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WO2012095726A1 - Association pharmaceutique contenant des sels de glucosamine et du paracétamol pour le traitement de l'arthrose - Google Patents

Association pharmaceutique contenant des sels de glucosamine et du paracétamol pour le traitement de l'arthrose Download PDF

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Publication number
WO2012095726A1
WO2012095726A1 PCT/IB2012/000026 IB2012000026W WO2012095726A1 WO 2012095726 A1 WO2012095726 A1 WO 2012095726A1 IB 2012000026 W IB2012000026 W IB 2012000026W WO 2012095726 A1 WO2012095726 A1 WO 2012095726A1
Authority
WO
WIPO (PCT)
Prior art keywords
glucosamine
paracetamol
pharmaceutical composition
composition according
pharmaceutically acceptable
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.)
Ceased
Application number
PCT/IB2012/000026
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English (en)
Other versions
WO2012095726A8 (fr
Inventor
Vedat EGILMEZ
Ferhat FARSI
Serdar Soylemez
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Abdi Ibrahim Ilac Sanayi Ve Ticaret AS
Original Assignee
Abdi Ibrahim Ilac Sanayi Ve Ticaret AS
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 Abdi Ibrahim Ilac Sanayi Ve Ticaret AS filed Critical Abdi Ibrahim Ilac Sanayi Ve Ticaret AS
Publication of WO2012095726A1 publication Critical patent/WO2012095726A1/fr
Publication of WO2012095726A8 publication Critical patent/WO2012095726A8/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7008—Compounds having an amino group directly attached to a carbon atom of the saccharide radical, e.g. D-galactosamine, ranimustine

