Pharamceutical agent for treatment of viral and different infections

FIELD: medicine; pharmacology.

SUBSTANCE: invention relates to chemical-pharmaceutical industry and applies to pharmaceutical formulations, which contain human recombinant alfa-2 interferon used to prevent and treat the viral and different infections with immunodeficiency. The pharmaceutical agent, applied for patent, is made as rectal suppository, which contains the human recombinant alfa-2 interferon, antioxidant complex, as well as a substance that promotes the expression of interferon receptors at mononuclear leucocytes of peripheral blood and hepatocytes, and the substance, which promotes complete release of interferon from suppository and its absorption per rectum. The pharmaceutical agent can also contain hepatoprotector and additional antioxidant.

EFFECT: invented pharmaceutical agent is highly efficient in interferon therapy of different viral diseases.

6 cl, 9 ex

 

The invention relates to medicine and the pharmaceutical industry and relates to dosage forms containing human recombinant interferon alpha 2, used for the prevention and treatment of viral and other diseases occurring on the background of immunodeficiency.

Known from the patent of the Russian Federation No. 2201212, class a 61 K 9/00, 2003, suppository "Generon containing natural or recombinant interferon interferon α-, βand/or γ-types and taurine (taufon) and auxiliary substances at a given ratio of ingredients per 1 g suppository mass 1-6,

Known from the patent of the Russian Federation No. 2073522, class a 61 K 38/21, 39/395, 1997, drug antiviral action Kipferon used in medicine for the treatment and prevention of viral diseases, containing human interferon and a synergist, which is known immunoglobulin preparation, in particular complex immunoglobulin preparation containing a mixture of classes of human immunoglobulins M and g Known drug also includes pharmaceutically acceptable additives, as a human interferon it contains recombinant alpha-or beta-, or gamma-interferon person. The combination of human interferon with immunoglobuline person causes the manifestation of a known drug synergy the definition, i.e. sverhsummarny antivirus action. Applied drug in pill form, powder, ointments and candles.

It is known from the patent of the Russian Federation No. 2187332, class AC 38/21, 1999, the drug containing alpha-or beta-, or gamma-interferon, acyclovir, stabilizer biological, physico-chemical properties and/or resistance to microbial contamination and pharmaceutically acceptable additives. The tool may further comprise immunomodulator, vitamins, anti-inflammatory medication, anti-microbial, and/or Antiprotozoal and/or antifungal agent, antioxidant, local analiziruyuschei tool ribavirin. The technical result is an expansion of the means protivovirusnogo, antibacterial, anti-inflammatory action.

Known from the patent of the Russian Federation No. 2024253, class AC 9/02, 1994, drug Viferon containing genetically engineered recombinant interferon Alfa-2, the antioxidants ascorbic acid (vitamin C) and α-tocopherol, a filler in certain specified proportions of the components. It is shown that the specific antiviral activity of interferon increases significantly in the presence of antioxidants. In addition, in the presence of antioxidants side effects, typical for products containing high doses of interferon, significantly attenuated or not p is ablauts at all. Applied product in the form of rectal suppositories.

This medicine is accepted as the nearest equivalent.

Despite the diversity of interferon preparations for injection, or for rectal application, there are types of viral diseases, in particular hepatitis b, C and D, where the efficiency interferonoterapii low regardless of the route of administration of interferon.

Also identified low efficiency interferonoterapii with adenoviral infections and some types of flu virus.

Thus, the main disadvantage of all interferonsource drugs, including drug, taken as the closest analogue, you can call them low efficiency in the treatment of some viral diseases

Technical problem on which this invention is directed, is the creation of complex dosage forms for rectal use, containing human recombinant interferon Alfa 2 and substances that increase efficiency interferonoterapii various diseases by increasing the bioavailability of interferon in a rectal and also by increasing the specific antiviral activity of interferon by the presence of substances synergists, to broaden the range of action of the drug Priego impact on the various links in the defensive reactions of the organism.

