Enteric-Coated Glucosinolates And Beta-Thioglucosidases

• US 20080311192A1
• Filed: 06/12/2007
• Published: 12/18/2008
• Est. Priority Date: 06/12/2007
• Status: Abandoned Application

• Current Assignee: Kraft Foods Group Brands LLC (The Kraft Heinz Company)
• Original Assignee: Kraft Foods Holdings Incorporated (Altria Group, Inc.)
• Inventors: Gaonkar, Anilkumar Ganapati, Ludwig, Cathy Jean, Matusheski, Nathan V., West, Leslie George, Windsor, Nicole Lee, Kim, Nam-Cheol, Lawrence, Leslie Lewis
• Application Number:
  US11/761,843
• Publication Number:
  US 20080311192A1
• Time in Patent Office: Days
• US Class Current: 424/463
• 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 31/375 Ascorbic acid, i.e. vitamin C; Salts thereof
• CPC Class Codes: A61K 31/7028 Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
• CPC Class Codes: A61K 38/47 acting on glycosyl compounds (3.2), e.g. cellulases, lactases
• CPC Class Codes: A61K 9/1652 Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin homeopathic globules A61K9/1623
• CPC Class Codes: A61K 9/5063 Compounds of unknown constitution, e.g. material from plants or animals oils, fats, waxes, shellac A61K9/5015
• 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 27/02 Ophthalmic agents
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 39/00 General protective or antinoxious agents
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system

Abstract

The present invention relates to a particulate composition comprising enteric-coated glucosinolate and beta-thioglucosidase particles. The present invention further provides a method of converting glucosinolate to isothiocyanate in the small intestine comprising orally administering to a subject an enteric-coated chemoprotectant precursor composition comprising enteric-coated glucosinolate and beta-thioglucosinodase particles. In another aspect, uncoated glucosinolate and beta-thioglucosinodase particles may be provided in an enteric-coated capsule. Preferably, the glucosinolate is glucoraphanin and the beta-thioglucosidase is myrosinase. The enteric coating targets the compound for release in the small intestine where beta-thioglucosinodase enzyme converts glucosinolate to chemoprotectant isothiocyanate.

Claims

1. A method of converting glucosinolate to isothiocyanate in the small intestine comprising orally administering to a subject an enteric-coated chemoprotectant precursor composition, said method comprising:

(1) enteric-coated beta-thioglucosidase particles;

(2) enteric-coated glucosinolate particles,

wherein beta-thioglucosidase and glucosinolate are released from the enteric-coated beta-thioglucosidase particles and enteric-coated glucosinolate particles, respectively, in the small intestine where beta-thioglucosidase converts glucosinolate to isothiocyanate.

2. The method of claim 1, wherein the beta-thioglucosidase is myrosinase, the glucosinolate is glucoraphanin, and the isothiocyanate is sulforaphane.

3. The method of claim 1, wherein the enteric-coated chemoprotectant precursor composition further comprises enzyme activator from the group consisting of ascorbic acid and its derivatives, or a combination thereof.

4. The method of claim 1, wherein the beta-thioglucosidase particles and glucosinolate particles are formed by spheronization.

5. The method of claim 1, wherein the enteric-coated chemoprotectant precursor composition further comprises a coating excipient selected from the group consisting of microcrystalline cellulose and its derivatives, oat fiber, lactose, carboxy methyl cellulose, or a combination thereof.

6. The method of claim 1, wherein enteric-coated chemoprotectant precursor composition further comprises a diluent selected from the group consisting of lactose, starch, dextrin, water, glycerol, sorbitol, propylene glycol, or a combination thereof.

7. The method of claim 1, wherein the enteric coating is selected from the group consisting of shellac, calcium alginate, zein, fatty acids, fats, or a combination thereof.

8. A method of converting glucosinolate to isothiocyanate in the small intestine comprising orally administering to a subject an enteric-coated capsule containing a chemoprotectant precursor composition comprising:

(1) beta-thioglucosidase particles;

(2) glucosinolate particles,

wherein beta-thioglucosidase and glucosinolate are released from the beta-thioglucosidase particles and glucosinolate particles, respectively, in the small intestine where beta-thioglucosidase converts glucosinolate to isothiocyanate.

