Interferon inductor suppositories

FIELD: medicine; pharmacology.

SUBSTANCE: proposed suppository along with consistent base (lipophilic, hydrophilic or diphilic) and stabiliser selected from chlorhexidine bigluconate, nypagine and sodium carboxymethyl cellulose as natural endogenous interferon inductor, is supplied with sodium salt complex of alpha-helical and double-helical RNA from killer yeast Saccharomyces cerevisiae. Quantitative amount of specified ingredients per suppository of mass 1.0 g is: sodium salt complex of alpha-helical and double-helical RNA from killer yeast Saccharomyces cerevisiae - 50-150 mcg; stabiliser - 10-30 mcg; additives - others.

EFFECT: extended range of therapeutic antiviral agents and reduced toxicity with maintained efficiency.

6 cl, 4 ex, 3 tbl

 

The invention relates to medicine and pharmacology, specifically to the development of antiviral drugs in the form of suppositories.

Effective means for the prevention and treatment of viral infections are inducers of interferon stimulating in humans and animals of endogenous interferon. Thus we need to search for tools that not only have the interferon-inducing activity, but can be simple to manufacture and use. Promising in this respect are drugs that do not require parenteral or injection, in particular suppositories. In addition, access to this kind of dosage form would extend the possibility of therapeutic use of interferon inductors due whiter clear dosed release of the active principle in excluding unwanted side effects are irritation, inflammation, etc. it Should also be noted that the refusal injection method of administration of antiviral drugs eliminates the risk of infection by hepatitis b and C and HIV infection; in addition, the introduction of antiviral compositions in the form of candles provides you with a quick intake of the drug in the blood and organs, rich macrobiotically and lymphoid elements.

The most active inductors, interfere is and include synthetic polyribonucleotide and double-stranded RNA (dsRNA) of natural origin [1].

Known use as an inducer of interferon datausage complex Polideportivo (poly-EN) and polyribosomes (poly rA) acids, which is called "Poludan" is used in viral diseases of the eye [2]. However, the preparations of interferon inductors on the basis of synthetic polyribonucleotides along with high efficiency have toxicity [3] and show mutagenic activity [4].

On the Russian pharmaceutical market is the ointment "Laifan" (made in Latvia) - they are polymer interferon inducer of natural origin, representing double-stranded RNA phage f2 [5]. The disadvantage of the drug is that its active basis is phage nucleic acid that represents a potential danger for a man in connection with the discovery of mass contamination by phage virus vaccines.

Interferon inducing drugs on the basis of double-stranded RNA is made in the form of a suppository, it is known very little. So the American company Merck Co. Inc. patented ointment, which is used to treat herpes infections of the eye and contains synthetic interferon inducer poly - rI - poly-rC, and the media: simple or complex esters of cellulose, polyvinyl alcohol, polyvinylpyrrolidone, carboxyvinyl esters and polyethylene glycol [6]. In this geezerette described vaginal and rectal suppositories based on the specified polyribonucleotides composition, which are of normal size and shape and contain from about 2.5 to 250 mg of interferon inducer on 1 g of the composition.

The closest drug interferon inducer is a dosage form datausage complex poly-EN* poly-rA* (200-250 g), made in the form of rectal suppositories, which in addition to interferon inducer contains more hyaluronic acid (10-20 mg) as immunomodulator and vitamins C and E (30-40 mg) in a mass ratio of 1:1 as antioxidants in the basis [7, prototype]. The disadvantage of the drug is that as interferon inducer is used dutrey complex poly-EN* - poly-rA*, which is of synthetic origin and, as mentioned above, exhibits the toxicity and mutagenic activity.

An object of the invention is to expand the range of antiviral drugs are inducers of nonspecific resistance of the organism through the creation of a dosage form of interferon inducer - suppository-based dsRNA of natural origin, with low toxicity.

The problem is solved by introducing into the composition of a suppository together with the grease-forming the basis (lipophilic, hydrophilic or difiles) and stabilizer as interferon inducer natural origin of the complex sodium salts one is - and double-stranded RNA of the yeast Saccharomyces cerevisiae.

Currently known drug interferon inducer for external use (ointment), with pronounced antiviral activity of the biologically active part of which is a complex of sodium salts of single - and double-stranded RNA killer yeast Saccharomyces cerevisiae [8]. This drug has a high efficiency, low toxicity and good tolerability.

We propose in this development suppository include as an inducer of interferon natural origin complex sodium salts of single - and double-stranded RNA killer yeast Saccharomyces cerevisiae, stabilizer and auxiliary substances. The quantitative content of the specified ingredients in the suppository mass of 1.0 g is:

Complex sodium salts of single - and double-stranded RNA
killer yeast Saccharomyces cerevisiae50-150 mcg
Stabilizer10-30 mcg
Excipientsthe rest of it.

