Combined drug, analgesic, hypotensive and spasmolytic effect, the method of its production

 

(57) Abstract:

The invention relates to medicine, specifically to the combined drug, analgesic, hypotensive and spasmolytic effect, containing dipyrone, Dibazol, papaverine hydrochloride and phenobarbital and pharmaceutically acceptable additives target, which used starch, talc and stearic acid, and the method of its production. 2 S. and 3 C.p. f-crystals.

The invention relates to medicine, specifically to the combined drug, used for reduction of pain associated with spasm of the peripheral arteries, smooth muscles of the gastrointestinal tract, blood vessels, brain and arterial hypertension.

Non-narcotic drug - analgin (international nonproprietary name Metamizole sodium) in addition to anti-inflammatory and antipyretic actions has a strong analgesic effect. As is well soluble and easily absorbed product, it is particularly suitable for use in those cases when you need to quickly create a high blood concentration of the active substance that abuseable the ranks of the combined drugs [Mashkovsky M. D. Medicines, T. 1, ed. 12-e, M, 1993, S. 200].

It is known (patent RF 2138252, publ. 1999) analgesic agent in the form of tablets for oral use, including aspirin, phenobarbital, purine alkaloid (caffeine or caffeine sodium benzoate), an opium alkaloid (codeine or codeine phosphate) and excipients in the following ingredients, by weight.h. 1 wt.h. dipyrone:

Analgin - 1,0

Phenobarbital - 0,028-0,039

Purine alkaloid - 0,15-0,19

Alkaloid of opium is 0.023-0,031

Starch - 0,08-0,12

Magnesium stearate - of 0,005 0,009

However, in the case of other combinations of active ingredients with the same qualitative and quantitative composition of auxiliary substances get pills with quality indicators do not meet the requirements of the current Gosfarmakapei XI edition of the index raspadaemost".

In the patent of the Russian Federation 2157190, publ. 2000, describes a combination drug made in the form of tablets of the following composition, wt.h. 1 wt.h. dipyrone:

Analgin - 1,0

Phenobarbital - 0,028-0,039

Caffeine base - 0,147-0,188

Codeine base - 0,023-0,031

Naproxen - 0,062-0,377

Starch - 0,698-0,870

Microcrystalline cu and quantitative composition of auxiliary ingredients also allows you to get a tablet dosage form for a new active substance satisfactory quality.

There is information about using the combination of analgin, Dibazol, papaverine hydrochloride, and phenobarbital as an analgesic, hypotensive and antispasmodic [Mashkovsky M. D. Medicines, T. 1, ed. 12-e, M, 1993, S. 201]. However, data on the composition and the method of obtaining the dosage form not available.

The method of obtaining well-known drugs (RF patents 2138252, 2157190) includes hydrating a mixture of ingredients, wet granulation, drying and pelleting. As the humidifier solution using opium alkaloid (codeine) 3-7% starch paste. Application of the above method allows to achieve uniformity of dosage of active substances, however, imposes strict limits on the temperature, which is conducted humidity (40-60oC).

The basis of the invention is the creation of a combined drug, analgesic, hypotensive and spasmolytic action and is intended to be used in the form of solid dosage forms quick release of the active substance, which meets all the requirements of Gosfarmakapei XI edition (GF XI).

The technical result, the TES tool meets all requirements of the current Gosfarmakapei pharmaceutical drug, dissolves easily, which provides high bioavailability of incoming components and correspondingly high therapeutic effect, and stable in storage, and in that the sequence of operations and their technological options that allow you to produce a dosage form of the required quality.

This technical result is achieved by the fact that the claimed combination drug, analgesic, hypotensive and spasmolytic action comprises as active ingredient a combination of analgin, Dibazol, papaverine hydrochloride and phenobarbital and pharmaceutically acceptable additives target, which used starch, talc and stearic acid in the following ingredients, by weight.h. 1 wt.h. dipyrone:

Analgin - 1,0

Dibazol - 0,06-0,1

Papaverine hydrochloride - 0,06-0,1

Phenobarbital - 0,06-0,1

Starch - 0,14-0,22

Talc - 0,01-0,05

Stearic acid - 0,005-0,02

The proposed ratio of ingredients is best found experimentally and ensures compliance with quality indicators of the composition requirements of the global Fund XI.

Thanks statement is but improves the release of active ingredients and therefore allows you to create the desired therapeutic concentration of the combination of active substances after oral administration. At the same time achieved stability of indicators of the quality of the dosage form during storage, which ensures a shelf life of not less than 2.5 years.

The proposed pharmaceutical composition is in the form of solid dosage forms, preferably in the form of tablets, which ensures accurate dosing of the combination of active ingredients and ease of use.

