History of enzymes - Generations of enzyme drugs

Enzymes and alchemy?

The word “fermentation” comes from the ancient times. In the medieval times the word meant “magical” processes, similar to fermentation of wine and dough. Alchemists were searching for those magical “ferments” – it was believes that “ferments” could start chemical processes without human work. But the actual cnowledge about ferments (enzymes) was collected piece by piece...

History of enzymes

In the mid of the 17th century, a scientist, anatomist and chemist Franciscus Sylvius proved, that human pancreas produces special fluid, which is then mixed with food. This lead to a long way of understanding of the nature and role of enzymes in the human body. The 19th century was more generous in discoveries:

Louis Pasteur, studying the process of vine fermentation, came to conclusion that certain “vital force” in the yeast is the cause of fermentation.
It was proven, that pancreatic fluid has alkaline reaction and contains much protein.
A hypothesis is made, that unlike saliva, pancreatic fluid breaks down carbohydrates and proteins with fats as well. This was especially important with regard to fats which are rather hard to break down. This lead to a conclusion that steatorrhea (non-absorption of fats) is a direct symptom of pancreatic illness, because without this organ assimilation of fats is not possible. Claude Bernard managed to derive digestive substance itself from the pancreatic fluid and called it pancreatine.
E.Buchner has discovered extracellular fermentation, for which he was awarded with the Noble prize.
For the first time, highly purified crystal enzyme was extracted (urease). For the next decade several more enzymes were extracted.
Extraction of calf pancreas was for the first time used in the treatment of the diabetes. As a result of treatment, patient started digesting fats and proteins much better.
Alexander Yakovlevich Danilevskiy has suggested that one and only enzyme pancreatine cannot break down fats, and proteins, and carbohydrates. While pancreatic fluid breaks down all three. He suggested there are three different enzymes.
The first information on successful treatment of pancreatic illness with the help of pancreatine appeared.
And finally the first patent was given for the production of the first enzyme preparation in tablets.

Generations of enzymes

At the end of 19th century it was found, that pancreatine in the stomach loses its activity significantly, because enzymes are destroyed by stomach fluid. In order to avoid that, company producing pancreatine started making it is the shell of tannin, and called it Pankreon. Over time the shell was improved, became more stabile so that is would dissolve only in the intestine – that was the second generation of enzymes.

After some time it was proven, that size of preparation particles is important. Smaller size would have allowed enzyme preparations to get faster with the crashed food from the stomach to the duodenum. Because “sliding” from stomach down with chime (crashed food mixed with stomach fluid) further to the intestine is only possible for particles no more than 1.5 mm in diameter. In addition, the smaller the granules, the faster enzymes are activated in the intestine. In 1963, enzyme drugs were improved again, and were produced as granules without shell.

So over time the third generation of enzymes has ”grown”. In 1983 microspheres were enclosed in a capsule (to protect enzymes from the stomach fluid). However, the technologies did not stop at that. It has been discovered that mini-microspheres 1.0-1.2 mm in diameter are a quarter more effective than microspheres with diameter 1.9-2.0 mm. So in 1993 a patent was received for production of pancreatine in the form of mini-microspheres (the fourth generation of enzyme preparations). Mini-microspheres have the diameter of approximately 1.2 mm – that diameter proved to be practically ideal for the best effectiveness of the preparations. And those are the enzyme drugs that are considered to be optimal for today. This is the technology used in producing Micrasim.