WO2000067708A2 - Compositions d'hormones steroides a administration orale et methodes d'utilisation - Google Patents

Compositions d'hormones steroides a administration orale et methodes d'utilisation Download PDF

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Publication number
WO2000067708A2
WO2000067708A2 PCT/US2000/012404 US0012404W WO0067708A2 WO 2000067708 A2 WO2000067708 A2 WO 2000067708A2 US 0012404 W US0012404 W US 0012404W WO 0067708 A2 WO0067708 A2 WO 0067708A2
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WO
WIPO (PCT)
Prior art keywords
estrogen
composition
derivative
oral
agent
Prior art date
Application number
PCT/US2000/012404
Other languages
English (en)
Other versions
WO2000067708A3 (fr
Inventor
Vassem Ali
Original Assignee
Board Of Regents, The University Of Texas System
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Board Of Regents, The University Of Texas System filed Critical Board Of Regents, The University Of Texas System
Priority to AU48252/00A priority Critical patent/AU4825200A/en
Publication of WO2000067708A2 publication Critical patent/WO2000067708A2/fr
Publication of WO2000067708A3 publication Critical patent/WO2000067708A3/fr

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/63—Steroids; Derivatives thereof

Definitions

  • the subject is a human subject.
  • the human subject is a female human subject.
  • the female human subject is a peri- or postmenopausal woman of about above the age of 45 or a woman with surgical menopause, a menopausal disorder, or premature menopause.
  • steroidal hormones include, but is not limited to, estrogen, an estrogen derivative, an estrogen-containing substance, an estrogen derivative containing substance; progestin, a progestin derivative, a progestin-containing substance, a progestin derivative containing substance; or testosterone, a testosterone derivative, a testosterone containing substance or a testosterone derivative containing substance.
  • Mouthwash composition is a mouthwash composition.
  • Conventional mouthwash composition components can comprise the carrier for the active agents of the present invention.
  • Mouthwashes generally comprise from about 20:1 to about 2:1 of a water/ethyl alcohol solution and preferably other ingredients such as flavor, sweeteners, humectants and sudsing agents such as those described herein.
  • the humectants, such as glycerin and sorbitol give a moist feel to the mouth.
  • each of the preceding compositions and combinations thereof are useful in a variety of therapeutic and medicinal embodiments.
  • y and in administering oral dentrifice compositions comprising at least a first steroidal hormone or derivative thereof to a subject in need thereof.
  • each of the preceding compositions and combinations thereof are useful in the manufacture of such.
  • subjects that may be in need of such compositions include, but are not limited to, subjects having or at risk of developing including, but not limited to, decreased bone density, osteoporosis, tooth loss, an steroidal hormone deficiency, infertility, reproductive or sex organs that do not synthesize and/or secrete steroidal hormones, nutrient deficiencies or sexual dysfuntion.
  • the present invention provides oral dentrifice compositions that comprise a therapeutically effective amount of at least a first steroidal hormone or steroidal hormone derviative, either alone or in combination with other therapeutic agents such as selective estrogen receptor modulators, progestins or progestogens, various steroid hormones such as testosterone and/or other agents effective in the treatment or prevention of osteoporosis.
  • a first steroidal hormone or steroidal hormone derviative either alone or in combination with other therapeutic agents
  • therapeutic agents such as selective estrogen receptor modulators, progestins or progestogens, various steroid hormones such as testosterone and/or other agents effective in the treatment or prevention of osteoporosis.
  • oral compounds designed to address erectile dysfunction may utilize formulations and administration methods disclosed herein.
  • estrogen was believed to be primarily a reproductive hormone, with effects limited to the uterus and mammary glands. Current concepts of estrogen action, however, are quite complex. Estrogen regulates the transcription of a limited number of genes. Unbound estrogens pass through cell membranes, spread within the cell and transport into the nucleus, where they bind and activate nuclear estrogen-receptor proteins found in tissues of the female reproductive system, breast, hypothalamus, pituitary, liver and bone of women. The activated estrogen-receptor complex then binds to specific acceptor proteins that recognize specific enhancer sites along the DNA sequence, enhancing transcription and stimulating the translation of those genes and as a result specific RNA and protein synthesis takes place.
