Dosage form with bacteriostatic action, and method of its manufacture

 

(57) Abstract:

The invention relates to the pharmaceutical field, in particular to solid dosage forms of the drug, with bacteriostatic action, and can be used in a variety of infections, especially respiratory, urogenital, skin and soft tissues. The invention lies in the fact that the core of the dosage form contains the following components roxithromycin, hydroxypropylcellulose, milk sugar, potato starch, calcium stearinovokisly, talc, and the shell contains the following components: one component selected from the group containing hypromellose, hydroxypropylcellulose and water-soluble methylcellulose, tween-80, titanium dioxide. Disclosed is also a method of manufacturing the aforementioned dosage forms. The invention provides a receiving dosage forms with improved pharmacokinetic and microbiological parameters. 2 N. p. F.-ly, 1 table.

The invention relates to medicine, in particular to a pharmacy, can be used in the manufacture of solid dosage forms of drugs with bacteriostatic action, in particular to macrolide antibiotics and disorders of protein synthesis, and can be used in a variety of infections, especially respiratory, urogenital, skin and soft tissues.

Known solid pharmaceutical composition with controlled release of medicinal products for oral use, comprising a therapeutically effective amount of at least one of the basic drug having a solubility in water less than 1 hour to 30 hours of water, a water-soluble alginate salt, a complex salt of alginic acid and an effective amount of an organic carboxylic acid to facilitate dissolution of the drug. As the primary drug form contains a drug selected from the group of macrolides - roxithromycin (see EN 2142793).

The closest to the invention is a pharmaceutical form with bacteriostatic action, which is a tablet compressed from granules, each of which includes a core containing as active substance roxithromycin and as an auxiliary substance polypropylenglycol, and a shell containing phthalate or succinate hydroxypropylmethylcellulose or other polymers (EN 2085190, 27.07.97).

The way the floor is the first tool, granulation of the obtained hydrated mixture, coating granules shell, then the granulate is dried, optivault and tabletirujut.

The disadvantages described dosage form, and method of its manufacture is that the drug has a low anti-inflammatory activity, and auxiliary substances used in this form have a high cost and difficult for mass production of medicines, and the method of manufacture is quite complicated.

The objective of the invention is the elimination of all the above drawbacks.

The problem is solved dosage form with bacteriostatic action, consisting of a kernel, containing as the active roxithromycin and excipients, and dissolving in the stomach of the shell in which the core contains as excipients hydroxypropylcellulose, starch, talc, calcium stearinovokisly and milk sugar, wt.%:

Roxithromycin 30-85

Hydroxypropylcellulose 4-10

milk sugar 5-22

starch 5-35

calcium stearinovokisly of 0.5-1.5

talc 0.5 to 1.5

and the shell contains xiphopenaeus and water-soluble methylcellulose, in the following ratio, wt.%:

the hypromellose, or hydroxypropylcellulose

or the water-soluble methylcellulose 30,0-84,0

tween-80 10,0-45,0

titanium dioxide 5,0-25,0

The task is also solved by a method of manufacturing a dosage form with bacteriostatic action, in accordance with which mix roxithromycin, milk sugar, starch, and the resulting mixture is moistened with a solution of hydroxypropylcellulose, re-mix, damp granulation, subsequent drying, dry granulation, the powder mixture hydroxypropylcellulose, potato starch, calcium stearinovokisly and talc, followed by pelletizing and coating shell of an aqueous suspension containing tween-80, titanium dioxide, and one component selected from the group containing hypromellose, hydroxypropylcellulose and water-soluble methylcellulose.

The invention consists in the following.

Roxithromycin the first semi-synthetic 14-membered macrolide "new" generation. Is erythromycin A, chemically, is a erythromycin a-9-who fostered him from erythromycin, give it a higher acid resistance, improved pharmacokinetic and microbiological parameters.

Like all other macrolide antibiotics roxithromycin implements its antibacterial action by binding to the 50S-subunit of the ribosome of the microbial cells and disruption of protein synthesis. It was found that its affinity to the binding site is less than that of erythromycin. However, this disadvantage is offset by higher concentrations of roxithromycin in tissues and body fluids, which are achieved with the improved parameters of absorption and distribution.

Its content in the dosage form to obtain a therapeutic dose should be from 30.0 to 85.0 wt.%.

As auxiliary substances forming the tablet, use hydroxypropylcellulose, milk sugar, potato starch, stearinovokisly calcium and medical talc, and as a substance forming the shell, use titanium dioxide, tween-80 and one component selected from the group containing hypromellose, hydroxypropylcellulose and water-soluble methylcellulose.

Data supplements allow you to get Leka who obrany thus, in order to protect the product from external influences and rapid absorption of roxithromycin after oral administration.

The set of operations in the way and their modes are selected in such a way as to simplify the method of manufacturing dosage forms without compromising their quality. Dry granulation allows you to standardize the weight of the drug particle sizes, which ensures uniformity of tablets by weight.

The invention is carried out as follows.

Get pills roxithromycin coated 0.05 g, 0.10 g and 0.15 g

Pre-sifted to 106.0 kg roxithromycin, 21,2 kg of sugar of milk, 18,0 kg of dry potato starch are thoroughly mixed and moistened with a 10% solution of hydroxypropylcellulose in the number of 31.8 kg, mix to a uniform moisture and granularit.

The wet granules are dried at a temperature of 50 to 55°C to a residual moisture of 3-4%.

The dried pellets are cooled to room temperature and conduct a dry granulation. Dry the granulate in the number 142,0 kg optivault adding pre-sifted hydroxypropylcellulose 9,4 kg of dry potato starch 11.6 kg, calcium, stearine is the tablet mass tabletirujut, receiving tablets-kernel biconvex shape with a diameter of 60.2 mm) to 0.05 g (80.2 mm) for 0,100 g (90.3 mm) for 0,150 g and a weight of 0.08 g, 0.16 g, 0.24 g in the amount of 162,5 kg

For coating the tablet cores using a water suspension containing 2.9 kg of hydroxypropylmethylcellulose, 1.86 kg of tween-80, 0,640 kg of titanium dioxide.

The application shell stop once the desired weight of the tablet. Get 165,6 kg of tablets.

The weight of the coated tablet is 0.0825 g, 0,165 g, 0,2475 g

The following table shows the composition obtained in accordance with the present invention pills.

This dosage form is characterized by a high acid resistance, improved pharmacokinetic and microbiological parameters.

1. Dosage form with bacteriostatic action, consisting of a kernel, containing as the active roxithromycin and excipients, and dissolving in the stomach of the shell, wherein the core additionally contains as excipients hydroxypropylcellulose, starch, talc, calcium stearinovokisly and milk sugar, wt.%:

Roxithromycin 30-85

Talc 0.5 To 1.5

and the shell contains titanium dioxide, tween-80 and one component selected from the group containing hypromellose, hydroxypropylcellulose and methylcellulose soluble in the following ratio, wt.%:

The Hypromellose,

hydroxypropylcellulose and

the water-soluble methylcellulose 30,0-84,0

Tween-80 10,0-45,0

Titanium dioxide 5,0-25,0

2. A method of manufacturing a dosage form with bacteriostatic action, which consists in the fact that mix roxithromycin, milk sugar, starch, the resulting mixture is moistened with a solution of hydroxypropylcellulose, re-mix, damp granulation, subsequent drying, dry granulation, the powder mixture hydroxypropylcellulose, starch, calcium stearinovokisly and talc, followed by pelletizing and coating shell of an aqueous suspension containing tween-80, titanium dioxide, and one component selected from the group containing hypromellose, hydroxypropylcellulose and water-soluble methylcellulose.



 

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