Prostate hypertrophy treatment composition and method

• US 20050271597A1
• Filed: 02/11/2005
• Published: 12/08/2005
• Est. Priority Date: 02/13/2004
• Status: Abandoned Application

• Current Assignee: Alec D. Keith
• Original Assignee: Alec D. Keith
• Inventors: Keith, Alec D.
• Application Number:
  US11/057,067
• Publication Number:
  US 20050271597A1
• Time in Patent Office: Days
• US Class Current: 424/46
• CPC Class Codes: A61K 31/56 Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• CPC Class Codes: A61K 31/57 substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
• CPC Class Codes: A61K 47/14 Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• CPC Class Codes: A61K 47/32 Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers , poly(meth)acrylates, or polyvinyl pyrrolidone
• CPC Class Codes: A61K 47/44 Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14
• CPC Class Codes: A61K 9/0034 Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
• CPC Class Codes: A61K 9/06 Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels composition of ointments, creams or gels A61K47/00

Abstract

The present invention provides a method and composition for treatment of benign prostate hyperplasia (BPH) in men via a transscrotal delivery system. The composition of the present invention includes the steroid hormone progesterone containing permeation enhancers that greatly facilitate permeation through the skin, thus preventing modification of the constituents therein and providing continuous and sustained delivery of progesterone for several hours that mimics the circadian rhythm of endogenous progesterone. The progesterone composition preferably is capable of delivering an effective dosage amount of about 65-100 mg of progesterone per ml when applied directly onto the surface of scrotum.

Claims

1. A transscrotal delivery system method for treating benign prostate hyperplasia in men in need of said treatment, comprising:

admixing a progesterone hormone with;

(i) at least one pharmaceutically effective excipient to make a progesterone composition suitable for application to scrotal tissue;

(ii) at least one permeation rate enhancer; and

applying an effective dosage amount of the progesterone composition directly onto at least a portion of the outer surface of the scrotum approximately every twelve hours, wherein said application mimics the normal circadian rhythm of endogenous progesterone.

2. The method of claim 1, wherein the progesterone hormone is a micronized progesterone, said micronized progesterone admixed in an amount ranging from between about 0.1-10 vol. %.

3. The method of claim 1, wherein the progesterone hormone is a micronized progesterone, said micronized progesterone admixed in an amount ranging from between about 0.5-5 vol. %.

4. The method of claim 1, wherein the progesterone hormone is a micronized progesterone and wherein the micronized progesterone is admixed in an amount of about 1 vol. %.

5. The method of claim 1, wherein the at least one pharmaceutically acceptable excipient is selected from the group consisting of effective carrier vehicles selected from the group consisting of about 1-8 vol. % mineral oil and 1-8 vol. % squalene oil;

rheology modifiers (suspension agents and stabilizers), such as about 0.1-1 vol. % Carbopol 934;

emulsifiers selected from the group consisting of about 1-5 vol. % polyethylene glycol 100 stearate, about 1-5 vol. % glycerol stearate, about 1-5 vol. % PEG 40 stearate, about 0.5-5 vol. % lanoline alcohol and about 0.1-1 vol. % dialkylsodium sulfonate;

humectants selected from the group consisting of about 1-5 vol. % propylene glycol and up to about 5 vol. % triethylolamine;

emollients, such as about 0.5-4 vol. % lanolin;

preservatives selected from the group consisting of about 0.1-1 vol. % imidazolidinyl urea, about 0.01-2 vol. % methylparaben and about 0.01-2 vol. % ethylparaben; and

metal sequestrants, such as about 0.01-5 vol. % ethylenediaminetetraacetic acid.

6. The method of claim 1, wherein the at least one pharmaceutically acceptable excipient is selected from the group consisting of effective carrier vehicles selected from the group consisting of about 3-6 vol. % mineral oil and 3-6 vol % squalene oil;

rheology modifiers (suspension agents and stabilizers), such as about 0.2-0.8 vol. % Carbopol 934;

emulsifiers selected from the group consisting of about 2-4 vol. % polyethylene glycol 100 stearate, about 2-4 vol. % glycerol stearate, about 2-4 vol. % PEG 40 stearate, about 1-4 vol. % lanoline alcohol and about 0.2-0.8 vol. % dialkylsodium sulfonate;

humectants selected from the group consisting of about 2-4 vol. % propylene glycol and up to about 5 vol. % triethylolamine;

emollients, such as about 1-3.5 vol. % lanolin;

preservatives selected from the group consisting of about 0.2-0.9 vol. % imidazolidinyl urea, about 0.05-1.8 vol. % methylparaben and about 0.05-1.8 vol. % ethylparaben; and

metal sequestrants, such as about 0.05-4 vol. % ethylenediaminetetraacetic acid.

