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Last Updated: March 29, 2024

Claims for Patent: 9,987,232


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Summary for Patent: 9,987,232
Title:Dissolution aids for oral peptide delivery comprising a biguanide
Abstract: A pharmaceutical composition comprising a mixture of: (c) an active macromolecular principle; (d) an aromatic alcohol absorption enhancer chosen from propyl gallate, butylated hydroxy toluene (BHT), butylated hydroxy anisole (BHA) and analogs and derivatives thereof, or mixtures thereof; and (d) a biguanide or a pharmaceutically acceptable salt thereof, capable of increasing the solubility of the aromatic alcohol absorption enhancer in an aqueous medium, wherein the aromatic alcohol absorption enhancer is present in an amount by weight greater than or equal to that of the active principle.
Inventor(s): New; Roger R. C. (London, GB)
Assignee: Axcess Limited (Jersey, GB)
Application Number:13/414,829
Patent Claims:1. A method of enhancing the absorption of an active macromolecular principle in a patient, which method comprises administering to the patient a composition comprising: an aromatic alcohol selected from the group consisting of propyl gallate, an analogue thereof and a derivative thereof, a dissolution aid which enhances the solubility of the aromatic alcohol in an aqueous medium wherein the dissolution aid is a biguanide or a pharmaceutically acceptable salt thereof and wherein the biguanide or pharmaceutically acceptable salt thereof is in an amount of from at least 94 mg to 178 mg per dose of the composition; and the active macromolecular principle; wherein the weight ratio of biguanide to aromatic alcohol is 2:1 to 10:1 wt/wt.

2. A method according to claim 1, wherein the active macromolecular principle to be absorbed is selected from the group consisting of a polypeptide, a protein, a polynucleotide, a polysaccharide and a mixture thereof.

3. A method according to claim 2, wherein the active macromolecular principle to be absorbed is selected from the group consisting of calcitonin, insulin, low molecular weight heparin, erythropoietin, granulocyte colony stimulating factor, interferon, C-peptide, GLP-1, human growth hormone, parathyroid hormone, an analogue thereof and a fragment thereof.

4. A method according to claim 3, wherein the active macromolecular principle to be absorbed is selected from the group consisting of insulin, calcitonin, parathyroid hormone, an analogue thereof, and a fragment thereof.

5. A method according to claim 4, wherein the active macromolecular principle to be absorbed is insulin, an analogue thereof, or a fragment thereof.

6. A method of enhancing the absorption of an active macromolecular principle in a patient, which method comprises administering to said patient a composition comprising: (a) an active macromolecular principle, (b) an aromatic alcohol absorption enhancer which is selected from the group consisting of propyl gallate, an analogue thereof and a derivative thereof, a dissolution aid which enhances the solubility of the aromatic alcohol absorption enhancer in an aqueous medium wherein the dissolution aid is a biguanide or a pharmaceutically acceptable salt thereof and wherein the biguanide or pharmaceutically acceptable salt thereof is in an amount of from at least 94 mg to 178 mg per dose of the composition; and wherein the aromatic alcohol absorption enhancer is present in an amount by weight greater than or equal to that of the active macromolecular principle, and wherein the weight ratio of biguanide to aromatic alcohol is 2:1 wt/wt to 10:1 wt/wt.

7. A method according to claim 6, wherein the composition comprises less than 5% by weight water.

8. A method according to claim 6, wherein the composition is a solution, a micro-particulate dispersion or a solid.

9. A method according to claim 6, wherein the active macromolecular principle is selected from the group consisting of insulin, C-peptide, GLP-1, and a mixture thereof; and wherein the method is for treating diabetes.

10. A method according to claim 6, wherein the active macromolecular principle is calcitonin or PTH; and wherein the patient has osteoporosis.

11. A method according to claim 6, wherein the active macromolecular principle is calcitonin; and wherein the patient has osteoarthritis.

12. A method according to claim 6, wherein the active macromolecular principle is selected from the group consisting of peptide YY, oxyntomodulin and a mixture thereof; and wherein the patient has obesity.

13. A method according to claim 6, wherein the active macromolecular principle is selected from the group consisting of erythropoietin, granulocyte-colony stimulating factor (GCSF), granulocyte-macrophage colony stimulating factor (GMCSF) and a mixture thereof; and wherein the patient has cancer.

14. The method of claim 1, wherein the biguanide is present in an amount of about 50% to about 90% by weight of the composition.

15. The method of claim 14 wherein the aromatic alcohol is present in an amount from 5% to 30% by weight of the composition.

16. The method of claim 6, wherein the biguanide is present in an amount of about 50% to about 90% by weight of the composition.

17. The method of claim 16, wherein the aromatic alcohol is present in an amount from 5% to 30% by weight of the composition.

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