RU2221566C1

RU2221566C1 - Medicinal agent for opiomania treatment

Info

Publication number: RU2221566C1
Application number: RU2003104582/15A
Authority: RU
Inventors: И.В. Романов
Original assignee: Открытое Акционерное Общество "Международная Научно-Технологическая Корпорация"
Priority date: 2003-02-17
Filing date: 2003-02-17
Publication date: 2004-01-20

Abstract

FIELD: medicine, narcology, pharmacy. SUBSTANCE: invention relates to agent used for treatment of opiomania. Medicinal agent consists of antagonists of opiate receptors and pharmaceutically acceptable carrier. As antagonists of opiate receptors esters of N-substituted 14-hydroxy- morphinans are used; as a carrier natural oils, esters of carboxylic acid with 8-16 carbon atoms and low-molecular alcohols are used, sulfolanes, propylene carbonate, N,N- dimethylacetamide or their mixture are used taken in the definite ratio of components. Invention provides the development of highly effective low toxic an antirelapse agent with prolonged opioprotective effect being after a single subcutaneous or intramuscular injection. EFFECT: enhanced effectiveness of agent, valuable medicinal properties. 4 cl, 3 tbl

Description

Текст описания в факсимильном виде (см. графический материал)а Description text in facsimile form (see graphic material) a

Claims

1. A drug for the treatment of opium addiction based on opiate receptor blockers and a pharmaceutically acceptable carrier, characterized in that esters of N-substituted 14-hydroxymorphinans of the general formula are used as opiate receptor blockers

where R is alkyl, cyclopropylmethyl;

R ^{1 is} selected from the group consisting of acid residues: saturated or unsaturated carboxylic acids with 3-20 carbon atoms, C ₁₀ -C ₁₈ polyunsaturated carboxylic acids with 2-3 double bonds, alkyl-substituted cyclopropane-, dicyclopropane- and tricyclopropanecarboxylic acids, where alk - 8-14 carbon atoms, cycloaliphatic carboxylic acids selected from the group of cyclopentane, cyclohexane, cycloheptane, cyclooctane carboxylic acids or their alkyl derivatives, where alk is 2-3 carbon atoms, spiranic carboxylic acids and polycyclic carboxylic acids from conjugated ring selected from the group bitsiklogeksan-bicycloheptane-tritsiklooktankarbonovyh acids, alkyl-, alkoxy- or tsiklopropilmetilzameschennyh aromatic carboxylic acids, alkyl substituted carboxylic acids frame where alk - H, C ₁ -C ₈ heterocyclic acids and acids with mixed functions.

R ″ represents —H or is selected from the group of said acid residues equal to or different from R ’,

and as a carrier use natural oils, esters of carboxylic acids with 8-16 carbon atoms and low molecular weight alcohols, sulfolanes, propylene carbonate, N, N-dimethylacetamide or a mixture thereof, in the following ratio of components wt.%:

Esters of N-substituted 14-hydroxymorphinans 10 - 26

Media 74 - 90

2. The drug according to claim 1, characterized in that as natural oils use olive, peanut, sesame, stone seed oils, for example peach.

3. The drug according to claim 1, characterized in that as the esters of carboxylic acids with 8-16 carbon atoms and low molecular weight alcohols, ethyl oleate, ethyl stearate, isopropyl myristate, isopropyl decanoate, and ethyl lactate are used.

4. The drug according to claim 1, characterized in that tetramethylene sulfolane and its methyl substituted are used as sulfolanes.