Antiviral agent in a liposomal form

 

(57) Abstract:

The inventive tool contains the following components based on 1 g of the mixture: alpha, or beta, or gamma interferon IU 500-5000000, stabilizer biological, physico-chemical properties and/or resistance to microbial contamination of 0.0001 to 0.4, phosphatidylcholine 40-90, cholesterol 2-20 and grease-forming the basis for the rest. As the stabilizer of biological, physico-chemical properties of the product contains polyvinylpyrrolidone or polyvinyl alcohol, or a derivative of cellulose. As a stabilizer resistance to microbial contamination, the product contains nipagin, or Quaternary ammonium compounds, or chlorhexidine. The invention solves the problem of expanding Arsenal of antiviral drugs in liposomal form. A new tool based on recombinant interferon is characterized by prolonged action, provides good penetration ability and has antiviral, antibacterial, anti-inflammatory, detoxifying, local anesthetic and regenerating action. 8 C.p. f-crystals.

The invention relates to medicine and the pharmaceutical industry and relates to a Le is Ron.

Known antiviral agent in a liposomal form, containing recombinant interferon, phosphatidylcholine, cholesterol, stabilizer is sucrose, the antioxidants alpha-tocopherol and ascorbic acid in a specific ratio of components.

(RU, patent N 2123328, class a 61 K 9/127, 38/21, 1998)

Accumulated in recent years, the experience of clinical application of interferons indicate the possibility of improving their efficiency by the use of dosage forms in liposomal form for local use. When interferon is used in lower doses and has antiviral, immunomodulatory effects, but is not shown neither cytotoxic nor other side effects. This causes the feasibility of developing various dosage forms in liposomal form of interferon for local use prolonged action, for example, ointment, gel, cream, liniment.

The technical result of the invention is to increase the Arsenal of antiviral drugs in liposomal form, the creation of the drug prolonged action on the basis of recombinant interferon, ensuring good penetration ability and with protivovirusny esteem.

To achieve the technical result antiviral agent containing recombinant interferon, phosphatidylcholine, cholesterol, according to the invention as recombinant interferon contains alpha, or beta, or gamma-interferon, and additionally contains a stabilizer biological, physico-chemical properties and/or resistance to microbial contamination and grease-forming the basis of the following ratio of components in 1 g of a mixture of:

Recombinant interferon, ME - 500-5000000

Stabilizer, g is 0.0001 to 0.4

Grease-forming the basis of the Rest.

As the stabilizer means includes polyvinylpyrrolidone or polyvinyl alcohol, or a derivative of methyl cellulose (Na CMC) and nipagin, or Quaternary ammonium compounds, or chlorhexidine.

As Quaternary ammonium compounds, the tool contains atony, or benzathine chloride or benzalkonium chloride.

As a grease-forming the basis of the tool contains a lipophilic or hydrophilic or lipophilic-hydrophilic base.

In addition, the tool further comprises an antioxidant: Trilon B and/or butylacetate 0,001-0,5 g per 1 g of the mixture.

The tool also contains tween-80 in the amount of 0.004-0.005 g to 1 g of the mixture.

In addition, the tool also contains beta-carotene in the amount is 0.0002-0,0006 g per 1 g of the mixture.

Antiviral agent is an ointment, a gel, a suppository, a paste, a cream, liniment in liposomal form.

The invention is illustrated in the following examples.

Example 1. Technology of production of antiviral agents.

To obtain gel take alcoholic solution of phosphatidylcholine and cholesterol. Evaporated the mixture on a rotary vacuum evaporator at a temperature of 35-40oC before the formation of thin films. The resulting film aeronaut for 1 hour with nitrogen gas to prevent oxidation. Then enter the prepared solution of the stabilizer of 1% nipagina, 6% polyvinylpyrrolidone, antioxidant - Trilon B. Add dimethyl sulfoxide. Mix the components, and sterilize by autoclaving. Then add alpha-interferon is dispersed mixture, and then speak for 10 minutes three times with 22 kHz at 10oC. the resulting suspension of liposomes is separated and mixed with grease-forming the basis of the alloy polietileno the spine (for example, tubes), seal and label. These components take the following ratio of 1 g of a mixture of:

Alpha-interferon ME - 5000000

Stabilizers, g:

Polyvinylpyrrolidon - 0,38

Nipagin - 0.02

Phosphatidylcholine - 40,0

Cholesterol - 2,0

Trilon B - 0,0001

Dimethyl sulfoxide - 0,001

Grease-forming base - Rest

Example 2. Carried out analogously to example 1. For more ointment take Gamma-interferon, polyvinyl alcohol, atony, phosphatidylcholine, cholesterol, Trilon B, beta-carotene, tween-80 and grease-forming base.

