Preparation and use of a composition for prevention and mitigation of the effects of radiation

Patent metadata

Field	Value
Publication number	US-9993456-B2
Application number	US-201415021376-A
Country	US
Kind code	B2
Filing date	Sep 15, 2014
Priority date	Sep 13, 2013
Publication date	Jun 12, 2018
Grant date	Jun 12, 2018

Abstract

Plant extracts, compositions, pharmaceutical compositions and methods of making and using the same are provided herein. The compositions comprise γ-tocotrienol (GT3) and δ-tocotrienol (DT3) in ratios wherein the DT3 is predominate. The compositions are useful for radioprotection and radiomitigation in subjects in need thereof.

First claim

We claim:

1. A method of preparing an annatto seed extract having a δ-tocotrienol to γ-tocotrienol ratio of between 7:1 to 9:1, comprising:
a. Extracting the oil from the annatto seeds to produce annatto seed oil, and
b. Enriching the tocotrienols from the annatto seed oil via chromatography, wherein the tocotrienols are separated by chromatography using a solvent comprising hexane,
wherein the total tocotrienols are between 15% and 95% of the composition and the tocopherols are less than 1% of the extract after the chromatography.

2. The method of claim 1 , wherein the oil is hexane extracted from the annatto seeds.

3. The method of claim 1 , wherein the tocotrienols are separated by chromatography using a hexane: ethyl acetate solvent or a hexane: isopropanol solvent.

4. The method of claim 3 , wherein the hexane: ethyl acetate solvent has a ratio of 90:10.

5. The method of claim 3 , wherein the hexane: isopropanol solvent has a ratio of 98:2.

6. A method of treating a subject comprising administering an effective amount of a composition comprising an annatto seed extract having a δ-tocotrienol to γ-tocotrienol ratio of between 7:1 to 9:1 to the subject, wherein the subject is in need of a radioprotectant or for treatment of radiation exposure wherein the total tocotrienols are between 15% and 95% of the composition and the tocopherols are less than 1% of the extract after the chromatography.

7. The method of claim 6 , wherein the subject has a condition of radiation exposure.

8. The method of claim 6 , wherein the composition is made by a method comprising:
a. extracting the oil from the annatto seeds to produce annatto seed oil, and
b. Enriching the tocotrienols from the annatto seed oil via chromatography, wherein the tocotrienols are separated by chromatography using a solvent comprising hexane.

9. The method of claim 6 , wherein the tocotrienols are more than 50% of the composition.

10. The method of claim 6 , wherein the composition is substantially free of tocopherols.

11. The method of claim 6 , wherein the composition comprises at least 100 mg/mL total tocotrienol.

12. The method of claim 6 , wherein the composition comprises at least 500 mg/mL total tocotrienol.

13. The method of claim 6 , wherein the composition is a pharmaceutical composition further comprising a pharmaceutically acceptable carrier.

14. The method of claim 12 , wherein the pharmaceutical composition comprises at least 1 g total tocotrienols in a dosage form.

15. The method of claim 1 , wherein the tocotrienols are more than 50% of the composition.

16. The method of claim 1 , wherein the composition is substantially free of tocopherols.

17. The method of claim 1 , wherein the composition comprises at least 100 mg/mL total tocotrienol.

18. The method of claim 1 , wherein the composition comprises at least 500 mg/mL total tocotrienol.

Assignees

• Bioventures Llc
• Univ Tecnica Particular De Loja
• Us Veterans Affairs
• Univ Arkansas

Inventors

• Compadre Cesar M
• Breen Philip
• Aykin-Burns Nukhet
• Hauer-Jensen Martin
• Enriquez Raul G
• Kharade Sujay
• Malagon Omar
• Ordonez Yadira
• Ojeda Edgar
• Thakkar Shraddha
• Pineda E Nathalie
• Jones Darin

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61P7/00

  Drugs for disorders of the blood or the extracellular fluid · CPC title

• A61P7/02

  Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors · CPC title

• A61P39/06

  Free radical scavengers or antioxidants · CPC title