  • Estrogen loss can also result in psychological effects, such as sleep disturbances, irritability, and mood disturbances, including depression. Physical changes such as vaginal atrophy, stress (urinary) incontinence, urinary tract infections, and onset of skin collagen loss signal intermediate changes associated with the decline in estrogen and can significantly affect a woman's quality of life.
  • estradiol converts reversibly to estrone. Both estradiol and estrone are converted to estriol.
  • estrone-sulfate estradiol- 17-glucuronide
  • estriol- 16- glucuronide estradiol- 16- glucuronide
  • estradiol is the primary intracellular human estrogen and is most 'potent' or provides the most stability of the activated estrogen-receptor complex when compared to estrone and estriol.
  • Estradiol is a white, odorless, crystalline powder that is almost insoluble in water, freely soluble in alcohol, soluble in acetone, ether and chloroform and sparingly soluble in vegetable oils.
  • Estradiol is chemically described as estra-l,3,5(10)-triene-3, 17 ⁇ -diol, having an empirical formula and molecular weight of C 18 H 24 0 2 and 272.37, respectively.
  • the structural formula of estradiol is:
  • Such combinations include but are not limited to, conjugated equine estrogen combined with medroxyprogesterone acetate (avalible dose: 0.625 mg combined with 5.0 mg, respectively), esterified estrogen combined with methyltestosterone (avalible dose: 1.25 mg plus 2.5 mg, respectively) and micronized estradiol combined with micronized progesterone (avalible dose: 1 or 2 mg combined with 100 or 200 mg, respectively).
  • Such homonal combinations may also be combined with other biological and/or therapeutic agents, including, but not limited to, progestins, selective estrogen receptor modulators, or other compounds useful in the treatment or prevention of osteoporosis.
  • Toothpaste binders are more fully described in U.S. Patent Nos. 2,839,448 and 3,962,307, inco ⁇ orated herein by reference.
  • Flavoring agents can also be added to the instant compositions. Suitable flavoring agents include oil of wintergreen, oil of peppermint, oil of spearmint, oil of sassafras and oil of clove. Sweetening agents which can be used include sucrose, lactose, maltose, sorbitol, xylitol, sodium cyclamate, perillartine, AMP (aspartyl phenyl alanine, methyl ester), saccharin, dextrose, levulose, aspartame, D-tryptophan, acetosulpham, dihydrochalcones, sodium cyclamate and the like. Flavoring agents are generally used in the instant compositions at levels of from about 0.01% to 2% by weight, and sweetening agents at levels of from about 0.05% to about 3% by weight.
  • the oral dentrifice compositions also comprise whitening agents, such as titanium dioxide. 4.14 STANNOUS SALTS
  • Participants' blood is redrawn at about 1, 2, 6, 12 and 24 hours later, centrifuged and the serum saved in a test tube labeled with the date, time and subject number, respectively. These samples are then tested for serum estradiol and progesterone levels.
  • Garnero et al "Increased bone turnover in late postmenopausal women is a major determinant of osteoporosis," J. Bone Min. Res. 11 :337-349, 1996a. Garnero et al., "Markers of bone reso ⁇ tion predict hip fracture in elderly women: The EPIDOS prospective study," J. Bone Min. Res. 11 :1531-1538, 1996b. Gillet et al., Maturitas 19:103-115, 1994.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Cosmetics (AREA)

Abstract

Cette invention concerne des compositions dentifrices comprenant une dose efficace d'oestrogène ou de substance renfermant un l'oestrogène. L'invention porte également sur diverses méthodes d'utilisation de ces compositions, notamment à titre prophylactique ou préventif en cas de perte de dents ou d'ostéoporose, ainsi que sur des kits thérapeutiques contenant une ou plusieurs de ces compositions.
PCT/US2000/012404 1999-05-07 2000-05-05 Compositions d'hormones steroides a administration orale et methodes d'utilisation WO2000067708A2 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU48252/00A AU4825200A (en) 1999-05-07 2000-05-05 Oral steroidal hormone compositions and methods of use

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US13308599P 1999-05-07 1999-05-07
US60/133,085 1999-05-07

Publications (2)

Publication Number Publication Date
WO2000067708A2 true WO2000067708A2 (fr) 2000-11-16
WO2000067708A3 WO2000067708A3 (fr) 2001-02-08

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2000/012404 WO2000067708A2 (fr) 1999-05-07 2000-05-05 Compositions d'hormones steroides a administration orale et methodes d'utilisation

Country Status (2)

