Treatment for gastrointestinal disorders using a selective, site-activated binding system

• US 20120329736A1
• Filed: 06/24/2011
• Published: 12/27/2012
• Est. Priority Date: 06/24/2011
• Status: Abandoned Application

• Current Assignee: LiveLeaf, Inc.
• Original Assignee: LiveLeaf, Inc.
• Inventors: Huang, Alexander L., Wu, Gin
• Application Number:
  US13/135,123
• Publication Number:
  US 20120329736A1
• Time in Patent Office: Days
• US Class Current: 514/25
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/05 Phenols cannabinoids A61K31/658
• CPC Class Codes: A61K 31/192 having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid cannabinoids A61K31/658
• CPC Class Codes: A61K 31/353 3,4-Dihydrobenzopyrans, e.g. chroman, catechin
• CPC Class Codes: A61K 31/7024 Esters of saccharides
• CPC Class Codes: A61K 33/40 Peroxides
• CPC Class Codes: A61K 36/82 Theaceae (Tea family), e.g. camellia
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 1/04 for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• CPC Class Codes: A61P 1/08 for nausea, cinetosis or vertigo; Antiemetics
• CPC Class Codes: A61P 1/12 Antidiarrhoeals
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 3/00 Drugs for disorders of the metabolism of the blood or the extracellular fluid A61P7/00
• CPC Class Codes: A61P 31/00 Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics

Abstract

The teachings provided herein generally relate to site-activated binding systems that selectively increase the bioactivity of phenolic compounds at target sites. More particularly, the systems taught here include a phenolic compound bound to a reactive oxygen species, wherein the phenolic compound and the reactive oxygen species react at a target area in the presence of an oxidoreductase enzyme.

Claims

1. A method of treating a gastrointestinal condition, the method comprising:

administering an effective amount of a binding system to a damaged tissue of the subject, the binding system comprising

a phenolic compound component comprising a tannin having a molecular weight ranging from about 500 Daltons to about 4000 Daltons; and

,

a reactive oxygen species component comprising hydrogen peroxide;

wherein,

the hydrogen peroxide is releasably bound to the tannin at a tannin;

peroxide weight ratio that ranges from about 1;

1000 to about 10;

1;

the binding system is bioactivated at a target site having an oxidoreductase enzyme that is expressed in response to a tissue damage of a subject;

the phenolic compound component binds to the target site selectively, the target site consisting of the damaged tissue; and

,

the binding system contains no, or substantially no, unbound hydrogen peroxide prior to the bioactivating at the target site;

wherein the binding system functions as an antitoxin, an anti-inflammatory, or an antimicrobial when bioactivated at the target site of a damaged tissue and assists in the healing of the damaged tissue by inactivating compounds that promote the condition at the target site.

2. The method of claim 1, wherein the phenolic compound component comprises a hydrolysable tannin, a condensed tannin, or a combination thereof.

3. The method of claim 1, wherein the phenolic compound component comprises a flavanol.

4. The method of claim 1, wherein the phenolic compound component comprises a catechin.

5. The method of claim 1, wherein the phenolic compound component comprises gallic acid, epigallic acid, or a combination thereof.

6. The method of claim 1, wherein the weight ratio of the tannin:

peroxide ranges from about 1;

1 to about 1;

50.

7. The method of claim 1, wherein the gastrointestinal disorder is irritable bowel syndrome.

8. The method of claim 1, wherein the gastrointestinal disorder is inflammatory bowel disease.

9. The method of claim 1, wherein the gastrointestinal disorder is food poisoning.

10. A method of treating acute diarrhea in a subject, comprising:

orally administering an effective amount of a binding system to a damaged tissue of the subject, the binding system comprising

a phenolic compound component comprising a tannin having a molecular weight ranging from about 500 Daltons to about 4000 Daltons; and

,

a reactive oxygen species component comprising hydrogen peroxide;

wherein,

the hydrogen peroxide is releasably bound to the tannin at a tannin;

peroxide weight ratio that ranges from about 1;

1000 to about 10;

1;

the binding system is bioactivated at a target site having an oxidoreductase enzyme that is expressed in response to a tissue damage of a subject;

the phenolic compound component binds to the target site selectively, the target site consisting of the damaged tissue; and

,

the binding system contains no, or substantially no, unbound hydrogen peroxide prior to the bioactivating at the target site;

wherein, the binding system prevents, inhibits, or ameliorates a symptom of acute diarrhea in the subject when compared to a second subject in a control group in which the binding system was not administered.

