Transdermal application of naturally occurring steroid hormones

• US 6,228,852 B1
• Filed: 07/08/1997
• Issued: 05/08/2001
• Est. Priority Date: 07/12/1996
• Status: Expired due to Fees

• Current Assignee: Carolyn V. Shaak
• Original Assignee: Carolyn V. Shaak
• Inventors: Shaak, Carolyn V.
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): WARE, TODD
• Application Number:
  US08/889,529
• Time in Patent Office: 1,400 Days
• Field of Search: 424/449, 424/400, 514/170, 514/178, 514/874, 514/937
• US Class Current: 514/178
• 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 31/565 not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
• 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: A61P 15/12 for climacteric disorders

Abstract

The invention features a physiologically acceptable cream that contains estrogen, progesterone, and testosterone molecules that are identical to the estrogen, progesterone, and testosterone molecules naturally produced by the human body. The cream may be self-administered to the skin and is useful as a means of hormone replacement therapy, which may begin at around the time of menopause.

Claims

1. A method of hormone replacement therapy, said method comprising administering to the skin of a patient in need of said therapy a physiologically acceptable formulation comprising native estrogen, native progesterone, and native testosterone in a ratio, by weight, of 1-5:

10-500;

1-5, in concentrations sufficient to raise circulating hormone levels to values found in the early luteal phase in premenopausal ovulatory women.

2. The method of claim 1, wherein said estrogen is estradiol, estrone, or estriol.

3. The method of claim 1, wherein said formulation further comprises dehydroepiandrosterone.

4. The method of claim 1, wherein said administration is begun at around the time of menopause.

8. The method of claim 1, whereby said circulating hormone levels are raised to at least 60 pg/ml estrogen, 1 ng/ml progesterone, and 30 pg/ml testosterone.

9. The method of claim 1, wherein said formulation comprises native estrogen, native progesterone, and native testosterone in a ratio, by weight, of 1-3:

300-500;

1-3.

13. The method of claim 1, wherein said formulation is a cream.

14. The method of claim 1, wherein said formulation is administered to an area in which thin skin overlies fatty tissue.

15. The method of claim 14, wherein said formulation is administered to the lower abdomen, inner thigh, hip, or upper inner arm.

16. The method of claim 1, wherein said formulation comprises native estrogen, native progesterone, and native testosterone in concentrations of 0.5-1.5 mg/ml, 150-250 mg/ml, and 0.5-1.5 mg/ml, respectively, and {fraction (1/16)} to {fraction (1/2)} teaspoon of said formulation is administered to the skin.

17. The method of claim 1, wherein said formulation is administered 1-3 times per day.

18. The method of claim 8, whereby said progesterone level is raised to at least 2.5 ng/ml.

5. A physiologically acceptable formulation comprising native estrogen, native progesterone, and native testosterone in a ratio, by weight, of 1-5:

10-500;

1-5, whereby administering said formulation to the skin of a patient in need thereof is sufficient to raise circulating estrogen, progesterone, and testosterone levels to values found in the early luteal phase in premenopausal ovulatory women.

6. The cream of claim 5, wherein said estrogen, progesterone and testosterone are synthesized from compounds obtained from a plant source.

7. The formulation of claim 5, wherein said formulation further comprises dehydroepiandrosterone.

10. The formulation of claim 5, said formulation comprising native estrogen, native progesterone, and native testosterone in a ratio, by weight, of 1-3:

300-500;

1-3.

11. A physiologically acceptable formulation comprising native estrogen, native progesterone, and native testosterone in concentrations of 0.5-1.5 mg/ml, 150-250 mg/ml, and 0.5-1.5 mg/ml, respectively, whereby administering said formulation to the skin of a patient in need thereof is sufficient to raise circulating estrogen, progesterone, and testosterone levels to values found in the early luteal phase in premenopausal ovulatory women.

12. The formulation of claims 5 or 11, wherein said formulation is a cream.

19. The formulation of claim 11, wherein said administration is sufficient to raise circulating estrogen to 40 pg/ml, circulating progesterone to at least 1 ng/ml, and circulating testosterone to greater than 30 ng/dl.

20. The formulation of claim 19, wherein said administration is sufficient to raise circulating progesterone to 2.5 ng/ml.