7. The method of claim 1, wherein the at least one pharmaceutically acceptable excipient is selected from the group consisting of effective carrier vehicles selected from the group consisting of about 5 vol. % mineral oil and 5 vol % squalene oil;

rheology modifiers (suspension agents and stabilizers), such as about 0.5 vol. % Carbopol 934;

emulsifiers selected from the group consisting of about 3 vol. % polyethylene glycol 100 stearate, about 3 vol. % glycerol stearate, about 3 vol. % PEG 40 stearate, about 3 vol. % lanoline alcohol and about 0.5 vol. % dialkylsodium sulfonate;

humectants selected from the group consisting of about 3 vol. % propylene glycol and up to about 5 vol. % triethylolamine;

emollients, such as about 3 vol. % lanolin;

preservatives selected from the group consisting of about 0.8 vol. % of imidazolidinyl urea, about 1.5 vol. % methylparaben and about 1.5 vol. % of ethylparaben; and

metal sequestrants, such as about 3 vol. % ethylenediaminetetraacetic acid.

8. The method of claim 5, wherein the progesterone composition also contains about 0.1-1 vol. % of the following agents selected from the group consisting of ascorbic acid, ascorbial palmitate, BHT, lecithin, beta-carotene, colloidal silver, neem oil, dimethylsulfoxide, coconut oil, EMU oil and any combination thereof.

9. The method of claim 6, wherein the progesterone composition also contains about 0.2-0.8 vol. % of the following agents selected from the group consisting of ascorbic acid, ascorbial palmitate, BHT, lecithin, beta-carotene, colloidal silver, neem oil, dimethylsulfoxide, coconut oil, EMU oil or any combination thereof.

10. The method of claim 7, wherein the progesterone composition also contains about 0.5 vol. % of the following agents selected from the group consisting of ascorbic acid, ascorbial palmitate, BHT, lecithin, beta-carotene, colloidal silver, neem oil, dimethylsulfoxide, coconut oil, EMU oil or any combination thereof.

11. The method of claim 1, wherein the at least one permeation enhancer is selected from the group consisting of polyethylene glycols, peptide/fatty acid complexes with about 10-20 carbon rings and mono, di, or triglycerides of fatty acids, and wherein the at least one permeation rate enhancer is present in concentrations ranging from between about 0.01-20 vol. %.

12. The method of claim 1, wherein the at least one permeation enhancer is selected from the group consisting of polyethylene glycols, peptide/fatty acid complexes with about 12-18 carbon rings, and preferably with about 12 to 18 carbon rings, and mono, di, or triglycerides of fatty acids, and wherein the at least one permeation rate enhancers is present in concentrations of 10 vol. %.

13. The method of claim 1, wherein the effective dosage amount of the progesterone composition is about 65-100 mg progesterone.

14. The method of claim 1, wherein the concentration of progesterone in the progesterone composition ranges from between about 6.5-10 mg/ml.

15. The method of claim 1, wherein the concentration of progesterone in the progesterone composition ranges from between about 65-100 mg/ml.

16. The method of claim 1, wherein about 1 to 10 ml of the progesterone composition is applied directly onto the outer surface of the scrotum about every twelve hours.

17. The method of claim 1, wherein the progesterone composition is formulated into a cream.

18. The method of claim 1, wherein the progesterone composition is formulated into a liquid spray.

19. The method of claim 18, wherein the liquid spray formulation of the progesterone composition contains a polymer binder selected from the group consisting of polyacrylate, polyester, and silicone.

21. A progesterone composition made according to the method of claim 1.

20. A transscrotal delivery system method for treating benign prostate hyperplasia, comprising:

admixing about 1 vol % of a micronized progesterone hormone with;

(i) at least one pharmaceutically effective excipient selected from the group consisting of effective carrier vehicles selected from the group consisting of about 5 vol. % mineral oil and about 5 vol % squalene oil;

rheology modifiers (suspension agents and stabilizers), such as about 0.5 vol. % Carbopol 934;

emulsifiers selected from the group consisting of about 3 vol. % polyethylene glycol 100 stearate, about 3 vol. % glycerol stearate, about 3 vol. % PEG 40 stearate, about 3 vol. % lanoline alcohol and about 0.5 vol. % dialkylsodium sulfonate;

humectants selected from the group consisting of about 3 vol. % propylene glycol and up to about 5 vol. % triethylolamine;

emollients, such as about 3 vol. % lanolin;

preservatives selected from the group consisting of about 0.8 vol. % of imidazolidinyl urea, about 1.5 vol. % methylparaben and about 1.5 vol. % of ethylparaben; and

metal sequestrants, such as about 3 vol. % ethylenediaminetetraacetic acid, and about 0.5 vol. % of the following agents selected from the group consisting of ascorbic acid, ascorbial palmitate, BHT, lecithin, beta-carotene, colloidal silver, neem oil, dimethylsulfoxide, coconut oil, EMU oil and combination thereof, in order to make a progesterone composition suitable for application to scrotal tissue;

(ii) at least one permeation rate enhancer selected from the group consisting of about 10 vol. % of polyethylene glycols, peptide/fatty acid complexes with about 12-18 carbon rings and mono, di, or triglycerides of fatty acids; and

applying about 1 ml of the progesterone composition directly onto the outer surface of the scrotum, wherein the concentration of progesterone in the progesterone composition ranges from between about 65-100 mg/ml.