As a stabilizer - bacteriostatic (stabilizer microbiological purity) offer suppository on the basis of a complex of sodium salts of single - and double-stranded RNA of the yeast Saccharomyces cerevisiae can contain nipagin or chlorhexidine biglycan the t and/or a derivative methylcellulose (Na).

Suppositories as auxiliary substances contain fat basis, including solid confectionery fat or cooking oil and emulsifier T-2, surface-active substances (SAS) tween - 80, which is also a high-polymeric solubilizer DS RNA; however, the base may further comprise cocoa butter to 0.15 g per 1 g of the mixture and paraffin to 0.10 g and the content of the surfactant tween - 80 is 0.03 g per 1 g of the mixture.

As a grease-forming bases can be used devilina base containing oxides, solid edible fat and surfactant tween - 80, or hydrophilic base containing oxides and glycerine (in the amount of 0.05 g per 1 g of the mixture).

As an antioxidant, the tool can optionally contain vitamin E in the amount of 0.0001-0.0005 g in 1 g of the mixture.

Grease-forming composition is prepared with the use of auxiliary substances permitted for medical use.

Additionally, the tool may further comprise dimethyl sulfoxide to increase the permeability of the mucous membranes in the amount of 0.0005-0.0025 g in 1 g of the mixture.

The combination of interferon inducer in the form of a complex of sodium salts of single - and double-stranded RNA of natural origin (of killer yeast Saccharomyces cerevisiae) with stabilizers - bacteriostatic (stabilizers microbiological purity) and antioxi what ants in suppozitornyj grease-forming the basis allows you to expand the range of therapeutic antiviral drugs - inductors nonspecific resistance of the organism with reduced toxicity, while maintaining efficiency.

We studied the stability of the physical properties and activity of the proposed suppositories inducers of interferon. Conducted pre-clinical trials on laboratory animals. Investigated the toxicity, progenote, local irritating action, pharmacokinetics, phagocytophilia activity suppositories on the model of genital herpes Guinea pigs, as well as interface-noninducible activity of the drug.

The results of the research on the model of laboratory animals show that the preparation of suppository is effective, harmless, low toxicity, has no pyrogenalum and locally irritant effect.

New dosage form is a suppository of interferon inducer used in clinical practice in the treatment of chlamydia. Shows his expressed interferon-inducing activity at effective healing properties.

For a better understanding of the invention the following specific examples of its implementation.

Example 1. Getting lipophilic suppositories with grease-forming.

To obtain suppositories weighing 1 g of the molten base - cooking oil, paraffin, cocoa butter and emulsifier T-2 injected surfactant tween-80 as a solubilizer in scopolamine DS RNA, the sulfoxide to enhance the permeability of the mucous membranes and chlorhexidine digluconate as a stabilizer microbiological purity. Then, the resulting mixture was added a solution of complex sodium salts of single - and double-stranded RNA in Saccharomyces cerevisiae. The mixture is then poured into the form of suppositories, cooled and Packed.

These components take the following ratio of 1 g of a mixture of:

Complex sodium salts of single - and double-stranded RNA50-150 mcg
Cocoa butter0-15 mg
Paraffin10 mg
Tween-803 mg
Purified water5 mg
Emulsifier T-23 mg
The sulfoxide100 mcg
Chlorhexidine digluconate250 mcg
Cooking fatrest

Example 2. Getting suppositories with hydrophilic grease-forming.

To obtain suppositories weighing 1 g in grease-forming the basis of the melt of oxides 1500 and 400 injected glycerin, dimethylsulfoxide to enhance the permeability of the mucous membranes and chlorhexidine digluconate as a stabilizer microbiological Chi is toty. In the prepared base, introduce a solution of the complex sodium salts, single - and double-stranded RNA in Saccharomyces cerevisiae. The mixture is then poured into the form of suppositories, cooled and Packed.

These components take the following ratio of 1 g of a mixture of:

Complex sodium salts of single - and double-stranded RNA50-150 mcg
Glycerin5 mg
Purified water5 mg
The polyethylene oxide 150020 mg
Chlorhexidine digluconate250 mcg
The polyethylene oxide 400rest

Example 3. Getting suppositories with difiles grease-forming.

To obtain suppositories weighing 1 g of molten hydrophilic base melt of oxides 1500 and 400, add a solution of the complex of sodium salts of single - and double-stranded RNA in Saccharomyces cerevisiae. Then injected molten hydrophobic base (TKJ), surfactant tween-80, emulsifier T-2, dimethylsulfoxide, antioxidant E-2 and nipagin as a stabilizer microbiological purity (bacteriostatic). The mixture is then poured into the form of suppositories, cooled and Packed.

