GB2507472A

GB2507472A - Enzyme composition for enhancing digestion

Info

Publication number: GB2507472A
Application number: GB1216395.2A
Authority: GB
Inventors: Ajit Ramanial Patel
Original assignee: Individual
Current assignee: Individual
Priority date: 2012-09-13
Filing date: 2012-09-13
Publication date: 2014-05-07
Also published as: GB201216395D0

Abstract

A composition for oral ingestion comprises protease, lipase, amylase, papain, bromelain, lactase and amyloglucosidase (gamma-amylase). Preferably the composition comprises 10-30% by weight protease; 10-30% by weight lipase; 10-30% by weight amylase; 10-40% by weight papain; 10-40% by weight bromelain; 5-10% by weight lactase; and 5-10% amyloglucosidase. Preferably the composition comprises 60mg protease; 50mg lipase; 60mg lipase; 80mg papain; 75mg bromelain; 25mg lactase; and 20mg amyloglucosidase. Preferably the composition is substantially free of vitamins, calcium, magnesium and potassium and compounds thereof and dietary minerals such that preferably the composition consists of protease, lipase, amylase, papain, bromelain, lactase and amyloglucosidase. Preferably the composition is useful in enhancing digestion or, in particular, treating the symptoms of irritable bowel syndrome, coeliac (celiac) disease, lactose intolerance or pancreatic insufficiency.

Description

A COMPOSITION FOR ENHANCING DIGESTION

This invention relates to a composition for enhancing digestion.

Background of the invention

Food is broken down in the body to release energy and micronutrients, which are essential to fuel processes in the body. Food is broken down mechanically (e.g. by chewing) and chemically (e.g. by acid hydrolysis in the stomach). In the gastrointestinal (GI) tract, large pieces of ingested food are broken down into smaller pieces and macromolecules are digested into forms that may be absorbed into the blood stream.

Enzymes present in the 01 tract assist with digestion by increasing the rates of reactions. Each enzyme increases the rate of break down of a particular substrate or class of substrates, such as proteins, carbohydrates and fats.

The body produces and secretes into the GI tract digestive enzymes in response to ingestion of a meal. This helps digest food quickly and efficiently, thus ensuring that energy and micronutrients present in the food are released and absorbed by the body to the greatest possible extent.

However, the capacity of the digestive system is finite. Ingestion of a heavy meal can overwhelm the digestive system, wherein for example the amounts of digestive enzymes required exceed the amounts produced. Thus, larger lumps of food and larger macromolecules remain in the 01 tract for longer. This can slow down digestion, leading to an uncomfortable, prolonged feeling of being full and "bloated". Additionally, slower transit of food through the digestive system can lead to partial fermentation of the food by bacteria naturally present in the 01 tract.

thereby producing increased flatulence or trapped wind, which can be embarrassing and painful.

Additionally, an overwhelmed digestive system can pass food undigested, which can lead to diarrhoea by irritating the intestinal wall or constipation caused by partial physical blockage of the 01 tract.

Problems associated with ingestion of a heavy meal are exacerbated in subjects who have a digestive disorder such as irritable bowel syndrome, coeliac disease or lactose intolerance, which can render the digestive system inflamed and/or less efficient. Furthermore, a subject's digestion can be compromised if their pancreas does not effectively produce digestive enzymes in a condition known as pancreatic insufficiency, which can be caused for example following pancreatic cancer.

Papain is a cysteine peptidase found in and produced from the latex of Carica papaya. Papain has historically been used to tenderise meat through the breakdown of muscle fibres and connective tissue. Suggested medical uses for papain include removing damaged body tissue and home-treatment of animal bites conferring peptide toxins (e.g. from jellyfish). Papain has an optimum activity at around pH 6 to 7.

Bromelain is a cysteine protease enzyme extracted from the plant family Bromellaceae, which includes pineapples (Ananas comosus). It can take the form of fruit bromelain (Enzyme Commission number 3.4.22.33) or stem bromelain (Enzyme Commission number 3.4.22.32). It is typically provided as an extract made from the stem of pineapples comprising both fruit and stem bromelain.

