Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
  • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
  • A61K31/568—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
  • A61K31/5685—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone having an oxo group in position 17, e.g. androsterone
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P25/00—Drugs for disorders of the nervous system
  • A61P25/28—Drugs for disorders of the nervous system 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

Definitions

• the invention relates to the use of pharmaceuticals and dietary supplements to improve memory.
• the term "healthy mammaF means a mammal having no diagnosed disease, disorder, infirmity, or ailment known to impair or otherwise diminish memory.
• the steroid ⁇ 5-androstene-3 ⁇ -ol-7,17 dione is a derivative of dehydroepiandrosterone (DHEA) which does not appreciably stimulate, increase or otherwise enhance the production of sex hormones.
• DHEA dehydroepiandrosterone
• the steroid is commercially available from a number of sources including Steraloids, Inc. of Newton, Rhode
• Precursors of ⁇ 5-androstene-3 ⁇ -ol-7,17 dione may also be usefully employed for improving memory. Such precursors are readily metabolized in vivo to the active ⁇ 5-androstene-3 ⁇ -ol-7,17 dione.
• One example of such a metabolizable precursor is the commercially available ⁇ 5-androstene-3 ⁇ -acetyl-7,17 dione.
• the 3 ⁇ - acetyl group is hydrolyzed in vivo by esterases located in the blood and various tissues to produce the active ⁇ 5-androstene-3 ⁇ -ol-7,17 dione, and is believed to be less susceptible to oxidation during the manufacturing process than the hydroxy group found on the active ⁇ 5-androstene-3 ⁇ -ol-7,17 dione.
• Other metabolizable precursors include ⁇ 5-androstene-3 ⁇ , 17 ⁇ -diol-7-one, ⁇ 5-androstene-3 ⁇ , 7 ⁇ -diol-17-one, ⁇ 5- androstene-3 ⁇ , 7 ⁇ -diol-17-one and the corresponding esters of these steroids.
• the steroid can be administered by virtually any of the commonly accepted practices for the administration of pharmaceutical preparations including specifically, but not exclusively, mucosal administration, oral consumption, ocular administration, subcutaneous injection, transdermal administration, etc.
• Mucosal administration of the steroid includes such routes as buccal, endotracheal, nasal, pharyngeal, rectal, sublingual, vaginal, etc.
• the steroid may be formulated as an emulsion, gum, lozenge, spray, tablet or an inclusion complex such as cyclodextrin inclusion complexes.
• Nasal administration is conveniently conducted through the use of a sniffing power or nasal spray.
• the steroid may be formulated as a cream, douch, enema or suppository.
• Oral consumption of the steroid may be effected by incorporating the steroid into a food or drink, or formulating the steroid into a chewable or swallowable tablet.
• Ocular administration may be effected by incorporating the steroid into a solution or suspension adapted for ocular application such as drops or sprays.
• Subcutaneous administration involves incorporating the steroid into a pharmaceutically acceptable and injectable carrier.
• the steroid may be conveniently incorporated into a lipophilic carrier and formulated as a topical creme or adhesive patch.
• range of dosages and dose rates effective for achieving the desired biological properties and characteristics may be determined in accordance with standard industry practices. These ranges can be expected to differ depending upon whether the desired response is the prophylactic, modulatory, ameliorative or curative in nature.
• mice Aged, two year old mice were tested in the Morris water maze procedure by training the mice to locate the pedestal in less than 15 seconds in three consecutive trials. Immediately upon completion of training one group of mice was treated with DHEA (20 mg/kg) and a second group treated with an eqimolar amount of ⁇ 5-Androstene-3 ⁇ -acetyl-7,17-dione. Two weeks after treatment the time to rescue was timed in the Morris water maze procedure at: Control 36 seconds, DHEA 27 seconds, and ⁇ 5-Androstene-3 ⁇ -acetyl-7,17-dione 13 seconds.
• mice Groups of 13 to 16 C57BL76 mice (35 gm) were tested in the Morris water maze procedure by training the mice to locate the pedestal in less than 15 seconds in three consecutive trials. Immediately upon completion of training the mice in each of three groups were treated with scopolamine (1 mg/kg), scopolamine + DHEA, or scopolamine + ⁇ 5-Androstene-3 ⁇ -acetyl-7,17-dione.

Landscapes

• Health & Medical Sciences (AREA)
• Medicinal Chemistry (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Life Sciences & Earth Sciences (AREA)
• Pharmacology & Pharmacy (AREA)
• Chemical & Material Sciences (AREA)
• Neurology (AREA)
• Neurosurgery (AREA)
• Epidemiology (AREA)
• Engineering & Computer Science (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Biomedical Technology (AREA)
• Organic Chemistry (AREA)
• Hospice & Palliative Care (AREA)
• Psychiatry (AREA)
• General Chemical & Material Sciences (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Steroid Compounds (AREA)

Priority Applications (5)

Applications Claiming Priority (2)

Publications (1)

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Citations (1)

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• 1998
  • 1998-10-16 US US09/174,235 patent/US6153606A/en not_active Expired - Lifetime
• 1999
  • 1999-10-13 DE DE69923988T patent/DE69923988T2/de not_active Expired - Fee Related
  • 1999-10-13 JP JP2000576854A patent/JP2002527481A/ja active Pending
  • 1999-10-13 AT AT99954931T patent/ATE289819T1/de not_active IP Right Cessation
  • 1999-10-13 CA CA002344677A patent/CA2344677A1/en not_active Abandoned
  • 1999-10-13 WO PCT/US1999/024076 patent/WO2000023080A1/en not_active Ceased
  • 1999-10-13 EP EP99954931A patent/EP1123100B1/en not_active Expired - Lifetime
• 2000
  • 2000-11-01 US US09/704,495 patent/US6489313B1/en not_active Expired - Lifetime

Patent Citations (1)

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