Around 4,000 or even 5,000 years ago, the ancient Sumerians discovered that consuming willow bark could alleviate pain. Over 2,800 years ago, the Ebers Papyrus recorded the use of dried willow leaves for pain relief by the ancient Egyptians. The earliest Chinese pharmacological work, “Shen Nong’s Herbal Classic,” mentioned that the roots, bark, branches, and leaves of the willow tree could be used medicinally to dispel phlegm, improve vision, clear heat and toxins, promote diuresis, and prevent wind-related conditions. Externally, it could be applied to alleviate toothache.
In 1758, an Englishman named Stone (E. Stone) proved that consuming powdered willow bark could treat fever and effectively relieve muscle and headache symptoms. Throughout the 19th century, the active ingredients of the medication were gradually discovered. In 1828, a German named Buchner (J. Buchner) extracted a yellow crystalline active component, known as salicin, from willow bark. In 1838, a French pharmacist named Leroux (H. Leroux) and an Italian chemist named Piria (R. Piria) isolated and purified salicin as an active ingredient. Due to its acidic taste, it was named salicylic acid. In 1852, a Frenchman named Gerhart (C. Gerhart) discovered the molecular structure of salicylic acid and synthesized it chemically for the first time. In 1876, MacLagan (T. J. MacLagan) published an article in The Lancet, confirming that salicin could relieve rheumatic fever and arthritis inflammation.
A German chemist named Kolbe (H. Kolbe) achieved the artificial synthesis of salicylic acid but found its taste extremely unpleasant and highly irritating to the stomach. In 1897, under the guidance of Eichengrün (A. Eichengrün), a scientist at the Bayer company in Germany, Hoffman (F. Hoffman) modified salicylic acid to synthesize high-purity acetylsalicylic acid. It was later confirmed that acetylsalicylic acid had clinical efficacy in pain relief, inflammation, and fever.
In March 1899, Bayer registered acetylsalicylic acid as “Aspirin,” making it the world’s first non-steroidal anti-inflammatory drug.
Although Aspirin was effective, the required dosage was high and could easily lead to side effects such as allergies, bleeding, and digestive problems. With the introduction of new analgesics (such as ibuprofen), the status of Aspirin gradually weakened.
In 1952, the inventor of ibuprofen, Adams (S. Adams), became a member of the British company Boots and focused on the development of drugs for rheumatoid arthritis. After getting drunk one night, he experienced severe headaches and thought of using the recently synthesized compound isobutylphenyl propionic acid (ibuprofen). After trying it himself, he found its analgesic effect to be surprisingly good. Upon sobering up, Adams immediately embarked on further research.
In 1962, Boots registered the patent for ibuprofen. In 1969, the UK approved ibuprofen as a prescription drug, and in 1983, it became an over-the-counter analgesic and antipyretic. Due to its affordable price and rapid analgesic effect, ibuprofen became popular worldwide. It had a significant effect in relieving menstrual pain, toothaches, lower back pain, and joint pain, making it one of the best-selling drugs in the world.