Solid preparation of high absorption

FIELD: medicine.

SUBSTANCE: the present innovation deals with a solid antibacterial preparation that contains efficient quantity of sitafloxacin or its salt, or its hydrates, and tartaric acid at the quantity ranged 0.1-1 M/0.5-1 M sitafloxacin. Tartaric acid provides steady sitafloxacin absorption at high dosage out of digestive tract.

EFFECT: higher efficiency.

2 cl, 4 ex, 4 tbl

 

The scope of the invention

The present invention relates to a solid preparation containing the active ingredient, slightly soluble in water at pH values near neutral. In particular, the invention relates to a solid preparation having improved absorption from the digestive tract of the active ingredient, slightly soluble in water at pH values around neutral, and method for improving absorbability of such active ingredient from the digestive tract.

Background of the invention

Sitafloxacin [name based on international nonproprietary names (INN), will be used in the future] represents the connection (registered with the Japan patent No. 2714597)having the following chemical structure:

This compound has a very high antibacterial activity and is high security, resulting assumes that this connection, which is currently under development, will serve as an excellent quinolone synthetic antibacterial drug. Sitafloxacin, as accepted in Japan names (JAN)has been registered in the form of a 3/2 hydrate. This 3/2 hydrate can be used as raw sitafloxacin for the preparation of solid drug in this image is ateneu. However, it is also possible to use other source form containing sitafloxacin, such as its anhydride, additive salt with acid and carboxylate.

In recent years there is an increasing need to improve solid preparations for oral administration, aimed at making their use for patients more comfortable while reducing the number of doses. In fact, in recent years, have become the dominant ways superior to the introduction, in which patients can reduce the number of doses to such a low as once per day. In foreign countries, especially in European countries and the USA, are required, as a rule, solid preparations containing the active ingredient at a high concentration, because people in these countries are relatively larger in body shape (body weight). For this reason, it became necessary to receive solid drugs that have a high concentration of active ingredient in a single dose. However, it turned out that there are some problems, such as the absorption of the active ingredient from the digestive tract, which is insufficient, and the concentration of the active ingredient in the blood is unstable in a wide range, while such problems are absent in the case of other solid preparations in which the active ingredient contained in neb is Lishou concentration. For example, it is known that sitafloxacin has this tendency. More specifically, it became apparent that some patients who undergo treatment with conventional solid preparations containing sitafloxacin in high concentration, subject to the aforementioned problems associated with absorption by oral administration (absorption from the digestive tract).

As a method of improving the absorption from the digestive tract it is possible to rely on drugs, having a good ability to disintegrate per se. However, in the case sitafloxacin there is no particular problem when raspadaemosti, even when the solid preparation, and also it was confirmed that easy to get hard drugs with good raspadaemost. Thus, it was found that weak raspadaemost solid drug is not responsible for the lack of absorption from the digestive tract.

As other methods of increasing absorption from the digestive tract are the classic ways that can increase the solubility by processing the active agent, for example the method the fine dispersion of the active ingredient, the method of application of dispersed solids in high-molecular compound and method for producing clathrate derived from a cyclodextrin.

For antibiotics βvarnish is amego type there is a way with the help of which you can improve the absorption from the digestive tract using citric acid or cyclodextrin.

However, when using citric acid with sitafloxacin have any problems with compatibility with sitafloxacin. On the other hand, when the cyclodextrin, it is necessary that the composition contained a large quantity of this connection with the formation of clathrate. Consequently, the use of cyclodextrin is impractical.

The aim of the present invention, therefore, is the provision of a solid drug that contains the active ingredient at a high concentration and has no problems with absorption from the digestive tract, specifically, issues such as reducing the availability of the active ingredient due to low suction and a wide variation in the level of active ingredient in the blood.

Disclosure of inventions

In connection with the above circumstances, the applicant has conducted extensive research. In the result, it was found that uniform absorption of the active ingredient at a high dose of the digestive tract can be improved by adding an acidic ingredient.

Thus, the present invention provides a solid preparation comprising: a) at least one compound selected from chinolone the s compounds and their salts, and hydrates data quinolone compounds and salts and (b) tartaric acid.

The best way of carrying out the invention

The above quinolone compounds may be in free form, salt or hydrate of the free acid or salt.

Quinolone compound, its salt or hydrate of any of the above preferably represents a quinolone compound, slightly soluble in water at pH values around neutral (about pH 7,0).

