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Aspirin bottle, 1899

Aspirin, probably the best known brand in medicine

Probably the best known drug brand in the world turns 120. Aspirin. The brand name, which was entered in the trademark register of the Kaiserliches Patentamt (Imperial Patent Office) in Berlin on 6 March 1899, has long since become an international generic term. Acetylsalicylic acid is effective against fever, pain and inflammation and is probably the best-selling medicine in history.

However, this anniversary marks only one milestone in a long history. Salicin, which is converted into salicylic acid in the body, is found in the bark of willows. Its therapeutic effect has been known since time immemorial. The progenitor of all physicians, Hippocrates of Kos, described it around 400 B.C. as a medicine against fever and pain; Teutons and Celts cooked a broth from willow bark as medicine.

Aspirin has many fathers

Certificate of Kaiserliches Patentamt for registration of the trademmark Aspirin, 1899

Certificate of Kaiserliches Patentamt for registration of the trademmark Aspirin, 1899

The centuries-old knowledge handed down was scientifically tested and confirmed for the first time in modern times in 1763 for the British Royal Society. In 1828 Johann Andreas Buchner and Pierre-Joseph Leroux isolated salicin from willow bark extracts.

Charles Frédéric Gerhardt synthesized acetylsalicylic acid in non-pure form in 1853 in Strasbourg; Hugo von Gilm won impure o-acetylsalicylic acid as a water-insoluble solid in 1859. In 1869 Karl Kraut investigated the experimental procedures of the two and improved the extraction process. And in 1874, Chemische Fabrik v. Heyden in Radebeul delivered salicylic acid as the world's first industrially produced and packaged drug.

Who "invented" aspirin?

Photo of  Felix Hoffmann, around 1894

Felix Hoffmann around 1894

However, salicylic acid has disturbing side effects such as stomach complaints, so that the decisive step towards a well-tolerated drug was still to be taken. This took place on 10 August 1897 in Wuppertal-Elberfeld: In the laboratory of the "Farbenfabriken vorm. Friedr. Bayer & Co." scientists succeeded for the first time in synthesizing o-acetylsalicylic acid from acetanhydride and salicylic acid.

This "invention" is mostly attributed (by Bayer, among others) to the chemist Felix Hoffmann (1868-1946). However, aspirin is more likely to have been the result of teamwork. Almost half a century later, Arthur Eichengrün claimed to have been the driving force behind the first chemically completely pure synthesis of acetylsalicylic acid (ASA) and the development of aspirin; Hoffmann merely implemented his instructions at the time.

(Co-)inventor in a concentration camp

Arthur Eichengrün (around 1900)

Arthur Eichengrün (around 1900)

Eichengrün made these claims for the first time in a letter to Bayer, which he wrote in the Theresienstadt concentration camp. The important chemist (he was involved in 47 patents, e.g. pdf-Datei DE390840A, pdf-Datei US1175728A)) with Jewish roots had been abducted there by the Nazis in 1944. Until his death in 1949, Eichengrün insisted that his authorship was denied only because of his Jewish ancestry. For a long time, his claims were largely ignored. Only more recently did studies come to the conclusion that Eichengrün had indeed played the decisive role in the development of Aspirin ( e.g. by Walter Sneader . The version of the "lone inventor" Hoffmann is in any case no longer sustainable.

No German patent for Aspirin

Felix Hoffmann´s laboratory log, entry of 10.8.1897

Felix Hoffmann´s laboratory log, entry of August 10, 1897

But how big was the inventive step actually? Not big enough, the Kaiserliches Patentamt found and refused a patent in 1899. The complex background to this decision included the fact that Chemische Fabrik v. Heyden began marketing acetylsalicylic acid as a remedy in 1897, first under the chemical name and then under the trade name acetylin. In 1898, however, Felix Hoffmann succeeded in applying for a patent for aspirin in the United States ( pdf-Datei US 644077); the following year Bayer applied for a patent in Great Britain ( pdf-Datei GB 189909123A).

Initially betting on the wrong horse

Another important protagonist was Heinrich Dreser (1860-1924), who had headed Bayer's Pharmacological Laboratory since 1897 and therefore received royalties on the German sales of aspirin - in contrast to Hoffmann and Eichengrün, who were left empty-handed. As their superior, Dreser probably played his part in Hoffmann's and Eichengrün's work; he also presented aspirin to the public for the first time pharmacologically. But Dreser long gave internal preference to another drug, which Felix Hoffmann had developed shortly before and which allegedly had fewer side effects, and pushed it onto the market as a cough suppressant: diacetylmorphine, better known under his brand name registered by Bayer: Heroin (word-picture mark DE 31650 of 16 May 1898, deleted).

Kurt Witthauer (1865-1911), senior physician at the Diakonissenkrankenhaus Halle/Saale, also played an important role. He conducted the first clinical study on the use of aspirin and published it in 1899.

Mechanism of action only clarified in 1971

Kurt Witthauer´s study on Aspirin in Therapeutische Monatshefte 13, S. 330 (1899)

Kurt Witthauer´s study on Aspirin (Therapeutische Monatshefte 13, S. 330, 1899)

These four men made decisive contributions to the establishment of aspirin. But they never understood it correctly. In 1971, John Robert Vane discovered that it inhibited the biosynthesis of prostaglandins and was later awarded the Nobel Prize in Medicine 1982).

This discovery opened the doors for further exploration of the potential of ASS. Today, acetylsalicylic acid is on the World Health Organization's three times: as a non-opioid analgesic for mild pain and fever, as a remedy for acute migraine attacks and as a thrombocyte aggregation inhibitor for prophylaxis against strokes and heart attacks.

Pictures: Bayer AG, Bayer AG/Public domain, BayerAG/via Wikimedia Commons, via Wikimedia Commons, Public domain

Last updated: 19/07/19 

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