Thus, based on the technical problem of the proposed medicinal product must possess antiviral and immunomodulatory activity, due to member interferon, and to contain in its composition of matter that enhances the expression of receptors for interferon on the surface of peripheral blood mononuclear cells and hepatocyte cells of the liver tissue). In addition, the pharmaceutical composition may also contain hepatoprotector, the complex of antioxidants and excipients that enhance the release of interferon from rectal dosage forms, and substances that increase the absorption of interferon through the epithelium of the rectum.

The technical result, which is the present invention is to increase the antiviral and immunomodulatory effect of interferon, its bioavailability of rectal dosage forms by introducing part of the preparation of auxiliary substances, so-called detergents, release of interferon from lipophilic bases and its absorbability through the epithelium of the rectum due to the introduction in its composition osmotically active substances that promote the penetration of aqueous solutions from the extravascular space into the plasma, increases the specific the th antiviral activity of the drug by extending the time of circulating interferon in systemic blood flow due to the introduction of the new advanced antioxidants and the use of antioxidants, with synergene activity while reducing the proteolytic activity of blood plasma, ensuring a long shelf life proposed composition through the use of auxiliary substances, stabilizing activity of interferon.

The achievement of the technical result is ensured by the fact that the proposed remedy in the form of rectal suppositories containing human recombinant interferon alpha 2, antioxidant complex consisting of ascorbic acid and alpha tocopherol acetate, retinol palmitate or retinol acetate as a substance that increases the expression of receptors for interferon on the surface mononuclear peripheral blood cells and hepatocytes, glycerin as a substance that helps to enhance the absorption of interferon in the rectum, Polysorbate 80 as substances that increase the bioavailability of interferon in a rectal dosage of the composition, dextran 40 or dextran 70 as substances that enhance the stability of interferon in the composition during its storage, as well as cocoa butter and tallow as the basis in the following ratio of these components contained in one suppositories weighing 1 g:

The human interferon
recombinant alpha-2100000 IU - 10000000 ME
Tocopherol acetate0.01 to 0.2 g
Ascorbic acid0,01-0,1 g
Retinol palmitate or retinol acetate1000-10000 ME
Glycerinof 0.0001-0.005 g
Lipoic acid or thioctic acid0.01 to 0.2 g
Polysorbate 80of 0.0005-0.01 g
Dextran 40 or dextran 700,01-0,1 g
Cocoa butter and tallowthe rest of it.

The complex of antioxidants may additionally include a synergistic antioxidants citric acid or para-aminobenzoic acid in an amount of from 0.01 g to 0.5 g, methionine or coenzyme Q10 in an amount of 0.01 g to 0.2 g per 1 g of the drug.

As substances that increase the expression of receptors for interferon in the liver, we offer you the medicine may contain isomers of retinoic acid all-TRANS retinoic acid, 13-CIS retinoic acid, 9-CIS-retinoic acid in an amount of from 0.01 g to 0.3 g per 1 g of medicines or preretinal - beta-carotene in an amount of from 0.01 g to 0.3 g per 1 g of the drug.

It is established that the main limiting factor for absorption of the drug is the result of a substance from recta in the blood system is its solubility in gliene (viscous mucus produced by some cells of the epithelium of the mucous membrane of the rectum). To increase the solubility and thus the absorption of the drug substance from recta used detergents are substances with surface-active (surfactant). In pharmaceutical practice, widely used surfactants such as sodium lauryl sulfate, the oleate combinatrial, Polysorbate 60 or Polysorbate 80.

The presence of the proposed pharmaceutical composition of detergents will increase the bioavailability of interferon in a rectal and thereby increase the efficiency interferonoterapii. As detergent proposed pharmaceutical composition may contain sodium lauryl sulfate, wax emulsion or Polysorbate 80 in an amount of from 0.05 to 1.00%.