9. The method of claim 8, wherein the beta-thioglucosidase is myrosinase, the glucosinolate is glucoraphanin, and the isothiocyanate is sulforaphane.

10. The method of claim 8, wherein the chemoprotectant precursor composition further comprises an enzyme activator from the group consisting of ascorbic acid and its derivatives, or a combination thereof.

11. The method of claim 8, wherein the beta-thioglucosidase and glucosinolate particles are formed by spheronization.

12. The method of claim 8, wherein the chemoprotectant precursor composition further comprises a coating excipient selected from the group consisting of microcrystalline cellulose and its derivatives, oat fiber, carboxy methyl cellulose, lactose, or a combination thereof.

13. The method of claim 8, wherein the chemoprotectant precursor composition further comprises a diluent selected from the group consisting of lactose, starch, dextrin, water, glycerol, sorbitol, propylene glycol, or a combination thereof.

14. The method of claim 8, wherein the enteric coating is selected from the group consisting of shellac, calcium alginate, zein, fatty acids, fats, or a combination thereof.

15. An enteric-coated chemoprotectant precursor composition comprising:

(1) about 0.5 to about 50 weight percent glucosinolate;

(2) about 0.5 to about 50 weight percent beta-thioglucosidase; and

(3) about 1 to about 99 weight percent composition comprising coating excipient and optionally diluent,

wherein the chemoprotectant precursor composition is encapsulated with enteric coating.

16. The enteric-coated chemoprotectant precursor composition of claim 15, wherein the beta-thioglucosidase particles are myrosinase particles and the glucosinolate particles are glucoraphanin particles.

17. The enteric-coated chemoprotectant precursor composition of claim 15, further comprising about 0.001 to about 10 weight percent enzyme activator selected from the group consisting of ascorbic acid and its derivatives, or a combination thereof.

18. The enteric-coated chemoprotectant precursor composition of claim 15, wherein the coating excipient is selected from the group consisting of microcrystalline cellulose and its derivatives, oat fiber, carboxy methyl cellulose, or a combination thereof.

19. The enteric-coated chemoprotectant precursor composition of claim 15, wherein the diluent is selected from the group consisting of lactose, starch, dextrin, water, glycerol, sorbitol, propylene glycol, or a combination thereof.

20. The enteric-coated chemoprotectant precursor composition of claim 15, wherein the enteric coating is selected from the group consisting of shellac, calcium alginate, zein, fatty acids, fats, or a combination thereof.

21. A food product comprising an effective amount of the enteric-coated chemoprotectant precursor composition of claim 15.

22. The food product of claim 21, wherein the glucosinolate is glucoraphanin and the beta-thioglucosinolate is myrosinase.

23. A pharmaceutical composition comprising an effective amount of the enteric-coated chemoprotectant precursor composition of claim 15.

24. The pharmaceutical composition of claim 23, wherein the glucosinolate is glucoraphanin and the beta-thioglucosinolate is myrosinase.

25. An enteric-coated capsule comprising a chemoprotectant precursor mixture, the chemoprotectant mixture comprising uncoated beta-thioglucosidase particles and uncoated glucosinolate particles in a ratio of about 1:

100 to about 100;

1, wherein the mixture is contained within an enteric-coated capsule.

26. The enteric-coated capsule of claim 25, wherein the beta-thioglucosidase is myrosinase and the glucosinolate is glucoraphanin.

27. The enteric-coated capsule of claim 25, wherein the chemoprotectant precursor mixture further comprises about 0.001 to about 10 weight percent enzyme activator selected from the group consisting of ascorbic acid and its derivatives, or a combination thereof.

28. The enteric-coated capsule of claim 25, wherein the chemoprotectant mixture comprises uncoated beta-thioglucosidase particles and uncoated glucosinolate particles in a ratio of about 1:

10 to about 10;

1.

29. The enteric-coated capsule of claim 25, wherein the enteric coating is selected from the group consisting of shellac, zein, fatty acids, fats, or a combination thereof.