Patents Pending on ENZALASE®

Enzalase®, with three patents pending, is the most advanced digestive enzyme supplement available. The following information summarizes the technologies that underpin these discoveries:

Patent #1: Protection from Stomach Acid

When food is present, the stomach produces hydrochloric acid, salt and a powerful proteolytic enzyme called pepsin. The pH of this gastric juice can range from 1.2-2.0 which is harshly acidic. Digestive enzymes are proteins that are sensitive to gastric juice and many lose activity when exposed for 1-2 hours, a typical transit time in the stomach.

When consumed unprotected, even plant based enzymes from fungal sources, often purported to be acid resistant, lose activity in the stomach. For example, the fungal lactase enzyme used in many commercial enzyme supplements loses over 96% of its activity (ability to digest lactose measured in ALU) after 2 hours at pH 1.2 (J Pharm Pharmaceutical Sci. 5(3): 234-244, 2002). This means a tablet containing 3,000 ALU of fungal lactase only delivers about 120 ALU into the small intestine where it needs to be to digest lactose. ENZALASE® by comparison delivers over 90% of its labeled lactase activity or 450 ALU. Another example of acid denaturation regards bromelain: When subjected to pH 2.0 spectroscopic studies reveal that a denatured state (unfolded polypeptide structure) that is irreversible (Eur. J. Biochem. 269, 47-52 , 2002); this sensitivity of bromelain is rarely acknowledged by enzyme formulators. Still another example of unacknowledged acid denaturation regards papain, the following statement was taken from Biochem. Biophys. Res. Commun. 341: 620-626, 2006 Jan. 13: “The four papain proteases have been found to undergo, at low pH, a conformational transition that instantaneously converts their native forms into molten globules that are quite unstable and rapidly degraded by pepsin.” Fungal proteases, commonly added to enzyme supplements and claimed to be acid resistant often are not, see Applied Microbiology, 30, No. 4, 507-513, Oct. 1975. And yeast Invertase, another enzyme found in commercial enzyme supplements, is also sensitive to acid denaturation, see Protein Science, 1, 120-131, 1992. The obvious conclusion here is that the reason many dietary supplements containing enzymes have not worked up to expectations is that a significant portion of their activity is lost in the stomach. ENZALASE® is the first digestive enzyme supplement to have significant acid-proof protection assuring that maximum activity gets delivered to the small intestine (Patent Pending).

The technology that makes ENZALASE® Acid-Proof® utilizes a natural, food grade carbohydrate from seaweed called sodium alginate. During production of ENZALASE® sodium alginate is mixed with 12 digestive enzymes and buffers and filled into cellulose capsules. When an ENZALASE® capsule enters the stomach it takes about 5-10 minutes for the capsule shell to dissolve, during this time a small amount of stomach acid enters the capsule and reacts with the sodium alginate that’s near the capsule shell. Instantly, a thin, insoluble gel of alginic acid forms and surrounds the enzymes, protecting them from stomach acid. This unique gel divides into fragments that stay intact until they enter the duodenum (first section of small intestine) where they revert back to soluble sodium alginate at the higher pH (6.5-7.5), releasing the enzymes unharmed. No other enzyme supplement has this degree of acid protection.

A word of caution: Some commercial enzyme supplements are enteric coated and claim acid resistance. Be sure to request the chemical name of the enteric coating used, do not use products coated with acrylic acid or related polymers (super glue) as they are potentially toxic. ENZALASE® is not enteric coated, its protective, food-grade, gel forms in the stomach.

Once in the small intestine ENZALASE’s Deep Release® technology, also part of the patent application, begins to operate. The sodium alginate that protected Enzalase® in the stomach now forms a new type of gel as it starts to dissolve and meets calcium ions, this resulting calcium alginate gel takes on a globular, cloud-like appearance as it moves deeper into the small intestine. As this gel-cloud moves along the length of the small intestine some of the enzymes separate in the duodenum and upper jujenum while others hang on and release deeper in the small intestine. In this way ENZALASE® provides not only primary digestive support in the upper small intestine (where the body’s pancreatic enzymes can use help) but also secondary digestive support much deeper in the small intestine where probiotics can benefit (See Probiotics + Enzymes = Gut Health for more details on Probiotic Stimulation by ENZALASE®).

