Antihistamine pharmaceutical composition

FIELD: medicine.

SUBSTANCE: the present innovation deals with applying antihistamine preparation named mebhydrolin. It is suggested to apply pharmaceutical composition that includes therapeutically efficient quantity of mebhydrolin and target additives as sugar, starch, polyvinyl pyrrolidone and salt of stearic acid. Pharmaceutical composition is designed in tableted form. The innovation provides correspondence of mebhydrolin tablets against all the standards of State pharmacopoeia XI, decreased quantity of additional substances and expiry period of 3 yr, not less.

EFFECT: higher efficiency of application.

5 cl, 3 ex, 2 tbl

 

The invention relates to medicine, specifically to the drug mebhydrolin (trade name diasorin, insidel, Emeril) (Mashkovsky PPM Medicines vol. 1, ed. 12-e, M, 1993, s.353)with antihistaminic activity and used in various allergic diseases (hay fever, urticaria, vasomotor rhinitis, itching dermatoses and other). Mebhydrolin is a blocker of H1receptors, but unlike most other drugs of the same do not have a sedative and hypnotic effect that can be used in cases where a dampening effect on the Central nervous system is undesirable. Usually the drug is well tolerated, but in some cases may cause irritation of the mucous membrane of the stomach and therefore is contraindicated in gastric ulcer and duodenal ulcer, inflammatory diseases of the gastrointestinal tract.

Due to unfavorable environmental conditions, malnutrition, poor quality of water and other number of allergic diseases increases, including among patients suffering from diseases of the gastrointestinal tract. Therefore, we search for conditions under which a dosage form of mebhydrolin, which would eliminate this undesired side effect.

In the patent of the Russian Federation 2121347, 1998 describes a pharmaceutical composition containing a combination of diazoline with zinc sulfate, which, as the authors state, combined have a synergistic effect. In specific examples of implementation of the present invention as excipients for solid dosage forms specified low-molecular polyvinylpyrrolidone, methylcellulose and magnesium stearate. In the patent of the Russian Federation 2140268, 1999, described the combination of diazoline with zinc sulfate, containing as special additives polyvinylpyrrolidone, potato starch and calcium stearate.

At the same time zinc-containing compounds have a strong and ambiguous effect on the patient's body caused by the participation of zinc in various physiological and pathological processes. When the domestic application of zinc, especially in children, marked adverse reactions (nausea, vomiting, heaviness and pain in the upper abdomen). Therefore, the use instead of diazoline its complex with other active ingredient (zinc sulfate) is not always acceptable.

The attempt to mitigate the adverse irritant effect diazoline, making it in the form of pellets, were not crowned with success. It is established that the bioavailability of diazoline in tablets relative to an oral ingested substance is 28-30% (Nazarov US, Tishchenkova IVAN, Halodule, Chem.-formats. zhurn., 25 (12), 11-13, 1991). Once taking the drug pharmacological effect occurs very slowly, which may be due to poor solubility of diazoline in the water. It should be noted that when the test Dissolve within 45 minutes of the tablets released less than 75% of diazoline that does not meet the requirements of the current RF Gosfarmakapei XI edition.

In the patent of the Russian Federation 2160095, 2000, proposed tablet diazoline, which is subjected to pelletizing the product of the interaction of the substance of diazoline with β-cyclodextrin in the presence of auxiliary substances: stearic acid, talc, starch and Aerosil in the following ratio to 1 tablet in g:

Diasorin0,046-0,054
β-Cyclodextrin0,13-0,15
Stearic acid0,0021-0,0025
Talc0,0063-0,0073
Starch0,0056-0,0065
Aerosil0,021-0,025

As stated in the patent, this arrangement allows to obtain tablets diazoline with high biological availability and significantly reduced in comparison with the substance and the other dosage form irritant effect on the mucous membrane of the stomach. However, the fault is m this composition is the excess of the individual requirements of Gosfarmakapei XI edition: the content of Aerosil in the tablet 10,081% (at the rate of not more than 10%), stearic acid - 1,008% (at the rate of not more than 1%), a large number of excipients on average 356,3% by weight of the active substance (desolina), as well as shelf life of 18 months.

The objective of the invention is to develop an antihistamine pharmaceutical compositions on the basis of mebhydrolin, which would comply with all regulatory requirements Gosfarmakapei XI ed., including percentage pills auxiliary substances, contained a smaller number of auxiliary substances and have a shelf life of not less than three years.

This is achieved antihistamine pharmaceutical composition comprising an effective amount of mebhydrolin and targeted supplements, which use sugar, starch, polyvinylpyrrolidone and a salt of stearic acid in the following ratio of components, % by weight of active ingredient:

Sugar84,8-105,6
Starch74,7-of 91.3
Polyvinylpyrrolidone16,2 is 21.8
Salt of stearic acid2,7-3,3

As sugar is mainly used milk sugar, starch suitable kartofelnye/or corn starch. As polyvinylpyrrolidone mainly use kollidon, as well as salts of stearic acid and magnesium or calcium salts.

The proposed ratio of the active substance and the target additives found experimentally and is optimal, meets all the requirements of Gosfarmakapei XI ed. and lets have a shelf life of mebhydrolin not less than 3 years (see table 2). In addition, the number of target components per unit of active ingredient (mebhydrolin) is an average of 200% (see table).

