Patches and method for the transdermal delivery of a therapeutically effective amount of iron

• US 8,996,104 B2
• Filed: 06/25/2009
• Issued: 03/31/2015
• Est. Priority Date: 06/25/2008
• Status: Active Grant

• Current Assignee: FE3 Medical Incorporated
• Original Assignee: FE3 Medical Incorporated
• Inventors: Berenson, Ronald J.
• Primary Examiner(s): Sirmons, Kevin C
• Assistant Examiner(s): Hall, Deanna K
• Application Number:
  US12/459,183
• Publication Number:
  US 20100130910A1
• Time in Patent Office: 2,105 Days
• Field of Search: 604/20, 604/21, 604/22, 604/501, 424/646, 424/647, 424/648, 514/184, 514/185, 514/6, 514/502, 514/492
• US Class Current: 604/20
• 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 31/295 Iron group metal compounds
• CPC Class Codes: A61K 33/26 Iron; Compounds thereof
• CPC Class Codes: A61K 38/1816 Erythropoietin [EPO]
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 9/0009 involving or responsive to electricity, magnetism or acoustic waves; Galenical aspects of sonophoresis, iontophoresis, electroporation or electroosmosis microelectromechanical systems A61K9/0097
• CPC Class Codes: A61K 9/0021 Intradermal administration, e.g. through microneedle arrays, needleless injectors mechanical aspects A61M
• CPC Class Codes: A61K 9/7023 Transdermal patches and similar drug-containing composite devices, e.g. cataplasms galenical aspects of iontophoretic devices A61K9/0009; microneedle arrays A61K9/0021; buccal patches A61K9/006
• CPC Class Codes: A61K 9/703 characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
• CPC Class Codes: A61N 1/0444 Membrane
• CPC Class Codes: A61N 1/0448 Drug reservoir
• CPC Class Codes: A61N 1/303 Constructional details electrodes for external use A61N1/0428
• CPC Class Codes: A61P 15/08 for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
• CPC Class Codes: A61P 25/28 for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• CPC Class Codes: A61P 25/32 Alcohol-abuse
• CPC Class Codes: A61P 3/00 Drugs for disorders of the metabolism of the blood or the extracellular fluid A61P7/00
• CPC Class Codes: A61P 3/02 Nutrients, e.g. vitamins, minerals
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 7/06 Antianaemics

Abstract

Embodiments of the invention provide patches for the transdermal delivery of iron-containing compositions to an individual suffering from an iron deficiency. Many embodiments provide an iontophoretic patch for the transdermal delivery of a therapeutically effective amount of iron. The patch comprises an electrode and a reservoir containing a composition comprising ionic iron for the delivery of the therapeutically effective amount of iron. Various embodiments provide methods of using embodiments of the iontophoretic patch for delivering a therapeutically effective amount of iron to an individual suffering from one more forms of iron deficiency including iron deficiency anemia. Such methods can be used for treating and/or preventing the iron deficiency. The amount of delivered iron can be adjusted depending upon various treatment parameters such as patient weight and type and amount of iron deficiency.

Claims

1. A method for the transdermal iontophoretic delivery of a composition comprising ionic iron to an individual in need thereof, comprising:

contacting the individual with a patch comprising an active electrode and a reservoir including a composition comprising ionic iron, the reservoir and composition being separate from the electrode; and

applying current from the active electrode to the reservoir to cause transdermal iontophoretic delivery of a therapeutically effective amount of ionic iron from the reservoir to the individual, wherein the composition does not include heme iron or heme iron polypeptide.

2. The method of claim 1, wherein the ionic iron is in the form of one or more ferrous salts.

3. The method of claim 2, wherein the one or more ferrous salts are selected from the group consisting of:

ferrous gluconate, ferrous chloride, ferrous sulfate, and ferrous fumarate.

4. The method of claim 1, wherein the composition comprises at least one agent selected from the group consisting of:

a vitamin supplement, erythropoietin, and an erythropoietin stimulating agent.

5. The method of claim 4, wherein the vitamin supplement is selected from the group consisting of thiamine, riboflavin, niacin, pantothenic acid, pyroxidine, biotin, folic acid, and cobalamin.

6. The method of claim 1, wherein the therapeutically effective amount of delivered ionic iron is in a range from about 1 mg to about 50 mg of elemental iron.

7. The method of claim 1, wherein the therapeutically effective amount of delivered ionic iron is in a range from about 1 mg to about 40 mg of elemental iron.