Bromelain has historically been used to tenderise meat, but also has a number of suggested medical uses, which include the following: treating hay fever, colitis and damaged body tissue; relaxing muscles; stimulating muscle contractions; slowing blood clotting; improving the absorption of antibiotics; and preventing cancer.

Bromelain has an optimum activity at around pH 4.5 to 5.5.

Pancreatic insufficiency may be treated using pancreatin or pancrelipase, which contain a mixture of pancreatic trypsin (serine protease), alpha amylase and lipase. However, this treatment is specifically targeted at dealing with pancreatic insufficiency. Furthermore, the optimal pH for trypsin activity is pH 7.5-8.5, thus the action of the enzyme is delayed while the enzyme passes through the acidic medium of the stomach before it reaches regions of the GI tract where the pH is mire optimal.

US 2010/0135919 relates to a formulation containing a number of proteolytic enzymes and dietary minerals.

US 2008/0268095. RU 2352147, US 6.203,797 and US 6.605.306 relate to formulations comprising papain and bromelain.

Thus, at present, numerous substances and combinations of substances have been used to improve digestion. However, there is a need for an alternative or improved nutritional supplement that improves digestion with a shorter delay while minimising the effects of food intolerance.

Summary of the invention

The present invention provides an alternative or improved composition for enhancing digestion.

Accordingly, in a first aspect, the invention provides a composition for oral ingestion comprising protease, lipase, amylase (alpha-amylase), papain, bromelain, lactase and amyloglucosidase (gamma-amylase).

In the invention, the protease, papain and bromelain break down proteins and peptides, the amylase, amyloglucosidase and lactase break down carbohydrates and the lipase breaks down fats.

Thus, the invention provides a composition that advantageously includes several components that work in tandem to enhance digestion.

In the invention, the term protease' refers to any protease or mixture of proteases that assists in proteolysis. The protease may be a serine protease (e.g. trypsin, chymotrypsin or carboxypeptidase), cysteine proteases (e.g. actinidin) or aspartate proteases (e.g. pepsin).

Inclusion of bromelain in the formulation of the invention advantageously allows proteolytic activity at reduced pH levels, thus catalysing proteolysis in the acidic environment of the stomach.

The term amylase' as used herein refers to alpha-amylase, which breaks down long-chain carbohydrates at random locations in the chain to yield short-chain carbohydrates and/or saccharide units. Amylase is naturally found in saliva and pancreatic excretion and is most efficient in neutral environments, having an optimum activity at around pH 7.

The term amyloglucosidase' as used herein refers to gamma-amylase, which cleaves ci(1-6) glycosidic linkages, as well as terminal ci(1-4)glycosidic linkages at the non-reducing end of amylose and amylopectin, yielding glucose.

Amyloglucosidase is most efficient in acidic environments and has an optimum activity at pH 3. Inclusion of amyloglucosidase in the formulation of the invention has the advantageously enhances carbohydrate digestion by being active in the acidic sections of the GI tract.

Lactase is involved in the hydrolysis of the lactose dimer into galactose and glucose monomers. The use of lactase in the formulation of the invention is thought to be particularly advantageous for those suffering from lactose intolerance. By breaking down lactose, the formulation of the invention is thought to reduce the level of intestinal mucosal inflammation, thereby enhancing absorption of all nutrients into the bloodstream in the GI tract.

The term lipase as used herein refers to any lipase or mixture of lipases that assists digestion of fat, for example, pancreatic lipase.

The composition may contain from 5 to 70 % by weight of the protease, from 5 to 70 % by weight of the lipase, from 5 to 70 % by weight of the amylase, from 5 to 80 % by weight of the papain, from 5 to 80 % by weight of the bromelain, from 2 to 50 % by weight of the lactase and from 2 to 50 % by weight of the amyloglucosidase.

