Pharmaceutical composition having choleretic and anti-bacterial action, and how you can get

 

(57) Abstract:

The invention can be used to treat cholecystitis, hepatitis, as well as urinary tract infections and gastroenteritis. The composition comprises, by weight. % N-hydroxymethyl nicotinamide (Nikodin") - 81,0-96,4, starch - 3,0-15,0, stearic acid, 0.3 to 1.0, talc - 0,3-3,0. The composition may be in the form of tablets. The production method of the composition involves the following stages: wetting of the active substance starch paste, wet granulation, drying, dry granulation, the powder and the molding granules. Optimouse agent is a mixture of starch with stearic acid and talc. The mass ratio optimouse agent:dry granulate is 1:4,4-30,0. The preferred mass ratio in apadravya mixture of starch:stearic acid: talc is 4,8-13,0: 0,33-1,33: 1. The invention allows to generate the desired therapeutic concentration of the active substance in the body after taking the medicine. Legform has a shelf life of up to 3 years. The form has a high content of active substances, stable during storage and has a satisfactory strength. 2 S. and 2 C.p. f-crystals, 1 table.

The invention relates to the field of medicine and is suitable for treatment cholecystotomy names - nicodin, Melamed and others) is one of the main drugs used as a choleretic or antibacterial [Mashkovsky M. D. Medicines, T. 1, ed. 12-e, M,1993, S. 611]. As the last connection is most effective in infections caused by Escherichia coli.

Under the influence of moisture N-(hydroxymethyl)nicotinamide easily decomposes with evolution of formaldehyde, which leads to its instability during storage and the difficulty of obtaining a stable dosage forms based on it.

In U.S. patent N 2793158, 1957, describes a pharmaceutical composition comprising N-(hydroxymethyl)nicotinamide. However, it is in the form of an aqueous injection solution. To prevent side effects during storage of products of decomposition of N-(hydroxymethyl)nicotinamide in the composition is injected ureides hydroxy(polyhydroxy)aldehydes or polyhydroxylated. However, the application of the specified target additive in solid dosage form, it is impractical and, in addition, does not give the opportunity to get a quality tablet N-(hydroxymethyl)nicotinamide.

In the United Kingdom patent N 835474, 1960 shows an example of pharmaceutical COAs. including calcium carbonate, 30 wt. including starch. These ingredients moisturize sufficient quantity of a 10% starch paste. Wet pasta granularit, dried, crushed, optivault 2 wt. CH stearate and the mixture tabletirujut. However, in this composition as an active ingredient used is not N-(hydroxymethyl)nicotinamide, and quinolone derivative. Use in the new compositions based on N-(hydroxymethyl)nicotinamide specified ingredients does not ensure the stability of quality parameters during storage, resulting in the expiration date of the medicinal product does not exceed 6 months.

The objective of this invention is to provide pharmaceutical compositions with choleretic and anti-bacterial action in the form of a solid dosage form that contains as an active ingredient N-(hydroxymethyl)nicotinamide (latest content should be not less than 81%), meets the requirements of the pharmaceutical agent, sustained over a sufficiently long period (at least 3 years), and how it was received.

This objective is achieved in that the proposed pharmaceutical composition with gelegenheiten contains as excipients starch, stearic acid and talc in the following ratio of ingredients, wt.%:

N-(hydroxymethyl)nicotinamide - 81,0-96,4

Starch - 3,0-15,0,

Stearic acid is from 0.3 to 1.0,

Talc - 0,3-3,0.

The claimed ratio of ingredients is best found experimentally and ensures compliance of the composition requirements of the global Fund XI.

The combined use of N-(hydroxymethyl)nicotinamid as the target additives, starch, stearic acid and talc increases stability of the dosage form during storage, thus increasing its shelf life up to 3 years. In addition, the use of the above target components in the claimed proportions with the ability to provide satisfactory strength tablets and a high content of N-(hydroxymethyl)-nicotinamide in the dosage form. The latter, together with high raspadaemosti and release of the active substance after 45 minutes on Wednesday dissolution becomes more than 96% of N-(hydroxymethyl)nicotinamide (GF XI - not less than 75%), allows you to generate the desired therapeutic concentration of the active ingredient after administration of the dosage form.