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

Gamma-interferon ME - 1000000

Stabilizers, g:

Polyvinyl alcohol - 0,3982

Atony - 0,0018

Phosphatidylcholine - 40,0

Cholesterol - 15,0

Trilon B - 0,0006

Beta-carotene - is 0.0002

Tween-80 - 0,004

Grease-forming base - Rest

Example 3. Carried out analogously to example 1. To prepare the cream taking beta-interferon, polyvinylpyrrolidon, benzathine chloride, phosphatidylcholine, cholesterol, butylacetyl, dimethylsulfoxide, beta-carotene, tween-80 and grease-interferon, ME - 1000000

Stabilizers, g:

Polyvinylpyrrolidon - 0.02

Benzathine chloride - 0,0018

Phosphatidylcholine - 40,0

Cholesterol - 2,0

Butylacetyl - 0,0001

Dimethyl sulfoxide - 0,001

Beta-carotene - is 0.0002

Tween-80 - 0,001

Grease-forming the basis of the Rest.

Example 4. Carried out analogously to example 1. For more ointment take beta-interferon Na, chlorhexidine, phosphatidylcholine, cholesterol, Trilon B, butylacetyl, dimethylsulfoxide, beta-carotene and grease-forming base.

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

Beta-interferon ME - 500000

Stabilizers, g:

NaKM - 0.02

Chlorhexidine - 0,0018

Phosphatidylcholine - 50,0

Cholesterol - 10,0

Antioxidants, g:

Trilon B - 0,0003

Butylacetyl - 0,0003

Dimethyl sulfoxide - 0,001

Beta-carotene - is 0.0002

Grease-forming base - Rest

Example 5. Carried out analogously to example 1. To obtain emulsions take gamma-interferon, polyvinylpyrrolidon, benzalkonium chloride, phosphatidylcholine, cholesterol, butylacetyl, dimethylsulfoxide, beta-carotene, tween-80 and consistentency interferon, ME - 500

Stabilizers, g:

Polyvinylpyrrolidon - 0.02

Benzalkonium chloride - 0,0018

Spatially to 90.0

Cholesterol - 20,0

Butylacetyl - 0,0006

Dimethyl sulfoxide - 0,5

Beta-carotene - 0,0006

Tween-80 - 0,005

Grease-forming the basis of the Rest.

Received antiviral agent has the form of ointments varying consistency in liposomal form.

Clinical trials on human volunteers aged 18-20 years of age show that the drug is safe, well tolerated, does not cause allergic reactions.

1. Antiviral agent in a liposomal form, containing recombinant interferon, phosphatidylcholine, cholesterol, characterized in that the product contains alpha or beta, or gamma-interferon, stabilizer biological, physico-chemical properties and/or resistance to microbial contamination and grease-forming the basis of the following ratio of components in 1 g of a mixture of:

Alpha, or beta, or gamma interferon IU - 500-5000000

The stabilizer biological, physico-chemical properties and/or resistance to microbial contamination, g is 0.0001 to 0.4

Phosphatidylcholine, Mr. 40-90

Cholesterine fact, as a stabilizer biological, physico-chemical properties it contains polyvinylpyrrolidone or polyvinyl alcohol, or a derivative of methyl cellulose (Na CMC).

3. Antiviral agent under item 1, characterized in that the stabilizer is resistance to microbial contamination it contains nipagin or Quaternary ammonium compounds, or chlorhexidine.

4. Antiviral agent under item 1, characterized in that additionally it contains antioxidant Trilon B and/or butylacetyl in the amount of 0.0001-0,0006 g per 1 g of the mixture.

5. Antiviral agent under item 3, characterized in that the Quaternary ammonium compounds it contains atony or benzathine chloride or benzalkonium chloride.

6. Antiviral agent under item 1, characterized in that it additionally contains beta-carotene in the amount is 0.0002-0,0006 g per 1 g of the mixture.

7. Antiviral agent under item 1, characterized in that it further comprises dimethyl sulfoxide at 0:001-0,5 g per 1 g of the mixture.

8. Antiviral agent under item 1, characterized in that it additionally contains tween - 80 in the amount of 0.004-0.005 g to 1 g of the mixture.

9. Antiviral drugs is a multidisciplinary, or lipophilic-hydrophilic base.

 

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