In the solid preparation of the present invention the absorption of its active ingredient from the digestive tract increases with the inclusion of tartaric acid as a component of the solid drug. This method is applicable to obtain the drug with improved absorption of the medicinal product, in particular quinolone compounds whose absorption from the digestive tract becomes low when the pH around neutral (pH 7.0) due to poor solubility at this pH value. The term "slightly soluble" drug in the sense in which it is used here, can be interpreted as defined in the General regulations of the Pharmacopoeia of Japan. For example, slightly soluble drug is a drug, to which you can apply the definition of "slightly soluble" or "almost insoluble", as described in the rules. Such drug may be in any of the following forms, such as free-form, its salt or hydrate of any of the above.

Preferred examples of poorly quinolone compounds include sitafloxacin having a chemical structure represented by the following formula:

(i.e. (- )- 7-[(7S)-7-amino-5-azaspiro[2.4]heptane-5-yl]-8-chloro-6-fluoro-1-[(1R,2S)-2-fluoro-1-cyclopropyl]-1,4-dihydro-4-oxo-3-quinoline-carboxylic acid), its salts and their hydrates (free form or salt).

Preferred according to the present invention is a solid preparation containing as an active ingredient, at least one representative from sitafloxacin, its salts and hydrate sitafloxacin or its salts (free form salt and hydrate sitafloxacin can be together called "sitafloxacin"), and tartaric acid.

In relation to salt sitafloxacin, as an example we can mention the hydrochloride salt of sulfuric acid, nitric acid salt, a salt of phosphoric acid, salt of p-toluensulfonate acid, salt methanesulfonic acid, salt of fumaric acid and a salt of maleic acid. Examples of the hydrate sitafloxacin or its salt include 3/2 hydrate and dehydrate, which typically use a 3/2 hydrate.

Examples of quinolone compounds of weakly rest the action in water at pH values around neutral include, in addition to the above sitafloxacin, sparfloxacin and ciprofloxacin not in the form of hydrochloride.

The above solid product can be a tablet or capsule while the capsule is preferred.

The solid preparation of the present invention, which is obtained by adding organic acids (in particular, tartaric acid) to the active ingredient having a low solubility at neutral pH, but showing the increase in solubility at higher or lower pH than 7, is improved absorbability of the active ingredient and reduced fluctuations in its level in the blood.

In respect of tartaric acid, you can use the isomers such as d-tartaric acid, L-(+)-tartaric acid and racemic tartaric acid. Of them, preferred is d-tartaric acid, especially of pharmacopoeial quality.

The presence of tartaric acid in quantity, fold to 0.1 mol, 0.1 mol (18,3 g) together with 500 mg sitafloxacin (dehydrate) leads to a marked improving effect on the dissolution sitafloxacin. It was found that the effect becomes maximum when 0.5 mol (92 mg) tartaric acid is used in combination with 500 mg sitafloxacin in number by a multiple of 0.5 moles. Therefore, tartaric acid is preferably added in an amount of from 0.1 to 1 mol is, preferably from 1/6 mol to 0.7 mol, more preferably from 0.25 to 0.5 mol, especially from about 0.5 mol to 1 mol quinolone compounds, in particular, sitafloxacin.

Solid, containing tartaric acid drug sitafloxacin of the present invention can be obtained by using, as the other ingredients commonly used additives. In particular, include excipients such as lactose, corn starch, mannitol and discouny calcium phosphate, disintegrant, such as crystalline cellulose, sodium salt of cross-carmellose, nizkozameshhennoj hydroxypropylcellulose, calcium carboxymethyl cellulose, carboxymethyl cellulose and sodium carboxymethyl cellulose, lubricants such as magnesium stearate, calcium stearate, sodium stearate, fumaric acid and utverjdenie oil, covering agents, such as macrogol and titanium oxide, a binder such as hydroxypropylcellulose, polyvinyl alcohol and hypromellose, and fluidizing agents, such as talc. In practice, the solid preparation may be obtained in the usual way using them, if necessary in combination.

Capsules can be obtained by means of filling powder, namely a mixture of excipients, active ingredient, disintegrator, lubricant and fluidizing agent with a wine acid click filling of the capsules obtained mixture; or a way to fill granules, namely the formation of granules from excipient, primary drug (active ingredient) and binders (these granules can be coated), add disintegrant, lube fluidizing agent and tartaric acid, and filling capsules mixture. In this case, tartaric acid can be added after granulation separately from other fillers, and, if necessary, the application shell. Tartaric acid mixed with the active ingredient, can be pelletized. In the preparation of the granules can be applied dry granulation or wet granulation.

With regard to capsules, according to this invention can be used generally applicable. For example, they can be obtained from gelatin, hydroxypropylcellulose or starch shells. Of these gelatin capsules are preferred.

