METHODS FOR TREATING OR PREVENTING SYMPTOMS OF HORMONAL VARIATIONS

• US 20090143344A1
• Filed: 12/02/2008
• Published: 06/04/2009
• Est. Priority Date: 12/04/2007
• Status: Active Grant

• Current Assignee: YUNG Shin Pharm IND Company Limited (Yung Shin Pharmaceuticals Industrial)
• Original Assignee: YUNG Shin Pharm IND Company Limited (Yung Shin Pharmaceuticals Industrial)
• Inventors: Chang, Yeong-Ming
• Granted Patent: US 8,420,624 B2
• Time in Patent Office: Days
• US Class Current: 514/171
• 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 31/519 ortho- or peri-condensed with heterocyclic rings
• CPC Class Codes: A61K 31/56 Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• CPC Class Codes: A61P 5/24 of the sex hormones

Abstract

The present invention relates to methods for treating or preventing symptoms of hormonal variation. The method comprises the steps of administering an effective amount of a receptor antagonist to a subject having one or more symptoms of hormonal variations, wherein the receptor antagonist binds to at least one receptor selected from the group consisting of a serotonin type 2A (5-HT_2A) and a dopamine type 2 (D₂) receptors.

Claims

1. A method for treating or preventing one or more symptoms of hormonal variation associated with surgery or androgen deprivation therapy in a subject,, comprising the steps of:

identifying a subject having one or more symptoms of hormonal variation associated with surgery or androgen deprivation therapy, and

administering an effective amount of risperidone and/or 9-hydroxyrisperidone to the subject, wherein the symptoms are selected from the group consisting of hot flashes, dizziness, nausea, palpitations, profuse sweating, and night sweats.

2. The method of claim 1, wherein the risperidone or 9-hydroxyrisperidone is selected from the group consisting of:

its pharmaceutically acceptable polymorphs, pharmaceutically acceptable isomer, pharmaceutically acceptable hydrate and pharmaceutically acceptable addition salt.

3. The method of claim 1, further comprises administering a second active ingredient selected from the group consisting of a natural compound for complementary and alternative medicine, a hormonal composition, an antidopaminergic composition, and an antidepressant composition.

4. The method of claim 3, wherein the natural compound for complementary and alternative medicine is plant sterols, soy, vitamin E, Red clover, dong quai, or black cohosh.

5. The method of claim 3, wherein the honnonal composition comprises estrogen, premarin, progestin, megestrol acetatem or depot medroxyprogesterone.

6. The method of claim 3, wherein the antidopaminergic composition comprises veralipride, methyldopa, bromocriptine, or domperidone.

7. The method of claim 3, wherein the antidepressant composition comprises venlafaxine, paroxetine, fluoxetine, gabapentin, or GABA-analog.

8. The method of claim 1, wherein the risperidone or 9-hydroxyrisperidone is provided in a pharmaceutically acceptable form of oral dosage form, injection, inhalation, or transdermal patch.

9. A method for treating or preventing one or more symptoms of hormonal variation associated with perimenopause or postmenopause in a subject, comprising the steps of:

identifying a subject having one or more symptoms of hormonal variation associated with perimenopause of postmenopause, and

administering an effective amount of risperidone and/or 9-hydroxyrisperidone and a second active ingredient to the subject, wherein the symptoms are selected from the group consisting of hot flashes, dizziness, nausea, palpitations, profuse sweating, and night sweats, and the second active ingredient is selected from the group consisting of a natural compound for complementary and alternative medicine, a hormonal composition, an antidopaminergic composition, and an antidepressant composition.

10. The method of claim 9, wherein the effective amount of risperidone or 9-hydroxyrisperidone is administered in a form selected from the group consisting of oral dosage form, injection, inhalation, and transdermal patch.

11. The method of claim 9, wherein the risperidone or 9-hydroxyrisperidone is selected from the group consisting of:

its pharmaceutically acceptable polymorphs, pharmaceutically acceptable isomer, pharmaceutically acceptable hydrate and pharmaceutically acceptable addition salt.

12. The method of claim 9, wherein the natural compound for complementary and alternative medicine is plant sterols, soy, vitamin E, Red clover, dong quai, or black cohosh.

13. The method of claim 9, wherein the hormonal composition comprises estrogen, premarin, progestin, megestrol acetatem or depot medroxyprogesterone.

14. The method of claim 9, wherein the antidopaminergic composition comprises veralipride, methyldopa, bromocriptine, or domperidone.

15. The method of claim 9, wherein the antidepressant composition comprises venlafaxine, paroxetine, fluoxetine, gabapentin, or GABA-analog.

16. The method of claim 10, wherein the oral dosage fonn comprises a porous network of a matrix composition that disperses rapidly in water, the dosage form is prepared by forming a matrix composition dispersion containing from about 0.1% to about 15% of the matrix composition by weight of the dispersion and subjecting the matrix composition dispersion to lyophilization or solid-state dissolution, the matrix composition comprising a matrix forming agent and one or more amino acids having from about 2 to 12 carbon atoms.

17. The method of claim 10, wherein the oral dosage form comprises at least a sustained-release microparticle produced by dissolving risperidone or 9-hydroxyrisperidone and a biodegradable and biocompatible polymer in a solvent to form an organic phase, and extracting the solvent to form microparticles.

18. The method of claim 10, wherein risperidone or 9-hydroxyrisperidone is in a form of a sustained-release microparticle comprising a biodegradable and biocompatible polymeric matrix.