More particularly, the composition may contain from 10 to 30 % by weight of the protease, from 10 to 30 % by weight of the lipase, from 10 to 30 % by weight of the amylase, from 10 to 40 % by weight of the papain, from 10 to 40 % by weight of the bromelain, from 5 to 10 % by weight of the lactase and from 5to 10% by weight of the amyloglucosidase.

The composition may contain from ito 10 parts by weight of the protease, from 1 to 10 pads by weight of the lipase, from ito 10 parts by weight of the amylase, from ito 15 parts by weight of the papain, from ito 15 parts by weight of the bromelain, from 0.3 to 9 parts by weight of the lactase and from 0.3 to 9 parts by weight of the amyloglucosidase.

More particularly, the composition may contain from 20 mg to 250 mg of the protease, from 20 mg to 250 mg of the lipase, from 20 mg to 250 mg of the amylase, from 30 mg to 300 mg of the papain, from 20 mg to 300 mg of the bromelain, from 5mg to 100mg of the lactase and from 5mg to 100mg of the amyloglucosidase.

For example, the composition may contain from 30 mg to 120 mg of the protease, from 25 mgto 100mg of the lipase, from 30 mgto 120mg of the amylase, from 40 mg to 160mg of the papain, from 30 mgto 150mg of the bromelain, from 10 mgto mg of the lactase and from 10 mg to 40 mg of the amyloglucosidase.

In one preferred embodiment, the composition may contain approximately 60 mg of the protease, approximately 50 mg of the lipase, approximately 60 mg of the amylase, approximately 80 mg of the papain, approximately 75 mg of the bromelain, approximately 25 mg of the lactase and approximately 20 mg of the amyloglucosidase.

The components (and the concentrations thereof) of the compositions of the invention are preferably selected such that there is a synergistic enhancement of digestion.

The composition is typically substantially or completely free of vitamins.

The composition is typically substantially or completely free of calcium, magnesium and potassium, and compounds thereof.

The composition may be substantially or completely free of dietary minerals.

The term dietary mineral' as used herein refers to chemical elements and compounds thereof that are essential for the biochemistry of mammals, other than carbon, nitrogen, sulphur, oxygen and hydrogen. Examples of dietary minerals are calcium, phosphorous, magnesium, potassium, sodium, zinc and iodine.

The composition is typically substantially or completely free of dietary trace elements.

The term dietary trace elements' as used herein refers to a dietary element that is essential in trace amounts for the physiology of the organism. This definition includes trace elements such as zinc, manganese, copper, iodine, selenium and molybdenum.

The term substantially free' means less than 5 pg, preferably less than 1 pg of the component is present in the composition of the invention.

In an embodiment of the invention, the composition consists or consists essentially of protease, lipase, amylase, papain, bromelain, lactase and amyloglucosidase, optionally with one or more pharmaceutically acceptable excipients such as fillers, colourants and flavourings. Preferably the filler is rice flour.

By consists essentially' it is meant that the compositions contain the recited components with less than 5 pg, preferably 1 pg of other components.

Thus, the formulation is targeted specifically at enhancing digestive enzyme levels and typically does not contain any additional nutritional components (e.g. vitamins or dietary minerals), the dosing of which would change when the dosing of the enzymes is changed. Since any additional nutritional components may e.g. become toxic at high doses, inclusion of such components could render dosing of the composition inflexible or difficult without medical supervision. Accordingly, the present compositions advantageously simplify dosing.

The compositions of the invention may be presented in any pharmaceutically acceptable form, such as capsules, tablets, powders or liquids, preferably capsules. Capsules of the invention may be filled with powder, pellets, gel or liquid.

Tablets of the invention may take the form of chewable tablets, dispersible tablets or tablets designed to be swallow whole. Powders of the inventions may be designed for dissolution or suspension in water and may optionally comprise an agent or agents that produce effervescence on addition to water. Liquids of the invention may take the form of a solution, suspension or emulsion.

