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
  • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
  • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
• • 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
  • A61K31/74—Synthetic polymeric materials
  • A61K31/765—Polymers containing oxygen
  • A61K31/77—Polymers containing oxygen of oxiranes
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
  • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
  • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
  • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/0012—Galenical forms characterised by the site of application
  • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P17/00—Drugs for dermatological disorders
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Definitions

• the term “topical treatment” means the treatment of the surface of the body of an animal or human or an internal surface of the human or animal that has been externalized either during surgery or by traumatic injury.
• damaged tissue means tissue damaged by surgery, ischemia, burns, toxins, trauma or other noxious insult.
• diseased tissue means tissue that is infected with a microorganism such as a yeast, bacteria or virus or a combination of organisms. The infection can be independent of or as a result of damage to the tissue.
• burns means tissue injuries caused by thermal, electrical, ionizing or solar radiation or chemical agents.
• the copolymer is and an acid mucopolysaccharide are dissolved in an aqueous solution. It is preferable that the acid mucopolysaccharide have little or no anticoagulant activity or to be of sufficient molecular size or charge so as not to be absorbed in the ciruculation to avoid the toxicity exhibited by many acid mucopolysaccharides.
• the composition is then topically applied to damaged tissue. This allows manifestation of the therapeutic effects of the acid mucopolysaccharide at concentrations producing minimal or no compromise to the blood coagulation system. Because the preferred copolymer is a liquid at room temperature or below, and is a gel at body temperature, the aqueous gel composition forms a protective gel over the damaged tissue.
• the surface active copolymer blocks are formed by condensation of ethylene oxide and propylene oxide at elevated temperature and pressure in the presence of a basic catalyst. There is some statistical variation in the number of monomer units which combine to form a polymer chain in each copolymer. The molecular weights given are approximations of the average weight of copolymer molecule in each preparation. It is to be understood that the blocks of propylene oxide and ethylene oxide do not have to be pure. Small amounts of other materials can be admixed so long as the overall physical chemical properties are not substantially changed. A more detailed discussion of the preparation of these products is found in U.S. Patent No. 2,674,619, which is incorporated herein by reference. Preparation of the copolymer portion of the present invention is described in U. S. Patent Nos. 3,925,241 and 3,867,533, both of which are incorporated herein by reference. Illustrative block copolymers of the following general formula:
• Chondroitin a major polysaccharide of cartilage proteoglycans, contains alternating units of D-glucuronic acid and N-acetyl-D-galactosamine. Chondroitin may be regarded as the parent material for other widely distributed polysaccharides, such as chondroitin sulfate A and chondroitin sulfate C, which differ only in the position in which sulfate is esterified to the galactosamine moiety.
• Dermatan consists of repeating disaccharide units of iduronosyl and acetylgalactosamine. It can be isolated from various tissues including blood vessel walls and skin. Dermatan sulfate catalyses the thrombin-heparin cofactor II interaction. Despite the antithrombotic effects of dermatan sulfate, dermatan compounds generally are weak anticoagulants.
• the copolymer in this example has the following general formula:
• Example IV The composition of Example HI is administered to a patient with a first degree bum on his leg.
• the composition is placed in a syringe and is cooled to approximately 20°C.
• the composition is slowly applied to the surface of the bum, allowing the liquid composition to gel on the bum. Enough of the composition is added to form a gel that is approximately 0.2 cm in depth.
• topically-applicable gel composition in the treatment of thermally injured tissue were studied in a guinea pig model ' of split thickness burns. Deeply anesthetised, hairless guinea pigs were subjected to thermal tissue injury by placing a 5 cm ⁇ , 80g metal probe (heated to 80°C) on their back for exactly 5 seconds. Thirty minutes post bum, animals were either left untreated (control), treated with the 20% gel of poloxamer 407 without dermatan or treated with 20% poloxamer 407 and 5% dermatan sulfate (Scientific Protein Labs, Waunakee, WS). Treated animals received 0.5 ml applications of the appropriate test article at 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 24, 28,
• the effects of the topically-applicable gel composition on erythema in the bum model are shown in Table V. Erythema was scored as 0 for little or no erythema to 3 for maximum erythema. As can be seen in Table V, the animals that were treated with the poloxamer/dermatan combination had less erythema than did the animals that were treated with poloxamer only or were left untreated.

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• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• Medicinal Chemistry (AREA)
• General Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Pharmacology & Pharmacy (AREA)
• Epidemiology (AREA)
• General Chemical & Material Sciences (AREA)
• Engineering & Computer Science (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Organic Chemistry (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Dermatology (AREA)
• Oil, Petroleum & Natural Gas (AREA)
• Molecular Biology (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Medicinal Preparation (AREA)

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• 1991
  • 1991-04-25 WO PCT/US1991/002912 patent/WO1991016058A1/en not_active Application Discontinuation
  • 1991-04-25 EP EP19910909402 patent/EP0526578A4/en not_active Withdrawn
  • 1991-04-25 AU AU78692/91A patent/AU647484B2/en not_active Ceased
  • 1991-04-25 CA CA002081340A patent/CA2081340A1/en not_active Abandoned
  • 1991-04-25 JP JP3509151A patent/JPH0776175B2/ja not_active Expired - Lifetime
  • 1991-04-25 BR BR919106377A patent/BR9106377A/pt not_active Application Discontinuation
  • 1991-04-25 IE IE140391A patent/IE911403A1/en unknown
  • 1991-04-26 CN CN91103430A patent/CN1058341A/zh active Pending
  • 1991-04-26 IL IL97976A patent/IL97976A0/xx unknown
  • 1991-04-26 PT PT97504A patent/PT97504A/pt not_active Application Discontinuation

Patent Citations (2)

Non-Patent Citations (3)

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