Patent #2: Enhancement of Fat Digestion

ENZALASE® contains 6,000 FIP Units of lipase activity, the principal enzyme responsible for fat digestion. This amount of lipase is much higher than what is found in other enzyme supplements. Since lipase is one of the most expensive enzymes few supplement manufacturers add a sufficient amount. It’s important for an enzyme supplement to have high lipase activity as this one enzyme significantly boosts the activity of the other enzymes. Here’s how it works: When food moves from the stomach into the duodenum (this mixture is called chyme) it is coated or adsorbed with fat, even when a low fat meal is consumed there is fat present as a coating. Since fat is not soluble in water it resists the churning and mixing operations in the stomach and surfaces as a resilient water-proof film, coating the other food substances. This fat coating interferes with the activity of the enzymes responsible for protein, carbohydrate and fiber digestion. For example, the enzyme alpha-amylase, which digests starches, does not attach to starch molecules effectively if fat is in the way. The same is true for the protein digesting enzymes papain and bromelain, proteins coated with fat are hard for them to digest. So lipase acts to remove fat from the chyme so the other enzymes can operate at peak efficiency.

Job #1 for an enzyme supplement is to provide sufficient lipase activity that, when combined with the body’s own lipase (produced by the pancreas), can effectively digest the fatty coatings from the food mixture as it moves into and through the small intestine. When this process is not efficient, undigested fat contributes to high blood triglycerides and ultimately moves into the colon where it can cause undesirable microbial action and/or be expelled with the stool. Fatty stools are a symptom of lipase deficiency.

This important process of fat digestion cannot occur if the fat is not emulsified first, regardless of whether a high lipase enzyme supplement is taken. Emulsified means effectively dispersed in water. To accomplish this task the body produces bile in the liver which is injected into the duodenum at the proper time. When all is running on schedule inside a healthy 25 year old the timing is right and bile meets the fatty food when it arrives; unfortunately, aging and disease can negatively delay this process. ENZASTIM®, our trademark for a unique fat emulsifier, is added to ENZALASE® to help emulsify fat so the lipase enzymes can do their job more effectively (Patent Pending).

ENZASTIM® is a special form of dry polysorbate-80, a food grade emulsifier that is generally recognized as safe (GRAS) by the United States FDA. Polysorate-80 is both lipophilic (fat loving) and hydrophilic (water loving) – so like bile it helps fat disperse in water. Polysorbate-80 has been around for many years and has a long history of use in foods but only as an oily, sticky liquid. As such it could not be added to enzyme formulations like ENZALASE® without negatively affecting their shelf life (it was hygroscopic and would pull water into the product). So the scientists at THERABIOTICS, Inc. went to work and discovered a method of making a dry powder out of polysorbate-80 that could be added to dry digestive enzymes without negatively affecting shelf life, ENZASTIM® was born (Patent Pending).

Patent #3: Probiotic Stimulation

Species of Lactobacillus and Bifidobacterium (Bifidus) bacteria comprise the majority of probiotic microorganisms that colonize the human intestinal tract. These are beneficial microorganisms that are vital to our health, they perform many functions but foremost they maintain the soft lining (wall) of the small and large intestine in a healthy condition so nutrients can be effectively absorbed, waste products easily eliminated, and pathogenic microorganisms competitively excluded. Lactobacillus species such as L. acidophilus function best in the small intestine while Bifidobacterium species such as B. bifidum work best in the large intestine.

It has been said that a good probiotic supplement is more important than a multivitamin. This makes sense since effective vitamin and mineral absorption depends on a healthy intestinal soft lining which probiotics help maintain. Once a probiotic supplement has been ingested it must first make it through the harsh acidity of the stomach (Probiotics are more sensitive to stomach acid than enzymes!) and then it must grow and multiply within the intestinal tract as it begins the process of colonization. Enzyme supplements help probiotics grow and multiply by releasing critical nutrients that are readily utilized by the probiotic bacteria. These nutrients fall into two categories: cobiotics and prebiotics.

Cobiotics

Simple nutrients that are utilized both by us and probiotics are referred to by the scientists at Therabiotics, Inc. as cobiotics. Examples of cobiotics include amino acids (released when protease enzymes like papain and bromelain digest meat and vegetable proteins), monosaccharides such as glucose (which is released by the cooperative effort of alpha-amylase and glucoamylase acting on starch), and fatty acids like acetic acid (released by lipases and esterases). ENZALASE® contains these and other enzymes that have a cobiotic releasing effect.

Lactobacillus probiotics respond best to cobiotic nutrients since they reside largely in the ileum section of the small intestine. Bifidobacterium probiotics on the other hand do utilize cobiotics but rarely see them since they reside primarily in the large intestine where it’s unusual to see free cobiotics floating around (most are absorbed by the body or utilized by microbes in the small intestine). The probiotic Theralac® (see www.theralac.com) contains three important Lactobacillus strains that benefit from cobiotics: Lactobacillus paracasei F-19, Lactobacillus acidophilus LA-1 and Lactobacillus rhamnosus H-1. All three of these strains benefit significantly from the cooperative action of digestive enzymes that release cobiotics. ENZALASE® has been formulated to release cobiotics deep within the ileum section of the small intestine where Lactobacillus colonization always needs help (Patent Pending).

