Pharmaceutical composition eliciting with anti-ulcer activity and method for its preparing

FIELD: medicine, gastroenterology, pharmacy.

SUBSTANCE: invention relates to a solid composition eliciting with an anti-ulcer activity and to a method for its preparing. Pharmaceutical composition consists of a core containing famotidine as an active component and starch, aerosil, stearic acid salt as accessory inert substances wherein a core is covered by polymeric envelope. Core comprises glucose and stearic acid as an accessory inert substance and magnesium stearate as a stearic acid salt. Polymeric envelope comprises oxypropylmethylcellulose, propylene glycol, castor oil, talc and titanium dioxide taken in the definite ratio of all components in the composition. Method for preparing pharmaceutical composition involves preparing raw, mixing therapeutically effective amount of famotidine with glucose and starch, moistening the mixture with starch paste, granulation, drying wetted granulate, repeated granulation, powdering dry granules, tableting and applying polymeric envelope containing oxypropylmethylcellulose on prepared cores with addition of titanium dioxide, propylene glycol, castor oil and talc. Invention provides enhancement of degradability, solubility and stability in storing.

EFFECT: improved method for preparing, valuable pharmaceutical properties of composition.

3 cl, 1 ex

 

The invention relates to medicine, more precisely to the pharmacy, and can be used for the preparation of solid pharmaceutical composition having anti-ulcer activity of the active compound which is famotidine.

Famotidine - blocker N2receptors of the third generation, providing a stronger and lasting effect on the structure and operation is similar to ranitidine and cimetidine, but much more active inhibition of secretion of hydrochloric acid.

Therefore, at present of great importance in the regulation of secretory activity of the stomach is attached medication - blockers N2receptor III generation.

The drug most often injected in the gastrointestinal tract through the mouth (peros). The advantage of this way is easy to use as it does not require the help of medical staff, as well as comparative safety and absence of complications specific for parenteral administration.

When administered orally, the drug must pass through a series of biological cell membranes (mucous membrane of the stomach, liver etc), and only part of it gets into the blood system. The effect of the drug depends largely on how big this part. This indicator characterizes the bioavailability of the drug. If e is ω on the bioavailability of drugs is influenced not only by the route of administration of the drug, but biopharmaceutical factors (dosage form, its composition, characteristics of the production technology of the drug).

After oral administration famotidine absorbed in the gastrointestinal tract and as a result, the drug inhibits the production of hydrochloric acid, both basal and stimulated by histamine or gastrinom. Simultaneously with the decrease in production of hydrochloric acid and increasing the pH decreases the activity of pepsin.

Among the variety of different pharmaceutical compositions based famotidine convenience and ease of use definitely produce solid dosage forms, therefore research and development of compounds to solid pharmaceutical compositions based famotidine continue up to the present time.

Mostly solid dosage forms for oral administration comprise one or more pharmaceutically active compounds and auxiliary inert substances, including solvents, fillers, diluents, preservatives and stabilizers, binders and sliding substances, flavorings, and which largely determine the rate of release of pharmaceutically active compounds, the speed and completeness of their absorption, as well as the stability and strength of the dosage form.

Known pharmacological antiulcer composition and SP is the property of its receipt (see Russian Federation patent No. 2179022, class a 61 K 31/425, a 61 K 9/20, And 61 R 1/04, the filing date 19.04.2001,, date of publication, 10.02.2002, the applicant: joint stock company "Chemical-pharmaceutical plant "Akrikhin"), selected as a prototype.

Renowned pharmaceutical composition having anti-ulcer activity, in the form of solid dosage forms, consists of a nucleus, containing as active compound famotidine and as an auxiliary inert substances lactose, starch, Aerosil, and salts of stearic acid coated with a polymer shell on the basis of a simple ester of cellulose, titanium dioxide and Tatana-80, the next part of the auxiliary inert substances kernel parts by weight to 1 parts by weight of famotidine:

- lactose3,20-4,30
- starch1,07-2,45
- salt of stearic acid0,02-0,05
- Aerosil0,08-0,12
- talc0,03-0,05

The shell contains these ingredients in the following ratio, % by weight of famotidine:

- oksipropilmetiltselljuloza6,72-13,02
- dioxide2.06 to 5,71
twin-801,23-8,01

The method of obtaining it is notizie involves mixing a therapeutically effective amount of famotidine with starch, the Aerosil and lactose, the hydration of a mixture of starch paste, granulation, drying the wet granulate, re-granulating, the powder of dry granules with a mixture of starch, talc and salt of stearic acid, tableting and coating the obtained kernel film shell.

