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
  • A61K31/425—Thiazoles
  • A61K31/428—Thiazoles condensed with carbocyclic rings
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P3/00—Drugs for disorders of the metabolism
  • A61P3/04—Anorexiants; Antiobesity agents

Definitions

• the invention relates to the use of pramipexole for the manufacture of a medicament for reducing excessive food intake in children.
• the object of the invention is to make it easier for the young patient between the ages of 6 and 18 to reduce the calorie intake and thus to reduce the health risks associated with obesity.
• pramipexole can be used in therapeutically well tolerated effective doses to reduce excessive food intake in children.
• the present invention aims to use pramipexole for the manufacture of a medicament for reducing excessive food intake in children.
• pramipexole for the manufacture of a medicament for reducing excessive food intake in children aged 6 to 18 years, preferably aged 12 to 18 years. Also preferred is use in children whose BMI is above the 90th percentile, preferably above the 97th percentile.
• the use is particularly preferred, with the children being given a daily dose of approximately 0.005 mg / kg to 0.02 mg / kg body weight, preferably approximately 0.1 mg / kg body weight, of pramipexole.
• pramipexole for the manufacture of a medicament for the treatment of obesity in type 2 diabetes in children.
• pramipexole for the manufacture of a medicament for continuous application in children is particularly preferred.
• pramipexole for the manufacture of a medicament for transdermal application in children.
• pramipexole is optionally used in the form of its enantiomers, preferably the (-) enantiomer, optionally in the form of the pharmacologically acceptable acid addition salts and optionally in the form of the hydrates and solvates.
• a pharmaceutical composition containing pramipexole as the active ingredient optionally in the form of its enantiomers, preferably the (-) enantiomer, optionally in the form of the pharmacologically acceptable acid addition salts and optionally in the form of the hydrates and solvates or their physiologically acceptable salts in combination with one or more active ingredients selected from the group of Dopamine-Dr, D 2 -, D 3 - or D 4 - agonists, anorectics, lipase inhibitors and sympathomimetics for the manufacture of a medicament for the treatment of children.
• Pramipexole has a high selectivity for the dopamine D 3 receptor. It can be shown that this reduces the side effects of pharmacologically influencing food intake.
• the D 3 receptor is predominantly located in regions of the brain that are associated with emotion.
• One . Activation of the D 3 receptor by pramipexole can occur via mood enhancement can help reduce excessive food intake or pathologically impaired food intake.
• the pramipexole used in the context of the present invention can optionally be used in the form of its enantiomers or its racemates, optionally in the form of the pharmacologically acceptable acid addition salts and optionally in the form of the hydrates and solvates.
• pramipexole includes the (+) enantiomer and the racemate. In the context of the present invention, however, the (-) enantiomer is of particular importance.
• the pramipexole which can be used according to the invention can optionally be used in the form of its pharmaceutically acceptable acid addition salts and, if appropriate, in the form of its hydrates and / or solvates.
• pharmaceutically acceptable acid addition salts of pramipexole are understood to be those salts which are selected from the salts of hydrochloric acid, hydrobromic acid, sulfuric acid, phosphoric acid, methanesulfonic acid, acetic acid, fumaric acid, succinic acid, lactic acid, citric acid, holy acid and maleic acid, the salts of hydrochloric acid, Hydrobromic acid, sulfuric acid, phosphoric acid, and acetic acid are particularly preferred.
• the salts of hydrochloric acid are of particular importance here.
• pramipexole dihydrochloride is of particular importance.
• the base of the pramipexole is preferably used.
• the pramipexole dihydrochloride monohydrate is particularly preferred:
• pramipexole can optionally be used in combination with other active ingredients.
• Preferred combination partners are compounds selected from the classes of dopamine Di, D 2, D 3 or D 4 - receptor agonist selected from the group consisting of Adrogolide, A- 86929, Rotigotine, NeurVex, Nolomirole, talipexol, CHF 1512 ( -) - Stepholidine, DAR-201, Diacrin / Genzyme, Bromocriptine, Bupropion, LEK-8829, BAM- ⁇ 110, AIT-203, NS-2330, Terguride, Aripiprazole, OPC-4392, GMC-1111, PD-148903, Apomorphine HCI, PD-89211, PD-158771, Cabergoline, Sumanirole, PNU- 14277E, POL-255, Dihydrexidine, GBR-12783, Quinagolide HCI, (R) -Bupropion, S-32504, S-3
