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EP0000015B1 - Médicament pour le traitement des dépressions - Google Patents

Médicament pour le traitement des dépressions Download PDF

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Publication number
EP0000015B1
EP0000015B1 EP78100027A EP78100027A EP0000015B1 EP 0000015 B1 EP0000015 B1 EP 0000015B1 EP 78100027 A EP78100027 A EP 78100027A EP 78100027 A EP78100027 A EP 78100027A EP 0000015 B1 EP0000015 B1 EP 0000015B1
Authority
EP
European Patent Office
Prior art keywords
acid
tablets
medicament
treatment
depressions
Prior art date
Legal status (The legal status 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 status listed.)
Expired
Application number
EP78100027A
Other languages
German (de)
English (en)
Other versions
EP0000015A1 (fr
Inventor
Karl Dr. Schmitt
Irmgard Dr. Hoffmann
Werner Dr. Fülberth
Willi Dr. Stammberger
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Hoechst AG
Original Assignee
Hoechst AG
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 Hoechst AG filed Critical Hoechst AG
Publication of EP0000015A1 publication Critical patent/EP0000015A1/fr
Application granted granted Critical
Publication of EP0000015B1 publication Critical patent/EP0000015B1/fr
Expired legal-status Critical Current

Links

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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/26—Psychostimulants, e.g. nicotine, cocaine

Definitions

  • the invention relates to a medicament for the treatment of depression, which contains a compound of the formula I or their acids (active ingredient A) and 7-chloro-1-methyl-5-phenyl-1 H-1,5-benzodiazepine-2,4- (3H, 5H) -dione (active ingredient B).
  • the compound used as active ingredient A is known from DBP 1 670 694 and bears the name "Nomifensin” (INN).
  • Nomifensin is used in the form of hydrogen maleate as a medicine for the therapy of depressive conditions. It is the first powerful antidepressant that is not derived from a tricyclic ring system. In contrast to the known tricyclic antidepressants, nomifensin is free from serious side effects, see e.g. "Drug Research", 23, (1973), 45-50.
  • the active ingredient A is a basic compound, which in most cases is used advantageously in the form of a physiologically acceptable salt.
  • Acids suitable for salts are e.g. Hydrochloric, bromic and hydroiodic acid, phosphoric acid, sulfuric acid, amidosulfonic acid, methylsulfuric acid, nitric acid, formic acid, acetic acid, propionic acid, succinic acid, tartaric acid, lactic acid, malonic acid, fumaric acid, citric acid, malic acid, mucic acid, benzoic acid, naphthalic acid, acetic acid, acetic acid, acetonic acid, acetic acid 1,5 - disulfonic acid, ascorbic acid, hydroxyethanesulfonic acid, benzenesulfonic acid, or synthetic resins containing acidic groups.
  • the active ingredient B is a neutral compound that is sparingly soluble in water. Ciobazam is therefore advantageously used in micronized form.
  • the active ingredient combination according to the invention can be used in the customary use forms, such as tablets, powders, capsules, suppositories or coated tablets. Capsules, tablets and coated tablets are preferably used.
  • the usual pharmaceutical auxiliaries for example inert diluents and binders such as milk sugar, microcrystalline cellulose, calcium carbonate, di- and tricalcium phosphate, polyethylene glycol 4,000-6,000, gelatin, starch gum, disintegrants such as starches, ultraamylopectin, cellulose and cellulose derivatives, aerosil, lubricants such as Talc, magnesium stearate, calcium stearate, stearic acid added.
  • Tablets which consist of several layers can also be used as tablets. They are produced, for example, by mixing the active ingredients with the pharmaceutical auxiliaries using customary pharmaceutical manufacturing methods.
  • Dragees can be made, for example, by coating cores with agents commonly used in coated tablets, e.g. Cane sugar, gelatin, gum arabic, talc, calcium carbonate, cera alba, cera carnauba, aerosil can be obtained.
  • Capsules are also produced in a manner known per se, inert carriers such as corn starch, talc, Aerosil being mixed and preferably gelatin capsules being used.
  • the combination according to the invention can also be used in the form of suppositories, the usual carriers such as triglycerides of saturated fatty acids and hydrogenated vegetable fats being added.
  • the preferred form of administration for the antidepressant pharmaceutical preparation according to the invention is oral administration.
  • the active ingredient A comes into consideration in a dose of 5 to 50 mg per administration unit.
  • Clobazam, active ingredient B uses 2 to 25 mg. In cases that require a higher dosage, a corresponding multiple of the above doses can be administered. Examples:
  • micronized active ingredients 1. and 2. are with the supplements 3.-7. homogeneously mixed.
  • the mixture is filled into hard gelatin capsules in a known manner.
  • the tablet mixture of substances 1-9. is granulated and compressed into biconvex tablets.
  • the tablets are coated with one of the usual film varnishes.
  • the granules made for the production of tablets are pressed into coated tablets.
  • the coated tablets are coated in a known manner.