Nesoblyudenie during storage.

The proposed pharmaceutical composition is in the form of solid dosage forms, preferably in tablet form that provides maximum adaptability subsequent packaging and precision dosing of the active substance.

The way to get a new pharmaceutical composition includes moisturizing active substances starch paste, wet granulation, drying, dry granulation, powder and molding the pellets at the same time as outrivaled agent, a mixture of the rest of starch with stearic acid and talc, and the mass ratio optimouse agent : dry granulate is 1 : 4,4-30,0. Use as outrivaled agent mixture of starch, stearic acid and talc when the claimed value outrivaled agent and the dry granulate provides good adhesion N-(hydroxymethyl)nicotinamide and auxiliary substances, which contributes to a significant increase in the durability of tablets and thereby reduces their rejection in the process of packing.

The preferred mass ratio of the part outrivaled agent starch, stearic acid and talc is(4,8-13,0): (0,33-1,33): 1 accordingly,. the tabletting process.

The obtained pharmaceutical composition complies with the requirements of the global Fund XI (in appearance, raspadaemosti, dissolution and other indicators), stable in storage and has a shelf life of over 3 years.

The invention is illustrated by the following examples (see Table).

Example 1. The sifted powder of N-(hydroxymethyl)nicotinamide (200,0 g) moisturize 66.5 g 2% starch paste, mix to a uniform distribution of moisture, granularit on the unit for the production of granulate through a grid hole diameter of 3 mm and dried to a residual moisture content of 2-3%. Dry granulation is performed on the device for producing granules of the dry mix through a mesh hole diameter 2 mm, Crushed granular optivault mixture 15,65 g of dry potato starch, 1.6 g of stearic acid and 1.2 g of talc (mass ratio optimouse agent : dry granulate is 1 : 10,8), then tabletirujut. Get 212,3 g of tablets with an average weight of 0.55 g, which satisfy the requirements of the pharmaceutical agent.

Example 2. The sifted powder M-(hydroxymethyl)nicotinamide (212,1 g) hydrate 1% starch paste in a mass ratio of 2.55:1, respectively. Subsequent operations are performed 1 : 30,0, and as outrivaled agent, a mixture of 5.7 g of starch, 0.65 g of stearic acid and 0.65 g of talc. The obtained tablets (211,2 g) satisfy the requirements of the pharmaceutical agent.

Example 3. Analogously to example 1 receive tablets from 178,2 g of N-(hydroxymethyl)nicotinamide and 2.5% starch paste. Download ingredients in outrivaled agent: starch of 31.2 g of stearic acid - 2.17 g of talc to 6.5, the Mass ratio of starch paste : N-(hydroxymethyl)nicotinamide is 1 : 3,35, and the mass ratio optimouse agent : dry granulate 1 : 4,4, respectively. The output of tablets that meet the requirements of the pharmaceutical agent is 211,2,

1. Pharmaceutical composition having choleretic and anti-bacterial action, which contains as active substance N-(hydroxymethyl)nicotinamide, characterized in that it additionally contains as special additives starch, stearic acid and talc in the following ratio of ingredients, wt.%:

N-(hydroxymethyl)nicotinamide - 81,0 - 96,4

Starch - 3,0 - 15,0

Stearic acid - 0,3 - 1,0

Talc - 0,3 - 3,0

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

3. The method receiving inim paste, wet granulation, drying, dry granulation, powder and molding the pellets at the same time as outrivaled agent, a mixture of starch with stearic acid and talc, and the mass ratio optimouse agent : dry granulate is 1:4,4-30,0.

4. The method according to p. 3, in which the mass ratio in apadravya mixture of starch : stearic acid : talc is(4,8 - 13,0) : (0,33 - 1,33) : 1 respectively.

 

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