8. The method of claim 1, wherein the therapeutically effective amount of delivered ionic iron is in a range from about 1 mg to about 30 mg of elemental iron.

9. The method of claim 1, further comprising adjusting the therapeutically effective amount of ionic delivered iron to the individual based on a treatment parameter.

10. The method of claim 9, wherein the treatment parameter is a patient characteristic, patient weight, type of iron deficiency being treated or selected therapeutic outcome.

11. The method of claim 1, wherein the ionic iron composition is delivered substantially continuously.

12. The method of claim 1, wherein the ionic iron composition is delivered over a period of about one day to about one month.

13. The method of claim 1, wherein the ionic iron composition is delivered over a period of about one day to about one week.

14. The method of claim 13, wherein the ionic iron composition is delivered over a period of about one day to about three days.

15. The method of claim 14, wherein the ionic iron composition is delivered over a period of about one day.

16. The method of claim 15, wherein the therapeutically effective amount of delivered ionic iron is in a range from about 1 mg to about 50 mg of elemental iron.

17. The method of claim 1, further comprising:

delivering sufficient iron to prevent and/or treat an iron deficiency in an individual.

18. The method of claim 17, further comprising administering a parental therapeutically effective amount of iron.

19. The method of claim 18, wherein the parental administration is done prior to transdermal delivery.

20. The method of claim 18, wherein the parental administration is intravenous or subcutaneous.

21. The method of claim 18, wherein at least one of the parental administration and the transdermal delivery are adjusted relative to the other.

22. The method of claim 21, wherein the adjustment is in at least one of a rate or amount of iron delivery.

23. The method of claim 17, further comprising administering an oral therapeutically effective amount of iron.

24. The method of claim 23, wherein the oral administration is done prior to the transdermal delivery.

25. The method of claim 17, further comprising administering an intravenous bolus of iron to the individual prior transdermal delivery wherein the bolus contains about 500 mg to 1 gram of iron.

26. The method of claim 17, wherein the individual has an iron deficiency without anemia.

27. The method of claim 26, wherein the iron deficiency is being treated in order to prevent growth retardation, cognitive disabilities, and/or mental retardation.

28. The method of claim 26, wherein the iron deficiency, is caused by chronic alcoholism;

poor nutrition;

decreased consumption of animal protein and absorbic acid;

increased iron demands of pregnancy, infancy, or adolescence;

malabsorption syndromes; and

foods or drugs that reduce the gastrointestinal absorption of iron.

29. The method of claim 17, wherein the individual has an iron deficiency anemia.

30. The method of claim 29, wherein the individual has an iron deficiency characterized by microcytosis of red blood cells, a hemoglobin iron binding capacity of less than 20%, ferritin levels less than about 10 μ

g/L, or transferrin iron saturation levels less than 20%.

31. The method of claim 17, wherein the individual has a functional iron deficiency with ferritin levels less than 100 μ

g/L.

32. The method of claim 17, wherein the individual is selected from the group consisting of a child, infant, and neonate.

33. The method of claim 17, wherein the therapeutically effective amount of delivered ionic iron is in a range from about 0.5 mg to about 40 mg of elemental iron.

34. The method of claim 17, wherein the therapeutically effective amount of delivered ionic iron is in a range from about 0.5 mg to about 20 mg of elemental iron.

35. The method of claim 17, wherein the therapeutically effective amount of delivered ionic iron is adjusted based on an anthropomorphic parameter or an indicator of iron deficiency.

36. The method of claim 17, wherein the ionic iron composition is delivered over a period of about one day to about one week.

37. The method of claim 1, further comprising:

creating a plurality of micro channels in the stratum corneum to enhance transdermal delivery of the ionic iron.

38. The method of claim 37, wherein the plurality of micro-channels are created mechanically.

39. The method of claim 38, wherein the plurality of micro-channels are created using a plurality of needles.

40. The method of claim 38, wherein the plurality of micro-channels are created using an electrical discharge on or into the skin.

41. The method of claim 40, wherein the discharge is created using a plurality of conductive microfilaments.

42. A method for the transdermal iontophoretic delivery of a composition comprising ionic iron to an individual in need thereof, the method comprising:

contacting the individual with a patch comprising an active electrode and a reservoir including a pharmaceutical composition comprising ionic iron, wherein the composition is uniformly distributed within the reservoir, the reservoir and composition being separate from the electrode; and

applying current from the active electrode to the reservoir to cause transdermal iontophoretic delivery of a therapeutically effective amount of ionic iron from the reservoir to the individual wherein the composition does not include heme iron or heme iron polypeptide.