Known technical solution is the prototype has a number of significant drawbacks.

Tablet with the stated composition and obtained in a known manner has a relatively low raspadaemost, solubility and stability during storage.

The objective of the proposed technical solution is to eliminate these disadvantages, as still relevant is the creation of a solid pharmaceutical composition based on famotidine that would satisfy all the requirements of the standard pharmaceutical agent.

Problem solving and advantages of the invention ensue from the subsequent detailed description of a pharmaceutical composition having anti-ulcer activity, on the basis of famotidine and specific examples of its manufacture.

The problem is solved due to the fact that the pharmaceutical composition having anti-ulcer activity, in the form of a solid dosage form consisting of a kernel, containing as active compound famotidine and support the additional inert substances starch, Aerosil coated with a polymer shell on the basis of a simple ester of cellulose and titanium dioxide, according to the invention, as an auxiliary inert substances it additionally contains glucose, stearic acid, magnesium stearate, and the polymer shell contains oksipropilmetiltselljuloza, with the following content, wt. including 1 wt. including famotidine:

- glucose0,735-3,675
- starch1,470-5,880
- Aerosil0,00735-0,0735
- stearic acid0,00075-0,00735
- stearate0,0014-0,00735
- oksipropilmetiltselljuloza0,1507-0,2027
- titanium dioxide0,0368-0,1838.

According to the invention, the shell further comprises propylene glycol, castor oil, talc.

When this sheath pharmaceutical composition contains the indicated ingredients in the following ratio, wt.%:

- oksipropilmetiltselljuloza41,03-55,17
- titanium dioxidethere is a 10.03-50,02
- castor oil0,12-2,33
- propylene glycol0,11-15,09
- is ALK 2,01-20,02

In addition, the problem is solved due to the fact that in a method of producing a pharmaceutical composition having anti-ulcer activity, including the preparation of raw materials, mixing a therapeutically effective amount of famotidine with glucose and starch, the hydration of a mixture of starch paste, granulation, drying the wet granulate, re-granulating, the powder of dry granules with a mixture of stearic acid, magnesium stearate and Aerosil, tableting and coating the obtained core of a polymeric shell containing oksipropilmetiltselljuloza with the addition of titanium dioxide, propylene glycol, castor oil, talc.

Thus according to the invention the pharmaceutical composition is made in the form of tablets.

Properties and quality of the final tablet to a large extent depends on the ancillary of inert substances, so in addition to the active compound of the proposed solid pharmaceutical composition as an auxiliary inert substances contains glucose, starch, magnesium stearate, stearic acid, Aerosil. The composition and quantity of the inert auxiliary substances are optimal and identified experimentally.

The proposed ratio connection is active and inert auxiliary substances is also protected areas is normal, found experimentally and provided quality tablets with high therapeutic effect of the active compounds and which meet the requirements of the State Pharmacopoeia XI strength, solubility, raspadaemosti etc.

Failure to comply with the limit of the ratio of one of the components of the composition in compliance with the proposed limits of the ratios of all other components of the composition does not allow to achieve a positive effect.

The claimed pharmaceutical solid composition structurally is compressed between the granules mostly 2-4 mm, containing the above active compound, glucose and starch.

In addition, the granules contain a matrix based on the starch formed from 2-4%solution of starch paste (0.5 to 1% wt. dry starch). An active connection is in close contact with these matrices. Granules Audrey apadravya mixture comprising magnesium stearate, stearic acid, Aerosil.

The inventive composition includes additives that facilitate the pressing of powder materials and give the tablets strength. As such a filler in the inventive compositions use a combination of starch and glucose. The presence in the claimed composition specified in the filler quantity of starch and is lukosi not only facilitates extrusion, it gives you a more solid tablet-core, excluding the effect of the destructive forces in the process of coating the shell.

In addition, the use of glucose can significantly increase the rate of release of active compounds, while providing high performance release.

As a binder, moving and loosening substances used starch, the amount of which was determined experimentally. The presence in the claimed composition specified number of starch largely determines the rate of release (the rate of acceleration of the disintegration of the tablet after swallowing to ensure rapid release of the active compound), the speed and completeness of absorption of the active compounds (bioavailability), as well as its stability. In addition, the starch provides the conditions for the penetration of liquid (water and/or digestive juices) into solid pharmaceutical composition. The reduction of starch (less than 1,47 by weight of famotidine) leads to an increase in time raspadaemosti tablets, and the increase in starch (more 5,88 by weight of famotidine) to reduce the strength, stability and increase the abrasion of the tablets.

