Compositions for the management of hyperglycemia and related conditions

Patent metadata

Field	Value
Publication number	US-2019192448-A1
Application number	US-201816232242-A
Country	US
Kind code	A1
Filing date	Dec 26, 2018
Priority date	Dec 27, 2017
Publication date	Jun 27, 2019
Grant date	—

Abstract

Disclosed is a method for therapeutic management of hyperglycemia in mammals using compositions containing thymohydroquinone. More specifically, the invention discloses compositions containing thymohydroquinone for inhibiting the activity of the enzyme α-glucosidase and increasing the cellular uptake of glucose by mammalian cells. The anti-oxidant, anti-inflammatory and anti-glycation effects of thymohydroquinone are also disclosed herein.

First claim

We claim:

1 . A method of inhibiting glucosidase enzyme, said method comprising steps of:
i) Bringing into contact glucosidase enzyme with a paranitrophenyl-α-d-glucopyranoside substrate; ii) Incubating with an effective doses of thymohydroquinone or a composition comprising thymohydroquinone under optimal conditions; iii) Reading the change in absorbance using spectrophotometric and fluorimetric methods; iv) Comparing the absorbance with a control blank and determining the percentage enzyme inhibition (IC 50 ) by thymohydroquinone or a composition comprising thymohydroquinone using the formula:
% Inhibition=[(absorbance of control−absorbance of inhibitor)/absorbance of control]×100.

2 . The method as in claim 1 , wherein the composition comprising thymohydroquinone comprises of about 0.1%-5% w/w thymoquinone, about 0.01%-10% w/w thymohydroquinone, about 20%-95% w/w fatty acids, about 0.001%-3% w/w α-hederin or hederagenin, 0.1%-4.0% w/w stabilizing agent and 0.2%-2% w/w bioavailability enhancer.

3 . The composition as in claim 2 , wherein the stabilizing agent is selected from the group comprising rosmarinic acid, butylated hydroxyanisole, butylated hydroxytoluene, sodium metabisulfite, propyl gallate, cysteine, ascorbic acid and tocopherols.

4 . The composition as in claim 2 , wherein the bioavailability enhancer is selected from the group comprising piperine, quercetin, garlic extract, ginger extract, and naringin.

5 . A method of increasing glucose uptake by mammalian cells, said method comprising steps of bringing into contact mammalian cells with effective dose of thymohydroquinone or a composition comprising thymohydroquinone, to increase glucose uptake by the cells.

6 . The method as in claim 5 , wherein the composition comprises of about 0.1%-5% w/w thymoquinone, about 0.01%-10% w/w thymohydroquinone, about 20%-95% w/w fatty acids, about 0.001%-3% w/w α-hederin or hederagenin, 0.1%-4.0% w/w stabilizing agent and 0.2%-2% w/w bioavailability enhancer.

7 . The composition as in claim 6 , wherein the stabilizing agent is selected from the group comprising rosmarinic acid, butylated hydroxyanisole, butylated hydroxytoluene, sodium metabisulfite, propyl gallate, cysteine, ascorbic acid and tocopherols.

8 . The composition as in claim 6 , wherein the bioavailability enhancer is selected from the group comprising piperine, quercetin, garlic extract, ginger extract, and naringin.

9 . The composition as in claim 6 , wherein the mammalian cells are human cells.

10 . A method for the therapeutic management of hyperglycemia and related conditions in mammals, said method comprising steps of administering effective dose of thymohydroquinone or a composition comprising thymohydroquinone, to bring about a reduction in the levels of glucose in the blood.

11 . The method as in claim 10 , wherein the management of hyperglycemia and related conditions is brought about by decreasing absorption of glucose by inhibiting glucosidase enzyme, increasing cellular uptake of glucose, reducing free radicals, reducing inflammation and decreasing glycation.

12 . The method as in claim 10 , wherein the hyperglycemia related conditions are present in disease states selected from the group comprising diabetes, obesity, hyperlipoproteiniemia, hyperlipidemia, cardiovascular complications, cancer, atherosclerosis, neurodegenerative diseases, allergy, inflammation, and osteoporosis.

13 . The method as in claim 10 , wherein the composition comprises of about 0.1%-5% w/w thymoquinone, about 0.01%-10% w/w thymohydroquinone, about 20%-95% w/w fatty acids, about 0.001%-3% w/w α-hederin or hederagenin, 0.1%-4.0% w/w stabilizing agent and 0.2%-2% bioavailability enhancer.

14 . The composition as in claim 13 , wherein the stabilizing agent is selected from the group comprising rosmarinic acid, butylated hydroxyanisole, butylated hydroxytoluene, sodium metabisulfite, propyl gallate, cysteine, ascorbic acid and tocopherols.

15 . The composition as in claim 13 , wherein the bioavailability enhancer is selected from the group comprising piperine, quercetin, garlic extract, ginger extract, and naringin.

16 . The method as in claim 10 , wherein the mammalian cells are human cells.

17 . The composition as in claim 13 , wherein the composition is formulated with pharmaceutically/nutraceutically acceptable excipients, adjuvants, diluents or carriers and administered orally in the form of tablets, capsules, soft gels, syrups, gummies, powders, suspensions, emulsions, chewables, candies or eatables.

Assignees

• Majeed Muhammed
• Nagabhushanam Kalyanam
• Mundkur Lakshmi

Inventors

• Majeed Muhammed
• Nagabhushanam Kalyanam
• Mundkur Lakshmi

Classifications

• A61K31/065 Primary

  Diphenyl-substituted acyclic alcohols · CPC title

• A61P29/00

  Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title

• A61K31/122 Primary

  having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin · CPC title

• A61P39/06

  Free radical scavengers or antioxidants · CPC title

• A61K31/19

  Carboxylic acids, e.g. valproic acid (salicylic acid A61K31/60) · CPC title