These components take the following ratio of 1 g of a mixture of:

Complex sodium salts of single - and double-stranded RNA50-150 mcg
TKJ240 mg
PEG 400350 mg
PEG 150025 mg
Tween-804 mg
Emulsifier T-22 mg
The sulfoxide100 mcg
Nipagin10 mg
Antioxidant E-210-20 mcg
Purified waterRest

The composition of suppositories with difiles grease-forming base may be somewhat different.

To obtain suppositories weighing 1 g of the hydrophilic base solution Na add a solution of the complex of sodium salts of single - and double-stranded RNA in Saccharomyces cerevisiae. Then enter the glycerol and the molten hydrophobic base (TKJ), emulsifier T-2, nipagin as a stabilizer microbiological purity (bacteriostatic). The mixture mix until homogenous at a temperature of 37°, poured in the form of suppositories, cooled and Packed.

These components take the following ratio of 1 g of a mixture of:

Complex sodium salts of single - and double-stranded RNA50-150 mcg
Na 300 mcg
Glycerin150 mcg
Emulsifier T-23 mg
Nipagin10 mg
TKJ240 mg
Purified waterRest

Example 4. Determination of biological activity of suppositories on the basis of a complex of sodium salts of single - and double-stranded RNA.

It is known that the herpes viruses are able to inhibit the functional activity of macrophages and interferon synthesis, which affects the inability to eliminate the virus from the body. It is obvious that the selection of promising Antiherpes virus effect funds should assess their effect on phagocytes.

The biological activity of the inventive suppositories appreciate phagocytic activity in the monolayer culture of peritoneal macrophages of mice ICR males. Samples of suppositories prepared according to examples 1-3, i.e. with different grease-forming bases and auxiliary substances injected mice rectally at a dose of 70 mg/mouse. In the control groups use the suppositories basis, which is injected in the same way.

The study of the phagocytosis of macrophages spend 24 hours after administration of suppositories.

Macrophages isolated from the peritoneal cavity of mice by leaching environment Hanks with HepB what renom (5 per act. per ml of medium). Cultivation and all subsequent operations are performed in an environment Hanks with 3% bovine serum (red). Suspension of macrophages (1×106in ml) were seeded on cover glass placed in tube diameter 35 mm

Incubation is carried out 1 h at 37 ° °C. To study the phagocytosis of the monolayer washed from reprecipitate cells and as the object of phagocytosis put 20 μl of the suspension opsonizing sheep red blood cells (EB) rate of 20 erythrocytes per macrophage. A monolayer of macrophages continue to incubate for 45 min, washed, dried, and prepared for microscopic analysis.

Assessment of phagocytosis is carried out by conversion of peritoneal macrophages that engulfed the sheep erythrocytes.

Phagocytic activity (F) estimate of the total number of macrophages. The significance of differences (P) data obtained in the experiment and the control, assessed using student's criterion for counting 250 cells on the monolayer. The percentage of stimulation determine the relative performance of the experimental groups of animals to control by the formula:

The results of these experiments are presented in Table 1.

Data are presented for suppositories prepared according to example 1.

Table 1.
Phagocytosis-stimulating activity suppositories
Conditions of experiencePhagocytosis indices
Drug

Series
Time studiesFA (%)Phagocytophilia activityThe significance of differences (P)
Suppositories with 020900

The basis of suppositories
24 hours22,3±3,2 15,8±1,8141,1%0,05
Suppositories with 010301

The basis of suppositories
24 hours27,8±1,8 was 12.75±2,6218,0%0,05
Suppositories with 091100

The basis of suppositories
24 hours27,1±2,2 11.3±0,9239,8%0,05

The study shows that patent suppositories have a pronounced ability to activate phagocytosis. This indicates that therapeutic Antiherpes virus effect of the drug.

Example 4. Study of interferon-inducing activity of suppositories on animal model.

The level of interferon-inducing activity of suppositories containing complex of sodium salts of single - and double-stranded RNA in a lipophilic base, assessed in the serum of mice received a day after intrabasin the high injection suppositories animals (experienced) or base (control), as well as in the intact group of animals. Blood samples with a volume of 0.8-1.0 ml collected in a sterile test tube; serum obtained by centrifugation at 2,5 Tyson/min, transferred to 0.3-0.5 ml in sterile tubes and frozen at - 20°until analysis.

