Aspirin: Turn of the Century Miracle Drug

Daniel R. Goldberg

The beginning of aspirin as we know it today dates from the same period when Farbenfabriken vorm. Friedrich Bayer and Company, a dye-manufacturing firm in Germany, began to shift its focus from the dye industry to pharmaceutical production. Because the Bayer Company was already well known, it easily developed brand-name recognition as a pharmaceutical maker. The company’s shift to pharmaceutical production coincided serendipitously with a boom in new pharmaceutical agents, making it seem that a new drug was put on the market almost daily.

Just as the medical benefits of salicylic acid had long been known, so too had some of the health issues related to prolonged use of large doses of the drug. Such use often led to gastrointestinal irritation, which could in turn lead to nausea, vomiting, bleeding, and ulcers. In 1895, to counteract such problems, Arthur Eichengrün, the head of chemical research at Bayer, assigned the task of developing a “better” salicylic acid to one of the company’s chemists, Felix Hoffmann. Eventually cited by many as the discoverer of aspirin, Hoffmann approached the task with a personal interest: his father suffered from rheumatism and was taking salicylic acid for it, but he could no longer ingest the drug without vomiting. Hoffmann’s search through the available scientific literature yielded a way to alter salicylic acid chemically through modification of the hydroxyl group on the benzene ring. The key to his discovery, although realized only later, was that this chemical transformation provided a new molecule that the body could absorb without significant gastrointestinal distress. Once ingested, the new molecule was converted back to salicylic acid in the stomach, liver, and blood, thereby providing the desired therapeutic benefits. As such, modern synthetic aspirin can be considered a drug-delivery system for a natural product that has been in medical use for literally thousands of years.

However, this new derivative of salicylic acid did generate some controversy. There was a difference in opinion regarding the potential benefits of acetylsalicylic acid, which would ultimately become a personal dispute as well as a scientific one. Heinrich Dreser, who was responsible for the standardized testing of pharmaceutical agents, disagreed with Eichengrün’s approach to the drug. Eichengrün had distributed Hoffmann’s compound to local physicians, whereas Dreser had no initial interest in supporting the new drug. Ironically, it would be Dreser who published the first article on aspirin, probably because his contract with Bayer provided him royalties for any drug he introduced; Hoffmann and Eichengrün could only gain monetary rewards on patentable compounds. In the article Dreser compared aspirin with other salicylates in an effort to demonstrate that it was more beneficial and less toxic. This work was coupled with human trials whose results were published in 1899 in the journals Die Heilkunde and Therapeutische Monatshefte, showing that aspirin was indeed superior to other known salicylates. On 6 March 1899 the Bayer Company registered the product under the trade name Aspirin and then actively began to distribute the white powder to hospitals and clinics.