WO2004082680A1 - Utilisation de pramipexol pour reduire l'absorption excessive d'aliments chez les enfants - Google Patents

Utilisation de pramipexol pour reduire l'absorption excessive d'aliments chez les enfants Download PDF

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Publication number
WO2004082680A1
WO2004082680A1 PCT/EP2004/002793 EP2004002793W WO2004082680A1 WO 2004082680 A1 WO2004082680 A1 WO 2004082680A1 EP 2004002793 W EP2004002793 W EP 2004002793W WO 2004082680 A1 WO2004082680 A1 WO 2004082680A1
Authority
WO
WIPO (PCT)
Prior art keywords
pramipexole
children
optionally
use according
manufacture
Prior art date
Application number
PCT/EP2004/002793
Other languages
German (de)
English (en)
Inventor
Joachim Mierau
Jürgen REESS
Marion Wienrich
Original Assignee
Boehringer Ingelheim International Gmbh
Boehringer Ingelheim Pharma Gmbh & Co Kg
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 Boehringer Ingelheim International Gmbh, Boehringer Ingelheim Pharma Gmbh & Co Kg filed Critical Boehringer Ingelheim International Gmbh
Priority to EP04721477A priority Critical patent/EP1608367A1/fr
Priority to CA002519584A priority patent/CA2519584A1/fr
Priority to JP2006504716A priority patent/JP2006520764A/ja
Publication of WO2004082680A1 publication Critical patent/WO2004082680A1/fr

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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
    • A61K31/33—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

Landscapes

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

Abstract

L'invention concerne l'utilisation d'agonistes des récepteurs de la dopamine pour produire un médicament servant à réduire l'absorption excessive d'aliments.
PCT/EP2004/002793 2003-03-21 2004-03-18 Utilisation de pramipexol pour reduire l'absorption excessive d'aliments chez les enfants WO2004082680A1 (fr)

Priority Applications (3)

Application Number Priority Date Filing Date Title
EP04721477A EP1608367A1 (fr) 2003-03-21 2004-03-18 Utilisation de pramipexol pour reduire l'absorption excessive d'aliments chez les enfants
CA002519584A CA2519584A1 (fr) 2003-03-21 2004-03-18 Utilisation de pramipexol pour reduire l'absorption excessive d'aliments chez les enfants
JP2006504716A JP2006520764A (ja) 2003-03-21 2004-03-18 子供による過剰な食物摂取を低減するためのプラミペキソール

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10312809.3 2003-03-21
DE10312809A DE10312809A1 (de) 2003-03-21 2003-03-21 Pramipexol zur Reduzierung übermäßiger Nahrungsaufnahme bei Kindern

Publications (1)

Publication Number Publication Date
WO2004082680A1 true WO2004082680A1 (fr) 2004-09-30

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2004/002793 WO2004082680A1 (fr) 2003-03-21 2004-03-18 Utilisation de pramipexol pour reduire l'absorption excessive d'aliments chez les enfants

Country Status (5)

Country Link
EP (1) EP1608367A1 (fr)
JP (1) JP2006520764A (fr)
CA (1) CA2519584A1 (fr)
DE (1) DE10312809A1 (fr)
WO (1) WO2004082680A1 (fr)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100168191A1 (en) * 2007-05-25 2010-07-01 Boehringer Ingelheim International Gmbh Pharmaceutical formulation comprising pramipexole
EP4245765A3 (fr) 2013-04-04 2024-03-20 Boehringer Ingelheim Vetmedica GmbH Traitement de troubles metaboliques chez des animaux equins
DK3082829T3 (da) 2013-12-17 2021-05-03 Boehringer Ingelheim Vetmedica Gmbh Sglt2-inhibitorer til behandlingen af metaboliske lidelser i kattedyr
LT3485890T (lt) 2014-01-23 2023-07-25 Boehringer Ingelheim Vetmedica Gmbh Sglt2 inhibitoriai, skirti šuninių gyvūnų medžiagų apykaitos sutrikimų gydymui
MX2016012705A (es) 2014-04-01 2016-12-16 Boehringer Ingelheim Vetmedica Gmbh Tratamiento de trastornos metabolicos en animales equinos.
EP3197429B1 (fr) * 2014-09-25 2024-05-22 Boehringer Ingelheim Vetmedica GmbH Polythérapie avec des inhibiteurs de sglt2 et des agonistes de la dopamine utilisée pour la prévention des troubles métaboliques chez des équidés
AU2016310535B2 (en) 2015-08-27 2021-08-19 Boehringer Ingelheim Vetmedica Gmbh Liquid pharmaceutical compositions comprising SGLT-2 inhibitors

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4855306A (en) * 1987-04-10 1989-08-08 Sandoz Ltd. Uses of dopamine receptor agonists
WO2001041763A1 (fr) * 1999-12-10 2001-06-14 University Of Cincinnati Traitement des troubles de l'accoutumance
US20010016582A1 (en) * 1997-04-28 2001-08-23 Anthony H. Cincotta Method and composition for the treatment of lipid and glucose metabolism disorders
WO2003028710A2 (fr) * 2001-09-28 2003-04-10 Boehringer Ingelheim Pharma Gmbh & Co. Kg Composes pour reduire la prise de nourriture excedentaire
WO2004010946A2 (fr) * 2002-07-29 2004-02-05 Gematria Sciences, Llc Traitement therapeutique pour le syndrome metabolique et les diabetes de type 2

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4855306A (en) * 1987-04-10 1989-08-08 Sandoz Ltd. Uses of dopamine receptor agonists
US20010016582A1 (en) * 1997-04-28 2001-08-23 Anthony H. Cincotta Method and composition for the treatment of lipid and glucose metabolism disorders
WO2001041763A1 (fr) * 1999-12-10 2001-06-14 University Of Cincinnati Traitement des troubles de l'accoutumance
WO2003028710A2 (fr) * 2001-09-28 2003-04-10 Boehringer Ingelheim Pharma Gmbh & Co. Kg Composes pour reduire la prise de nourriture excedentaire
WO2004010946A2 (fr) * 2002-07-29 2004-02-05 Gematria Sciences, Llc Traitement therapeutique pour le syndrome metabolique et les diabetes de type 2

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
FERNANDEZ-LOPEZ J-A ET AL: "PHARMACOLOGICAL APPROACHES FOR THE TREATMENT OF OBESITY", DRUGS, ADIS INTERNATIONAL LTD, AT, vol. 62, no. 6, 2002, pages 915 - 944, XP009001892, ISSN: 0012-6667 *
TERRY P ET AL: "DOPAMINE RECEPTOR SUBTYPE AGONISTS AND FEEDING BEHAVIOR", OBESITY RESEARCH, BATON ROUGE, LA,, US, vol. 3, no. SUPPL 4, November 1995 (1995-11-01), pages 515S - 523S, XP001062494, ISSN: 1071-7323 *
WILLNER P ET AL: "REVERSAL OF STRESS-INDUCED ANHEDONIA BY THE DOPAMINE RECEPTOR AGONIST, PRAMIPEXOLE", PSYCHOPHARMACOLOGY, SPRINGER VERLAG, BERLIN, DE, vol. 115, no. 4, August 1994 (1994-08-01), pages 454 - 462, XP009003272, ISSN: 0033-3158 *

Also Published As

Publication number Publication date
JP2006520764A (ja) 2006-09-14
DE10312809A1 (de) 2004-09-30
CA2519584A1 (fr) 2004-09-30
EP1608367A1 (fr) 2005-12-28

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