Oral pharmaceutical products containing 17β-estradiol-3-lower alkanoate, method of administering the same and process of preparation

• US 7,572,779 B2
• Filed: 04/29/2004
• Issued: 08/11/2009
• Est. Priority Date: 12/21/2001
• Status: Active Grant

• Current Assignee: Allergan Therapeutics LLC (Abbvie Incorporated)
• Original Assignee: Warner Chilcott Company LLC (Abbvie Incorporated)
• Inventors: deVries, Tina M, Aloba, Oluwole T.
• Primary Examiner(s): Padmanabhan; Sreeni
• Assistant Examiner(s): Javanmard; Sahar
• Application Number:
  US10/833,997
• Publication Number:
  US 20040209856A1
• Time in Patent Office: 1,930 Days
• Field of Search: 514/170, 514/171, 514/178, 514/182
• US Class Current: 514/170
• 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: A61K 9/2018 Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
• CPC Class Codes: A61K 9/2027 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/4858 Organic compounds
• CPC Class Codes: A61K 9/4866 Organic macromolecular compounds
• CPC Class Codes: A61P 13/02 of urine or of the urinary tract, e.g. urine acidifiers
• CPC Class Codes: A61P 13/08 of the prostate
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/12 for climacteric disorders
• CPC Class Codes: A61P 15/18 Feminine contraceptives
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 19/10 for osteoporosis
• CPC Class Codes: A61P 25/02 for peripheral neuropathies
• CPC Class Codes: A61P 25/06 Antimigraine agents
• CPC Class Codes: A61P 25/20 Hypnotics; Sedatives
• 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 35/00 Antineoplastic agents
• CPC Class Codes: A61P 5/24 : of the sex hormones
• CPC Class Codes: A61P 5/30 : Oestrogens
• CPC Class Codes: A61P 5/34 : Gestagens
• CPC Class Codes: A61P 9/00 : Drugs for disorders of the cardiovascular system

Abstract

A pharmaceutical dosage unit for oral administration to a human female comprising a therapeutically effective amount of 17β-estradiol-3-lower alkanoate, most preferably 17β-estradiol-3-acetate, and a pharmaceutically acceptable carrier is disclosed. Also disclosed is a method for treating a human female in need of 17β-estradiol and a contraceptive method by oral administration of the pharmaceutical dosage unit and a method of preparing a pharmaceutical composition that may be used to form the pharmaceutical dosage unit of the invention.

Claims

1. A method of treating a human female having a deficiency of 17β

-estradiol comprising the step of orally administering to said human female a solid dosage unit comprising a therapeutically effective amount of 17β

-estradiol-3-acetate and a pharmaceutically acceptable carrier, wherein the percent moisture of said dosage unit is less than or equal to 5%, and the amount of 17β

-estradiol-3-acetate is from about 0.1 to about 10 mg as estradiol equivalent, wherein the oral solid dosage unit further comprises a pharmaceutically acceptable inhibitor of ester hydrolysis that is acetic acid.

2. The method according to claim 1, wherein said dosage unit further comprises one or more additional medicaments.

3. The method according to claim 2, wherein at least one additional medicament has progestational activity.

4. The method according to claim 1, wherein the dosage unit is a tablet, capsule, powder, lozenge, troche or suspension.

5. The method according to claim 4, wherein the dosage unit is a tablet or capsule.