11. The method of claim 10, wherein the symptom is selected from the group consisting of a stool score, heartburn, indigestion, urgency of defecation, nausea, vomiting, stomach pain, and bloating.

12. The method of claim 10, wherein the phenolic compound component comprises a hydrolysable tannin, a condensed tannin, or a combination thereof.

13. The method of claim 10, wherein the phenolic compound component comprises a flavanol.

14. The method of claim 10, wherein the phenolic compound component comprises a catechin.

15. The method of claim 10, wherein the phenolic compound component comprises gallic acid, epigallic acid, or a combination thereof.

16. The method of claim 10, wherein the weight ratio of the tannin:

peroxide ranges from about 1;

1 to about 1;

50.

17. A method of promoting weight gain in a subject, comprising:

orally administering an effective amount of a binding system to a damaged tissue of the subject, the binding system comprising;

a phenolic compound component comprising a tannin having a molecular weight ranging from about 500 Daltons to about 4000 Daltons; and

,

a reactive oxygen species component comprising hydrogen peroxide;

wherein,

the hydrogen peroxide is releasably bound to the tannin at a tannin;

peroxide weight ratio that ranges from about 1;

1000 to about 10;

1;

the binding system is bioactivated at a target site having an oxidoreductase enzyme that is expressed in response to a tissue damage of a subject;

the phenolic compound component binds to the target site selectively, the target site consisting of the damaged tissue; and

,

the binding system contains no, or substantially no, unbound hydrogen peroxide prior to the bioactivating at the target site;

wherein, the binding system increases the feed conversion ratio of the subject when compared to a second subject in a control group in which the binding system was not administered.

18. The method of claim 17, wherein the symptom is selected from the group consisting of a stool score, heartburn, indigestion, urgency of defecation, nausea, vomiting, stomach pain, and bloating.

19. The method of claim 17, wherein the phenolic compound component comprises a hydrolysable tannin, a condensed tannin, or a combination thereof.

20. The method of claim 17, wherein the phenolic compound component comprises a flavanol.

21. The method of claim 17, wherein the phenolic compound component comprises a catechin.

22. The method of claim 17, wherein the phenolic compound component comprises gallic acid, epigallic acid, or a combination thereof.

23. The method of claim 17, wherein the weight ratio of the tannin:

peroxide ranges from about 1;

1 to about 1;

50.

24. A method of improving or maintaining the gastrointestinal health of in a subject, comprising:

orally administering a binding system that selectively increases the bioactivity of phenolic compounds at a target site in the gastrointestinal tract, the system comprising;

a binding molecule component comprising a tannin having a molecular weight ranging from about 500 Daltons to about 4000 Daltons; and

,

a reactive oxygen species component comprising hydrogen peroxide;

wherein,

the hydrogen peroxide is releasably bound to the tannin at a tannin;

peroxide weight ratio that ranges from about 1;

1000 to about 10;

1;

the binding system is bioactivated at the target site, the target site having an oxidoreductase enzyme;

the binding molecule binds to the target site; and

,

the binding system contains no, or substantially no, unbound hydrogen peroxide prior to the administering.

wherein, the binding system improves the gastrointestinal health in the subject when compared to a second subject in a control group in which the binding system was not administered.

25. The method of claim 24, wherein the gastrointestinal health is measured by the amelioration of a symptom selected from the group consisting of a stool score, heartburn, indigestion, urgency of defecation, nausea, vomiting, stomach pain, and bloating.

26. The method of claim 24, wherein the gastrointestinal health is measured using a food conversion ratio.