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)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Claims (1)

1. Médicament pour le traitement des dépressions, caractérisé en ce qu'il contient un composé de formule 1
Figure imgb0005
ou ses sels avec des acides (substance active A) et la 7-chloro-1-méthyl-5-phényl-1 H-1,5-benzodiazépine-2,4-(3H, 5H)-dione (substance active B).
EP78100027A 1977-06-01 1978-06-01 Médicament pour le traitement des dépressions Expired EP0000015B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE2724683 1977-06-01
DE19772724683 DE2724683A1 (de) 1977-06-01 1977-06-01 Antidepressiv wirksame pharmazeutische praeparate

Publications (2)

Publication Number Publication Date
EP0000015A1 EP0000015A1 (fr) 1978-12-20
EP0000015B1 true EP0000015B1 (fr) 1980-07-23

Family

ID=6010390

Family Applications (1)

Application Number Title Priority Date Filing Date
EP78100027A Expired EP0000015B1 (fr) 1977-06-01 1978-06-01 Médicament pour le traitement des dépressions

Country Status (11)

Country Link
US (1) US4189478A (fr)
EP (1) EP0000015B1 (fr)
JP (1) JPS545045A (fr)
AT (1) AT362491B (fr)
AU (1) AU517779B2 (fr)
CA (1) CA1102242A (fr)
DE (2) DE2724683A1 (fr)
DK (1) DK242078A (fr)
IL (1) IL54809A (fr)
IT (1) IT1094898B (fr)
ZA (1) ZA783123B (fr)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS6153404A (ja) * 1984-08-23 1986-03-17 Toshiba Corp 蒸気タ−ビンのノズルダイアフラム製造方法
JPS6355307A (ja) * 1986-07-16 1988-03-09 Kawasaki Heavy Ind Ltd タ−ビンダイヤフラムの製造方法
BG45572A1 (en) * 1986-10-23 1989-07-14 Druzhestven N Izsledovatelski Antiulcer means
US20180344648A1 (en) * 2015-11-30 2018-12-06 Piramal Enterprises Limited Clobazam tablet formulation and process for its preparation
TR2023013455A1 (tr) * 2023-10-20 2025-04-21 Bi̇ocure Ki̇mya İlaç Arge Danişmanlik Sanayi̇ Ve Ti̇caret Anoni̇m Şi̇rketi̇ Kapsül formunda klobazam formülasyonu

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1670694B2 (de) * 1966-05-05 1976-07-22 Hoechst Ag, 6000 Frankfurt Verfahren zur herstellung von tetrahydroisochinolinen

Also Published As

Publication number Publication date
DE2724683A1 (de) 1978-12-14
EP0000015A1 (fr) 1978-12-20
IT1094898B (it) 1985-08-10
ATA395178A (de) 1980-10-15
CA1102242A (fr) 1981-06-02
DE2860033D1 (en) 1980-11-13
IT7823995A0 (it) 1978-05-30
US4189478A (en) 1980-02-19
JPS545045A (en) 1979-01-16
AU517779B2 (en) 1981-08-27
IL54809A (en) 1981-10-30
DK242078A (da) 1978-12-02
AU3670478A (en) 1979-12-06
ZA783123B (en) 1979-06-27
AT362491B (de) 1981-05-25

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