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
  • A61K31/33—Heterocyclic compounds
  • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
• • 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
  • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
  • A61K31/19—Carboxylic acids, e.g. valproic acid
• • 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
  • A61K31/33—Heterocyclic compounds
  • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
  • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
• • 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
  • A61K31/33—Heterocyclic compounds
  • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
  • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
  • A61K31/404—Indoles, e.g. pindolol
  • A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
• • 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
  • A61K31/33—Heterocyclic compounds
  • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
  • A61K31/425—Thiazoles
• • 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
  • A61K31/33—Heterocyclic compounds
  • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
  • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
• • 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
  • A61K31/33—Heterocyclic compounds
  • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
  • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
• • 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
  • A61K31/33—Heterocyclic compounds
  • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
  • A61P7/10—Antioedematous agents; Diuretics

Definitions

• the non-steroidal anti-inflammatory drugs are the non-steroidal anti-inflammatory drugs.
• NSAID NSAID
• NSAID have been utilized in the treatment of pain/ inflammation and have been disclosed as useful in the treatment, management and mitigation of cold symptoms and the pain associated therewith.
• Ibuprofen (2-(4-isobutylphenyl)propionic acid) is a well known and commonly employed NSAID. Recently, it has been found that a faster onset of pain relief and an enhanced analgesic response can be obtained by the utilization of the single enantiomer S(+)-ibuprofen in comparison to racemic ibuprofen, (see for example U.S. Patent 4,877,620). Diuretics, such as the thiazides, are useful in the relief of water retention. In optional combination with a tension reliever such as
• diuretics may offer relief of a variety of symptoms often appearing in the menstrual cycle such as cramps, bloating, tension, and
• This invention relates to a pharmaceutical composition for use in the relief of pain, cramps, bloating and tension experienced during menstruation or premenstruation in a female in need of such relief comprising administering to such female:
• This invention is also directed to a method of relieving pain, cramps, bloating and tension, experienced during menstruation or premenstruation in a female in need of such relief comprising
• This invention is also directed to a method of eliciting an onset hastened and enhanced response for the relief of pain, cramps, bloating and tension experienced during menstruation or premenstruation in a female in need of such relief, comprising
• Substantially free of (R)-ibuprofen should be taken to mean that the ration of (S)-ibuprofen to (R)-ibuprofen is at least 90:10.
• Salts of (S)-ibuprofen include salts with alkali metals, such as sodium or potassium, salts with alkaline earth metals, such as calcium, or salts with other metals such as magnesium, aluminum, iron, zinc, copper, nickel or coaalt.
• Salts of (S)-ibuprofen further include the amino acid salts, particularly the basic amino acids such as lysine and arginine. Specifically included within the above composition is (S)-ibuprofen- (S)-lysine.
• (S)-ibuprofen may be prepared following the procedures disclosed in U.S. Patent 4,877,620.
• Metal salts of ibuprofen may be obtained by contacting a hydroxide, or carbonate with ibuprofen.
• Amino acid salts of ibuprofen may be obtained by contacting an amino acid in solution with ibuprofen.
• (S)-ibuprofen provides a faster onset of pain-antiinflammatory relief and an enhanced degree of relief compared to racemic ibuprofen.
• These benefits are increased in an (S)-ibuprofen/diuretic combination as the inhibition of prostaglandin synthetase and the water volume minimization may synergistically cooperate.
• This has not heretofore been observed because the art has not proposed the combination of the (S)-ibuprofen enantiomer, absent (R)-ibuprofen, with a diuretic. The presence of the (R)-ibuprofen may blur the synergistic effect.
• the subject using the (S)-ibuprofen/diuretic combination will no longer need to divert metabolic energy to the inversion of the (R)-enantiomer or the removal of this enantiomer.
• the absence of inversion reduces or eliminates the formation and incorporation into fatty tissue of hybrid-ibuprofen containing triglycerides.
• combination dosage form particularly a sustained release dosage form.
• a sustained release dosage of ibuprofen may have required 800 to 1000 mg
• the employment of (S)-ibuprofen reduces the weight to 400 to 500 mg, and provides for a more practical size tablet for an ibuprofen/diuretic combination.
• An effective amount of (S)-ibuprofen, or a pharmaceutically acceptable salt thereof, for use in a unit dose composition of this invention may range from 50 to 800 mg (S)-ibuprofen.
• the preferred amount of (S)-ibuprofen is about 100 to 400 mg.
• the amount of a salt such as (S)-ibuprofen-(S)-lysine is determined based on the amount of (S)-ibuprofen contained therein.
• the diuretic employed herein may be selected from the benzothiadiazides or acetazolamide and its analogs, or ethacrynic acid, or furosemide or
• bumetanide or a potassium-sparing diuretic such as amiloride or triamterene, or a xanthine or a
• combination diuretic such as pamabrom.
• Preferred diuretics include: Acetazolamide, dichlorophenamide, methazolamide, chlorothiazide, hydrochlorothiazide, benzthiazide, indapamide, trichlormethazide,
• methylclothiazide polythiazide, ethacrynic acid, torasemide, furosemide, bumetamide, panabrom, amiloride, or triamterene.
• a particularly preferred diuretic is hydrochlorothiazide.
• the amount of diuretic useful in the practice of the present invention may-vary from about 2 mg to 50 mg depending on the specific diurectic.
• compositions may be administered in the form of tablets, capsules, elixirs, syrups or a suspension.
• active components may be admixed with a pharmaceutically acceptable carrier such as lactose, starch, sucrose, cellulose, magnesium stearate, dicalcium phosphate, calcium sulfate, mannitol and in a liquid
• composition ethyl alcohol.
• Acceptable binders such as PVP starch, gelatin, natural sugars, corn
• sweeteners natural and synthetic gums such as acacia, sodium alginate, carboxymethylcellulose, polyethylene glycol and waxes, may also be admixed with the active components. Where necessary, natural and synthetic gums such as acacia, sodium alginate, carboxymethylcellulose, polyethylene glycol and waxes, may also be admixed with the active components. Where necessary, natural and synthetic gums such as acacia, sodium alginate, carboxymethylcellulose, polyethylene glycol and waxes, may also be admixed with the active components. Where necessary
• lubricants such as boric acid, sodium benzoate, sodium acetate, sodium chloride and disintegrators such as starch, methylcellulose, agar, bentonite and guar gum and super disintegrators such as docusate sodium, sodium starch glycollate or cross-linked PVP may also be included.
• the active components may also be formulated in sustained release formulations.
• formulations may be employed in oral, dermal, rectal or vaginal administration. Such sustained release
• forms also include layered formulations which provide for distinct release ratio and thus may be more
• compositions of the present invention and as such are not to be considered as limiting the invention set

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• Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Life Sciences & Earth Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Epidemiology (AREA)
• Engineering & Computer Science (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Diabetes (AREA)
• Hematology (AREA)
• Chemical Kinetics & Catalysis (AREA)
• General Chemical & Material Sciences (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Organic Chemistry (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

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• 1991
  • 1991-09-25 CA CA002092565A patent/CA2092565A1/en not_active Abandoned
  • 1991-09-25 WO PCT/US1991/007008 patent/WO1992005786A1/en not_active Application Discontinuation
  • 1991-09-25 EP EP91919392A patent/EP0550689A1/de not_active Withdrawn
  • 1991-09-25 AU AU87106/91A patent/AU8710691A/en not_active Abandoned
  • 1991-09-25 JP JP3516780A patent/JPH06501475A/ja active Pending

Patent Citations (2)

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