A big role in the effectiveness interferonoterapii hepatitis plays a liver condition, namely the condition of the membranes of hepatocytes, because on the membrane of hepatocytes, as well as on the membranes of peripheral mononuclear blood cells expressed receptors for interferon. Means of protecting the liver from the damaging effects of chemicals and viruses, called hepatoprotectors. Inclusion in this medicinal form of hepatoprotectors will improve the efficiency interferonoterapii due to protection membranes of hepatocytes from damage. Kacha is the firmness of the hepato consider dosage form may contain ursodeoxycholic acid or its sodium salt, glutamyl - cysteinyl - glycine disodium, ribofuranosylhypoxanthine disodium.

The main site of absorption of the drug when it is rectal is the ampulla of the rectum. The lower part of the ampoule covered with a large number of capillaries through which the substance passes first in small paired veins of the rectum, and then in large veins and thereby in the systemic circulation. In this way, the penetration the greater the amount of injected substance into the blood system bypassing the liver, and only 20% is absorbed through the upper vein in the rectal ampulla reaches the liver. This mechanism of penetration into the liver is unique because all other ways of introduction into the organism (per os, infusion, injection) allow the medication to get into the liver only or through the gastrointestinal tract or systemic blood flow over a fairly long time after the introduction of the drug.

To ensure a more rapid absorption of drugs through the mucosa of recta possible to use osmotically active compounds, which, by increasing the osmotic pressure, promote the transfer of fluid from extravascular channel in the plasma. The use of osmotically active substances in the concerned medicinal composition is Oswalt to increase the absorbability of interferon by the mucosa of the rectal ampulla and its more rapid flow in the plasma and liver. As osmotically active component of the proposed pharmaceutical composition may contain glycerin, and dimethysulfoxide (DMSO), each in an amount of from 0.0001 to 0.005 g per 1 g of the drug.

As the basis for the creation of medicines proposed to use cocoa butter, hard fat, the basis for suppositories Witepsol or a mixture of all the above components or parts thereof in a quantity sufficient to obtain the suppository mass 1,

The invention is illustrated by the following examples showing the different quantitative composition of the possible ways to execute one suppository weighing 1 g:

Example 1.

Rectal suppositories containing 1 g of the following components:

The human interferon
recombinant alpha-2500000 ME
Tocopherol acetate0.06 g
Ascorbic acid0.02 g
Retinol palmitate or retinol acetate1000 IU
Glycerin0.005 g
Lipoic acid0.2 g
Polysorbate 800.005 g
Dextran 400.01 g
Oil Kaka and tallow the rest of it.

Example 2.

The human interferon
recombinant alpha-21000000 ME
Tocopherol acetate0.06 g
Ascorbic acid0.02 g
Retinol palmitate or retinol acetate1000 IU
Ursodeoxycholic acid0.01 g
Glycerin0.005 g
Lipoic acid0.2 g
Polysorbate 800.005 g
Dextran 700.01 g
Cocoa butter and tallowthe rest of it.

Example 3.

/tr>
The human interferon
recombinant alpha-21000000 ME
Tocopherol acetate0.06 g
Ascorbic acid0.02 g
Retinol palmitate or retinol acetate10000 ME
Ursodeoxycholic acid0.01 g
Glycerin0.005 g
Polysorbate80 0.005 g
Dextran 700.01 g
Thioctic acid
Witepsolthe rest of it.

Example 4.

The human interferon
recombinant alpha-21000000 ME
Tocopherol acetate0.06 g
Ascorbic acid0.02 g
Retinol palmitate or retinol acetate10000 ME
Ursodeoxycholic acid0.01 g
Glycerin0.005 g
Citric acid0.01 g
Coenzyme Q100.05 g
Lipoic acid0.2 g
Polysorbate 800.005 g
Dextran 700.01 g
Witepsolthe rest of it.

Example 5.

The human interferon
recombinant alpha-21000000 ME
Tocopherol acetate0.06 g
Ascorbic acid0.02 g
Beta carotene0.01 g
Glutamyl cysteinyl glycine disodium0.01 g
Glycerin0.005 g
A pair of oxybenzone acid0.01 g
Coenzyme Q100.05 g
Lipoic acid0.2 g
Polysorbate 800.005 g
Dextran 700.01 g
Cocoa butter and tallowthe rest of it.