The titer of interferon determine micromethods in 96-well polystyrene tablets with a flat bottom. About the presence of interferon judged by the inhibition of the cytopathic action of the test virus in cell culture murine fibroblast line L-929. As the test virus was used virus encephalomyocarditis (EMC) strain "Columbia" in a dose of 100 JRS50to 0.1 ml For the serum titer of interferon take the value of the highest dilution at which there is a protection of 50% cell culture from 100 JRS50the test virus. The data obtained are presented in Table 2 show that the proposed remedies suppositories have pronounced interferon-inducing activity.

Table 2
Interferon-inducing activity of suppositories on animal model
The group of animals

The preparation of suppository
No. of seraThe titer of interferon
Individual valueM±m
1. Control vividly fair.1

2
<1:10

1:10
Lipophilic base.31:10
4<1:10<1:10
5<1:10
6<1:10
2. Experimental animals71:10
Therapeutic candles81:10
91:80
101:2023,3±11,5
111:10
121:10
3. Intact animals13<1:10
14<1:10
15<1:10<1:10
16<1:10
17<1:10
Ȋ 18<1:10

Example 5. The study of induction of interferon using suppositories in clinical practice.

Candles, obtained according to Example 1, the hospital treated patients (men) about chlamydia. The course of treatment was 10 candles 1 suppository daily in the morning or in the evening. The control titer of interferon conducted in the serum of patients before treatment, while taking suppositories for 2, 3, 5 day and 10 days after completing therapy. Interferon-inducing activity was determined by titration of serum samples obtained from patients in 96-well tablets in transplantable cell line lung of a human embryo L-68 by a standard method in the environment of Needle-MEM with the addition of 7% cattle serum. The obtained data are presented in Table 3.

Table 3.
Interferon-inducing activity of suppositories
PatientThe titer of interferon in the serum before treatmentThe titer of interferon in the serum during treatmentThe titer of interferon in the serum after treatment
Patient K., 311:81:321:2
Patient Including, 571:21: 161:2
Patient B., aged 261:21:161:4

Data from laboratory studies suggest that rectal candles actively induce endogenous interferon in vivo, providing a systemic effect. It is shown that in response to treatment (course of 10 candles) the level of serum interferon increases after 48 hours on average 2-4 times.

All the patients showed a significant decrease or complete disappearance of inflammatory processes.

Thus, the obtained data showed a high efficacy of the interferon inducer on the basis of a complex of sodium salts of single - and double-stranded RNA of natural origin in the form of candles.

LITERATURE

1. Pierson, Vmigunov in the book. "Interferon inducers", M, 1982, p.7-18.

2. Medmaravis in the book. "Medicinal product", M.: Medicine, 1988, Vol.2, str-387.

3. Whimsical, Ichneumoninae // Acute toxicity and cumulative properties polyribonucleotide complexes of poly I: poly C and poly G: poly C // Pharmacol. toxicol. // 1981, No. 3, str-358.

4. Ugulava // study of the mutagenic activity of synthetic inducers of interferon on laboratory mice // Matters. Virology // 1982, No. 5, SCR-543.

5. Pierson, Npia, Subtitulado is a // Antivirals (directory) // St. Petersburg, 1993, UDC 616.988-085.281.8, p.68-70.

6. U.S. patent No. 4283393, CL AC 31/70, publ. 11.08.1981,

7. RF patent №2162687, CL AC 9/02, publ. BI # 4, 2001

8. RF patent №2123339, CL AC 31/70, publ. BI No. 35 in 1998

1. The suppository-based interferon inducer, characterized in that it contains as an interferon inducer complex sodium salts of single double-stranded RNA of natural origin of killer yeast Saccharomyces cerevisiae, the stabilizer is selected from the group chlorhexidine digluconate, nipagin, sodium carboxymethylcellulose, and as auxiliary substances, hydrophilic or lipophilic, or dipilou basis in the following ratio of ingredients on 1 suppository mass of 1.0 g:

Complex sodium salts of single - and double-stranded RNA killer yeast Saccharomyces cerevisiae50-150 mcg
Stabilizer selected from the group chlorhexidine digluconate, nipagin, sodium carboxymethylcellulose10-3 0 mcg
ExcipientsRest

2. The suppository according to claim 1, characterized in that as auxiliary substances it contains fat basis, including solid confectionery fat or cooking oil and emulsifier T-2, and surface-active substance (surfactant) tween - 80, and the basis of mo is no further comprise cocoa butter to 0.15 g per 1 g of a mixture of paraffin and 0.10 g, and the content of the emulsifier T-2 and the surfactant tween-80 is 0.03 g per 1 g of the mixture.

3. The suppository according to claim 1, characterized in that it contains a hydrophilic base comprising oxides (1500 and 400) and glycerol in the amount of 0.05 g per 1 g of the mixture.