The compositions of the invention may also be presented as medical devices, the term medical device as used herein referring to a substance which whilst providing a medical benefit to a subject, is not absorbed significantly from the subject's 01 tract and does not exert its actions by pharmacological means.

The composition, capsule or medical device of the invention as defined herein may be used for enhancing digestion.

The composition, capsule or medical device of the invention as defined herein may be used for treating the symptoms of irritable bowel syndrome, coeliac disease, lactose intolerance or pancreatic insufficiency.

The components of the formulation of the invention may be obtained a number of commercial enzyme suppliers.

Alternatively, the enzymes may be sourced from one or more natural sources. For example, bromelain may be obtained from pineapple stems or fruit, and papain may be obtained from the latex of Carica papaya. Each may be isolated from the natural source, or taken as powdered natural source.

Accordingly, the bromelain may be presented in the form of a liquid or powdered extract of pineapple stem or fruit. When presented as a pineapple extract, the bromelain is preferably presented in powder form, wherein at least 99.5% by weight of the particles forming the powder have a particle size (e.g. diameter) of 600 pM or less. Such particles will pass through a 30 mesh sieve. In one embodiment, at least 99.5% by weight of the particles have a particle size (e.g. diameter) of 400 pM or less. Such particles will pass through a 40 mesh sieve. In another embodiment, at least 99.5% by weight of the particles have a particle size (e.g. diameter) of 300 pM or less. Such particles will pass through a 50 mesh sieve. In a further embodiment, at least 95% by weight of the particles have a particle size (e.g. diameter) of 210 pM or less. Such particles will pass through a mesh sieve. In another embodiment, at least 75% by weight of the particles will pass through a 50 to 60 mesh sieve and have particle sizes in the range from 230 to 280 pM.

The papain may be presented in the form of a liquid or powdered extract of C. papaya latex. When presented as a papaya extract, the papain is preferably presented in powder form, wherein at least 99.5% by weight of the particles forming the powder have a particle size (e.g. diameter) of 600 pM or less. Such particles will pass through a 30 mesh sieve. In one embodiment, at least 99.5% by weight of the particles have a particle size (e.g. diameter) of 400 pM or less. Such particles will pass through a 40 mesh sieve. In another embodiment, at least 99.5% by weight of the particles have a particle size (e.g. diameter) of 300 pM or less.

Such particles will pass through a 50 mesh sieve. In a further embodiment, at least 95% by weight of the particles have a particle size (e.g. diameter) of 210 pM or less. Such particles will pass through a 70 mesh sieve. In another embodiment, at least 75% by weight of the particles will pass through a 50 to 60 mesh sieve and have particle sizes in the range from 230 to 280 pM.

In the compositions of the present invention, all the enzymes may be presented in powder form.

The compositions of the invention are typically administered with or without meals one or more times per day. For example, the compositions may be administered from one to four times per day.

The compositions may be administered so that the daily intakes of the components areasfollows: Protease: 10 mg to 0.59 Lipase: 10 mg to 0.59 Amylase: 10 mg to 0.59 Papain: 10 mg to 0.69 Bromelain: 10 mg to 0.69 Lactase: 5 mg to 0.2 g Amyloglucosidase: 5 mg to 0.2 g The compositions of the invention enhance the capacity of the digestive system to digest food by replacing missing enzymes or replenishing enzymes used following aheavymeal.

The compositions of the invention may also enhance the level of absorption of nutrients by the intestine by reducing the level of diet-induced irritation, for example, by breaking down lactose.

The compositions of the invention may also reduce the level of digestive disturbances such as constipation, diarrhoea, flatulence and trapped wind caused by mucosal lining irritation or the passage of undigested food.

The invention will now be illustrated, but not limited, by reference to the following

specific example.

