The History of Aspirin and Salicin

The History of Aspirin and Salicin Aspirin or acetylsalicylic acid is a derivative of salicylic acid. It is a mild, non-narcotic analgesic that’s useful in the relief of headache as well as  muscle and joint aches. The drug works by inhibiting the production of body chemicals known as prostaglandins,  which are necessary for blood clotting and  for sensitizing nerve endings to pain. Early History The father of modern medicine was  Hippocrates, who lived sometime between 460 B.C and 377 B.C. Hippocrates left historical records of pain relief treatments that included the use of powder made from the bark and leaves of the willow tree to help heal headaches, pains and fevers. However, it wasn’t until 1829 that scientists discovered that it was a compound called salicin in willow plants that relieved the pain. In From A Miracle Drug Sophie Jourdier of the Royal Society of Chemistry wrote: It was not long before the active ingredient in willow bark was isolated; in 1828,  Johann Buchner, professor of pharmacy at the University of Munich, isolated a tiny amount of bitter tasting yellow, needle-like crystals, which he called salicin. Two Italians,  Brugnatelli  and Fontana, had in fact already obtained salicin in 1826, but in a highly impure form. By 1829, [French chemist]  Henri Leroux had improved the extraction procedure to obtain about 30g from 1.5kg of bark. In 1838,  Raffaele Piria  [an Italian chemist] then working at the Sorbonne in Paris, split salicin into a sugar and an aromatic component (salicylaldehyde) and converted the latter, by hydrolysis and oxidation, to an acid of crystallised colourless needles, which he named salicylic acid. So while Henri Leroux  had extracted salicin in crystalline form for the first time, it was Raffaele Piria  who succeeded in obtaining the salicylic acid in its pure state. The problem, though, was that salicylic acid was hard on the stomach and a means of buffering the compound was needed. Turning an Extract Into Medicine The first person to achieve the necessary buffering  was a French chemist named  Charles Frederic Gerhardt. In 1853, Gerhardt neutralized salicylic acid by buffering it with sodium (sodium salicylate) and acetyl chloride to create acetylsalicylic acid. Gerhardts product worked but he had no desire to market it and abandoned his discovery. In 1899, a German chemist named  Felix Hoffmann, who worked for a German company called  Bayer, rediscovered Gerhardts formula. Hoffmann made some of the formula and gave it to his father who was suffering from the pain of arthritis. The formula worked and so Hoffmann then convinced Bayer to market the new wonder drug. Aspirin was patented on February 27, 1900. The folks at Bayer came up with the name Aspirin. It comes from the â€Å"A in acetyl chloride, the spir in spiraea ulmaria (the plant they derived the salicylic acid from) and the â€Å"in† was a then familiar name ending for medicines. Before 1915, Aspirin was first sold as a powder.  That year, the first Aspirin tablets were made. Interestingly, the names Aspirin and Heroin were once trademarks belonging to Bayer. After Germany lost World War I, Bayer was forced to give up both trademarks as part of the Treaty of Versailles in 1919.