Pharmaceutical composition with anti-diarrhea effect

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to pharmaceutical compositions with anti-diarrheic effect. Pharmaceutical composition comprises the therapeutically effective amount of loperamide hydrochloride as an active component and special additives. Lactose, starch, aerosil, talk and stearate are used as special additives. Pharmaceutical composition is prepared in the form of solid gelatinous capsules. Loperamide capsules satisfy all requirement of the State Pharmacopoeia of XI Edition. Invention provides bioavailability of the pharmaceutical composition of loperamide capsules at the level 98.5%.

EFFECT: improved and valuable pharmaceutical properties of composition.

3 cl, 1 tbl, 3 ex

 

The invention relates to medicine, specifically to drugs with anti-diarrhoeal effect.

Widespread in medical practice in recent years has received loperamide as a symptomatic treatment for acute and chronic diarrhea.

According to literature data, the most common form of loperamide are bikinie tablets containing layer of loperamide and layer simeticone (polydimethylsiloxane). Thus, in European patent EP 0428296, 1991, shows the composition for chewing bisloinoi tablets and bisloinoi pill to swallow. The ratio of semicolon: loperamide ranges from 100:1 to 10:1. In chewing bisloinoi tablet layer simeticone consists of dicalcium phosphate, colloidal silicon dioxide, simethicone, stearic acid, aspartame and flavor additives. The layer of loperamide along with loperamide hydrochloride contains sugar, mannitol, stearic acid, colloidal silicon dioxide, aspartame and flavor additives. Layer simeticone in bisloinoi pill to swallow contains the first four components, and instead of aspartame and flavor additives in the layer is enabled nitroglycol starch. In the layer loperamide instead of aspartame and flavor additives included microcrystalline cellulose and nitroglycol starch. The patent describes a technology of manufacturing is the service tablets which is rather time-consuming nature: separate granulation is carried out simeticone and separate loperamide, and then the granules of loperamide and simeticone pressed as separate layers with the use of a press for belayneh tablets. Complex composition and rather laborious method of manufacturing belayneh compositions have not found use in medical practice.

Describes the composition and method of preparing solid dosage forms of loperamide for oral administration (international application WO 92/02223, 1992). The composition contains from 0.1 to 5.0% of loperamide and from 95,0 to 99.9% of pharmaceutically acceptable additives. The tablet includes the following components, wt.%:

Loperamide hydrochloride- 0,80
Polyvinylpyrrolidone- 4,00
Nitroglycol starch- 4,00
Microcrystalline cellulose- 90,95
Magnesium stearate- 0,25

The process of making tablets is also rather time-consuming: loperamide hydrochloride is dissolved in ethanol to obtain a true solution. Then a mixture of polyvinylpyrrolidone, matriptase starch and microcrystalline cellulose is granulated with an alcoholic solution of loperamide hydrochlo the IDA. Next, the composition is dried in the fluidized bed and sifted through a sieve, then add the magnesium stearate, and the composition is compressed into tablets.

Described pharmaceutical composition of loperamide (U.S. Pat. Of the Russian Federation No. 2172172, 2002), made in the form of capsules containing an effective amount of loperamide and special additive in the following ratio of components, % by weight of active ingredient:

Lactose- 4500-5500
Potato starch and/or corn- 1350-1650
Stearic acid- 180-220
Polyvinylpyrrolidone- 180-220

The disadvantage of this composition are encountered when scaling unstable results for the quantitative determination of loperamide hydorchloride capsule mixture.

The objective of the invention is a pharmaceutical composition loperamide made in the form of capsules, which allow to obtain stable results for the quantitative determination of loperamide hydrochloride in capsule mixture when zooming in conditions of industrial production.