EXAMPLE 1

Capsule formulation 1 Two part capsule shells formed from hydroxypropyl methylcellulose are filled with a mixture of protease, lipase, amylase, papain, bromelain, lactase, amyloglucosidase and filler in the following amounts per capsule: Protease: 60 mg Lipase: 50 mg Amylase: 60 mg Papain: 80 mg Bromelain: 75 mg Lactase: 25 mg Amyloglucosidase: 20 mg Filler (rice flour): 120 mg Two to three capsules per day are taken as a food supplement after meals.

It will readily be apparent that numerous modifications and alterations may be made to the specific embodiments of the invention described above without departing from the principles underlying the invention. All such modifications and alterations are intended to be embraced by this application.

Claims

CLAIMS1. A composition for oral ingestion comprising protease, lipase, amylase, papain, bromelain, lactase and amyloglucosidase.
2. A composition according to claim 1 comprising from 5 to 70 % by weight of the protease, from 5 to 70 % by weight of the lipase, from 5 to 70 % by weight of the amylase, from 5 to 80 % by weight of the papain, from 5 to 80 % by weight of the bromelain, from 2 to 50 % by weight of the lactase and from 2 to 50 % by weight of the amyloglucosidase.
3. A composition according to claim 2 comprising from 10 to 30% by weight of the protease, from 10 to 30 % by weight of the lipase, from 10 to 30 % by weight of the amylase, from 10 to 40 % by weight of the papain, from 10 to % by weight of the bromelain, from 5 to 10 % by weight of the lactase and from 5 to 10 % by weight of the amyloglucosidase.
4. A composition according to claim 1 comprising from ito 10 parts by weight of the protease, from ito 10 parts by weight of the lipase, from ito 10 parts by weight of the amylase, from ito 15 parts by weight of the papain, from ito 15 parts by weight of the bromelain, from 0.3 to 9 pads by weight of the lactase and from 0.3 to 9 parts by weight of the amyloglucosidase.
5. A composition according to claim 1 comprising from 20 mg to 250 mg of the protease, from 20 mg to 250 mg of the lipase, from 20 mg to 250 mg of the amylase, from 30 mg to 300 mg of the papain, from 20 mg to 300 mg of the bromelain, from 5mg to 100 mg of the lactase and from 5 mg to 100 mg of the amyloglucosidase.
6. A composition according to claimS comprising from 30mg to 120 mg of the protease, from 25mg to iOU mg of the lipase, from 30mg to 120mg of the amylase, from 40 mgto 160mg of the papain, from 30 mgto 150mg of the bromelain, from 10 mg to 50 mg of the lactase and from 10 mg to 40 mg of the amyloglucosidase.
7. A composition according to claim 6 comprising approximately 60 mg of the protease, approximately 50 mg of the lipase, approximately 60 mg of the amylase, approximately 80 mg of the papain, approximately 75 mg of the bromelain, approximately 25 mg of the lactase and approximately 20 mg of the amyloglucosidase.
8. A composition according to claim 7 comprising 60 mg of the protease, 50 mg of the lipase, 60 mg of the amylase, 80 mg of the papain, 75 mg of the bromelain, 25 mg of the lactase and 20 mg of the amyloglucosidase.
9. A composition according to any previous claim consisting of protease, lipase, amylase, papain, bromelain, lactase and amyloglucosidase.
10. A composition according to any previous claim that is substantially free of vitamins.
11. A composition according to any previous claim that is substantially free of calcium, magnesium and potassium, and compounds thereof.
12. A composition according to any previous claim that is substantially free of dietary minerals.
13. A composition according to any previous claim, wherein one or more of protease, lipase, amylase, papain, bromelain, lactase and amyloglucosidase in the form of a powder, gel or liquid.
14. A capsule oi tablet containing a composition according to any one of claims ito 13.
15. A medical device comprising a composition according to any one of claims itol3.
16. A composition, capsule, tablet or medical device according to any one of claims ito 15 for use in enhancing digestion or, in particular, treating the symptoms of irritable bowel syndrome, coeliac disease, lactose intolerance or pancreatic insufficiency.