Pharmaceutical composition for allergic diseases

FIELD: medicine.

SUBSTANCE: invention refers to medicine, particularly the preparation fexofenadine for allergic diseases. The pharmaceutical composition contains an effective amount of fexofenadine as an active ingredient, and excipients - hydroxypropyl cellulose, a filler, desintegrant glidant, a solubiliser and stearic acid salt. The filler represents a combination of lactose and starch. As glidant, the composition contains colloidal silicon dioxide.

EFFECT: pharmaceutical composition is presented in the form of tablets and is characterised by a high degree of release of the active substance and storage stability.

7 cl, 1 tbl, 3 ex

 

The invention relates to medicine, specifically to the drug Fexofenadine. Fexofenadin belongs to the third generation reseating antihistamines, its structure is close to antihistamine drug terfenadine, moreover, is its metabolite. Studies of the pharmacological properties of Fexofenadine conducted over the last ten years, it was found that it selectively blocks the peripheral histamine H1-receptors stabilizes the membranes of the fat cells prevents the release of histamine. Eliminate Allergy symptoms: sneezing, rhinorrhea, itching, redness and watery eyes. Antihistamine effect by 1 hour after ingestion, reaches its maximum after 2-3 hours and lasts for 12 hours or more. Within 28 days not seen the development of tolerance. Does not holino - adrenolytic, sedative action. Does not cause changes in calcium and potassium channels, of the QT interval. Inhibits bronchoconstriction caused by histamine. In experimental studies have been found carcinogenic, mutagenic and teratogenic effects (encyclopedia of medicine", Moscow, LLC "radar-2005", 2004, s-898).

Many antihistamines cause such side effects as dry mouth, sedation, gastrointestinal disorders, constipation or dia is it and terfenadine, having substantially reduced such effects, causes other side effects: cardiac arrhythmia, including ventricular tachyarrhythmia, Torsade de pointes and ventricular fibrillation. Recently, practitioners in the clinics of the increasing number of cases of cardiac arrhythmia in a joint introduction of terfenadine with other drugs, for example with ketoconazole, erythromycin, or overdose of terfenadine (Brian P. Monahan et al., JAMA, 5thDec 1990, Vol.264, N21, pp.2788-2790). So there was a search of the drug with the advantages of terfenadine, but which would not have the aforementioned disadvantages.

In the patent of the Russian Federation 2167657, 2001 (the equivalent of U.S. patent 5375693, 1994) proposed for treatment of allergic diseases metabolites of terfenadine and their optically pure isomers. One of these metabolites and is fexofenadin. In this patent it is shown that fexofenadin in therapeutically effective amounts not prone to cause cardiac arrhythmia.

Positive properties of Fexofenadine as antihistamine drug allowed him to enter the world pharmaceutical market, but the domestic manufacturers of the drug is not performed.

Given the positive pharmacological properties of Fexofenadine that distinguishes it from other antihistamines, n is the necessity of its introduction into the Russian market urgent problem is the development of the pharmaceutical compositions of Fexofenadine.

In French patent 2453854, 1980, describes derivatives of ω-(4-diphenylbutylpiperidines)-2-phenylalkanoic, method of their production and use as antihistamines. Secure yourself compounds, their pharmaceutically acceptable salts and optical isomers. Compounds used as antihistamine drugs in a daily dose of 0.01-20 mg/kg body weight, for example, in the form of tablets containing 1-50 mg of the active component 1-4 times a day. However, the specific example fexofenadina only given a suspension for aerosol.

In the patent of the Russian Federation 2167657, 2001 describes the metabolites of terfenadine and their optically pure isomers for the treatment of allergic diseases. In the examples described methods for obtaining optically pure metabolite of terfenadine, the activity of compounds against H1 receptors, it was shown that fexofenadin not prone to cause cardiac arrhythmia, the generalized examples of making gelatin capsules and tablets containing fexofenadin. Getting the tablets described literally as follows. The active ingredient, which can be a instead of (R)-terfenadinecyclosporine (S)-terminalinmarsat or the racemic turbinegeneration, sieved and mixed with lactose to education odnorodnymi. Add appropriate amount of water and powder granularit. After drying, the granules are sieved and mixed with magnesium stearate. The resulting granules are compressed into tablets of the desired shape. In table 4 of the patent of the Russian Federation 2167657 the following formulations of tablets containing fexofenadin.