This is achieved by using a pharmaceutical composition containing as active ingredient a therapeutically effective amount of loperamide is of hydrochloride and target additive in a certain ratio. As the target additives used lactose, starch, Aerosil, talc and salt of stearic acid in the amount 62,0-76,0 wt. including 1 wt. including the active substance in the following ratio, wt. including 1 wt. hours of active ingredient:

Lactoseand 47.0-of 57.5
Starch- 13,5-16,5
Aerosil- 0,3-0,4
Talc- 0,6-0,8
Salt of stearic acid- 0,6-0,8

As use corn starch and/or potato starch, 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, allowing to obtain stable results for the quantitative determination of loperamide hydrochloride in capsule when zooming, and the transition to industrial production of capsules loperamide. In addition, the inventive pharmaceutical composition ensures compliance with all requirements of the current Gosfarmakapei XI publications, including, for example, uniformity of capsule mixture when considering the naked eye, the deviation in the determination of the average mass of capsules composition is employed: to 0.1 g - ±15%, from 0.11 to 0.30 g - ±10%, etc.

The pharmaceutical composition of antidiarrheal actions made in the form of hard gelatin capsules filled with a homogeneous mixture of powders of loperamide hydrochloride and special additives.

The following examples illustrate the invention.

Example 1. (Trust supplements - 62,0 wt. including 1 wt. including the active substance, see Table 1).

In the mixer and mixed until uniform distribution of the ingredients of 0.2 g of loperamide hydrochloride, 9,40 g of lactose, 2.70 g of potato starch, 0.06 g of Aerosil, 0.12 g of magnesium stearate and 0.12 g of talc. By visual examination with the naked eye capsule mixture has a homogeneous character. Encapsulation mixture into hard gelatin capsules to produce a machine for encapsulation. Receive an average of 84 capsules with each capsule 0.002 g ±5% of loperamide hydrochloride, fully meet the requirements of Gosfarmakapei XI ed.

Example 2. (Trust supplements - 76,0 wt. including 1 wt. including the active substance, see Table 1).

Getting capsules loperamide hydrochloride carried out as in example 1, based on 200 g of loperamide hydrochloride, 11500 g of lactose, 3300 g of corn starch 80 g of Aerosil, 160 g of talc and 160 g of calcium stearate. Get 92500 capsules with each capsule 0.002 g ±5% of loperamide hydrochloride. The obtained capsules meet the requirement of the requirements of Gosfarmakapei XI ed. (capsule uniformity of the mixture, the deviation in the determination of the average weight of powder less than 10%). The composition of the capsule mixture is stable under scaling.

Example 3. (Trust supplements - 69,0 wt. including 1 wt. including the active substance, see Table 1).

Getting capsules loperamide carried out as in example 1, on the basis of 20 kg of loperamide hydrochloride, 1045 kg of lactose, 300 kg of corn starch, 7 kg of Aerosil, 14 kg of talc and 14 kg of magnesium stearate. The composition of the capsule mixture homogeneous and stable when zooming. Received, on average, 9850000 capsules with an average content in each capsule 0.002 g ± and 4.9% of loperamide hydrochloride. Thus, as in the previous examples, the proposed pharmaceutical composition allows to obtain a capsule mixture, the properties of which are not affected by the scaling, and capsules, derived from it, meet the requirements of Gosfarmakapei XI ed.

Additional studies confirmed the identity of the pharmacological action of the inventive composition in the form of capsules loperamide with standard sample, which used the well-known drug Imodium firm Gedeon Richter, Hungary. The bioavailability of the proposed structure of the capsules loperamide is 98.5%, which allows to make a conclusion about the equivalence of the pharmacological action of the claimed composition and the standard sample.

Table 1
IngredientsContent, wt. including 1 wt. hours of loperamide hydrochloride
Examples
123
Lactose47,0of 57.552,25
Starch13,516,515,0
Aerosil0,30,40,35
Talc0,60,80,7
Salt of stearic acid0,60,80,7

1. The pharmaceutical composition of the antidiarrheal action in the form of hard gelatin capsules containing as active ingredient a therapeutically effective amount of loperamide hydrochloride, and the target additives, lactose, potato starch and/or corn, characterized in that it further comprises Aerosil, talc and salt of stearic acid and the total number of target components is 62,0-76,0 parts by weight to 1 parts by weight of active substance.

2. The pharmaceutical composition according to claim 1, characterized in that it contains a special additive in the following ratio of components, parts by weight to 1 parts by weight of active ingredient:

Lactose47,0-of 57.5
Potato starch and/or corn13,5-16,5
Aerosil0,3-0,4
Talc0,6-0,8
Salt of stearic acid0,6-0,8

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



 

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