The main criteria for choosing the number of glucose and starch were pharmaceutical and therapeutic usefulness.

As RMS is esasy substances in the inventive compositions use an auxiliary inert substances, which reduce the friction between the particles inside the tablet, reducing the reaction forces that appear on the walls of the matrix. In the proposed composition as moving substances used magnesium stearate, stearic acid, and Aerosil. The inclusion of these substances in the inventive composition enhances glide and ensures uniform filling of the space in the matrix, while receiving the tablets with a constant weight.

The presence in the claimed composition of magnesium stearate and stearic acid provides the effect of slip required at the stage of pressing, as it is the effect of slip causes the uniformity of the mechanical and physical properties in the volume of the dosage form, thereby facilitating the formation of the smooth surface of the tablet. The presence in the claimed composition of talc provides not only the effect of the sliding, but also gives the finished tablets Shine.

For masking unpleasant organoleptic properties of famotidine tablet core covered with a shell of ethers of cellulose, mostly from oksipropilmetiltselljulozy with the addition of titanium dioxide, propylene glycol, castor oil, talc.

Due to the fact that talc is hydrophobic substance that slows the process of dissolution of the tablets, it was decided to enter it into the shell in a smaller number (Zam the NIV part of the talc Aerosil).

The use of propylene glycol and castor oil can have a shell, which is more plastic around the sharp corners of the tablet, while improving the appearance of the tablets.

As can be seen from the above, only the proposed intervals of the ratios of components are optimal and can achieve a non-toxic drug in tablet form that meets the requirements of scientific and technical documentation on all counts.

New in the proposed method, compared with the prototype is that a therapeutically effective amount of famotidine is mixed with glucose and starch, powder of dry granules carried out with a mixture of stearic acid, magnesium stearate and Aerosil, and the resulting tablet cores cover a polymer shell of ethers of cellulose, mostly from oksipropilmetiltselljulozy with the addition of titanium dioxide, propylene glycol, castor oil, talc.

The number you enter in the composition of the humidifier starch is 0.5-1% of the total weight of starch, containing in the claimed composition. The rest of the starch used as a filler together with glucose in a mass ratio of 1:2 respectively. The change in these ratios impair the technological properties of the granules (flowability, compressibility) and hampers the process of tableture the project.

Use for dusting mixture consisting of stearic acid, magnesium stearate and Aerosil, also provides good adhesion of the active compound and the inert auxiliary substances, which contributes to a significant increase in the durability of tablets and thereby reduces their rejection in the process of packing.

Thus, the combination of these features of the claimed composition was allowed to achieve its raspadaemosti when administered for 5-7 minutes. The solubility of the claimed composition has considerably increased and as a consequence, improved bioavailability of the active compounds - famotidine.

While the claimed composition has good mechanical strength is not destroyed when the load reaches 4 kg

The inventive composition has a high chemical stability - after 2 years of storage the content of impurities was within the limits specified in the regulatory documentation, and amounted to less than 1.0%.

The claimed technical solution is different from the prototype (see Russian Federation patent No. 2179022, class a 61 K 31/425, a 61 K 9/20, And 61 R 1/04, the filing date 19.04.2001,, date of publication, 10.02.2002, the applicant: joint stock company "Chemical-pharmaceutical plant "Akrikhin"), and therefore meets the criterion of "novelty", should not be explicitly studied art, t which has an inventive step.

The claimed technical solution can be obtained and used in industry, therefore, meets the criterion of "industrial applicability".

An example of a specific implementation.

Preparation of solid pharmaceutical compositions on the basis of famotidine is carried out by preparation of raw materials, mixing a therapeutically effective amount of famotidine with glucose and starch, moistening the mixture of starch paste, granulation, drying the wet granulate, re-granulation, powder of dry granules with a mixture of stearic acid, magnesium stearate and Aerosil, tabletting and coating the obtained core of a polymeric shell containing oksipropilmetiltselljuloza, with the addition of titanium dioxide, propylene glycol, castor oil, talc.

1. Preparation of raw materials includes screening famotidine, glucose, starch, and drying the starch to a moisture content of 3-5%).

2. Preparation of the humidifier

Prepare a 2%solution of starch paste.

3. Mixing

On the scales weighing 150 g of famotidine, 200 g of starch 20% humidity, 530 g of glucose.

