METHODS AND COMPOSITIONS FOR TREATING CONDITIONS RELATED TO LACK OF BLOOD SUPPLY, SHOCK AND NEURONAL INJURIES

• US 20120087956A1
• Filed: 10/14/2011
• Published: 04/12/2012
• Est. Priority Date: 12/22/2007
• Status: Active Grant

• Current Assignee: Vivacelle BIO, Inc.
• Original Assignee: Cuthbert O. Simpkins
• Inventors: SIMPKINS, Cuthbert O.
• Granted Patent: US 8,618,056 B2
• Time in Patent Office: Days
• US Class Current: 424/400
• CPC Class Codes: A23L 29/10 containing emulsifiers
• CPC Class Codes: A23L 33/115 Fatty acids or derivatives thereof; Fats or oils
• CPC Class Codes: A23L 33/175 Amino acids
• 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 31/4172 Imidazole-alkanecarboxylic acids, e.g. histidine
• CPC Class Codes: A61K 31/66 Phosphorus compounds
• CPC Class Codes: A61K 38/33 derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 9/0019 Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner non-active ingredients are additionally classified in A61K47/00
• CPC Class Codes: A61K 9/0026 Blood substitute; Oxygen transporting formulations; Plasma extender
• CPC Class Codes: A61K 9/107 Emulsions ; Emulsion preconcentrates; Micelles composition of emulsions A61K47/00
• CPC Class Codes: A61P 7/00 Drugs for disorders of the blood or the extracellular fluid
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• CPC Class Codes: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

A pharmaceutical composition comprising a lipid component; an amphiphilic emulsifier; and a polar liquid carrier. The lipid component and the amphiphilic emulsifier form free-moving lipid-carrying micelles (LMs) in the polar liquid carrier. The pharmaceutical composition is free of hemoglobin and fluorocarbon and can be used for treating conditions related to lack of blood supply and to raise the blood pressure.

Claims

1. A pharmaceutical composition comprising:

a lipid component;

an amphiphilic emulsifier; and

a polar liquid carrier,

wherein the lipid component and the amphiphilic emulsifier form free-moving lipid-carrying micelles (LMs) in the polar liquid carrier, and wherein the pharmaceutical composition is free of hemoglobin and fluorocarbon.

2. The pharmaceutical composition of claim 1, wherein said LMs have an average diameter of 100 to 500 nm.

3. The pharmaceutical composition of claim 1, further comprising an amino acid at a final concentration of 0.5-10 mM.

4. The pharmaceutical composition of claim 1, further comprising an amino acid at a final concentration of about 1 mM.

5. The pharmaceutical composition of claim 1, further comprising glycerol or mannitol in an amount of 2-5% (w/v).

6. The pharmaceutical composition of claim 1, further comprising glycerol or mannitol in an amount of about 2.25% (w/v).

7. The pharmaceutical composition of claim 1, further comprising albumin in an amount of 3-7% (w/v).

8. The pharmaceutical composition of claim 1, further comprising albumin in an amount of about 5% (w/v).

9. The pharmaceutical composition of claim 1, wherein said amphiphilic emulsifier is egg yolk phospholipids or α

-phosphatidylcholine in an amount of 1%-5% (w/v).

10. The pharmaceutical composition of claim 1, wherein said amphiphilic emulsifier is egg yolk phospholipids or α

-phosphatidylcholine in an amount of about 2.4% (w/v).

11. The pharmaceutical composition of claim 1, wherein said lipid component is selected from the group consisting of soybean oil, chia bean oil and algae oil in an amount of 10%-40% (w/v) of said pharmaceutical composition.

12. The pharmaceutical composition of claim 1, wherein said lipid component is selected from the group consisting of soybean oil, chia bean oil and algae oil in an amount of about 20% (w/v) of said pharmaceutical composition.

13. The pharmaceutical composition of claim 1, wherein said composition is free of Ca⁺⁺, Mg⁺⁺ and K⁺.

14. The pharmaceutical composition of claim 1, wherein said composition is free of Al⁺⁺⁺.

15. A pharmaceutical composition comprising:

10%-80% (w/v) of a lipid component selected from the group consisting of soybean oil, chia bean oil and algae oil;

1%-5% (w/v) of an amphiphilic emulsifier selected from the group consisting of egg yolk phospholipids and α

-phosphatidylcholine;

2%-5% (w/v) glycerol or mannitol;

5% (w/v) albumin;

0.1 fM-10 mM histidine or cysteine; and

a polar liquid carrier,

wherein the lipid component and the amphiphilic emulsifier form free-moving lipid-carrying micelles (LMs) in the polar liquid carrier, wherein said LMs have an average diameter of 100 to 500 nm and wherein the pharmaceutical composition is free of hemoglobin and fluorocarbon.

16. The pharmaceutical composition of claim 15, wherein said composition is free of Ca⁺⁺, Mg⁺⁺ and K.

17. The pharmaceutical composition of claim 15, further comprising β

-endorphin at a final concentration of 0.1-10 nM.

18. A method for raising blood pressure in a shock patent, comprising:

infusing into said patient, an effective amount of a pharmaceutical composition comprising;

a lipid component;

an amphiphilic emulsifier; and

a polar liquid carrier,

wherein the lipid component and the amphiphilic emulsifier form free-moving lipid-carrying micelles (LM) in the polar liquid carrier, wherein the pharmaceutical composition is free of hemoglobin and fluorocarbon, and wherein said pharmaceutical composition is infused in an amount that equals to, or is greater than, 10% of the normal blood volume of the shock patient at a rate greater than 200 ml/min.

19. The method of claim 18, wherein said pharmaceutical composition is infused in an amount that equals to, or is greater than, 20% of the normal blood volume of the shock patient at a rate greater than 500 ml/min.

20. The method of claim 18, wherein said pharmaceutical composition is infused in an amount that equals to, or is greater than, 30% of the normal blood volume of the shock patient at a rate of about 1000-4000 ml/min.

21. A method for treating a shock patent, comprising:

(a) infusing into said patient, an effective amount of a first pharmaceutical composition comprising;

a first lipid component comprising soy bean oil;

a first amphiphilic emulsifier; and

a first polar liquid carrier,

wherein the first lipid component and the first amphiphilic emulsifier form free-moving lipid-carrying micelles (LM) in the first polar liquid carrier, wherein the first pharmaceutical composition is free of hemoglobin and fluorocarbon; and

(b) infusing into said patient, an effective amount of a second pharmaceutical composition comprising;

a second lipid component comprising chia bean oil;

a second amphiphilic emulsifier; and

a second polar liquid carrier,

wherein the second lipid component and the second amphiphilic emulsifier form free-moving LMs in the second polar liquid carrier, wherein the second pharmaceutical composition is free of hemoglobin and fluorocarbon.