Example 6.

The human interferon
recombinant alpha-21000000 ME
Tocopherol acetate0.06 g
Ascorbic acid0.02 g
Beta carotene0.01 g
Ribofuranosylhypoxanthine
disodium0.01 g
Glycerin0.005 g
A pair of oxybenzone acid0.01 g
Coenzyme Q100.05 g
Lipoic acid0.2 g
Polysorbate 800.005 g
Dextran 700.01 g
Cocoa butter and tallowthe rest of it.

Example 7.

The human interferon
recombinant alpha-21000000 ME
Tocopherol acetate0.06 g
Ascorbic acid0.02 g
Beta carotene0.01 g
Ribofuranosylhypoxanthine
disodium0.01 g
Glycerin0.005 g
A pair of oxybenzone acid0.01 g
Coenzyme Q100.05 g
Lipoic acid0.2 g
Sodium lauryl sulfate or
reinsulate sodium0.005 g
Dextran 700.01 g
Cocoa butter and tallowthe rest of it.

Example 8.

The human interferon
recombinant alpha-21000000 ME
Tocopherol acetate0.06 g
Ascorbic acid0.02 g
Beta carotene0.01 g
Ribofuranosylhypoxanthine
Dina is ry 0.01 g
Glycerin0.005 g
A pair of oxybenzone acid0.01 g
Coenzyme Q100.05 g
Lipoic acid0.2 g
Polyoxyethyleneglycol sodium0.005 g
Dextran 700.01 g
Cocoa butter and tallowthe rest of it.

Example 9.

The human interferon
recombinant alpha-21000000 ME
Tocopherol acetate0.06 g
Ascorbic acid0.02 g
13-CIS retinoic acid
or 9-CIS-retinoic acid0.01 g
Ribofuranosylhypoxanthine
disodium0.01 g
Glycerin0.005 g
A pair of oxybenzone acid0.01 g
Coenzyme Q100.05 g
Lipoic acid0.2 g
Polysorbate 800.005 g
Dextran 700.01 g
Oil is about and tallow the rest of it.

Thus, the proposed drug, made in the form of a rectal suppository, lets increase the effectiveness interferonoterapii in the treatment of various viral diseases through its constituent medicinal components and their weight ratio in the composition per 1 g of the drug.

1. Drug for the treatment of viral and other infections, is made in the form of a rectal suppository containing human recombinant interferon alpha-2, ascorbic acid and alpha tocopherol acetate, characterized in that it further contains retinol palmitate or retinol acetate as a substance that increases the expression of receptors for interferon on the surface of mononuclear peripheral blood cells and hepatocytes, glycerin as a substance that helps to enhance the absorption of interferon in the rectum, Polysorbate 80 as substances that increase the bioavailability of interferon in a rectal dosage of the composition, dextran 40 or dextran 70 as substances that enhance the stability of interferon in composition during its storage, or lipoic thioctic acid as an antioxidant, as well as cocoa butter and tallow as the basis in the following ratio at azannyh components, contained in one suppositories weighing 1 g:

The human interferon
recombinant alpha-2100000 ME - 10000000 ME
Tocopherol acetate0.01 to 0.2 g
Ascorbic acid0,01-0,1 g
Retinol palmitate or retinol acetate1000-10000 ME
Glycerinof 0.0001-0.005 g
Lipoic acid or
thioctic acid0.01 to 0.2 g
Polysorbate 80of 0.0005-0.01 g
Dextran 40 or
dextran 700,01-0,1 g
Cocoa butter and
tallowRest

2. The drug according to claim 1, characterized in that it further comprises hepatoprotector selected from the group: ursodeoxycholic acid, ursodeoxycholic sodium, glutamyl - cysteinyl - glycine disodium, ribofuranosylhypoxanthine disodium in an amount of from 0.001 g to 0.1 g per 1 g of the drug.