Definitions

  • This invention relates to a pharmaceutical composition
  • a pharmaceutical composition comprising a combination of glucosamine or its pharmaceutically acceptable salts (preferably glucosamine sulphate or glucosamine hydrochloride) and paracetamol for decreasing pain while simultaneously improving joint movement, for the treatment of osteoarthritis.
  • This invention also relates to kits containing a pharmaceutical combination of: a) therapeutically effective amount of glucosamine or its pharmaceutically acceptable salts and b) therapeutically effective amount of paracetamol to treat patients suffering from osteoarthritis, as well as the production method of such combination.
  • the first ingredient of the combination is a member of the amino sugars class.
  • Glucosamine is a compound having molecular formula (C 6 Hi 3 N0 ) and the chemical name (3R,4R,5S, 6R)- 3-Amino-6- (hydroxymethyl)oxane-2,4,5-triol (or) 2- Amino-2-deoxy-D-glucose chitosamine.
  • Glucosamine is represented by structural Formula I.
  • Glucosamine sulphate is a naturally occurring chemical found in the human body. It is in the fluid that is around joints. Glucosamine sulphate is also found in other places in nature. For example, glucosamine sulphate that is used in dietary supplements is often harvested from the shells of shellfish. Glucosamine sulphate is produced commercially by the hydrolysis of crustacean exoskeletons or, less commonly, by the fermentation of grains, such as corn or wheat. In the United States, glucosamine sulphate is one of the most common non-vitamin, non-mineral, dietary supplement used by adults. Glucosamine sulphate attracted the attention of scientific community after long-term clinical trials showed that it could slow the progression of anatomic joint structure changes and also control the progression of symptoms.
  • the second ingredient of the combination is chemically described as N-(4-hydroxyphenyl) acetamide monohydrate and has structural Formula II.
  • Panadol the trade name of paracetamol, is a widely available brand of paracetamol. Being sold in over 80 countries, Panadol is marketed throughout Africa, Asia, Europe, Central America and Australasia. Paracetamol is available in tablet, capsule, liquid suspension, suppository, intravenous and intramuscular forms. The common adult dose is from 500 mg to 1000 mg. The recommended maximum daily dose, for adults, is 4000 mg. In recommended doses, paracetamol generally is safe for children and infants, as well as for adults, although rare cases of acute liver injury have been linked to amounts lower than 2500 mg per day.
  • Osteoarthritis also osteoarthroses or degenerative joint disease, is the most common type of arthritis.
  • OA is a chronic condition characterized by the breakdown of the joint's cartilage.
  • Cartilage is the part of the joint that cushions the ends of the bones and allows easy movement of the joint. The breakdown of cartilage causes the bones to rub against each other, thus causing stiffness, pain and loss of movement in the joint.
  • Treatment of OA varies with the severity of symptoms and focuses on decreasing pain or improving joint movement.
  • Treatment plans may include a combination of drugs, rest, physical activity, joint protection, use of heat or cold to reduce pain, and physical or occupational therapy.
  • This present invention relates to a pharmaceutical combination of therapeutically effective amounts of glucosamine or its pharmaceutically acceptable salts and therapeutically effective amounts of paracetamol and using of such combination to treat patients suffering pain during the joint movement.
  • glucosamine and paracetamol combination provides benefits to patients and physicians.
  • the combination helps to reduce the pain, while simultaneously improving joint movements. Additionally, glucosamine and paracetamol combination will increase patient compliance.
  • the combination also improves physician and pharmacist efficiencies. As glucosamine and paracetamol are formulated together, the physician will write a single prescription. The pharmacist would dispense a single combination rather than multiple prescriptions.
  • the invention discloses the use of a combination of glucosamine or its pharmaceutically acceptable salts and paracetamol for the preparation of a medicament for reducing pain while simultaneously improving joint movement, for the treatment of indications such as osteoarthritis.
  • present disclosure provides a pharmaceutical composition
  • a pharmaceutical composition comprising;
  • Glucosamine is typically presented in an amount from 500mg to 1500mg.
  • Paracetamol is typically presented in an amount from 500 mg to 1000 mg. These ranges are only exemplary.
  • the present invention includes solid unit dosage forms, which may be prepared by direct compression, dry granulation or wet granulation.
  • kits comprising a combination of: a) therapeutically effective amount of glucosamine or its pharmaceutically acceptable salts, b) therapeutically effective amount of paracetamol, c) at least one pharmaceutically acceptable excipient and d) a container, for the treatment of pain and improving joint movement.
