Antiinflammatory, antiseptic, and regenerating suppositories

FIELD: pharmaceutical industry.

SUBSTANCE: rectal- and vaginal-administration suppositories contain 1,3-diethylbenzimidazolium triiodide as active principal, polyvinylpyrrolidone as solubilizer and stabilizer, and lipophilic base with specified proportions of components.

EFFECT: extended therapeutical activity and reduced occurrence of side effects.

4 cl, 2 ex

 

The invention relates to medicine, in particular to pharmacology, and can be used in the manufacture of rectal and vaginal suppositories.

For similar inventions made means the same destination - Indomethacin 50 Berlin-CHEMIE, candles, containing the active principle of antimicrobial action, and hydrophobic, lipophilic base (guide to drug Information for the consumer - Indomethacin 50 Berlin-CHEMIE”).

However, the known tool has anti-inflammatory effect that reduces its therapeutic activity.

The closest to the essential features of the composition of the same purposes are suppositories povidone-iodine (BETADINE), containing the active principle antimicrobial (antiseptic) action based on the connection active iodine and base (instruction for medical use of the drug BETADINE (BETADIN)).

The disadvantages of the prototype is irritating when it is used, low therapeutic activity, consisting only of antiseptic effects.

The invention, which defines its purpose is to expand the range of therapeutic activity and reduced side effects.

The technical result that can be achieved with the implementation of the invention, zakluchaetsa using active principle, which combines in its anti-inflammatory and antiseptic action and expressed regenerative properties, in addition, the active principle does not have a local irritant. The invention - suppositories anti-inflammatory, antiseptic and regenerative action, containing the active principle, polyvinylpyrrolidon as a solubilizer and stabilizer medical and molecular basis, is that as the active agent include 1,3-diethylbenzamide triode, and as a basis contain hydrophobic, lipophilic basis in the following ratio, wt%:

1,3-diethylbenzamide triode - 1,5-3

polyvinylpyrrolidone 6-12%

hydrophobic, lipophilic base the rest

Suppositories contain as hydrophobic, lipophilic bases cocoa butter.

Suppositories contain as hydrophobic, lipophilic bases tallow.

Suppositories contain solid fat assupol.

In the prior art unknown technical solution with the declared set of essential features of the independent claim, which confirms the conformity of the invention the condition of patentability - novelty. “

The claimed technical solution is characterized by the fact that its composition is administered triode 1,3-dieselben imidazole, the use of which allows to combine anti-inflammatory and antimicrobial properties without irritation with subsequent restoration to them of the affected tissues. The use of hydrophobic lipophilic bases with the specified active early can significantly extend its validity and to standardize the composition of suppositories and consequently their properties.

Justification of the selected limits of the concentrations of the components of the composition is the following. When the concentration of the active principle - triode 1,3-diethylbenzamide below 1.5 wt.% reduced therapeutic activity of the composition. When the concentration of triiodide 1,3-diethylbenzamide higher than 3.0 wt.% there is no enhancement of therapeutic effect of the composition, causing it wasted. The concentration of polyvinylpyrrolidone below 6 wt.% does not provide the necessary solubility of triiodide 1,3-diethylbenzamide in hydrophilic environment - the environment of the organism. When the concentration of the polyvinylpyrrolidone above 12 wt.% less emulsified in a hydrophobic, lipophilic basis.

Cocoa butter or tallow (massol) as the basis to 100 wt.%.

The essential distinguishing features of the independent claims of the claimed invention is not to follow the expert in the obvious way from the prior art, which confirms the line is their invention to condition patentability - “inventive step”.

Suppositories anti-inflammatory, antiseptic and regenerative action can be obtained with the implementation of this assignment as follows.

The method of producing suppositories anti-inflammatory, antiseptic and regeneration steps can be carried out with the implementation of the specified destination as follows. As an active principle obtained suppositories used triode 1,3-diethylbenzamide, which led to their qualitative and quantitative composition. Crystals triiodide 1,3-diethylbenzamide mechanically mixed with the white powder of low molecular weight polyvinylpyrrolidone medical (Pharmacopeia 42-1194-98), used as a solubilizer and stabilizer of the active principle. Received therapeutically active mixture is mechanically mixed with melted at a temperature of 40°With the Foundation, which use cocoa butter or tallow (massol). On therapeutic activity of the resulting suppositories are not affected by the fact that it will be taken as its basis cocoa butter or tallow (massol). The process of mixing therapeutically active compounds of triiodide 1,3-diethylbenzamide with polyvinylpyrrolidone with base is carried out at a temperature of from 40°because at lower the the temperature value will be hardening the basics and at a higher temperature, will be the destruction of the active principle. Then the mixture is poured into cooled to -20°split forms of 1.6 grams per well to obtain the desired consistency and set form of suppositories. After 3-5 min form dismantle and remove the finished candle with pharmacological activity. Rectal and vaginal suppositories can be made the same shape and the same size, including the same weight.

The method of producing suppositories anti-inflammatory, antiseptic and regenerative action is safe for individuals involved in the process. Examples obtain suppositories anti-inflammatory, antiseptic and regenerative and actions are based on necessary and sufficient qualitative and quantitative material features of the proposed suppositories anti-inflammatory, antiseptic and regenerative actions that formed the basis of the developed process procedures of its production and are subject to approval.

EXAMPLE 1.

Finely ground crystals of 1,3-diethylbenzamide of triiodide in the amount of 0.5 g mechanically mixed with 2.0 g of low-molecular polyvinylpyrrolidone medical (Pharmacopeia 42-1194-98), the resulting mixture is mesilat with 20 g melted at +40° With cocoa butter (GF X S.R. 474) and poured into cooled to -20°With split shape 1.6 g in the hole. After 3-5 min the form dismantle and remove the finished candle with pharmacological activity.