3. The drug according to claim 1, characterized in that optionally contains a synergistic antioxidant selected the C group: citric acid, para-aminobenzoic acid in an amount of from 0.01 g to 0.5 g per 1 g of the medicinal product, methionine, coenzyme Q10 in an amount of 0.01 g to 0.2 g per 1 g of the drug.

4. The drug according to claim 1, characterized in that as substances that increase the expression of receptors for interferon may contain a substance selected from the group of beta-carotene isomers transretinoic acid - fully transretinoic acid, 13-cisretinoic acid, 9-cisretinoic acid in an amount of from 0.01 g to 0.3 g per 1 g of the drug.

5. The drug according to claim 1, characterized in that the detergent may contain a substance selected from the group: sodium salt of lauryl sulfate, reinsulate, polyoxyethylenesorbitan, tween-20 in an amount of from 0.0005 g to 0.02 g per 1 g of the drug.

6. The drug according to claim 1, characterized in that as an osmotically active component may contain dimethyl sulfoxide (DMSO) in an amount of from 0.0001 g to 0.005 g per 1 g of the drug.



 

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Suppository base // 2323716

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Suppository // 2322968

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2 tbl, 4 ex

Vaginal suppository // 2320319

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1 tbl, 4 ex

FIELD: biotechnology, pharmacy.

SUBSTANCE: invention relates to creature of a interferon-base solution for injections and to recombinant strains of Escherichia coli (E. coli) and plasmids for its preparing. Invention proposes a novel recombinant multicopy plasmid DNA pSX50 that encodes synthesis of human leukocyte alpha-2b-interferon expression of that is under control of lactose and tryptophan promoters and transcription terminator. The strain E. coli SX50 as a producer of human recombinant leukocyte alpha-2b-interferon with productivity up to 0.901.0 g of alpha-2b interferon is obtained by transformation of the recipient strain E. coli BL21 cells with recombinant plasmid DNA pSX50. Method for preparing recombinant alpha-2b interferon is based on using the created recombinant strain E. coli SX50 and involving its submerged culturing on nutrient medium with decreased content of tryptophan and at continuous addition of nutrient substrates in the process of biosynthesis. The method involves mechanical destruction of microbial cells under high pressure, dissolving precipitated protein in the concentrated solution of guanidine hydrochloride followed by renaturation of interferon in physiological buffer solutions in the presence of chaotropic agents and its purification using three-step chromatography purification of interferon on resins of type Chelating Sepharose Fast Flow immobilized with Cu2+ ions, ion-exchange chromatography on ion-exchange resins of type CM Sepharose Fast Flow and gel-filtration chromatography on resins of type Superdex-75. Three-step chromatography purification of interferon provides preparing interferon substance of purity above 98% by data of electrophoresis under reducing and non-reducing conditions, and above 95% by data RF HPLC, and this interferon substance doesn't contain pyrogenes (LAL-test). The yield of the end product is 400 mg from 1 l of cultural medium, not less. Invention provides enhancing yield of interferon and stability of its solution.

EFFECT: improved preparing method of interferon.

12 cl, 5 tbl, 6 dwg, 2 ex

FIELD: medicine, gynecology, chemical-pharmaceutical industry.

SUBSTANCE: invention relates to development of vaginal suppository used for dilation of uterus cervix. Agent for dilation of uterus cervix is made as vaginal suppository and comprises Japanese or sugary laminaria micronized powder of particles size 200 mmc, not above, and in the ratio of active substance to suppository base = 1:1 and wherein Vitepsol H15 or Supacir are used as suppository base. Suppository is used in complex therapy for dilation of uterus cervix or in carrying out monotherapy and represents safety and effective method for dilation of uterus cervix.

EFFECT: improved and valuable medicinal properties of agent.

4 ex

Antibacterial agent // 2318523

FIELD: medicine, chemical-pharmaceutical industry, pharmacy.