• Figure 1 describes the results of a 4-day long application of pramipexole (PPX) compared to the single application on 4 consecutive days.
• PPX pramipexole
• Figure 2 describes the reduction in body weight during 14 days of continuous subcutaneous (sc) infusion of pramipexole and 7 days of follow-up.
• Pramipexole inhibits food intake in mice when administered continuously.
• the continuous application by means of osmotic pumps led to a permanent, statistically highly significant inhibition of feed intake (Figure 1). in the
• mice (strain: C57BL / 6) were deprived of their food for 24 h with free access to drinking water. 15 20 min before the end of the fasting period, pramipexole (2.5 mg / kg body weight SC) was applied.
• the control group also 10 mice, received physiological saline, the solvent used for pramipexole. After that, the animals were offered feed and the feed consumption was measured over a period of 4 days every 30 minutes. 0
• mice 10 mice (strain: C57BL / 6) were deprived of their food for 24 h
• the alzet® Mini-osmotic 5 pump (model 2002) was implanted subcutaneously in the animals 20 min before the end of the fasting period with a release dose of 2.5 mg pramipexole / 24 h s.c.
• the pumping rate was 0.54 ⁇ U.
• a group of 10 control animals received the solvent, physiological saline solution, applied at the same pumping rate in an analog test.
• the continuous release of the substance or solvent was measured for 4 days. Feed intake 0 was measured every two hours for the first ten hours, later daily.
• the change in weight for the long-term application was measured over a period of 22 days, the pramipexole administration being ended after 14 days 5.
• the change in weight was measured daily.
• dosages for the administration of pramipexole are included here Children specified. These can be used in doses of about 0.05 to 3 mg, preferably from about 0.1 to 1.5 mg, per day. These dosages are based on pramipexole in the form of its free base. Based on the preferred salt form of pramipexole dihydrochloride monohydrate, the above-mentioned dosages correspond to about 0.07 to 4.26 mg, preferably 0.14 to 2.13 mg, of pramipexole dihydrochloride monohydrate per day.
• Week 2 1 tablet containing 0.18 mg pramipexole 3 times a day
• pramipexole can be administered orally, transdermally, intrathecally, by inhalation, nasally or parenterally, preferably transdermally or parenterally, particularly preferably transdermally.
• Suitable forms of use are, for example, tablets, preferably slow release tablets, capsules, suppositories, solutions, juices, emulsions, dispersible powders, implants or plasters, preferably plasters, particularly preferably micron plasters.
• Tablets can, for example, by mixing the active ingredient (s) with known auxiliaries, for example inert diluents such as calcium carbonate, calcium phosphate or milk sugar, disintegrants such as corn starch or alginic acid, binders such as starch or gelatin, lubricants such as magnesium stearate or talc, and / or agents for Achievement of the depot effect, such as carboxymethyl cellulose, cellulose acetate phthalate, or polyvinyl acetate can be obtained.
• auxiliaries for example inert diluents such as calcium carbonate, calcium phosphate or milk sugar, disintegrants such as corn starch or alginic acid, binders such as starch or gelatin, lubricants such as magnesium stearate or talc, and / or agents for Achievement of the depot effect, such as carboxymethyl cellulose, cellulose acetate phthalate, or polyvinyl acetate can be obtained.
• the tablets can also consist of several layers.
• Pramipexole dihydrochloride monohydrate 0.3 mg sodium chloride 0.8 mg benzalkonium chloride 0.01 mg agua ad injectionem ad 100 ml

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• Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Pharmacology & Pharmacy (AREA)
• General Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Obesity (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Hematology (AREA)
• Diabetes (AREA)
• General Chemical & Material Sciences (AREA)
• Child & Adolescent Psychology (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Engineering & Computer Science (AREA)
• Organic Chemistry (AREA)
• Epidemiology (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

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• 2003
  • 2003-03-21 DE DE10312809A patent/DE10312809A1/de not_active Withdrawn
• 2004
  • 2004-03-18 WO PCT/EP2004/002793 patent/WO2004082680A1/de not_active Application Discontinuation
  • 2004-03-18 EP EP04721477A patent/EP1608367A1/de not_active Withdrawn
  • 2004-03-18 CA CA002519584A patent/CA2519584A1/en not_active Abandoned
  • 2004-03-18 JP JP2006504716A patent/JP2006520764A/ja active Pending

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