Pelletised drug showing antiviral and interferonogenic action, and method for preparing it

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry. A pelletised form of amison contains the active substance amison-N-methyl-4-benzylcarbamidopyridinium iodide, as an excipient - lactose, basic magnesium carbonate, or dibasic calcium phosphate, or pre-gelled starch, and also microcrystalline cellulose, as binding agents - saccharose and povidone, as an anti-cleavage agent - copolyvidone, as a desintegrant - crospovidone or sodium croscarmellose and as sliding agents - stearic acid, and/or a calcium stearate, and/or magnesium stearate. An amison pellet can be film-coated. The amison pellet is prepared by wet granulation.

EFFECT: amison pellets under the invention are characterised by high fracture and abrasion strength and have no cleavages.

6 cl, 1 tbl

 

The invention relates to the pharmaceutical industry, namely pharmaceutical compositions having antiviral interferonogenna action.

Well-known pharmaceutical drug Amizon, which was synthesized at the Institute of pharmacology and toxicology, Academy of medical Sciences of Ukraine. Amizon refers to a derivative of isonicotinic acid and has the chemical name N-methyl-4-benzylcarbamoyl iodide. In the patent of Ukraine No. 6752, published on December 29, 1994, disclosed Amizon as a painkiller with interferonogenami, anti-inflammatory and antipyretic properties and the method of its synthesis.

Known tableted dosage form batches containing 0.25 g of amyzon and excipients: lactose monohydrate, microcrystalline cellulose, povidone (polyvinylpyrrolidone low molecular weight PVP), sodium croscarmellose and calcium stearate (see http://37.com.ua/notes.php?lek=41728).

The technical result of the invention is to increase the strength of tablets containing Amizon, namely improving the tensile fracture and abrasion, as well as the exception chips pills.

The technical result is achieved in that the preformed shape of amyzon contains the active substance Amizon - N-methyl-4-benzylcarbamoyl iodide, as filler lactose or magnesium carbonate on the main, or disubstituted calcium phosphate, or pregelatinized starch and microcrystalline cellulose, the binder components sucrose and povidone as a component that protects against chips, copolyvidone, as disintegrant crosspovidone or croscarmellose sodium, as moving components stearic acid and/or calcium stearate and/or magnesium stearate, with the following content, wt.%:

Amizon50-80
lactose or magnesium carbonate basic,
or disubstituted phosphate calcium
or pregelatinized starch15-29
microcrystalline cellulose1-15
sucrose1-12
povidone0.5 to 3
copolyvidone0.5 to 3
crosspovidone or croscarmellose sodium1-5
stearic acid or stearate feces is tion
or stearate0,5-1,8

In addition, as the moving component, it can optionally contain talc in the amount of 0.5-3 wt.%.

In addition, it may further comprise a film shell in an amount of about 3 wt.% from the mass of the nucleus.

The technical result is also achieved by a method of obtaining a tablet form of amyzon, namely, that crushed Amizon mixed with lactose or magnesium carbonate basic, or disubstituted calcium phosphate, or pregelatinization starch and microcrystalline cellulose, moisten the mixture with a mixture of solutions of povidone, sucrose in water, stirred, granularit, dried, subjected to dry granulation, optivault mixture of copolyvidone, crosspovidone or croscarmellose sodium and stearic acid or calcium stearate, or magnesium stearate and tabletirujut.

In addition, for dusting can use the mixture, optionally containing talc.

In addition, after tabletting can cause the film to the shell.

Use as a binder sucrose and PVP, which are introduced in the form of solutions to hydrate before granulation, and copolyvidone when dusting together with the stated quantitative content to the components allows to obtain tablets, with a high resistance to fracture and wear and no chipping.

The tablet can be without the shell or the shell that weighs about 3% by weight of the core. In preferred embodiments, the tablet contains 0.125 g or 0.25 g batches. In the first case, the mass of the tablet (core) 190 mg, with sheath 196 mg. In the second case, the mass of the tablet (core) 380 mg, with sheath 392 mg.

Below is an example of implementation of the proposed method to obtain tablets of amyzon.

Grind the substance batches on the cage. Mix Amizon filled with lactose and microcrystalline cellulose. Prepare a 20%solution of PVP and 50%sucrose solution in water. Moisten the mixture of amyzon filled with a mixture of mud, stirred for 2-5 minutes, granularit, dried in a fluidized bed (or heaters in the dryer) at a temperature of 40°C to a residual moisture content of not more than 1.5%. The granulate is passed through a granulator with a cell diameter of 1 mm, optivault mixture of copolyvidone, crosspovidone (polyplasdone XL-10), talc and calcium stearate. Tabletirujut.