SUBSTANCE: invention relates to an antibacterial agent as a suppository containing iodine and designated for treatment of inflammatory diseases of female genital region. Agent prepared as a suppository and containing iodine as an active substance and a filling agent comprises active substance as a complex of iodine-DMSO (dimethylsulfoxide) taken in the ratio = 1:(1-10) wherein it contains a fat-soluble base as a filling agent and wherein the content of iodine is 10 mg. Proposed suppository shows broad spectrum of antibacterial effect and without adverse effect. Active substance penetrates into deep tissues and shows selective effect on microorganisms. The claimed agent is suitable for using and it doesn't pollute skin and dress.

EFFECT: improved and valuable properties of agent.

5 cl, 2 tbl, 5 ex

FIELD: medicine, pharmaceutical industry, pharmacy.

SUBSTANCE: invention relates to suppository used in treatment of genital condylomae and neoplastic diseases of reproductive organs. Agent for treatment of genital condylomae and neoplastic diseases of reproductive organs as a suppository comprises metindol (3,3'-diindolylmethane) as an active component, lipophilic base containing solid confectionary fat, polyvinylpyrrolidone and butylhydroxyanisole taken in the definite ratio. Proposed agent promotes to effective treatment of genital condylomae and neoplastic diseases of reproductive organs.

EFFECT: valuable medicinal properties of suppository.

2 cl, 4 dwg, 1 tbl, 5 ex

Anti-viral agent // 2316320

FIELD: pharmaceutical industry, in particular agents for viral disease treatment including HIV infection (AIDS and HIV-associated diseases).

SUBSTANCE: claimed agent in form of suppository contains per one 2 g suppository Fullevir (fullerenopolyaminocaproic acid sodium salt) 20 mg as active ingredient and ancillary substances such as propylene glycol 200 mg and balance: Vitepsol.

EFFECT: effective agent having no adverse influence on peripheral blood and body systems.

FIELD: pharmaceutical industry, pharmacy.

SUBSTANCE: invention relates to producing interferon-containing suppositories. Interferon-containing suppository comprises a fatty base, emulsifier and human lyophilized interferon purified from low-molecular and high-molecular components of the definite antiviral activity. Mixture of mono-, di- and triglycerides and saturated fatty acids from coconut oil and palm oil of sort "Vitepsol" H-15 and W-35 taken in equal ratio are used as a fatty base. Distilled monoglycerides taken in the definite ratio are used as an emulsifier. Above describes suppositories retain specific activity and effectiveness in treatment of viral and bacterial diseases for a long time and show stability against mechanical effects.

EFFECT: improved and valuable properties of suppository.

1 tbl, 1 ex

FIELD: medicine.

SUBSTANCE: it is necessary to carry out complex medicinal therapy including specific antiviral preparations, group B-vitamins, immunocorrectors, injection of antiherpetic vaccine, and, also local therapy with derinate. Additionally, since the 1st d of exacerbation it is important to inject flosteron once i/m at 1.0 ml, cefotaxym i/m twice daily per 1.0 mg for 10 d. Immunomodulator halavit on the 1st d should be prescribed i/m at the dosage of 200 mg, and then for the next 15 d - twice daily per 100 mg i/m. Diazepam for 1 mo should be injected per 5.0 mg 4 times daily, and then per 2.5 mg 4 times daily for 1 mo, as well. One should daily inject atarax per 100 mg nocturnally for 1 mo and ketorol internally per 10 mg thrice daily for 10 d. Moreover, it is necessary to apply the composition out of 50.0 g zinc oxide, 5.0 ml ACD fraction and 25.0 g "Aciclovir" cream 4 times daily for 10 d. The innovation enables to considerably increase the efficiency of therapy due to improving the main immunological values, weakening local autoimmune reactions and, also, preventing the development of psychic disorders in such patients due to affecting viral neurotropic properties.

EFFECT: higher efficiency of therapy.

3 dwg, 1 ex

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