  • 'therapeutically effective amount as used herein means the amount of glucosamine (or its pharmaceutically acceptable salts) or paracetamol that, when administered to a mammal for treating a joint disorder or condition, is sufficient to effect such treatment.
  • the therapeutically effective amount will vary depending on the compound, the disease and its severity as well as the age, weight, physical condition and responsiveness of the mammal to be treated.
  • present disclosure provides a pharmaceutical composition
  • a pharmaceutical composition comprising;
  • Suitable pharmaceutically acceptable salts used to prepare the pharmaceutical composition include, but are not limited to: glucosamine hydrochloride, glucosamine sulphate, N-acetyl glucosamine and chlorohydrate salt. These salts are only exemplary. Preferably, glucosamine sulphate or glucosamine hydrochloride will be used. The therapeutically effective amount of glucosamine sulphate or glucosamine hydrochloride used in the pharmaceutical composition is from 100 mg to 2000mg.
  • the therapeutically effective amount of paracetamol used in the pharmaceutical composition is from 100 mg to 2500 mg.
  • Paracetamol employed in this invention includes any pharmaceutically acceptable salt, solvent, ester or salt of ester.
  • Step c at least one pharmaceutically acceptable excipient
  • the excipient present in the composition according to the invention can be diluents such as microcrystalline cellulose, powdered cellulose, lactose (anhydrous or preferably monohydrate), compressible sugar, fructose, dextrates, other sugars such as mannitol, sorbitol, lactitol, sacharose or a mixture thereof, siliconised microcrystalline cellulose, calcium hydrogen phosphate, calcium carbonate, calcium lactate or mixtures of diluents.
  • the excipients include at least one diluent, selected from microcrystalline cellulose and lactose monohydrate.
  • composition according to the invention can also comprise binders, such as polyvinyl pyrrolidone, microcrystalline cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, low-substituted hydroxypropyl cellulose, hydroxypropylmethyl cellulose or other cellulose ethers, starch, pregelatinised starch, or polymethacrylate or mixtures of binders.
  • binders such as polyvinyl pyrrolidone, microcrystalline cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, low-substituted hydroxypropyl cellulose, hydroxypropylmethyl cellulose or other cellulose ethers, starch, pregelatinised starch, or polymethacrylate or mixtures of binders.
  • the excipients include at least one binder selected from hydroxypropyl cellulose, starch, in particular corn starch, pregelatinised starch and hydroxypropylmethyl cellulose.
  • hydroxypropyl cellulose comprising from 5 to 16 % by weight of hydroxypropoxy groups.
  • Suitable low-substituted hydroxypropyl celluloses are commercially available from Shin- Etsu Chemical Co., Ltd. under the trade names LH-11 , LH-20, LH-21, LH-22, LH-30, LH- 31 and LH-32.
  • disintegrants can also be present, such as starch, e.g. pregelatinised starch, corn starch or others, sodium starch glycolate, crospovidone, microcrystalline cellulose, carboxymethylcellulose sodium, polacrilin potassium, low-substituted hydroxypropyl cellulose or mixtures thereof.
  • microcrystalline cellulose is preferably used in an amount of 5 to 15 % by weight. It is preferred that the excipients include at least one disintegrant selected form starch, crospovidone and low-substituted hydroxypropyl cellulose.
  • the disintegrants can be added to the other excipients according to the process used in the state of the art, either in the process of granulating and/or in the preparation of the compression mixture.
  • lubricants can also be present as excipients, such as stearic acid, magnesium stearate, calcium stearate, sodium laurylsulphate, hydrogenated vegetable oil, hydrogenated castor oil, sodium stearyl fumarate, talc, or macrogols or mixtures thereof. It is preferred that the excipient include at least one lubricant selected from hydrogenated castor oil, talc and magnesium stearate. Further, stabilizers can also be present as excipients, such as sodium chloride, or potassium chloride.
  • the present invention includes solid unit dosage forms such as tablets, which may be prepared by direct compression, dry granulation or wet granulation.
  • compositions of the present invention may be formulated as: solid oral dosage forms, such as, for example, powders, granules, pellets, tablets, and capsules.
  • the formulations may be immediate release, delayed release, or modified release formulations.
  • Immediate release compositions may be conventional, dispersible, chewable, mouth dissolving, or flash melt preparations.
  • Modified release compositions may comprise hydrophilic and/or hydrophobic release rate controlling substances to form matrix and/or reservoir systems.