Going beyond the lower limit of the ratios of the basic substance and the target additives leads to deterioration of the technological parameters of the process of obtaining the dosage form of mebhydrolin, and the increase of target components is impractical, because it reduces the quality of some indicators pharmacopoeial product.

Dosage form of mebhydrolin made in the form of solid dosage forms, mainly in the form of tablets.

The obtained tablets meet all regulatory requirements and have a shelf life of not less than 3 years (see table 2).

Comparative Toxicological study on bioequivalence of mebhydrolin obtained according to the invention and of the reference preparation. Sub-chronic experiment conducted on randombred rats male with an average mass is th 229± 7, Compare the drugs were injected intragastrically at doses 35,0 (therapeutic) and 175,0 mg/kg once a day for 2 weeks. According to the results of the experiment in laboratory animals revealed no irritating effect on the mucous membrane of the gastrointestinal tract and material effect on the integral performance (weight gain, feed consumption, water and the General behavior of animals). The drugs tested doses did not cause structural abnormalities in organs and tissues.

Thus, studies, firstly, confirm the bioequivalence of actions preformed legform of mebhydrolin and reference drug on the animal organism, and secondly, the absence of irritants offer antihistamine pharmaceutical compositions of mebhydrolin.

The following examples illustrate the invention.

Example 1. A mixture of 100 g of powder of mebhydrolin, 83 g of corn starch and 96 g of milk sugar moistened with a 15%aqueous solution of polyvinylpyrolidone (18,15 g kollidon), mix until smooth and pass through a granulator. The granulate is dried at 30-50°to a residual moisture of 2.0 to 3.0%. The dried granules are passed through a granulator and optivault the calcium stearate in the amount of 2,73 g and tabletirujut on the press. Receive 1875 tablets with an average weight of each tablet 0.152 g, and the medium containing the receiving the tablets of 0.05 g of mebhydrolin. The obtained tablets comply with all requirements of Gosfarmakapei XI ed. and have a shelf life of over 3 years (see table 1).

Example 2. Obtaining tablets mebhydrolin carried out as in example 1 based on 100 g of mebhydrolin, of 91.3 g of potato starch, of 84.8 g of sugar, 16.2 g of kollidon and 2.7 g of magnesium stearate. Get 1793 tablets with an average weight of one tablet 0,147 g and an average content in one tablet 0,052 g mebhydrolin. The obtained tablets meet all regulatory requirements and have a shelf life of 3 years (see table 1).

Example 3. Obtaining tablets mebhydrolin carried out as in example 1 based on 100 g of mebhydrolin, to 74.7 g of potato starch, is 105.6 g of milk sugar, 21.8 g of kollidon and 3.2 g of magnesium stearate. Receive 977 tablets with an average weight of 0.31 g, and the average content in one tablet 0,098 g mebhydrolin. The resulting tablets have a shelf life of 3 years and meet all regulatory requirements (see table 1).

Table 1
To download components
№ p/pAdditives target
NameAmount, % by weight of active ingredient
Example 1Example 2Example 3
1Sugar96,084,8,5105,6
2Starch83,0for 91.374,7
3Polyvinylpyrrolidone18,116,221,8
4Salt of stearic acid2,92,73,3

Table 2
Quality tablets mebhydrolin
Name

quality score
Standards requirements

quality
The actual indicators
Example 1Example 2Example 3
Average weight0,15±17,5%, i.e. a0,1520,147
tablets, gfrom was 0.138 to 0,161
0,3±5%, i.e. a0,31
from 0,285 to 0,315
The deviation in mass20 of 20Ȋ
separate tabletsnot more than 5-1,8+1,9-1,9+2,1-2,2+2,1
from the average mass %
Raspadaemost, minNot more than 158610
Dissolution, %At least 75100,098,888,0
45 min
Strength, kgNot specified15,815,416,1
Contents megid-0,05±7,5%, i.e0,050,052-
rolina 1 tab., gfrom 0,046 to 0,054
0,1±5%, i.e. a--0,098
from 0,095 to 0,105
Salt of stearicNo more than 1%0,70,850,73
acid
The term g is desti 3 yearsmore than 3 years3 years3 years

1. Antihistamine pharmaceutical composition comprising as active ingredient mebhydrolin and target additives, characterized in that it contains a therapeutically effective amount of mebhydrolin, and the target additives, sugar, starch, polyvinylpyrrolidone and a salt of stearic acid in the following ratio of components, % by weight of active ingredient:

Sugar84,8-105,6
Starch74,7-of 91.3
Polyvinylpyrrolidone16,2 is 21.8
Salt of stearic acid2,7-3,3

2. The pharmaceutical composition according to claim 1, characterized in that the starch it contains potato and/or corn starch.

3. The pharmaceutical composition according to claim 1 or 2, characterized in that as the sugar it contains mainly lactose.

4. The pharmaceutical composition according to claim 1 or 2, characterized in that salts of stearic acid it contains magnesium or calcium salt.

5. The pharmaceutical composition according to claim 1, characterized in that it is made in the form of solid dosage forms.

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



 

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