Pharmaceutical antimicrobial composition

 

(57) Abstract:

The invention relates to medicine, specifically to a pharmaceutical composition having antimicrobial activity comprising as active principle an effective amount sulfalena and targeted supplements, which are used potato starch and/or corn, oxypropylation, magnesium stearate and/or calcium. The drug has improved release of the active substance. 2 C.p. f-crystals.

The invention relates to medicine, specifically to medicines which have an antimicrobial effect.

Among these drugs, along with antibiotics leading position occupied by sulfonamides. They are used to treat infections caused by a large group of gram-positive and gram-negative bacteria, they are effective for diseases caused by some protozoa (malaria, toxoplasmosis) and hlamidiozah (trachoma, paratracheal). Different drugs in this group have different validity when administered single dose: 4-5 hours up to 2-7 days.

The most prolonged action known to date of sulfonamides has sulfalen (Moskovskaia concentration in the blood is detected within 4-6 hours The preparation of long-circulating in the blood. The half-life of blood is on average 65 hours; 60% of the administered dose excreted within 9 days. A positive feature of sulfalena is that the drug in therapeutic doses does not impair the function of the kidneys (no crystalluria). The prolonged therapeutic effect (drug 1 every 7-10 days), and lower than other sulfonamides, side effects, allocate sulfalen from the group of the sulfonamides.

Renowned pharmaceutical composition, which contains as active substance sulfalen and as excipients starch, agarose, preservative and meglumine, as well as physiological solution (patent RF N 2115419, 1998).

The most convenient form for the treatment of most infectious diseases, where applicable sulfalen is a tablet. However, the use of these auxiliary substances for the manufacture of solid dosage forms sulfalena not possible to obtain the product with satisfactory results of release of the active substance.

In the claimed invention, the aim was to obtain a pharmaceutical composition sulfalena with characteristical CLASS="ptx2">

This is achieved by a pharmaceutical composition comprising an effective amount sulfalena and targeted supplements, which are used potato starch and/or corn, magnesium stearate and/or calcium and oxypropylation, in the following ratio of components, % by weight of active ingredient:

Potato starch and/or corn - 19,1-23,5

Oxypropylation - 0,7-1,4

Magnesium stearate and/or calcium - 2,2-2,8

The proposed ratio of the active substance and the target additives found experimentally and is optimal, satisfying all the requirements of the current Gosfarmakapei XI edition. Going beyond the lower limit of the ratios of the basic substance and the target additives leads to deterioration of the technological parameters of the process of obtaining tablets sulfalena, and the increase of target components is impractical, because it reduces the quality of some indicators pharmacopoeial product.

Thus, the claimed pharmaceutical composition sulfalena allows to obtain a stable tablet sulfalena that meet all regulatory requirements.

The following examples illustrate the invention.

Example 1.

Sm oxypropylation (0.39 g). Wet weight granularit through a sieve, wet granulate is dried at a temperature of 505oWith up to a residual moisture of 2.5-3.5%. The dry weight of the grind on the granulator. For dusting mix the obtained granulate, 0.3 g of potato starch and 1.13 g of calcium stearate. Tabletow mass tabletirujut on the tablet press. Get 225 tablets with content in each tablet of 0.2 G4,7% sulfalena. The obtained tablets meet all the standards requirements Gosfarmakapei XI ed. and regulations on sulfalen, namely: average weight, g - 0,2432 (norm 0,257,5%, i.e. from 0,22313 to 0,2686); raspadaemost - 3 min (norm - "no more than 15 minutes"); height pills, mm - 2,87-3,05 (norm - 2,80,4); quantitative content sulfalena, g - 0,198 (the rate of 0.25 %, i.e. to 0.19 to 0.21); dissolution of, % - 95,1 ("75"); tablets, in addition, have a good compressive strength, kg/s - 5,3-6,9 (this indicator is not standardized).

Example 2.

Obtaining tablets sulfalena carried out as in example 1, on the basis of 50 g sulfalena substance of 11.7 g of corn starch, 0.65 g of oxypropylation and 1.35 g of magnesium stearate. Receive an average of 235 tablets sulfalena that meets all the requirements of normative documents, namely: the average weight of tablet - 0,2503 g; 8%.

1. Pharmaceutical composition having antimicrobial activity comprising as active principle an effective amount sulfalena and as the target additives potato starch and/or corn, oxypropylation and magnesium stearate and/or calcium in the following ratio of components, % by weight of active ingredient:

Potato starch and/or corn - 19,1-23,5

Oxypropylation - 0,7-1,4

Magnesium stearate and/or calcium - 2,2-2,8

2. The pharmaceutical composition under item 1, characterized in that it is made in the form of solid dosage forms.

3. The pharmaceutical composition according to paragraphs. 1 and 2, characterized in that it is made mainly in the form of tablets.

 

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