  • the compositions may be prepared by direct blending, dry granulation, wet granulation, extrusion, and spheronization.
  • the compositions may be presented as uncoated, film coated, sugar coated, powder coated, enteric coated or modified release coated.
  • the tablets may be film coated in a conventional manner, e.g. for cosmetic, palatability or production purposes.
  • Suitable coatings include hydroxypropylcellulose, acrylate and/or methacrylate co-polymers, resins etc.
  • the coating may be an enteric coating, e.g. which is insoluble in acidic gastric juice but soluble in alkaline digestive juice. Such a coating enables the tablet to pass through the stomach into the duodenum, where it dissolves.
  • Suitable enteric coatings include cellulose acetate phthalate.
  • kits comprising a combination of glucosamine or its pharmaceutically acceptable salts and paracetamol for the treatment of pain and improving joint movement.
  • Kit is emanated from sachet and per unit dosage forms mentioned above.
  • the kit includes glucosamine sulphate and paracetamol.
  • kits and pharmaceutical compositions suitable for use in the above methods are packaged with directions for using the contents thereof for reducing or eliminating pain and improving joint movement.
  • kits comprising:
  • Kit is emanated from sachet and per unit dosage forms mentioned above.
  • the kit includes glucosamine sulphate and paracetamol.
  • the disclosed powder formulation is typically dissolved and/or suspended in an ingestible liquid such as water.
  • the resulting mixture has a pleasant mouth-feel and therefore can be conveniently administered to patient as a drink.
  • the drink may be a suspension or a solution.
  • the drink can be even more palatable with one or more sweeteners and/or flavorants.
  • the disclosed powder formulation can be mixed with foods, such as mashed potatoes or oatmeal.
  • the powder formulations of the invention can be conveniently packaged in a container.
  • a "container" is a non-ingestible containment device which can hold and preserve the stability of the powder formulation for a sufficient period of time, i.e., from the time of manufacture to the time of consumption by patient.
  • the powder formulation is uncapsulated and free-flowing.
  • Containers suitable for the present invention include a sachet, such as a paper bag, powder bag of plastic films or metal foils; a bottle, such as a glass, plastic or metal bottle; a tub; and an ampule.
  • the container of the invention is a sachet.
  • the container material is preferably impermeable to water and water vapor in order that the stability of the active agent contained in the container is ensured.
  • the container materials can contain substances which impart a particular type of protection, for example protection against light.
  • suitable containers include, but are not limited to: plastics, such as MATT LACQUER/PET 23 JPX 12GR/AL 12 J2/SURLYN 23GR (AMCOR Flexibles in Victoria, Australia), coated papers, such as Coated Paper 40GRIPX 12 GRIAL 12 /SURLYN 23 GR (AMCOR Flexibles in Victoria, Australia), foil pouches, such as TPC- 2475 (TOLAS Health Care Packaging in Feasterville, PA), or any combination of these materials (e.g., laminates).
  • plastics such as MATT LACQUER/PET 23 JPX 12GR/AL 12 J2/SURLYN 23GR (AMCOR Flexibles in Victoria, Australia
  • coated papers such as Coated Paper 40GRIPX 12 GRIAL 12 /SURLYN 23 GR (AMCOR Flexibles in Victoria, Australia)
  • foil pouches such as TPC- 2475 (TOLAS Health Care Packaging in Feasterville, PA), or any combination of these materials (e.g., laminates).
  • the container is a multi-layer container having multiple layers of different container materials discussed above.
  • the container containing the powder formulation of the invention can be a unit- dose or a multi-dose container.
  • the container of the invention can contain a single dose sachet.
  • the powder formulations of the invention can be prepared by any of the methods known in the art of pharmacy. For example, standard pharmaceutical formulation techniques such as those described in Remington's Pharmaceutical Sciences, 18th ed. (1990), Mack Publishing Company, Easton, PA., the disclosure of which is incorporated herein by reference, can be used.
  • Glucosamine is typically presented in an amount from 500mg to 1500mg.
  • Paracetamol is typically presented in an amount from 500 mg to 1000 mg. These ranges are only exemplary.
  • present disclosure provides pharmaceutical dosage form comprising: a) 50-95%, preferably 70-90%, especially 70-80% by weight of the first active substance (i.e., glucosamine or its pharmaceutically acceptable salts, preferably glucosamine sulphate); b) 5-50%, preferably 15-30%, especially 20-25%o by weight of the second active substance (i.e., paracetamol); and c) at least one pharmaceutically acceptable excipient.
  • the first active substance i.e., glucosamine or its pharmaceutically acceptable salts, preferably glucosamine sulphate
  • at least one pharmaceutically acceptable excipient i.e., paracetamol