Tablets can be obtained one way of mixing excipient, active ingredient, disintegrant, lube and fluidizing agent with wine acid and pressing the mixture directly into tablets; or a method of obtaining pellets from excipient, the active ingredient and binder (these granules can be coated), the addition of tartaric acid and other ingredients to the obtained granules and presses the m resulting mixture into tablets. In the latter case, similarly to obtain granules for capsules, can be pelletized tartaric acid or can be pelletized tartaric acid with the active ingredient together. On the thus obtained uncoated tablets can be applied to the shell. The above-described methods for producing capsules or tablets are offered only as examples and the process of obtaining the solid preparation of the present invention is not limited to them.

Organic acid that is to be included, is preferably tartaric acid, but you can choose another organic acid. As such an acid, you can use any that is applied in the form of pharmaceutical compounds. Needless to say, that the acid should not cause any change in the composition during preparation. Examples of such acids include dicarboxylic acids having two carboxyl groups. Of them, preferred are dicarboxylic acid, the acid having one or more hydroxyl groups. Examples include fumaric acid, maleic acid, malonic acid and citric acid. You can use the monosodium salt of such acid.

In the following the present invention will be described in detail using specific examples. However, it should be borne in mind that the present invention is not limited to them.

) Receiving each drug and injection solution

Sitafloxacin (used hydrate sitafloxacin, in particular 3/2 hydrate) as an active ingredient and d-tartaric acid (Pharmacopoeia of Japan) in advance was dispersively (Fitzmill Pulverizer).

Example of preparation 1 (comparative example):

In the granulator/dryer fluidized bed (FLO-30) were loaded active ingredient (10,66 kg), sifted mannitol (11,20 kg), corn starch (4,440 kg) and nitrosamino hydroxypropylcellulose (1,500 kg). Granulation was performed while spraying an aqueous solution (about 6% wt./vol.), contains hydroxypropylcellulose (1,000 kg). After drying the obtained granules were sieved through sieve No. 16, thus obtained granules having the same size. The resulting homogeneous granules (28,80 kg), nitrosamino hydroxypropylcellulose (to 0.900 kg) and magnesium stearate (0.300 kg) was mixed in a V-shaped mixer. The resulting mixture was in the form of granules for tableting. These granules for tableting extruded on a rotating apparatus for making tablets (HP-RA) uncoated tablets in the form of drips, each weighing about 750 mg. Tablets were loaded in the apparatus for coating the shell (Perfect Coater). The membrane was applied by spraying 10% solution of the powder mixture for coating, OPADRY" (use, Inc.), thus obtained film-coated tablets, each weighing approximately 767 mg a table 1 ol who dstanley weight of the ingredients in the pill.

Table 1
IngredientQuantity per tablet (mg)
Sitafloxacin hydrate (sitafloxacin)266.5

(250)
D-mannitol280
Corn starch111
Nizkozameshhennoj hydroxypropylcellulose60
Hydroxypropylcellulose25
Magnesium stearate7.5
Total750
OPADRY OY-S-22845)17
Total767

Example of preparation 2 (example):

In the granulator/dryer fluidized bed (FLO-MINI) was loaded active ingredient (186,5 g), sifted mannitol (33,67 g) and crospovidone (12,60 g). Granulation was performed while spraying an aqueous solution (about 6% wt./vol.), contains hydroxypropylcellulose (7,910 g). After drying the obtained granules were sieved through sieve No. 16, thus obtained granules having the same size. The resulting homogeneous granules (240,7 g), crystalline cellulose (33,67 g, crosspovidone (53,55 g), d-tartaric acid (the Pharmacopoeia of Japan; 32,20 g), magnesium stearate (3,675 g) and talc (3,675 g) were mixed, thereby obtaining granules for tabletirovanie is. These granules for tableting extruded on odnopozova apparatus for making tablets (CT-II) in the disc-shaped tablets, each weighing approximately 525 mg Tablets were loaded in the apparatus for coating the shell (HCT-MINI), and deposited them 10% solution of the powder mixture for coating, OPADRY" (use, Inc.), thus obtained film-coated tablets, each weighing approximately 536 mg table 2 presents the weight of the ingredients in the pill.

Table 2
IngredientQuantity per tablet (mg)
Sitafloxacin hydrate266.5
D-mannitol48.1
Crystalline cellulose48.1
Crospovidon94.5
Hydroxypropylcellulose11.3
d-Tartaric acid (Pharmacopoeia of Japan)46.0
Magnesium stearate5.25
Talc5.25
Total525
OPADRY OY-S-22845)11.0
Total536

Example of preparation 3 (example):

Active ingredient (319,8 g) was loaded into the granulator/dryer fluidized bed (FLO-MINI). When spraying aq the solution (about 2% wt./vol.), contains Polysorbate-80 (4,320 g)were mixed. After drying the powder mixture was sieved through sieve No. 30, thereby was obtained a powder mixture having the same particle size. The resulting homogeneous powder mixture (324,1 g), d-tartaric acid (the Pharmacopoeia of Japan; 55,20 g), light silicic anhydride (0,360 g) and magnesium stearate (4,320 g) was mixed as a powder mixture for filling capsules. This powder mixture was filled in a capsule No. 0 by means of the apparatus for filling capsules (Dott Bonapace & Co.) so in one capsule was about 320 mg. table 3 presents the mass of the ingredients in the capsule.

