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
  • A61K31/41—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
  • A61K31/415—1,2-Diazoles
• • 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
  • A61K33/00—Medicinal preparations containing inorganic active ingredients
  • A61K33/24—Heavy metals; Compounds thereof
  • A61K33/26—Iron; Compounds thereof
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P33/00—Antiparasitic agents
  • A61P33/10—Anthelmintics

Definitions

• This invention relates to novel pharmaceutical and veterinary compositions for the treatment or prevention of helminthiasis, more particularly to such compositions comprising iron and an anthelmintic.
• Helminthiasis is a major problem in many parts of the world, affecting both animals and humans. In poorer countries, infestation of humans and livestock with Q helminths aggravates shortages of food by increasing the nutritional demand of the host.
• anthelmintic compounds are known. These have proved effective in the treatment of helminthiasis, but anthelmintic resistance in helminths is a growing 5 problem. This can be combatted by use of new anthelmintic compounds, but the research needed to identify or synthesise novel anthelmintic compounds is both expensive and time-consuming.
• a pharmaceutical or veterinary composition comprising iron and an anthelmintic.
• the iron is preferably present in the form of an iron-carbohydrate complex.
• Iron-carbohydrate complexes which may be mentioned include iron-dextran complexes and iron-dextrin complexes, for example ferric hydroxide-dextran complex, ferric hydroxide-dextran heptonic acid complex and ferric hydroxide-dextrin heptonic acid complex.
• ferric hydroxide-dextran heptonic acid complex Of particular interest is ferric hydroxide-dextran heptonic acid complex.
• Ferric hydroxide-dextran heptonic acid complex and ferric hydroxide-dextrin heptonic acid complex were disclosed in UK Patent 1183940.
• Suitable anthelmintics include benzimidazole derivatives, for example oxfendazole, albendazole, thiabendazole, parbendazole, mebendazole, fenbendazole and thiophanate; imidazothiazole derivatives, for example levamisole, pyrantel and morantel; avermectins, for example ivermectin; piperazines, for example piperazine citrate; anilids and substituted phenols; and organophosphates.
• benzimidazole derivatives for example oxfendazole, albendazole, thiabendazole, parbendazole, mebendazole, fenbendazole and thiophanate
• imidazothiazole derivatives for example levamisole, pyrantel and morantel
• avermectins for example ivermectin
• piperazines for example piperazine citrate
• compositions according to the invention may be administered to mammals including pigs, sheep, horses, cattle and humans.
• the preferred dosages of the active ingredients will vary with the nature of the preparation used and the mammal to which the composition is administered. For example, a 1.5ml injection comprising 20% by weight of ferric hydroxide-dextran heptonic acid complex containing 300mg of iron in an aqueous dispersion may be administered to a lamb of about 3 weeks of age, whereas a similar 10ml injection containing 2g of iron may be administered to a human.
• the dosage of the anthelmintic is preferably within the normal dosage for the compound concerned, for example a 1.5ml injection may contain 7.5% by weight of leyamisole for a lamb of about 3 weeks of age.
• a unit dose of the composition to provide from 0.5 to 50mg, more preferably 1 to 25mg, of anthelmintic per kg of body weight; and from 0.5 to lOOOmg, more preferably 10 to lOOmg, of iron per kg of body weight.
• the composition of the invention may be administered orally (for example as a drench to animals) or by injection (intravenous or intramuscular) . In either case we prefer the composition to be in the form of an aqueous dispersion.
• dispenser we mean a colloidal dispersion, a suspension or a solution, depending ⁇ upon the solubility of the materials to be dispersed in the aqueous phase.
• the active ingredients may be worked up with inorganic or organic pharmaceutically or veterinarily acceptable adjuvants, carriers or excipients.
• adjuvants, carriers or excipients are: for tablets and dragees: diluents, for example lactose; binders, for example cellulosic materials such as microcrystalline cellulose and methyl cellulose; disintegrating agents, for example starches such as maize starch; stabilisers, for example to prevent hydrolysis of the active ingredients; flavouring agents, for example sugars; fillers; stearates; and inorganic diluents, for example talc; for syrups, suspensions, dispersions, solutions and drenches: a liquid vehicle in which the active ingredients may be dissolved or suspended, for example water; and suspending agents, for example cellulose derivatives and gums.
• Drenches may be administered with a drenching gun or bottle or a similar device adapted to administer a metered dose to an animal.
• the drench may be supplied in the form of a wettable powder which can be dissolved or dispersed in water by a user.
• a powder may comprise the active ingredient, a colloid to make a drench of suitable viscosity for the gun, and a surface active agent to assist in dispersion or dissolution of the powder in water.
• the drench may also be supplied in li-quid form in which case it is desirable to incorporate a preservative such as glycerin or sodium benzoate; for hard or soft capsules: diluents, eg lactose; glidants, for example stearates; inorganic materials, for example silica or talc; stabilisers; and dispersing agents.
• a preservative such as glycerin or sodium benzoate
• diluents eg lactose
• glidants for example stearates
• inorganic materials for example silica or talc
• stabilisers for example silica or talc
• compositions may also contain further adjuvants, for example a composition for use in a tablet may contain lubricants and glidants to assist in tabletting, for example magnesium stearate, or wetting agents to assist in granulation, eg dioctyl sodium sulphosuccinate.
• a composition for use in a tablet may contain lubricants and glidants to assist in tabletting, for example magnesium stearate, or wetting agents to assist in granulation, eg dioctyl sodium sulphosuccinate.
• the composition may also, if desired, contain pharmaceutically or veterinarily acceptable dyes or colourants, and may, if desired, be coated using conventional film or sugar coating techniques.
• the composition may also be in the form of a slow release formulation, for example a sustained release bolus, injection or capsule.
• a method of treatment which comprises administering an anthelmintic in conjunction with iron to a mammal infested with, or at risk of being infested with, helminths. This method of treatment could be executed by sequential administration of anthelmintic and then iron.
• products containing an anthelmintic and iron as a combined preparation for simultaneous, separate or sequential use in the treatment or prevention of helminthiasis are provided.
• we prefer to execute the method of treatment by administration of a composition according to the invention as this has the advantage of single administration resulting in a saving of time for the person carrying out the treatment, and less distress for the mammals being treated.
• the overall efficacy of oxfendazole alone was 48.1%.
• the overall efficacy of iron injection alone (day 21) was 4.7%.
• the overall efficacy of simultaneous administration of oxfendazole and iron injection was 67.9%.

Landscapes

• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Veterinary Medicine (AREA)
• Chemical & Material Sciences (AREA)
• Public Health (AREA)
• Medicinal Chemistry (AREA)
• General Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Pharmacology & Pharmacy (AREA)
• Epidemiology (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Organic Chemistry (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• General Chemical & Material Sciences (AREA)
• Inorganic Chemistry (AREA)
• Tropical Medicine & Parasitology (AREA)
• Molecular Biology (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Priority Applications (1)

Applications Claiming Priority (2)

Publications (1)

Family

ID=10651388

Family Applications (1)

Country Status (5)

Cited By (6)

• 1989
  • 1989-02-09 GB GB898902894A patent/GB8902894D0/en active Pending
• 1990
  • 1990-02-09 BR BR909005081A patent/BR9005081A/pt unknown
  • 1990-02-09 JP JP2503352A patent/JPH03504506A/ja active Pending
  • 1990-02-09 WO PCT/GB1990/000204 patent/WO1990009182A1/en not_active Application Discontinuation
  • 1990-02-09 AU AU50836/90A patent/AU5083690A/en not_active Abandoned

Non-Patent Citations (1)

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