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

Abstract

Cette invention porte sur une composition pharmaceutique comprenant une association de glucosamine ou de ses sels pharmaceutiquement acceptables (de préférence le sulfate de glucosamine ou le chlorhydrate de glucosamine) et de paracétamol pour la réduction de la douleur et l'amélioration simultanée du mouvement des articulations, pour le traitement de l'arthrose. Cette invention porte également sur des trousses contenant une association pharmaceutique de : a) une quantité thérapeutiquement efficace de glucosamine ou de ses sels pharmaceutiquement acceptables et b) une quantité thérapeutiquement efficace de paracétamol pour traiter des patients souffrant d'arthrose, ainsi que sur le procédé de production d'une telle association.
PCT/IB2012/000026 2011-01-10 2012-01-10 Association pharmaceutique contenant des sels de glucosamine et du paracétamol pour le traitement de l'arthrose Ceased WO2012095726A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
TR2011/00209 2011-01-10
TR2011/00209A TR201100209A2 (tr) 2011-01-10 2011-01-10 Osteoartrit tedavisi için glukozamin tuzları ve parasetamol içeren farmasötik bileşim.

Publications (2)

Publication Number Publication Date
WO2012095726A1 true WO2012095726A1 (fr) 2012-07-19
WO2012095726A8 WO2012095726A8 (fr) 2012-09-13

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PCT/IB2012/000026 Ceased WO2012095726A1 (fr) 2011-01-10 2012-01-10 Association pharmaceutique contenant des sels de glucosamine et du paracétamol pour le traitement de l'arthrose

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TR (1) TR201100209A2 (fr)
WO (1) WO2012095726A1 (fr)

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20010046971A1 (en) * 2000-02-18 2001-11-29 Milton Hammerly Analgesics combined with naturally-occurring chondroprotective agents
US20020058642A1 (en) * 2000-09-26 2002-05-16 Temple University Of The Commonwealth Of Higher Education Analgesic and glucosamine compositions
WO2003099013A1 (fr) * 2000-01-24 2003-12-04 Omni Nutraceuticals, Inc. Composition a base de glucosamine et medicament anti-inflammatoire a base de paracetamol/non steroide
WO2007008752A2 (fr) * 2005-07-07 2007-01-18 Farnam Companies, Inc. Compositions pharmaceutiques a liberation prolongee pour medicaments tres solubles dans l'eau
US20070249735A1 (en) * 2004-09-17 2007-10-25 Jf C Technologies, Llc Halide-free glucosamine-acidic drug complexes
US20070248677A1 (en) * 2004-09-17 2007-10-25 Jame Fine Chemicals, Inc. Method for treating warm-blooded vertebrates with a salt of a halide-free glucosamine base and a therapeutic drug

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003099013A1 (fr) * 2000-01-24 2003-12-04 Omni Nutraceuticals, Inc. Composition a base de glucosamine et medicament anti-inflammatoire a base de paracetamol/non steroide
US20010046971A1 (en) * 2000-02-18 2001-11-29 Milton Hammerly Analgesics combined with naturally-occurring chondroprotective agents
US20020058642A1 (en) * 2000-09-26 2002-05-16 Temple University Of The Commonwealth Of Higher Education Analgesic and glucosamine compositions
US20070249735A1 (en) * 2004-09-17 2007-10-25 Jf C Technologies, Llc Halide-free glucosamine-acidic drug complexes
US20070248677A1 (en) * 2004-09-17 2007-10-25 Jame Fine Chemicals, Inc. Method for treating warm-blooded vertebrates with a salt of a halide-free glucosamine base and a therapeutic drug
WO2007008752A2 (fr) * 2005-07-07 2007-01-18 Farnam Companies, Inc. Compositions pharmaceutiques a liberation prolongee pour medicaments tres solubles dans l'eau

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
"Remington's Pharmaceutical Sciences", 1990, MACK PUBLISHING COMPANY
NORMAN TM NG; KRISTIANN C HEESCH; WENDY J BROWN: "Efficacy of a progressive walking program and glucosamine sulphate supplementation on osteoarthritic symptoms of the hip and knee: a feasibility trial", ARTHRITIS RESEARCH & THERAPY, vol. 12, 2010, pages R25, XP021070745

Also Published As

Publication number Publication date
WO2012095726A8 (fr) 2012-09-13
TR201100209A2 (tr) 2012-07-23

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