Laboratory studies conducted by Therabiotics, Inc. demonstrate that cobiotics, such as amino acids, glucose and acetic acid, stimulate Lactobacilli by 100-800% in flask cultures when controlled against simulated intestinal juice. People in a state of intestinal health usually produce sufficient cobiotics from the action of their body’s pancreatic enzymes and experience the benefits of a good probiotic without using a digestive enzyme supplement; however, such a supplement can confer additional benefits to these individuals if it fosters the deep release of cobiotics as ENZALASE® does. People with reduced pancreatic enzyme production (due to age, disease or genetics) may not experience the benefits conferred by probiotics without the help of an enzyme supplement.

Probiotics and digestive enzymes are, indeed, synergistic within the intestinal tract. Enzymes process and digest food as it moves through the intestines and in doing so help feed probiotics. Probiotics stimulate digestive enzymes by enhancing the absorption of nutrients released by these enzymes since the end products of enzyme action can inhibit further enzyme activity if not removed by absorption.

Prebiotics

Up until recently there has been a missing link in the process of feeding probiotics: The Bifidobacteria were left out. Bifidobacteria require special feeding in order to do well in the colon; although our research shows they gain a small advantage from cobiotics (cobiotics are so bioactive they disappear in the ileum and rarely make it into the colon) they need a more direct source of nutrition in order to effectively colonize the colonic wall. Prebiotics are that source of nutrition. Prebiotics are soluble fiber substances, mostly oligosaccharides or short chain sugar polymers, present in fruits and vegetables and certain grains. Prebiotics are not digested in the human small intestine but pass into the colon where they support Bifidobacteria growth and colonization and can be called bifidogenic. Fructooligosaccharides (FOS) and inulin are two bifidogenic prebiotics that get attention today although there are others such as partially hydrolyzed guar gum, PHGG, and certain marine hydrocolloids like sodium alginate that are equally effective. FOS type prebiotics are now added to a variety of functional foods with a mixed bag of results that range from improved intestinal function to the exact opposite: Pain, bloating and excess gas. Part of the problem stems from the use of synthetic FOS which is never found alone in nature but always in foods that contain other compounds that moderate bloating and gas (probably by controlling the growth of undesireable microbes that also consume FOS).

The answer you may think is to eat more fruits, vegetables and grains that are bifidogenic. Bananas, asparagus and rye bread, for example, contain 0.3%, 0.4% and 0.6% FOS respectively. Garlic contains a full 1% FOS. But, eating these foods is just half the answer. This brings us to the heart of the third patent application on ENZALASE®. The problem with bifidogenic foods like those above is prebiotics that don’t release and become available to the Bifidobacteria in the colon. The prebiotic soluble fibers are often bound within a matrix of insoluble fibers and lignins that varies in complexity from one food to another. For example, the fiber matrix in rye bread is quite complex and many people don’t get the FOS released so it passes out in the stool and is wasted. ENZALASE®, in addition to its protein, carbohydrate and fat digesting enzymes, contains a powerful group of fiber digesting enzymes that assist in the release of prebiotics from natural foods (Patent Pending). When you take ENZALASE® you stop wasting these precious prebiotics and start utilizing them to feed your Bifidobacteria.

The big three fiber digesting enzymes in ENZALASE® are:

• Cellulase* - 3000 CU/capsule
• Hemicellulase - 6,400 HCU/capsule
• Pectinase - 7,500 AJDU/capsule

* With significant Beta-glucanase and Xylanase side activity

This unique high potency mixture of fiber digesting enzymes goes after the insoluble fibers that bind the soluble prebiotic fibers, releasing the latter into the lower digestive tract. The digestion does not go to completion, this would not be desirable, it proceeds just enough to open up the complex fiber matrix to let the prebiotics out. The secret behind this discovery lies not just with the enzyme blend above but with the deep release technology that gets a portion of the enzyme activity into the lower intestinal tract. This assures that the prebiotics will show up close to where the Bifidobacteria live.

In the work that lead to our patent application we used rye bread in one of the examples demonstrating how this technology works: A beaker containing rye bread in deioinzed water was held for 24 hours at body temperature (37 C) with slow magnetic stirring before the bread was filtered off and the filtrate used (after autoclaving) as a growth medium for two different Bifidobacteria species. In a second beaker the rye bread was treated with one Enzalase® capsule for the same time period and a similar filtrate was made. The results were very pronounced in favor of the ENZALASE® treated rye bread: The filtrate from the ENZALASE® treated beaker supported 1,000 times more Bifidobacteria growth (both species!) than the untreated, control beaker.

See Probiotics + Enzymes = Gut Health for more information on Probiotic Stimulation with ENZALASE®.

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