EP0550689A1 - Ibuprofen-diuretic combinations - Google Patents
Ibuprofen-diuretic combinationsInfo
- Publication number
- EP0550689A1 EP0550689A1 EP91919392A EP91919392A EP0550689A1 EP 0550689 A1 EP0550689 A1 EP 0550689A1 EP 91919392 A EP91919392 A EP 91919392A EP 91919392 A EP91919392 A EP 91919392A EP 0550689 A1 EP0550689 A1 EP 0550689A1
- Authority
- EP
- European Patent Office
- Prior art keywords
- ibuprofen
- diuretic
- effective amount
- salt
- tension
- Prior art date
- Legal status (The legal status 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 status listed.)
- Withdrawn
Links
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
Landscapes
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Cette invention se rapporte à une composition pharmaceutique utilisée pour le soulagement des douleurs, des crampes, des ballonnements et des tensions ressenties au cours de la menstruation ou de la période prémenstruelle par une femme nécessitant un tel traitement, et qui consiste à administrer à cette femme: (i) une quantité de (S)-ibuprofène ou d'un sel de celui-ci, produisant un effet analgésique et anti-inflammatoire et pratiquement dépourvue de (R)-ibuprofène; et (ii) une quantité d'un diurétique produisant un effet diurétique; et (iii) éventuellement une quantité de maléate de pyrilamine suffisante pour réduire la tension.The present invention relates to a pharmaceutical composition used for the relief of pain, cramps, bloating and tension experienced during menstruation or the premenstrual period by a woman in need of such treatment, which comprises administering to this woman : (i) an amount of (S) -ibuprofen or a salt thereof, producing an analgesic and anti-inflammatory effect and practically devoid of (R) -ibuprofen; and (ii) an amount of a diuretic producing a diuretic effect; and (iii) optionally an amount of pyrilamine maleate sufficient to reduce the tension.
Description
Claims
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US58924290A | 1990-09-28 | 1990-09-28 | |
US589242 | 1990-09-28 |
Publications (2)
Publication Number | Publication Date |
---|---|
EP0550689A1 true EP0550689A1 (en) | 1993-07-14 |
EP0550689A4 EP0550689A4 (en) | 1994-02-16 |
Family
ID=24357215
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP91919392A Withdrawn EP0550689A1 (en) | 1990-09-28 | 1991-09-25 | Ibuprofen-diuretic combinations |
Country Status (5)
Country | Link |
---|---|
EP (1) | EP0550689A1 (en) |
JP (1) | JPH06501475A (en) |
AU (1) | AU8710691A (en) |
CA (1) | CA2092565A1 (en) |
WO (1) | WO1992005786A1 (en) |
Families Citing this family (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5462950A (en) * | 1993-12-21 | 1995-10-31 | Eli Lilly And Company | Methods of treating menstrual symptoms and compositions therefore |
GB9613470D0 (en) * | 1996-06-27 | 1996-08-28 | Ciba Geigy Ag | Small solid oral dosage form |
JP2015520748A (en) * | 2012-05-08 | 2015-07-23 | セリックスビオ プライヴェート リミテッド | Compositions and methods for inhibiting carbonic anhydrase activity |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1989000421A1 (en) * | 1987-07-10 | 1989-01-26 | Abraham Sunshine | A pharmaceutical composition containing s(+) ibuprofen substantially free of its r(-) antipode |
US4877620A (en) * | 1986-11-14 | 1989-10-31 | MEDICE Chem.- Pharm. Fabrik Putter GmbH & Co. KG | Ibuprofen-containing medicament |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4888343A (en) * | 1986-09-15 | 1989-12-19 | Bristol-Myers Company | Pharmaceutical compositions for relief of dysmenorrhea and/or premenstrual syndrome and process |
-
1991
- 1991-09-25 AU AU87106/91A patent/AU8710691A/en not_active Abandoned
- 1991-09-25 EP EP91919392A patent/EP0550689A1/en not_active Withdrawn
- 1991-09-25 JP JP3516780A patent/JPH06501475A/en active Pending
- 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
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4877620A (en) * | 1986-11-14 | 1989-10-31 | MEDICE Chem.- Pharm. Fabrik Putter GmbH & Co. KG | Ibuprofen-containing medicament |
WO1989000421A1 (en) * | 1987-07-10 | 1989-01-26 | Abraham Sunshine | A pharmaceutical composition containing s(+) ibuprofen substantially free of its r(-) antipode |
Non-Patent Citations (1)
Title |
---|
See also references of WO9205786A1 * |
Also Published As
Publication number | Publication date |
---|---|
JPH06501475A (en) | 1994-02-17 |
EP0550689A4 (en) | 1994-02-16 |
AU8710691A (en) | 1992-04-28 |
CA2092565A1 (en) | 1992-03-29 |
WO1992005786A1 (en) | 1992-04-16 |
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Legal Events
Date | Code | Title | Description |
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PUAI | Public reference made under article 153(3) epc to a published international application that has entered the european phase |
Free format text: ORIGINAL CODE: 0009012 |
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17P | Request for examination filed |
Effective date: 19930324 |
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AK | Designated contracting states |
Kind code of ref document: A1 Designated state(s): DE ES FR GB IT |
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RHK1 | Main classification (correction) |
Ipc: A61K 31/19 |
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A4 | Supplementary search report drawn up and despatched |
Effective date: 19931223 |
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AK | Designated contracting states |
Kind code of ref document: A4 Designated state(s): DE ES FR GB IT |
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STAA | Information on the status of an ep patent application or granted ep patent |
Free format text: STATUS: THE APPLICATION HAS BEEN WITHDRAWN |
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18W | Application withdrawn |
Withdrawal date: 19940629 |