CompositionQuantity per tablet, mg
AndIn
Active ingredient - (R)-terminalinmarsat30,060,090,0
Functional filler168,5138,5108,5
(lactose, starch, including
pre gelatinizing)
Magnesium stearate1,51,51,5
The mass is pressed200,0200,0200,0

However, the known composition unsuitable for coating the shell, although there are indications that in ≤2% of patients treated with Fexofenadine, observed side effects gastro-intestinal tract - nausea, dyspepsia, constipation and other ("encyclopedia of drugs," ibid.). Also known composition is characterized by poor release of the active substance.

In the patent of Russian Federation №2283649 described pharmaceutical composition for treating allergic diseases comprising a therapeutically effective amount of Fexofenadine and excipient - excipient (lactose, or milk sugar, microcrystalline cellulose), polyvinylpyrrolidone, disintegrant (crosscarmellose sodium) and salt of stearic acid. The composition is characterized by rapid raspadaemost, but unstable during storage, in particular significantly reduced the release of the active substance.

The objective of this invention to provide pharmaceutical compositions of Fexofenadine with a high degree of release of the active substance and stable during storage,

To solve this problem is proposed pharmaceutical composition for the treatment of allergic dis is evani, comprising as active ingredient a therapeutically effective amount of Fexofenadine and as auxiliary agents hydroxypropylcellulose, filler, disintegrant and salt of stearic acid, characterized in that it contains as a filler combination of lactose and starch, and optionally a solubilizer and as glidant silica colloid in the following ratio of ingredients, parts by weight to 1 parts by weight of active substance.

Hydroxypropylcelluloseof 0.005 to 0.15
The filler in the form of a combination of lactose and starchof 0.2-1.4
Disintegrant0,03-0,2
Silicon dioxide colloidal0,006-0,2
The solubilizerof 0.002 to 0.05
Salt of stearic acid0,004-0,03

The phrase "therapeutically effective amount" means such amount of Fexofenadine, which provides favorable therapeutic effect with antihistamine treatment, including treatment or assistance in allergic diseases. Fexofenadin pre is respectfully used in the form of hydrochloride.

As auxiliary substances in obtaining tablets-kernel selected filler, disintegrant, hydroxypropylcellulose, glidant, a solubilizer and a salt of stearic acid. More preferably hydroxypropylcellulose (or hyprolose) is introduced into the composition in an amount 0,008-0,12 M.Ch. 1 M.Ch. active substance.

The filler preferably is applied lactose, for example, in the form of a monohydrate, starch (including modified, for example Pregelatinised starch, more preferably applies a combination of lactose monohydrate and pregelatinization starch. Can also be used microcrystalline cellulose,

As disintegrant can be used sodium carboxymethyl starch, crosspovidone or croscarmellose sodium, preferably carboximetilkrahmal sodium.

As glidant it is preferable to use colloidal silicon dioxide, can also be used silica methylated, talc, or a combination of glidants, as a solubilizer, preferably using ionic surfactant, preferably sodium lauryl sulfate as the salt of stearic acid is preferably used magnesium or calcium salts.

The proposed ratio of active substances and auxiliary is exectv found experimentally and is optimal. The proposed arrangement provides a high degree of release of the active substance and, consequently, its high bioavailability. The release of Fexofenadine of the new composition is more than 90% (according to the requirements of Gosfarmakapei XI edition - not less than 75%), while the inventive composition is stable during storage, including exhibits stability in terms of Release of the active substance in contrast to the prototype. So, after 2 years of storage contents of Fexofenadine and impurities corresponds to the initial values and the release of the active substance is 97-99 wt.%.

The proposed composition is performed in a solid dosage form, mainly in the form of tablets. If necessary, the tablet is covered with a shell.

Preferably the shell is based on a derivative of cellulose, more preferably a mixture of hydroxypropylmethylcellulose and hydroxypropylcellulose. The use of a mixture of hydroxypropylmethylcellulose and hydroxypropylcellulose in the composition of the shell enhances the adhesion of the film to the nucleus and increases the moisture resistant properties of the coating.

In the most preferred embodiment, the gastro-soluble shell contains hypromellose, hydroxypropylcellulose, polyethylene glycol-6000, glycerol, talc, dye.

As the dye can is to be used by titanium dioxide, iron(III) oxide red, iron oxide yellow, or preferably a combination thereof, providing a more pleasant perception of color. The combination of hydroxypropylcellulose and hydroxypropylmethylcellulose provides better adhesion.

Tablet Fexofenadine get known method of wet granulation. The preferred content of Fexofenadine (as hydrochloride) in a unit dose of 0.12 g ± 5% or 0.18 g ± 5%.

Examples illustrating the invention are presented in the table.