Possible application shell. Put the water film membrane in the apparatus of the firm Pelligrini in an amount of about 3% by weight of the kernel by a 13.5%aqueous solution ADVANTIA Prime (hypromellose, titanium dioxide, capryl/kaprilat (Caprylic/capric triglyceride), the colorant iron oxide yellow, KRA is ITIL iron oxide red, dye quinoline yellow) or OPADRY (partially hydrolyzed polyvinyl alcohol, PEG 3350, talc, titanium dioxide) or other suitable.

Experiments were conducted in which the hydration was carried out only starch paste, or just sugar syrup, or only PVP solution, or the only solution copolyvidone. Worked tablets low strength.

The table shows the formulations 4, 7, 8, 9 of the proposed composition of the tablets amyzon (uncoated tablets or cores tablet shell) and for comparison of formulations 1 and 2, does not contain sucrose, and recipes 1, 3, 5, 6, 10, not containing copolyvidone and their properties.

An objective assessment of the mechanical properties of the tablets was obtained by the method of determination of their strength in two ways: on the destruction and attrition. This is because the tablets the drug, satisfying the requirements for destruction is easy abrasion of the edges, which leads to the formation of dust and the occurrence of chipping in the process of packing, applying a film of membrane and storage. For this reason, the product is substandard.

The table shows that the drug formulations 1 and 2, not containing sucrose, has a low resistance to erosion and abrasion, which leads to the chips pills. Introduction to the composition of sucrose, which is a binder, Uwe is icepay strength tablets.

The drug formulations 3, 5, 6, 10, containing sucrose but not containing copolyvidone, has a high resistance to erosion and abrasion, but insufficient for complete absence of chipping tablets.

The drug formulations 4, 7-9, containing sucrose and copolyvidone, which is in this case not only disintegrants, but binding, increases the strength (compared with formulations 3, 5, 6, 10) and the plasticity of the tablet, allowing you to get tablets without chipping.

1. The preformed shape of the batches containing the active substance Amizon - N-methyl-4-benzylcarbamoyl iodide, as filler lactose or magnesium carbonate basic, or disubstituted calcium phosphate, or pregelatinized starch and microcrystalline cellulose, the binder components sucrose and povidone as a component that protects against chips, copolyvidone, as disintegrant crosspovidone or croscarmellose sodium, as moving components stearic acid and/or calcium stearate and/or magnesium stearate, with the following content, wt.%:

Amizon50-80
lactose or magnesium carbonate basic,or disubstituted phosphate calcium
or pregelatinized starch15-29
microcrystalline cellulose1-15
sucrose1-12
povidone0.5 to 3
copolyvidone0.5 to 3
crosspovidone or croscarmellose sodium1-5
stearic acid or calcium stearate,
or stearate0,5-1,8

2. Tablet form according to claim 1, characterized in that the moving component further comprises talc in the amount of 0.5-3 wt.%.

3. Tablet form according to claim 1, characterized in that it further comprises a film shell in an amount of about 3 wt.% from the mass of the nucleus.

4. The method of obtaining a tablet form batches according to any one of claims 1 to 3, namely, that crushed Amizon mixed with lactose or magnesium carbonate basic, or disubstituted calcium phosphate, or pregelatinization the m starch, and microcrystalline cellulose, moisten the mixture with a mixture of solutions of povidone, sucrose in water, stirred, granularit, dried, subjected to dry granulation, optivault mixture of copolyvidone, crosspovidone or croscarmellose sodium and stearic acid or calcium stearate, or magnesium stearate and tabletirujut.

5. The method according to claim 4, characterized in that for dusting use a mixture, optionally containing talc.

6. The method according to claim 4, characterized in that after tabletting put the film sheath.



 

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13 cl, 2 ex, 3 tbl, 11 dwg

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23 cl, 9 dwg, 6 tbl, 20 ex

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16 cl, 1 dwg, 4 tbl, 26 ex

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1 tbl

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2 tbl, 3 ex

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12 cl, 8 tbl, 16 ex

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42 cl, 2 dwg, 4 tbl, 2 ex

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23 cl, 4 tbl, 7 ex

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5 cl, 2 ex, 1 tbl

FIELD: medicine, pharmaceutics.

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EFFECT: method ensures high effective preparation of the composition.

14 cl, 2 dwg, 3 tbl, 4 ex

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