for a European patent for this novel course of.

Alongside the event of latest lively pharmaceutical components, bettering the properties of established pharmaceutical merchandise is a specialist space of analysis. A technique to enhance properties is thru the intelligent design of crystalline substances often called co-crystals. Along with the lively ingredient, they comprise molecules of different substances, so-called co-formers, that are organized in a well-structured method within the crystalline materials.

“Image these two substances like a married couple: they’re at all times subsequent to one another, however they don’t seem to be firmly linked,” says Klaus Merz. “If the co-crystal comes into contact with water, the bond dissolves and the lively ingredient is launched, whereas the excipient is degraded or excreted.”

When the water solubility of ASA is improved on this means, the lively ingredient is of specific curiosity, as a result of it is used as a platelet aggregation inhibitor: It promotes blood move and reduces the danger of thrombosis. In sufferers with suspected myocardial infarction, ASA is used for speedy therapy. Early administration of ASA reduces mortality by 1 / 4.

“The substance patented right here, which incorporates the lively ingredient ASA, is considerably extra water-soluble than typical medicine and ensures that the lively ingredient is absorbed extra rapidly into the bloodstream and might consequently take impact extra rapidly,” says Klaus Merz.