World Unique Innovation

A new “aspirin” after 50 years

Aspirin is an effective and inexpensive medicine that millions take daily to prevent heart attacks and strokes. Who could improve on that?

The inventor of aspirin

In ancient times, salicylate-containing plants such as willow were commonly used to relieve pain and fever. A salicylate is a salt or ester of salicylic acid . Salicylates are thought to protect the plant against insect damage and disease. Aspirin is a derivative of salicylic acid. It is known as acetylsalicylic acid.

In 1897, a German chemist, Dr. Felix Hoffman, working for the Bayer company, was able to modify salicylic acid to create acetylsalicylic acid, which was named aspirin. However, the company dismissed the market potential of aspirin on the ground that it had an “enfeebling” action on the heart. At that time, the company was more interested on the potential of another new drug-heroin, which was also synthesized by the company.

Subsequently, aspirin was found to be more tolerable to the stomach than salicylic acid, which led to the widespread use of aspirin for pain relief. Furthermore, Hoffman’s acetylation of salicylic acid also proved its ability to prevent cardiovascular events. Aspirin, was considered by many as a wonder drug.   

One common adverse effect of aspirin is an upset stomach. More significant side effects include stomach ulcers, stomach bleeding and worsening asthma. Aspirin is not recommended in the last part of pregnancy.  

Aspirin is one of the most widely used medications globally, with an estimated 40,000 MT  (50 to 120 billion pills) consumed each year. It is on the World Health Organization’s List of Essential Medicines. It is available as a generic medication. In 2018, it was the 40th most commonly prescribed medication in the US, with more than 19 million prescriptions (wikepedia).

According to Bayer, the history of aspirin can be summarized in the following milestones.

1897

In a Bayer laboratory in Wuppertal, Germany, Dr Felix Hoffman was the first to succeed in synthesizing a chemically pure and stable form of acetylsalicylic acid (ASA), which became  the active ingredient of aspirin.

1899

Aspirin was registered as a trademark. It was launched on the market in powder form. Bayer delivered the medicine to pharmacies in small 250-grams glass vials. 500 mg of the powder was then weighed out and dispensed to customers in small paper bags. One year later, Bayer launched the analgesic in the classic tablet form-one of the first medicines to be marketed in dosage form.   

1915

Aspirin became available without prescription and became a best-seller in the US.

1949

Aspirin turned 50, and the following year, was the first time it featured in the Guinness Book of Records as the most frequently sold pain reliever in the world.

1969

A box of aspirin flied to the moon aboard Apollo 11.

1977

A study reported that aspirin could prevent ischemic stroke in appropriate patients. In the same year, the World Health Organization introduced its “Essential Drug List. Aspirin was included right from the start as an essential analgesic.

1997

Acetylsalicylic acid, the active ingredient in aspirin, celebrated its centenary.

1999

Aspirin took its place among such medical advances as the stethoscope and artificial heart when it was inducted into the Smithsonian Institution’s Museum of American History, US.

2004

British researcher Professor Derek W. Gilroy elucidated the anti-inflammatory properties of aspirin.

2012

Publication in the journal Headache by Lampl et al, which reaffirmed the effectiveness of aspirin as a first-time treatment of migraine or episodic tension type headache and found that pre-treatment headache did not predict potential success or failure of aspirin.

2014

The active ingredient of new aspirin, acetylsalicylic acid, was used in the form of microparticles that were on average 10 per cent of size of particles found in previous aspirin tablets.

Microparticles were combined with sodium carbonate, which acted as a disintegrant and local buffer, helping new aspirin dissolved more quickly, entered the bloodstream faster, and relieved  pain twice as fast as previous aspirin tablets.

(Source: bayer.com/en/products/aspirin)     

Enter a “new aspirin”: Vazalore

A US-based company, PLx Pharma (www.plxpharma.com) is trying to do that. According to the Barron’s online on September 20th, 2021, there has been no innovation in the aspirin market in over 50 years. The company, based in Sparta, New Jersey, US, is seeing an opportunity to launch a new product, Vazalore, in some 30,000 retail drug stores in the US.

The aspirin market is a crowded field, where aspirin has been around since 1899. The company noted that Vazalore’s advantage is that it reduces aspirin’s tendency to irritate the stomach for people who use it regularly, a problem that can lead to ulcers. In addition, Vazalore has been shown to achieve better absorption than coated aspirin, according to studies by Harvard Medical School cardiologist Deepak Bhatt, who heads PLx Pharma scientific advisory board. PLx Pharma is facing the challenge of convincing existing users of aspirin to switch to Vazalore. Vazalore will cost US$25 a month versus a few dollars for coated aspirin. It is estimated that 43 million Americans take aspirin on their doctor’s advice, plus millions more to treat the symptoms of arthritis and other ailments.  The company estimates that every new customer will be worth US$230 a year to PLx Pharma, so that it could realize US$100 million in annual revenue from each 1 pe cent of those 43 million people.    

The Vazalore capsule holds a liquid formulation of aspirin bound up in lipid, which prevents the aspirin’s release until it passes through the stomach to the intestine. It was reported that PLx Pharma will apply its patented technology to ibuprofen and other drugs that give some users stomach problems.

We doubt users of aspirin will drop it anytime soon.