Table 3
IngredientWeight per capsule (mg)
Sitafloxacin hydrate266.5
d-Tartaric acid46
Polysorbate-803.6
Light silicic anhydride0.3
Magnesium stearate3.6
In General320
White gelatin capsule No. 0 PR white

An example of obtaining injectable solution:

Active ingredient (533,0 g) and sodium chloride (2250 g) was added to water and is of jacci (210 l). To the resulting mixture portions was added hydrochloric acid (concentration: 1 mol/l; 1250 ml) followed by addition of water for injection (20 l) to dissolve first in last at room temperature. To the resulting solution was added a solution of sodium hydroxide (0.1 mol/l) to bring the pH to 4.0. Water for injection was added until the concentration sitafloxacin does not become equal to a predetermined. After membrane filtration, the resulting solution was poured into ampoules, followed by steam sterilization, high pressure at 121°C for 20 minutes

2) Test drugs

Conducted the following test raspadaemost tablets (product of example 1) without tartaric acid and containing sitafloxacin in high concentrations, tablets (preparation according to example 2), including tartaric acid and containing sitafloxacin in high concentrations, and capsules (product from example 3), including tartaric acid and containing sitafloxacin in high concentrations. These drugs were administered to people and compared bioavailability and its variations, as described below.

Test raspadaemost drugs

In accordance with the test raspadaemost General tests Pharmacopoeia of Japan, the test was performed using water as the fluid for testing.

Determining the concentration sitafloxacin in the plasma of human blood and it is hodoscopes:

a) determining the concentration of the preparation in example 1 in plasma:

Twenty-four healthy volunteers (12 men and 12 women) were randomly divided into groups (one group consisted of 6 volunteers). Each member of the group were injected 2 tablets of the preparation of example 1. After a period of time did intravenous injection (400 mg sitafloxacin). In each case, at appropriate intervals of time, the blood was collected within 48 hours after injection. Selected blood were analyzed by liquid chromatography to determine the concentration sitafloxacin in plasma.

b) determining the concentration of drugs in examples 2 and 3 in plasma:

Thirty healthy volunteers (18 men and 12 women) were randomly divided into groups (one group consisted of 6 volunteers). Each member of the group were injected 2 tablets of the drug in example 2 and 2 capsules of the drug according to example 3 and after a predefined time interval did intravenous injection (400 mg sitafloxacin). In each case, at appropriate intervals of time, the blood was collected within 48 hours after injection. Selected blood were analyzed by liquid chromatography to determine the concentration sitafloxacin in plasma.

(C) Determination of bioavailability:

Set values not exceeding the pre is eating definitions were taken at 0. The area under the curve concentration in plasma was determined by the method of trapezoids on concentrations in serum, determined within 48 h after injection of each of the drugs. The ratio of each of the areas under the curve concentration in plasma for the preparations of examples 1, 2 and 3, equal to 1.25, the area under the curve concentration in the blood plasma while injecting meant as apparent bioavailability. At the same time was determined by fluctuations in the apparent bioavailability among individuals. The results are presented in table 4.

Table 4
Drug/indexThe preparation of example 1: a pill that does not contain tartaric acidThe preparation according to example 2: a pill that contains tartaric acidThe product from example 3: a capsule containing tartaric acid
The time spent on raspadaemost (min)3-5 min3-4 min3-5 min
Bioavailability68%87%87%
Fluctuations38%23%19%

As shown in table 4, it was found that there is no difference in raspadaemosti among drugs, but containing the other acid drugs (examples 2 and 3) showed a significant increase bioavailability and reduce its fluctuations, compared with not containing tartaric acid of the drug (for example 1).

The method of application in industry.

The present invention provides a solid preparation that can reduce the failure and instability of absorption of the drug containing the active ingredient at a high concentration, from the digestive tract so that it is possible to reduce the number of doses, and thus it becomes more convenient for patients. In addition, the present invention provides a solid preparation containing the active ingredient at a high concentration, for patients with large body shape (body weight).

1. Solid antibacterial preparation containing an effective amount sitafloxacin, represented by the following formula:

or its salts or its hydrates and tartaric acid in an amount of 0.1 - 1 mol 0.5 - 1 mol sitafloxacin.

2. The solid preparation according to claim 1, which is in the form of tablets or capsules.

3. The solid preparation according to claim 1, which is in the form of capsules.



 

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