Oral interferon in the form of tablets

 

(57) Abstract:

The invention relates to medicine, the pharmaceutical industry and relates to the creation of new dosage forms containing CLI. The invention lies in the fact that oral tablet contains human leukocyte interferon, purified and concentrated 2000-20000 IU, and powdered water-soluble filler in a ratio of components. The invention improves the efficiency of the local effects of the administered dose interferon for clinical process, does not cause adverse effects and without flaws injectable forms. 1 C.p. f-crystals.

The invention relates to pharmaceutical industry, medicine and the receipt of tablets containing interferon (IFN) for treatment and prophylaxis of viral diseases of the oral cavity and nasopharynx.

The following dosage form of interferon: injection solutions, lyophilized form, liposomes, rectal and vaginal legform, ointments, aerosols, eye drops and films, and oral solutions.

Closest to the proposed drug is a method for enteral product containing IFN-a is and of the following composition:

human recombinant genetically engineered alpha-2 interferon, lactose, sucrose, calcium stearate, acetylpenicillamine, castor oil in the following ratio:

human recombinant genetically engineered alpha-2 interferon, IU 1105-1106;

and Mac. : lactose 72-79; sucrose 9-16; calcium stearate 2; acetylcholinesterase 8; castor oil 20. (Patent N 2083222, class A 61 K 38/21, 9/20, 1997).

Unlike enteric drug in the form of tablets offer oral tablet form of interferon easy to manufacture, because there is no time-consuming stage of the enteric coating of the shell. When the resorption of tablets in the oral cavity interferon associated with receptors in the pharynx and throat, strengthens the immune system against viruses (Kovesi G., K. Onody , 1992). In addition, the release and the effect of interferon on infectious process begins earlier (1.5-3 min) than in enteric tablets (after 2.5-3 h). Oral ensures long contact (up to 3 min) applicable beginning with infected surface in comparison with the liquid drugs.

Offer oral tablet form of human leukocyte interferon (CLI) call the preventive action. In contrast to recombinant IFN leukocytes in the process of interferonogenesis, in addition to interferon, synthesize a complex mediators of the immune response, which remain in the product after purification steps.

The technical result, which can be obtained by carrying out the invention, is to improve the effectiveness of the drug in the treatment of viral diseases, its ease of use and simplification of the process of preparation of tablets.

The invention consists in the following.

Invited oral tablet with IFN, including human leukocyte concentrated purified IFN and water-soluble filler in the following ratio:

Interferon purified concentrated lyophilized - 103-2105IU

Water-soluble filler, g - 0,1-0,5

Dose the beginning of the current (2000-20000 IU) is defined in clinical studies. In the filler to impart taste use sterile sucrose, or lactose, or glucose, or attracts, as a stabilizer - sterile aerosol, and as lubricants - sterile magnesium stearate or calcium. All substances used in the research Institute of tablets loss of antiviral activity was not observed.

Composition per tablet: human leukocyte purified concentrated interferon with antiviral activity 2000-20000 IU; water-soluble filler (sucrose, glucose, lactose, lures) 0,0904-0,4864 g; Aerosil (A300 or A380) 0,0043 g; magnesium stearate (calcium) 0,001-0,003 g

IFN mixed with a filler and pressed.

Manufacturing tablets

Example 1. Obtaining tablets containing

CLI with antiviral activity 2000 IU each. The composition contains, g:

Lactose - 127

Aerosil-380 - 1,935

Magnesium stearate - 1,35

Dried, CLI in the number corresponding to the total specific activity 9105IU (per 1 tablet 2103IU), mixed with a filler. The composition is pressed into a pill mass of 0.3 g Tablets obtained as follows: sterile lactose, Aerosil and magnesium stearate are mixed, add the powder interferon and again mix. Tablets obtained by compressing in a tablet machine (get about 450 tablets 0.3 g, given the waste mass).

Example 2. Obtaining tablets containing CLI with antiviral activity 8000 IU each.

The composition contains, g:

Glucose - 40,68

Aerosil A-300 - 1,935

Stay interferon in the tablet (8103IU). For this purpose, the total specific activity should be 3105IU. The composition is formed into tablets weighing to 0.1, the Output 450 of pills to 0.1 g, given the waste mass.

Example 3. Obtaining tablets containing CLI with antiviral activity 20000 IU each.

Tablet suspension is prepared analogously to example 1 with the exception of the estimated activity of interferon in the tablet (2104IU). For this purpose, the total specific activity should be 9106IU, the filler is used sucrose. The output 450 tablets 0.3 g, given the waste mass.

Example 4. Obtaining tablets containing CLI with antiviral activity 4000 IU each.

The composition contains, g:

Beckons - 218,88

Aerosil-380 - 1,935

Calcium stearate - 1,35

Dried, CLI that corresponds to the total specific activity 18105IU (per 1 tablet). The composition is formed into tablets 0.5 g analogously to example 1.

Thus was used the following technology for oral forms of human leukocyte interferon: a source of biologically active material mixed with a filler, the mixture alloy preformed by weight of 0.1 - 0.5,

1. filler, characterized in that it contains human leukocyte interferon, and a purified concentrated as the water-soluble excipient is sucrose, or glucose, or lactose, or mannitol and Aerosil, magnesium stearate or calcium.

2. Oral interferon under item 1, characterized in that it contains components in the following ratio, g:

Human leukocyte interferon, and a purified concentrated - 2000 - 20000 IU

Sucrose, or glucose, or lactose, or mannitol - 0,0904 - 0,4864

Aerosil - 0,0043

Magnesium stearate or calcium - 0,001 - 0,003

 

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