Country Link
AU (1) AU4825200A (fr)
WO (1) WO2000067708A2 (fr)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002040022A1 (fr) * 2000-11-17 2002-05-23 Warner-Lambert Company Llc Traitement des dysfonctionnement sexuels par l'antagoniste de la bombesine
US7030157B2 (en) 2001-07-31 2006-04-18 Pfizer Inc. Pharmaceutical compositions, kits and methods comprising combinations of estrogen agonists/antagonists, estrogens and progestins
WO2021061847A1 (fr) * 2019-09-23 2021-04-01 The Board Of Trustees Of The Leland Stanford Junior University Procédés de traitement de prolongation de la gestation et des complications des menstruations ou de la gestation

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6503894B1 (en) 2000-08-30 2003-01-07 Unimed Pharmaceuticals, Inc. Pharmaceutical composition and method for treating hypogonadism

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2058564A (en) * 1979-09-07 1981-04-15 Horton J E Pharmaceutical compositions comprising anti-osteoporotic agents
EP0345039A2 (fr) * 1988-05-31 1989-12-06 AMER & COMPANY, INC. Procédé et composition pour le traitement ou la prévention de la plaque ou du tartre dentaires ou de la gingivite
EP0455503A1 (fr) * 1990-05-04 1991-11-06 Colgate-Palmolive Company Composition pour le traitement de l'ostéoporose et du déséquilibre hormonal
US5310545A (en) * 1991-04-11 1994-05-10 Drore Eisen Method of treatment using mouthwashes containing steroids and antifungal agents and compositions of matter
WO1994016673A1 (fr) * 1993-01-19 1994-08-04 The Gillette Company Bain de bouche
EP0671175A2 (fr) * 1989-11-17 1995-09-13 The Procter & Gamble Company Compositions pharmaceutiques à libération prolongée pour le traitement des maladies périodontales
US5939047A (en) * 1996-04-16 1999-08-17 Jernberg; Gary R. Local delivery of chemotherapeutic agents for treatment of periodontal disease
DE19832169A1 (de) * 1998-07-17 2000-01-27 Jenapharm Gmbh Lokal anwendbare pharmazeutische Präparate zur Prophylaxe und Therapie atrophischer Erscheinungen in der Mundhöhle

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2058564A (en) * 1979-09-07 1981-04-15 Horton J E Pharmaceutical compositions comprising anti-osteoporotic agents
EP0345039A2 (fr) * 1988-05-31 1989-12-06 AMER & COMPANY, INC. Procédé et composition pour le traitement ou la prévention de la plaque ou du tartre dentaires ou de la gingivite
EP0671175A2 (fr) * 1989-11-17 1995-09-13 The Procter & Gamble Company Compositions pharmaceutiques à libération prolongée pour le traitement des maladies périodontales
EP0455503A1 (fr) * 1990-05-04 1991-11-06 Colgate-Palmolive Company Composition pour le traitement de l'ostéoporose et du déséquilibre hormonal
US5310545A (en) * 1991-04-11 1994-05-10 Drore Eisen Method of treatment using mouthwashes containing steroids and antifungal agents and compositions of matter
WO1994016673A1 (fr) * 1993-01-19 1994-08-04 The Gillette Company Bain de bouche
US5939047A (en) * 1996-04-16 1999-08-17 Jernberg; Gary R. Local delivery of chemotherapeutic agents for treatment of periodontal disease
DE19832169A1 (de) * 1998-07-17 2000-01-27 Jenapharm Gmbh Lokal anwendbare pharmazeutische Präparate zur Prophylaxe und Therapie atrophischer Erscheinungen in der Mundhöhle

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002040022A1 (fr) * 2000-11-17 2002-05-23 Warner-Lambert Company Llc Traitement des dysfonctionnement sexuels par l'antagoniste de la bombesine
US7030157B2 (en) 2001-07-31 2006-04-18 Pfizer Inc. Pharmaceutical compositions, kits and methods comprising combinations of estrogen agonists/antagonists, estrogens and progestins
WO2021061847A1 (fr) * 2019-09-23 2021-04-01 The Board Of Trustees Of The Leland Stanford Junior University Procédés de traitement de prolongation de la gestation et des complications des menstruations ou de la gestation

Also Published As

Publication number Publication date
AU4825200A (en) 2000-11-21
WO2000067708A3 (fr) 2001-02-08

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