4. The suppository according to claim 1, characterized in that it contains dipilou basis, including oxides (1500 and 400), solid edible fat and emulsifier T-2 and the surfactant tween-80.

5. The suppository according to any one of claims 1 to 4, characterized in that it further contains as an antioxidant vitamin E in the amount of 0.0001-0.0005 g in 1 g of the mixture.

6. The suppository according to any one of claims 1 to 4, characterized in that it further comprises dimethyl sulfoxide to increase the permeability of the mucous membranes in the amount of 0.0005-0.0025 g in 1 g of the mixture.



 

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12 cl, 3 tbl, 6 dwg, 4 ex

FIELD: medicine, pharmacy.

SUBSTANCE: invention describes a pharmaceutical composition for its using in treatment of symptoms of catarrhal diseases and influenza, or as an analgesic drug. Composition represents a single dose as an aqueous medicinal formula of the total volume less 100 ml and containing paracetamol and a masking component that attenuates or masks its bitter taste and consisting of at least two components chosen from the following groups (i)-(vi): (i) magnesium chloride, gluconate, hydroxide, carbonate or hydrocarbonate, and/or a mixture of magnesium chloride and magnesium sulfate in the molar ratio from 0.0001:1 to 0.01:1 measured as the ratio magnesium atoms : paracetamol; (ii) gingerin and/or ginger oil in the weight ratio from 1:20000 to 1:10000 with respect to paracetamol; (iii) sweetening agent of the sustained onset effect and prolonged effect chosen from taumatin, neohesperidin DC and/or glycyrrhizin taken in the weight ratio from 1:20000 to 1:100 with respect to paracetamol; (iv) soluble starch taken in the weight ratio from 1:10 to 1:1 with respect to paracetamol; (v) sucrose ester having value of hydrophilic-lipophilic balance (HLB) above 10 and taken in the weight ratio from 1:10 to 2:1 with respect to paracetamol, and (vi) glycine taken in the molar ratio from 1:4 to 2:1 with respect to paracetamol. Proposed composition provides effective taste masking or bitterness of paracetamol being especially in liquid preparations containing less 100 ml of water, and in using the combination of different masking agents also.

EFFECT: improved and valuable properties of composition.

10 cl, 3 tbl, 3 ex

FIELD: medicine.

SUBSTANCE: invention relates to system for controlling oral or anal administering of biological component and method for prolonged bacteria administering into living body. Claimed system contains hydrophilic agent and bacterium; or viscosity modifier, hydrophilic agent and bacterium; or viscosity modifier, electrolytic agent, hydrophilic agent and bacterium. Hydrophilic agent provides viscosity from 4000 mPa to 15000 mPa and is selected from at least one group comprising: a) gum, such as tragacant gum, locust gum, acacia gum, guar gum, xantan gum, etc.; b) polysaccharide such as pectin and maltodextrin; c) cellulose derivative such as methylcellulose, carboxymethyl cellulose, methylcellulose hydroxyethyl, methylcellulose hydroxypropyl, etc.; d) polypeptide such as gelatin, collagen, casein of heterogeneous protein mixture. Claimed systems are obtained by component drying, blending and pressing. Bacterium/hydrophilic agent ratio is from 1:0.33 to 1:1.33.

EFFECT: system for controlling administering of biological component in desired regions of gastrointestinal tract.

32 cl, 13 ex, 13 tbl, 13 dwg

FIELD: medicine; pharmacology.

SUBSTANCE: agent contains antibacterial substance of fluoroquinolones, hydrophilic base and optionally at least one adjuvant. As hydrophilic base agent contains silicone glycerohydrogel of composition Si(C3H7O3)4 · xC3H8O3 · yH2O, where 3 ≤ x ≤ 10, 20 ≤ y ≤40. As antibacterial substance of fluoroquinolones agent contains perphloxacyn, ophloxacyn, cyprophloxacyn, norphloxacyn, lomephloxacyn, moxyphloxacyn, csparphloxacyn or enoxacyn. Agent can contain as adjuvant chlorhexidine bigluconate, lydocaine hydrochloride, sea-buckthorn oil, brier oil or mixture. New agent for treatment of suppurative-inflammatory skin and soft tissues diseases including decubitus ulcers, burns, trophic ulcer, has high antibacterial effect due to wide antibacterial action (fluoroquinolones) and high transcutaneous and anti-edematous activity (silicone glycerohydrogel), and do not carry negative by-effects.

EFFECT: agent is stable, easy for keeping and well wipe-off.

6 cl, 5 dwg, 3 tbl, 6 ex

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