EXAMPLE 2.

Finely ground crystals of 1,3-diethylbenzamide of triiodide in the amount of 0.6 g mechanically mixed with 2.0 g of low-molecular polyvinylpyrrolidone medical (Pharmacopeia 42-1194-98). The resulting mixture was mixed with 20 g melted at +40°moscopole (ND 42-4223-95) and poured into cooled to -20°With split shape 1.6 g in the hole. After 3-5 min the form dismantle and remove the detachable form 1.6 g into the hole. After 3-5 min the form dismantle and remove the finished candle with pharmacological activity.

Describes the tools and methods by which it is possible to implement the anti-inflammatory composition, regeneration and antimicrobial action, with the implementation of the specified destination, confirm the compliance of the claimed invention to condition patentability of “industrial applicability”.

1. Suppositories anti-inflammatory, antiseptic and regenerative action, containing the active principle, the low-molecular polyvinylpyrrolidone health as a solubilizer and stabilizer and a base, characterized in that they contain as Akti the aqueous beginning 1,3-diethylbenzamide triode, and as bases contain hydrophobic, lipophilic basis in the following ratio, wt.%:

1,3-Diethylbenzamide triode 1,5-3

Polyvinylpyrrolidone 6-12

Hydrophobic, lipophilic base the Rest

2. Suppositories according to claim 1, characterized in that they contain as hydrophobic, lipophilic bases cocoa butter.

3. Suppositories according to claim 1, characterized in that they contain as hydrophobic, lipophilic bases tallow.

4. Suppositories according to claim 3, characterized in that it contains as a solid fat assupol.



 

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where W denotes the R1-A-C(R13or

where the ring system may be substituted by 1, 2 or 3 identical or different substituents R13and where L denotes C(R13and ml and m2 independently of one another denote 0, 1, 2, 3 or 4, and the sum of m l + m2 is 3 or 4; Y represents a carbonyl group; A represents a direct bond or a bivalent residue of a phenylene, A denotes a divalent (C1-C6)-alkalinity balance, and (C1-C6)-alkilinity the residue is unsubstituted or substituted by one or more identical or different residues from the series (WITH1-C8)-alkyl and (C3-C10-cycloalkyl-(C1-C6)-alkyl, F denotes R10CO., HCO, or R8O-CH2; R is H or (C1-C8)-alkyl, (C3-C12-cycloalkyl-(C1-C8)-alkyl or, if necessary, substituted (C6-C14)-aryl, and all residues R are independently from each other may be the continuously or repeatedly substituted by fluorine, or the rest of the X-NH-C(=NH) -R20, X - N, R2- N or (C1-C8) -alkyl; R3- N, (C1-C10) -alkyl, which optionally can be substituted one or more times by fluorine, optionally substituted (C6-C14)-aryl, optionally substituted heteroaryl, (C6-C12-bicycloalkyl, R11NH, COOR21, CONHR4or CONHR15; R4- (C1-C10)-alkyl, which is unsubstituted or substituted once or many times, equal or different residues from the series hydroxycarbonyl, aminocarbonyl, mono - or di-((C1-C10)-alkyl)-aminocarbonyl, (C1-C8-alkoxycarbonyl, R5, R6-CO, R5denotes optionally substituted (C6-C14)-aryl, R6denotes the residue of a natural or unnatural amino acid, R8- N or (C1-C10)-alkyl, and R8independently from each other may be the same or different, R10hydroxy, (C1-C10)-alkoxy, (C1-C8-alkylsulphonyl hydroxy-(C1-C6)-alkoxy, (C1-C8)-alkoxycarbonyl-(C1-C6)-alkoxy, amino, mono - or di-((C1-C10)-alkyl)-amino, or R8R8N-CO-(C1-C means R12a-O-CO-or R12a-S(OH)2, R12ameans (C1-C10)-alkyl, optionally substituted (C6-C14)-aryl, optionally substituted in the aryl residue (C6-C14)-aryl-(C1-C4)-alkyl, or R15, R13- N or (C1-C6)-alkyl, which may optionally be substituted one or more times by fluorine, R15means R16-(C1-C6)-alkyl, or R16; R16denotes a 6-membered to 24-membered bicyclic or tricyclic residue, R20denotes a direct bond or (C1-C6-alkylen; R21- N or (C1-C8)-alkyl, R30represents one of the residues R32(R)N-CO-N(R)-R31or R32(R)N-CS-N(R)-R31; R32-CO-N(R)-R31or R12AO-CO-N(R)-R31and R30cannot mean R32-CO-N(R)-R31,ifat the same time W denotes R1-A-C(R13), And denotes a direct bond and R1andR13- N, R31denotes the divalent residue of R33-R34-R35-R36and R36linked to the nitrogen atom in the ring of imidazolidine in formula 1, R32means (C1-C8)-alkyl, which, when neobloc substituted (C6-C14)-aryl, optionally substituted in the aryl (C6-C14)-aryl-(C1-C8)-alkyl or optionally substituted heteroaryl, R33denotes a direct bond, R34denotes a bivalent residue of a number (C1-C8-alkylene, optionally substituted (C6-C14)-Allen; R35denotes a direct bond or a bivalent residue (C1-C8)-alkylene; R36denotes a direct bond, e and h represent independently from each other 0 or 1; in all their stereoisomeric forms and their mixtures in all ratios, and their physiologically acceptable salts, process for the preparation of compounds I; pharmaceutical drug that has the ability to inhibit the adhesion and/or migration of leucocytes and/or VLA-4 receptor

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EFFECT: higher efficiency.

10 cl, 6 ex

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