Medicinal formulation eliciting nonsteroid anti-inflammatory effect and method for its making

FIELD: chemical-pharmaceutical industry, pharmacy.

SUBSTANCE: invention relates to manufacturing solid medicinal formulations of preparations. Invention proposes a medicinal formulation consisting of a core comprising the following components: indometacin, lactose, calcium phosphate, hydroxypropylcellulose, magnesium stearate, sodium croscarmellose and envelope comprising collicute MAE 100P, propylene glycol, pigment titanium dioxide, talc, collidon-30, brown sycovite-70. Also, invention discloses a method for preparing the formulation. Invention provides enhancing stability of envelope to effect of stomach juice, rapid and complete release of active substance, simultaneous simplifying the process of applying the envelope for a single step.

EFFECT: improved and valuable pharmaceutical properties of formulation.

3 cl, 1 tbl

 

The invention relates to medicine, in particular to a pharmacy, can be used in the manufacture of solid dosage forms of drugs, enteric-coated shell and having a non-steroidal anti-inflammatory for use in articular syndrome, infectious-inflammatory diseases of ENT organs and urinary system.

The closest to the invention is a pharmaceutical form tablets with nonsteroidal anti-inflammatory action, consisting of a kernel, containing as active substance indomethacin, and a shell containing an ester of fatty acids and polyglycerol, and polyvinylpyrrolidone, talc, magnesium stearate, kaolin, starch, crystalline cellulose (EN 2072836, 10.02.1997). There is also known a method of manufacturing a solid dosage form, including the production of granules containing the active substance, and applying them to the shell by spraying them water suspension containing hydrochloride phenylpropanolamine and corn starch, and then the solution containing Penta(Tetra)glycerol ester of stearic acid and methylene chloride (ibidem).

In the famous decision of the shell provided continuous release of active ingredients over a long period of time (0.5 to 48 hours). However, this membrane is not resistant to the action is Yu gastric juice, and the release of active ingredient begins in the stomach, which is highly undesirable for such an active substance, as indomethacin, which has undesirable effects on gastric mucosa.

The objective of the invention is to provide a dosage form with the least undesirable action of the active component.

The technical result of the invention is to improve the stability of the membrane to the action of gastric juice and ensuring rapid and complete release of indomethacin in the Department of the gastrointestinal tract with a higher pH, while simplifying the process of applying the sheath at one time.

The technical result is achieved that the dosage form with non-steroidal anti-inflammatory action, consisting of a nucleus containing indomethacin, and shell, according to the invention the core additionally contains milk sugar, calcium phosphate, oxypropylation, magnesium stearinovokisly and sodium croscarmellose at the following content, wt.%:

Indometacinof 10.0 to 35.0
Sugar milk58,7-75,0
Calcium phosphate5,0-10,0
Oxypropylation0,5-2,0
The magnesium with eosinophilia 0,5-2,0
Sodium croscarmellose0.3 to 1.0,

and the shell contains collicut MAE 100 P, propylene glycol, titanium dioxide pigment, talc, kollidon 30 and cikovic brown 70 at the following content, wt.%:

Collicut MAY 100P50,0-80,0
Propylene glycol3,0-10,0
The titanium dioxide pigment1,0-3,0
Talcfrom 9.0 to 20.0
Kollidon 306,0-14,0
Cikovic brown 701,0-3,0

The technical result is also achieved by the fact that the method of manufacture of dosage forms with non-steroidal anti-inflammatory effect, characterized by the fact that mixed powders milk sugar, indometacin and calcium phosphate hydrate solution oksipropilmetiltselljulozy, re-mix, damp granulation, subsequent drying, dry granulation, add to the granular sodium croscarmellose and magnesium stearinovokisly, tabletirujut and put a coating of an aqueous suspension containing collicut MAE 100 P, kollidon 30, titanium dioxide, talc, propylene glycol and cikovic brown 70.

When this coating is applied by spraying aqueous suspensions

The invention consists in the following.

Use as active substances indometacin provides pharmacological anti-inflammatory, antipyretic and analgesic effect. Inhibiting cyclooxygenase, indomethacin reduces the synthesis of PG, causing the inflammation to the development of pain, fever and increased tissue permeability.