In the mixer download famotidine, starch, glucose and stirred for at least 5-10 minutes.

After completion of the mixing process in the mixer serves humidifier and stirred tablets weight for 10-15 minutes to achieve equal is rnost moisture.

4. Wet granulation

The wetted tablet mass is passed through a granulator with a grid cell size of 2 mm.

The formation of granules consisting of famotidine, starch, glucose.

5. Drying granulator

Drying granulator is produced in a vacuum drying Cabinet at a temperature of 45-50°within 1.5-4 hours. When drying, an optimum particle size tablet mass to a residual moisture 2-3%.

6. Dry granulating and dusting

On the scales weighed Aerosil, magnesium stearate and stearic acid.

The dried pellet mass is passed through a granulator and add to it in small portions weighed quantity of Aerosil, magnesium stearate and stearic acid.

The dry granules are poured into the mixer, add outrivals mixture and stirred for 5-10 minutes.

7. Tableting

Prepared tablets weight tabletirujut on a tablet press, after adjusting the average weight of the tablets and selecting the optimal pressure. During the extrusion of starch granules forms a matrix that provides quick raspadaemost and release the body to the active compound - famotidine and sufficient strength tablets.

8. Preparation of film-forming solution

In boiling water, fill oksipropilmetiltselljuloza, mix up is hladiny, add the propylene glycol and the plasticizer is castor oil. The resulting mixture was stirred for 10 minutes. Add talc and titanium dioxide. Again stirred for 30 minutes. Then filtered through a sieve.

9. Coating of tablets-shell nuclei

The finished tablets-kernel is loaded into the installation heated to a temperature 38-41°C. is Then applied film-forming solution.

Tablets based on famotidine are white with a yellowish white color, smooth surface, face shape with beveled edges and scored.

The average weight of 230 mg tablets, 8 mm in diameter and a height of 3.6 ± 0,4 mm

Tablets of geometric shape and size meet industrial standard (OST 67-7-170-75), appearance, strength, dissolution, raspadaemosti and other indicators meet the requirements of the State Pharmacopoeia XI.

The obtained experimental series of tablets were laid on accelerated and natural storage for studying the stability of the preparation and establishment of shelf life. The result indicated that tablets, the active compound which is famotidine, stable during storage and do not change their rates within 2 years.

Thus, in comparison with the prototype, the claimed technical solution is more stable during storage, easily releases the active compound - famot the Dean, which ensures its high bioavailability.

While the application of a gastric-soluble shell allows you to give the tablets a beautiful appearance, increase their mechanical strength, to hide the unpleasant taste of famotidine.

The sequence of operations and their technological options allow you to produce a pharmaceutical composition having anti-ulcer activity, on the basis of famotidine, the quality of which meets all of the requirements for qualitative and quantitative indicators standard pharmaceutical agent.

1. Pharmaceutical composition having anti-ulcer activity in the form of a solid dosage form consisting of a kernel, containing as active compound famotidine and as an auxiliary inert substances starch, Aerosil, salts of stearic acid coated with a polymer shell on the basis of a simple ester of cellulose and titanium dioxide, characterized in that as a subsidiary of inert substances the core additionally contains glucose as a salt of stearic acid, magnesium stearate and stearic acid, and a polymeric shell further comprises propylene glycol, castor oil, talc in the following ingredients to 1 parts by weight of famotidine, parts by weight:

the contents of the kernel:

glucose0,735-3,675
starch1,470-5,880
Aerosil0,00735-0,0735
stearic acid0,00075-0,00735
magnesium stearate0,0014-0,00735

the content of the polymer shell, wt.%:

oksipropilmetiltselljuloza41,03-55,17
titanium dioxidethere is a 10.03-50,02
castor oil0,12-2,33
propylene glycol0,11-15,09
talc2,01-20,02.

2. A method of obtaining a pharmaceutical composition having anti-ulcer activity, including the preparation of raw materials, mixing a therapeutically effective amount of famotidine with glucose and starch, the hydration of a mixture of starch paste, granulation, drying the wet granulate, re-granulating, the powder of dry granules with a mixture of stearic acid, magnesium stearate and Aerosil, tableting and coating the obtained core of a polymeric shell containing oksipropilmetiltselljuloza with the addition of titanium dioxide, propylene glycol, castor oil, talc.

3. The method according to claim 2, characterized in that a pharmaceutical composition having FR is Vaswani activity made in the form of tablets.



 

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