The way to get a new pharmaceutical composition includes a wetting mixture of dipyrone, Dibazol, papaverine hydrochloride, phenobarbital and parts of starch starch paste and subsequent wet granulation, drying, dry granulation, adding talc and stearic acid, and molding the mixture.

The preferred amount of starch, administered in a formulation in dry form, is to 0.108-0,218 wt.h. 1 wt.h. dipyrone. The remaining quantity of starch is introduced into the structure of the humidifier - starch paste. The optimal concentration of the latter - 1,0-2,95 wt.% starch.

According to the proposed method, the operation of the humidification does not require strict temperature interval and can be performed without complications in the workshop temperature, for example 18-haspdinst, uniformity of dosage and other factors), stable in storage and has a shelf life of not less than 2.5 years.

The invention is illustrated by the following examples:

Example 1. Mix the sifted powders of dipyrone (150,0 g), Dibazol (12.0 g; 0.08 wt.h. 1 wt.h. dipyrone), papaverine hydrochloride (12.0 g; 0.08 wt. including 1 wt.h. dipyrone), phenobarbital (12.0 g; 0.08 wt.h. 1 wt. h dipyrone) and part of dry potato starch (24.8 g; 0,165 wt.h. 1 wt.h. dipyrone) moisturize 110g starch paste (from 2.2 g of starch), mix to a uniform moisture mass granularit on the unit for the production of granulate through a grid hole diameter of 2.5-3.0 mm and dried at a temperature of 30-45oC. Dry granulation is performed on the device for producing granules of dry mixes. It crushed the granulate add a mixture 5,91 g of talc (0,04 wt.h. 1 wt.h. dipyrone) and 1.48 g (0.01 wt. including 1 wt.h. dipyrone) of stearic acid and tabletirujut. Get tablets with an average weight of 0.37 g, which satisfy the requirements of normative documents on pharmaceutical agent.

Example 2. Mix the sifted powders of dipyrone (150,0 g), Dibazol (9.0 g; 0.06 wt.h. 1 wt.h. dipyrone), papaverine hydrochlorideapo starch (16.2 g; to 0.108 wt.h. 1 wt.h. dipyrone) moisturize 2,95% starch paste (the total number of corn starch - 21,0 g 0.14 wt.h. 1 wt.h. dipyrone). Subsequent operations are performed analogously to example 1, with the difference that to the dry crushed to granules add a mixture of 1.48 g (0.01 wt.h. 1 wt. h dipyrone) talc and 2.95 g (0.02 wt.h. 1 wt.h. dipyrone) stearic acid. The obtained tablets meet the requirements of normative documents on pharmaceutical agent.

Example 3. Analogously to example 1 receive tablets of 150 g of aspirin. Total consumption other ingredients: Dibazol - 15.0 g (0.1 wt.h. 1 wt. h dipyrone), papaverine hydrochloride - 9.0 g (0.06 wt.h. 1 wt.h. dipyrone), phenobarbital - 15.0 g (0.1 wt.h. 1 wt.h. dipyrone), potato starch - 33,0 g (0.22 wt.h. 1 wt.h. dipyrone), of which 0.3 g load in the form of 0.5% starch paste, talc - of 7.4 g (0.05 wt.h. 1 wt.h. dipyrone), stearic acid, 0.74 g (0.005 wt.h. 1 wt. h dipyrone). The obtained tablets satisfy regulatory requirements in the pharmaceutical agent.

1. Combined drug, analgesic, hypotensive and spasmolytic effect, which includes the quality is efticiency acceptable additives target, characterized in that as a pharmaceutically acceptable target additives it contains starch, talc and stearic acid in the following ingredients, by weight. including 1 wt. h dipyrone:

Analgin - 1,0

Dibazol - 0,06 - 0,1

Papaverine hydrochloride - 0,06 - 0,1

Phenobarbital - 0,06 - 0,1

Starch - 0,14 - 0,22

Talc - 0,01 - 0,05

Stearic acid - 0,005 - 0,02

2. Combined drug under item 1, characterized in that it is made in the form of tablets.

3. The method of obtaining a combined drug, characterized in PP. 1 and 2, which comprises moistening a mixture of dipyrone, Dibazol, papaverine hydrochloride, phenobarbital and parts of starch starch paste and subsequent wet granulation, drying, dry granulation, adding talc and stearic acid, and molding the mixture.

4. The method according to p. 3, characterized in that the starch is introduced into a formulation in dry form, is to 0.108-0,218 wt. including 1 wt. hours of dipyrone.

5. The method according to p. 3, characterized in that the concentration of starch paste is 1.0-2,95 wt. % starch.

 

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