Introduction to collectively as excipients sugar, dairy, magnesium stearinovokisly, calcium phosphate, oxypropylation and sodium croscarmellose in the claimed limits allows us to give the tablet a mixture of good technological properties, get the tablet that meets all the requirements for bioavailability, stability during storage and is well compatible with the enteric coat.

Use as shell collicut MAE 100 P (trade name of methacrylic acid copolymer type C (USP) - the main film-forming component, propylene glycol, titanium dioxide, talc, kollidon 30 (trade name polyvinylpyrrolidone) and sikavica brown 70 E 172 (trade name pigment brown iron oxide) allows the application of the enteric coating from the aqueous medium. The resulting framework provides a rapid passage of tablets across the stomach unchanged, and rapid and complete release of the active substance in the intestine.

The invention is carried out as follows.

The sifted powders indometacin, sugar, milk, calcium phosphate are thoroughly mixed and moistened with a solution of oxypropylation, mix to a uniform moisture and granularit. The wet granules are dried at a temperature of 50-55°to a residual moisture from 1.0 to 2.0%.

The dried pellets are cooled to room temperature and conduct a dry granulation. The dry granulate optivault adding sodium croscarmellose and magnesium stearinovokisly. The mixture is stirred until a homogeneous tablet mass.

Then the mass tabletirujut, receiving tablets-kernel biconvex shape with a diameter of 7.0±0.02 mm) and a weight of 0.12,

For coating the tablet cores using a water suspension containing collicut MAE 100 P, kollidon 30, titanium dioxide, talc, propylene glycol and cikovic brown 70 (E 172).

The application shell carry spray and stop when you reach the required weight of the tablet. The weight of the coated tablet is 0.13,

%
The table below shows the formulations of the claimed solid form.
Retz. No. 1Retz no.2Retz no.3
The kernel:g%%
1. Indometacin0,02520,8310,0035,00
2. Sugar milk0,08268,3375,0058,7
3. Calcium phosphate0,0108,3310,005,00
4. Oxypropylation0,00131,082,000,50
5. Magnesium stearinovokisly0,00100,832,000,50
6. Sodium croscarmellose0,00070,601,000,30
Weight pills0.12 g100%100%100%
The composition shell:
Callicut MAY 100 R0,006767,050,080,0
2. Propylene glycol0,00066,010,03,0
3. The titanium dioxide pigmentis 0.00022,03,01,0
4. Talc0,001414,020,09,0
5. Kollidon 30 0,00099,014,06,0
6. Cikovic brown 70 Sis 0.00022,03,01,0
The weight of the shell0,01100%100%100%
Weight pills0,13 g

The proposed dosage form with non-steroidal anti-inflammatory effect obtained by the proposed method, in comparison with the known has a milder effect on the mucous membrane of the stomach. The shell is resistant to gastric juice for 1 hour, during this time, the tablet into the intestine, in the alkaline environment of which it is dissolved and released no less than 75% of the active substance in 45 minutes.

1. Dosage form with non-steroidal anti-inflammatory action, consisting of a nucleus containing indomethacin, and a shell, wherein the core additionally contains milk sugar, calcium phosphate, oxypropylation, magnesium stearinovokisly and sodium croscarmellose at the following content, wt.%:

Indometacinof 10.0 to 35.0
Sugar milk58,7-75,0
Calcium phosphate5,0-10,0
Oxypropylation0,5-2,0
Magnesium stearinovokisly0,5-2,0
Sodium croscarmellose0.3 to 1.0,

and the shell contains collicut MAE 100 P, propylene glycol, titanium dioxide pigment, talc kollidon 30 and cikovic brown 70 at the following content, wt.%:

Collicut MAY 100P50,0-80,0
Propylene glycol3,0-10,0
The titanium dioxide pigment1,0-3,0
Talcfrom 9.0 to 20.0
Kollidon 306,0-14,0
Cikovic brown 701,0-3,0

2. The method of manufacture of dosage forms with non-steroidal anti-inflammatory effect, characterized in that the mixed powders milk sugar, indometacin and calcium phosphate hydrate solution oksipropilmetiltselljulozy, re-mix, damp granulation, subsequent drying, dry granulation, add to the granular sodium croscarmellose and magnesium stearinovokisly, tabletirujut and put a coating of an aqueous suspension containing collicut MAE 100 P, kollidon 30, titanium dioxide,talc, propylene glycol and cikovic brown 70.

3. The method according to claim 2, characterized in that the coating is applied by spraying a water suspension.



 

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