Example 1. A mixture of Fexofenadine (as hydrochloride), filler and disintegrant hydrate aqueous solution of hydroxypropylcellulose, which contains a solubilizer for the installation of the fluidized bed, the resulting granulate is dried, sieved through a metal sieve and sieved to granulate consistently add glidant and salt of stearic acid under stirring and the resulting mixture tabletirujut on a tablet press. The content of Fexofenadine hydrochloride - 0,120 g (the average weight of tablets 0.24 g), the content of impurities (HPLC) 0,061%. The strength of the tablets - 18 kg, raspadaemost - 1 min, dissolution 99% of Fexofenadine (after 45 min, the environment, 0.001 M HCl).

Composition for gastric-soluble coating is prepared as follows. A mixture of 14.4 g of hydroxypropylmethylcellulose and 4.8 g of hydroxypropy the cellulose while stirring, pour in 260 g of water and leave to swell under stirring (a). Separately prepare a solution of polyethylene glycol-6000 from 4.8 g of dry matter and 43 ml of water (b). Mix of 8.4 g of 3.45 g of titanium dioxide, 0,096 g iron oxide yellow, 0,056 g of iron(III) oxide red, a solution of polyethylene glycol (b) and 4.0 g of glycerol (in). The mixture is stirred until smooth and transfer to a vessel with a mass of (a), the capacity under (C) washed twice with water and 28 ml, the washing water is also placed in the vessel with a mass of (a), thoroughly mixed, and used for coating the tablet cores to produce a uniform coating with an average weight gain of the tablets approximately 3.4 to 3.7%.

Examples 2, 3 perform similarly, with the difference that in example 2, the content of Fexofenadine hydrochloride is 0,180, Received tablet Fexofenadine have a shelf life of more than 2 years. After 2 years of storage contents of Fexofenadine hydrochloride is 0,120 g (or 0,180 g for example 2), impurities, % (HPLC) - to 0.060-0,061, dissolution, % active ingredient after 45 min - 97-99.

Conducted Toxicological investigation of drug Fexofenadine obtained according to the invention. The study was conducted with the use of modern physiological, biochemical, hematological and histological methods in accordance with the requirements of FC RF Ministry of health. The drug was administered intragastrically in a water suspension daily what UPE once daily for 2 weeks at a dose of 200 mg/kg, a tenfold excess of therapeutic dose for rats and 70 times for the people in mg/kg based On the experimental results in laboratory animals revealed no irritating effect on the mucous membrane of the gastro-intestinal tract, and significant effects on integral performance (weight gain, feed consumption, water and the General behavior of animals). Drug tested doses did not cause structural abnormalities in organs and tissues.

Thus, the obtained experimental data confirm the absence of irritants offer antihistamine pharmaceutical compositions of Fexofenadine.

IngredientsThe content by mass in parts of Fexofenadine
Examples
123
Fexofenadin111
Hydroxypropylcellulose0,040,0050,15
Filler0,78 1,40,2
Disintegrant0,120,030,2
Glidant0,020,20,06
The solubilizer0,010,0020,05
Salt of stearic acid0,020,0050,03

1. Pharmaceutical composition for treating allergic diseases comprising as active ingredient a therapeutically effective amount of Fexofenadine and as auxiliary agents hydroxypropylcellulose, filler, disintegrant and salt of stearic acid, characterized in that it contains as a filler combination of lactose and starch, and optionally a solubilizer and as glidant - silica colloid in the following ratio of ingredients, by mass, per 1 parts by weight of active substance:

Hydroxypropylcelluloseof 0.005 to 0.15
A filler comb the nation lactose and starch of 0.2-1.4
Disintegrant0,03-0,2
Silicon dioxide colloidal0,006-0,2
The solubilizerof 0.002 to 0.05
Salt of stearic acid0,004-0,03

2. The pharmaceutical composition according to claim 1, characterized in that it contains fexofenadin as hydrochloride.

3. The pharmaceutical composition according to claim 2, characterized in that it contains lactose monohydrate form and starch in the form of pregelatinization starch.

4. The pharmaceutical composition according to claim 3, characterized in that it is made in the form of tablets.

5. The pharmaceutical composition according to claim 4, characterized in that it contains fexofenadin in the amount of 0.12 g ± 5%.

6. The pharmaceutical composition according to claim 4, characterized in that it contains fexofenadin in the amount of 0.18 g ± 5%.

7. The pharmaceutical composition according to claim 5 or 6, characterized in that it is made in the form of tablets, coated.



 

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