WO1992004892A1 - Utilisation de la nabumetone contre l'appauvrissement en calcium - Google Patents

Utilisation de la nabumetone contre l'appauvrissement en calcium Download PDF

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Publication number
WO1992004892A1
WO1992004892A1 PCT/EP1991/001750 EP9101750W WO9204892A1 WO 1992004892 A1 WO1992004892 A1 WO 1992004892A1 EP 9101750 W EP9101750 W EP 9101750W WO 9204892 A1 WO9204892 A1 WO 9204892A1
Authority
WO
WIPO (PCT)
Prior art keywords
nabumetone
treatment
prophylaxis
pharmaceutical composition
calcium depletion
Prior art date
Application number
PCT/EP1991/001750
Other languages
English (en)
Inventor
Enzo Grossi
Original Assignee
Dr. Lo. Zambeletti S.P.A.
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 Dr. Lo. Zambeletti S.P.A. filed Critical Dr. Lo. Zambeletti S.P.A.
Publication of WO1992004892A1 publication Critical patent/WO1992004892A1/fr

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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
    • A61K31/12—Ketones

Definitions

  • the present invention relates to a method for the treatment of disorders associated with calcium depletion in the bone and to a compound for use in such a method.
  • Patent 1,474,377 discloses the compound 4-(6'- methoxy-2'-na ⁇ hthyl)-butan-2-one and in example 5, a process by which it can be prepared.
  • the compound which is referred to herein by its common name, nabumetone, is described as possessing anti-inflammatory activity and is therefore useful in the treatment of arthritis.
  • nabumetone also has potential therapeutic utility as a calcium reabsorption agent.
  • the present invention provides a method for the prophylaxis and/or treatment of disorders associated with calcium depletion in the bone in human or non-human animals, which method comprises administering an effective, non-toxic amount of nabumetone to human or non-human animals suffering from such a disorder.
  • the present invention also provides the use of nabumetone in the manufacture of a medicament for use in the prophylaxis and/or treatment of disorders associated with calcium depletion in the bone.
  • a nabumetone medicament for use in the prophylaxis and/or treatment of disorders associated with calcium depletion in the bone may be prepared by admixture of nabumetone with an appropriate carrier, which may contain a diluent, binder, filler, disintegrant, flavouring agent, colouring agent, lubricant or preservative in conventional manner.
  • an appropriate carrier which may contain a diluent, binder, filler, disintegrant, flavouring agent, colouring agent, lubricant or preservative in conventional manner.
  • disorders associated with calcium depletion in the bone include osteoporosis, ricketts and calcium depletion in females associated with pregnancy.
  • the medicament is in unit dosage form and in a form adapted for use in the medical or veterinarial fields.
  • preparations may be in a pack form accompanied by written or printed instructions for use as an agent in the treatment of calcium depletion in bone.
  • the suitable dosage range for nabumetone depends on the nature of the calcium depletion and on the condition of the patient. It will also depend, inter alia, upon the relation of potency to absorbability and the frequency and route of administration.
  • Nabumetone may be formulated for administration by any route, and examples are oral, rectal, topical, parenteral, intravenous or intramuscular administration. Preparations may, if desired, be designed to give slow release of nabumetone.
  • the medicaments may, for example, be in the form of tablets, dispersible tablets, capsules, sachets, vials, powders, granules, lozenges, reconstitutable powders, or liquid preparations, for example solutions or suspensions, or suppositories.
  • the medicaments may contain conventional excipients such as binding agents, for example syrup, acacia, gelatin, sorbitol, tragacanth, or polyvinylpyrrolidone; fillers, for example lactose, sugar, maize-starch, calcium phosphate, sorbitol or glycerine; tabletting lubricants, for example magnesium stearate; disintegrants, for example starch, polyvinylpyrrolidone, sodium starch glycollate or microcrystalline cellulose; or pharmaceutically acceptable setting agents such as sodium lauryl sulphate.
  • binding agents for example syrup, acacia, gelatin, sorbitol, tragacanth, or polyvinylpyrrolidone
  • fillers for example lactose, sugar, maize-starch, calcium phosphate, sorbitol or glycerine
  • tabletting lubricants for example magnesium stearate
  • disintegrants for example starch, polyvinylpyrrolidon
  • Solid medicaments may be obtained by conventional methods of blending, filling, tabletting or the like. Repeated blending operations may be used to distribute nabumetone throughout those medicaments employing large quantities of fillers.
  • any carrier suitable for formulating solid pharmaceutical compositions may be used, examples being magnesium stearate, starch, glucose, lactose, sucrose, rice flour and chalk. Tablets may be coated according to methods well known in normal pharmaceutical practice, in particular with an enteric coating.
  • the medicament may also be in the form of an ingestible capsule, for example of gelatin containing nabumetone if desired with a carrier or other excipients.
  • Medicaments for oral administration as liquids may be in the form of, for example, emulsions, syrups, or elixirs, or may be presented as a dry product for reconstitution with water or other suitable vehicle before use.
  • Such liquid medicaments may contain conventional additives such as suspending agents, for example sorbitol, syrup, methyl cellulose, gelatin, hydroxyethylcellulose, carboxymethylcellulose, aluminium stearate gel, hydrogenated edible fats; emulsifying agents, for example lecithin, sorbitan monooleate, or acacia; aqueous or non-aqueous vehicles, which include edible oils, for example almond oil, fractionated coconut oil, oily esters, for example esters of glycerine, or propylene glycol, or ethyl alcohol, glycerine, water or normal saline; preservatives, for example methyl or propyl p-hydroxybenzoate or sorbic acid; and if desired conventional flavouring
  • Nabumetone may also be administered by a non-oral route.
  • the medicaments may be formulated, for example for rectal administration as a suppository. They may also be formulated for presentation in an injectable form in an aqueous or non-aqueous solution, suspension or emulsion in a pharmaceutically acceptable liquid, e.g. sterile pyrogen-free water or a parenterally acceptable oil or a mixture of liquids.
  • the liquid may contain bacteriostatic agents, an i-oxidants or other preservatives, buffers or solutes to render the solution isotonic with the blood, thickening agents, suspending agents or other pharmaceutically acceptable additives.
  • Such forms will be presented in unit dose form such as ampoules or disposable injection devices or in multi- dose forms such as a bottle from which the appropriate dose may be withdrawn or a solid form or concentrate which can be used to prepare an injectable formulation.
  • the effective dose of nabumetone depends on the nature of the calcium depletion in the bone, the condition of the patient and on the frequency and route of administration.
  • a unit dose will generally contain from 20 to 2000 mg of nabumetone and preferably will contain from 30 to 1000 mg, in particular 50, 100, 150, 200, 250, 300, 350, 400, 450, 500, 750, 800 or 1000 mg.
  • the composition may be administered once or more times a day for example 2, 3 or 4 times daily, and the total daily dose for a 70 kg adult will normally be in the range 100 to 3000 mg.
  • the unit dose will contain from 2 to 20 mg of nabumetone and be administered in multiples, if desired, to give the preceding daily dose.
  • nabumetone compositions are in the form of 500 mg swallow tablets.
  • the present invention further provides a pharmaceutical composition for use in the prophylaxis and/or treatment of disorders associated with calcium depletion in the bone which comprises an effective amount of nabumetone and a pharmaceutically acceptable carrier.
  • a pharmaceutical composition for use in the prophylaxis and/or treatment of disorders associated with calcium depletion in the bone which comprises an effective amount of nabumetone and a pharmaceutically acceptable carrier.
  • Such compositions may be prepared in the manner as hereinbefore described.
  • the average reduction was 31.8%: from 25.7 mg/ml/hr. to 17.5 mg/ml/hr. (P ⁇ 0.05).
  • nabumetone may be able to reduce the amount of bone resorption in patents with IH and may have a prophylactic role in hypercalciuric patients with high bone turnover who are candidates for developing osteoporosis.

