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
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P19/00—Drugs for skeletal disorders
  • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis

Definitions

• This invention relates to injectable pharmaceutical compositions containing panthenol and their use in the alleviation of inflammation and pain in joints affected by traumatic arthritis.
• Pain or loss of movement in joints is a common occurrence for those who have suffered damage to cartilage, bone surfaces or ligaments, particularly among the elderly.
• Standard methods of treatment include the administration of corticosteroids by injection into the site of the inflammation.
• relief tends to be temporary and long term use carries a number of contraindications.
• Pantothenic acid sometimes known as vitamin B5
• Pantothenic acid has been used as a dietary supplement and for treatment of bronchial asthma, hay-fever, sinusitis and neurodermatitis.
• pantothenic acid salts may be used in an injectable formulation for treatment of joint pain.
• panthenol the alcohol derivative of pantothenic acid
• panthenol is of value in reducing pain and inflammation when injected into or adjacent to an affected joint.
• panthenol in the preparation of a injectable pharmaceutical composition for administration by injection into a joint, or into a body region closely adjacent to the joint, for alleviation of inflammation or pain caused by traumatic arthritis.
• the alcohol is optically active and the dextro-rotatory isomer dexpanthenol is the preferred active agent.
• Dexpanthenol is commercially available in forms approved by the European Pharmacopiea. There is no evidence of toxicity associated with the ingestion of panthenol. Dexpanthenol has rarely been associated with contact dermatitis when applied topically, and pain, numbness and difficulty breathing following injection.
• the injectable composition contains a dose of at least about 250 mg, typically at least about 400 mg of dexpanthenol, preferably at least about 500 mg, more preferably at least about 800 mg, and most suitably about 1000 mg i.e. about 1 gram of dexpanthenol.
• the exact dosage will vary with the condition treated, and the age and condition of the patient. A course of injections may be required, given at intervals of about one week. Reduced inflammation and increased freedom of movement is usually noticeable shortly after administration and a review of the response can be made after about a week of treatment. A second dose can then be given if necessary.
• an injectable pharmaceutical composition is prepared by dissolving the panthenol in a suitable solvent, e.g. water, and injecting the solution into, or closely adjacent to, the affected joint.
• a suitable solvent e.g. water
• the initial treatment may cause some pain and it may, therefore, be desirable to co-administer a local anaesthetic, such as bupivicaine or lignocaine, either as a separate injection at the same time or shortly before the injection of the panthenol, or as a coformulation with panthenol.
• physiologically active materials may be co-administered, if desired, e.g. cysteine or glucosamine.
• the injectable pharmaceutical compositions of this invention may be used in the treatment of several painful conditions associated with inflammation or reduced movement of joints. Although some relief may be obtained using the present invention to treat rheumatoid arthritic conditions, such treatment is not recommended because it will be only temporary due to the immune reaction cause of the disease.
• the main aim of the invention is to treat traumatic arthritic conditions, which are normally found to occur in only one joint at a time. Examples include tennis elbow, housemaid's knee, frozen shoulder, inflamed knee joints, ankle joints and hip joints and back pain associated with inflammation or restricted movement in the spinal vertebrae, such as posttraumatic spondylitis.
• the injectable pharmaceutical composition may be injected into the capsule of the joint by intra-articular injection.
• the injectable pharmaceutical composition may also be administered closely adjacent to the joint, but outside the capsule so that it can diffuse into the capsule, by peri-articular injection.
• injection outside the capsule is preferred, to avoid the risk of damage to the joint; this also enables the use of large dose (and hence large volume) injections which would be difficult to accommodate in small joints.
• Facet joints requiring injection are identified by an area of extreme tenderness in the area of pain and spasm in the patient's back. A needle inserted at right angles into this area will be located in or close to the facet joint. The solution does not have to be injected directly into the joint as it will diffuse into it; injections into and around the joint are equally effective.
• An injection into the region of a joint may be within about 5, 4, 3, 2 or 1 cm of the capsule of the joint, or closer.
• a dose of about 2 mis of an aqueous solution containing about 500 mg of dexpanthenol can be effective.
• the dose contains about 1000 mg of dexpanthenol, for example, as about 4 mis of an aqueous solution containing about 250 mg/ml.
• a programme of injections is generally desirable in which dosages similar to that indicated above are given at intervals of a few days to a few weeks.
• When administering an injection of 2 mis containing 500 mg dexpanthenol if the injection is painful, it may be appropriate to discontinue the injection at delivery of 1 ml, providing 250 mg of dexpanthenol, and repeat the dose at a later time.
• the preferred 1 ,000 mg dose may be given as, for example, two consecutive 500 mg doses.
• a suitable injectable formulation comprises 1000 mg of dexpanthenol and 1-10 mg of bupivicaine, for example, as 4 mis of an aqueous solution containing 250 mg/ml. dexpanthenol and 1 ml of a solution containing 1 mg of bupivicaine or 2 ml of a 0.5% solution of bupivicaine.
• the dose of bupivicaine can be adjusted dependin on the reaction of indivaula patiens to the injection.
• the bupivicaine, or other local anaesthetic can be administered as a separate injection immediately before an injection of dexpanthenol.
• Example 1 62 patients (26 men; 33 women) aged 21 to 85 years were treated for traumatic inflammatory conditions. The patients were administered one or more intra-articular or peri-articular injections, ie into the inflamed joint or nearby area, of dexpanthenol in combination with a long acting local anaesthetic [4 ml of an aqueous solution of dexpanthenol Ph Eur (providing 1000 mg of dexpanthenol); 1 ml of 0.1 % bupivacaine (providing 1 mg of bupivacaine)].
• a long acting local anaesthetic [4 ml of an aqueous solution of dexpanthenol Ph Eur (providing 1000 mg of dexpanthenol); 1 ml of 0.1 % bupivacaine (providing 1 mg of bupivacaine)].
• Example 1 The cohort of patients assessed in Example 1 primarily reported back pain to the test physician. Treatment of some patients who reported specific joint pain is summarised below.
• Bepanthene is a aqueous solution containing 250 mg/ml of dexpanthenol Ph Eur, 4 mis bepanthene provides 1000 mg dexpanthenol

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• Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
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• General Health & Medical Sciences (AREA)
• Pharmacology & Pharmacy (AREA)
• Chemical & Material Sciences (AREA)
• Veterinary Medicine (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Organic Chemistry (AREA)
• Physical Education & Sports Medicine (AREA)
• Orthopedic Medicine & Surgery (AREA)
• Immunology (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Engineering & Computer Science (AREA)
• Rheumatology (AREA)
• Epidemiology (AREA)
• General Chemical & Material Sciences (AREA)

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• 2007
  • 2007-07-13 WO PCT/GB2007/050406 patent/WO2009010707A1/en active Application Filing
  • 2007-07-13 EP EP07766447A patent/EP2178526A1/de not_active Withdrawn

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