Landscapes

  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention décrit l'utilisation de la nabumétone dans la fabrication d'un médicament servant à la prophylaxie et/ou au traitement de maladies associées à l'appauvrissement en calcium dans les os.
PCT/EP1991/001750 1990-09-22 1991-09-13 Utilisation de la nabumetone contre l'appauvrissement en calcium WO1992004892A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB9020697.0 1990-09-22
GB909020697A GB9020697D0 (en) 1990-09-22 1990-09-22 Treatment

Publications (1)

Publication Number Publication Date
WO1992004892A1 true WO1992004892A1 (fr) 1992-04-02

Family

ID=10682612

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1991/001750 WO1992004892A1 (fr) 1990-09-22 1991-09-13 Utilisation de la nabumetone contre l'appauvrissement en calcium

Country Status (5)

Country Link
AU (1) AU8521591A (fr)
GB (1) GB9020697D0 (fr)
IE (1) IE913315A1 (fr)
WO (1) WO1992004892A1 (fr)
ZA (1) ZA917520B (fr)

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
Drugs, volume 40, suppl. 5, 1990, P. M]nzel et al.: "Efficacy and safety of nabumetone in 4541 elderly patients from a drug monitoring study", pages 62-64, see the whole article *
La Clinica Therapeutica, volume 133, fasc. 6, no. 812, 30 June 1990, F. Catalano et al.: "Analgesic and anti-inflammatory effect of nabumetone in osteo-articular deseases in the acute phase", pages 379-386, see abstract in english *
Pharmatherapeutica, volume 3, no. 9, 1984, J. Gillgrass et al.: "Nabumethone: a double-blind study in osteoarthrosis", pages 592-594, see the whole article *

Also Published As

Publication number Publication date
GB9020697D0 (en) 1990-11-07
IE913315A1 (en) 1992-02-25
ZA917520B (en) 1992-07-29
AU8521591A (en) 1992-04-15

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