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:
|- salt of stearic acid||0,02-0,05|
The shell contains these ingredients in the following ratio, % by weight of famotidine:
|- dioxide||2.06 to 5,71|
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:
|- stearic acid||0,00075-0,00735|
|- titanium dioxide||0,0368-0,1838.|
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.%:
|- titanium dioxide||there is a 10.03-50,02|
|- castor oil||0,12-2,33|
|- propylene glycol||0,11-15,09|
|- 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.
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.
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:
the content of the polymer shell, wt.%:
|titanium dioxide||there is a 10.03-50,02|
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.
FIELD: medical virology and microbiology.
SUBSTANCE: new bacteriophage strain Helicobacter pylori, having lytic activity is disclosed. Method for production of antigastritis and antiulcer drug based on the new bacteriophage strain also is disclosed. Claimed method includes providing of purified suspension of bacteriophage Helicobacter pylori with lytic activity of 109 FFU/ml and addition of 1 % chinozole thereto. Moreover sorbitole and gelatose also may be introduced into said agent. Obtained mixture is frozen and lyophilized.
EFFECT: high effective antigastritis and antiulcer drug useful in medicine.
3 cl, 1 tbl, 2 ex
SUBSTANCE: eradication of infection Heliobacter pylory in stomach comprises oral administration of corresponding drugs in powdered form mixed with orange juice. In particular, mixture of colloidal bismuth subcitrate (De-nol), Nifuratel (Macmirror), and Amoxycyllin (Flemoxin solutab) are used. Administration is performed on an empty stomach at least 30-40 min before the food intake. Patient then lies at least 30 min on the both sides alternatively.
EFFECT: suppressed water-repellent property of near-wall layer of stomach mucus and slowed down evacuation of liquid from stomach thereby ensuring fast diffusion of therapeutical substances into infect persisting zone and, therefore, direct bactericidal effect on Heliobacter pylory.
SUBSTANCE: peptide of the following formula: X-Pro-Gly-P, where X = Thr-Lys-Pro-Arg-; Lys-pro-Arg-; pro-Arg-; Arg-, being of untiulcerous activity. They should be applied at intraperitoneal injection at the dosage of 0.58-3.20 mcM g/kg for preventing and treating ulcers of gastro-intestinal tract.
EFFECT: higher efficiency and prophylaxis.
4 dwg, 5 ex
FIELD: medicine, gastroenterology.
SUBSTANCE: traditional eradication therapy should be supplemented with licopid at the dosage of 10 mg per os once daily before breakfast for 10 d. The present innovation prevents transfer of microorganisms into inactive form, accelerates restoration of mucosal epithelial layer in gastroduodenal area, provides complete eradication of microorganisms, that in its turn, favors to prevent disease exacerbation and restoration of gastroduodenal functions.
EFFECT: higher efficiency of therapy.
3 dwg, 2 ex
SUBSTANCE: the present innovation deals with peroral liquid compositions which could be designed into gelatinous capsules. The suggested pharmaceutical composition includes a pharmaceutically active agent, a solubilizing agent and, not obligatory, a surface-active substance and a plastifying agent. The pharmaceutically active agent has got, at least, one acidic fragment, preferrably, that of carbonic acid being chosen out of the group of non steroid antiphlogistic preparations being acid-soluble at acid : dissolved substance ratio being from 3:1 to 10000:1. New compositions provide increased rates and degrees of absorption of pharmaceutically active agent and minimize side effects caused by such active substances.
EFFECT: higher efficiency of application.
42 cl, 39 ex
SUBSTANCE: method involves applying eradicative anti-helicobacterial therapy comprising Omeprazol administration at a dose of 20 mg twice a day and Ximedone at a dose of 500 mg twice a day in 12 days long course.
EFFECT: enhanced effectiveness of eradication; reduced adverse side effects risk.
FIELD: medicine, gastroenterology.
SUBSTANCE: invention relates to methods for treatment of chronic helicobacter pylori-associated gastritis. Method is carried out by monotherapy with the probiotic "Laminolakt" in the dose 3 dragees per 24 h for 1 month. Method provides elimination of Helicobacter pylori cells on the background of activation of the immune response in stomach mucosa by effect on microflora and the colon intestine immune system.
EFFECT: enhanced effectiveness of treatment.
2 tbl, 1 ex
SUBSTANCE: method involves introducing endoscope, clearing injured surface and applying gel produced on Tisol substance base (aqua-complex of titanium glycerosolvate) as medicinal composition via the endoscope. Tisol is administered as aqueous solution of concentration not less than 60% after Tisol. The composition is applied to injured surface in the amount of 2 to 8 ml for one session. The number of treatment sessions is equal to 1 to 7 with 3-5 days long pauses. The composition is prepared by mechanically mixing medicinal microadditives with Tisol substance. The medicinal microadditives are introduced in total amount of 7.26% of composition mass. The ingredients are selected depending on disease. The medicinal composition is applied as 1-2 mm thick layer. When treating the cases of erosion or gastritis, sea-buckthorn oil and/or propolis solution are of preference to be introduced into Thysol as the medicinal microadditives. When treating the cases of gastric or duodenal peptic ulcer, methyluracyl, hydrocortisone, cycloferon or aecol are preferentially introduced into Tisol as the medicinal microadditives. The composition formula is adjusted from session to session on the basis of treatment results visual control and analysis data. Taking meals and drinks is restricted for a patient for half an hour or longer.
EFFECT: enhanced effectiveness in administering drugs into mucous membrane and soft tissues without using needle injectors.
5 cl,4 tbl
FIELD: medicine, pharmacy.
SUBSTANCE: invention relates to medicinal formulations. Tablet consists of a mixture of medicinal agents and accessory substances and made with internal cavity filled with air. Cavity can involve isolated cells and the reduced specific weight of tablet is less 1 g/cm3. Invention provides enhanced effectiveness and safety of orally ingested tableted medicinal agents and safety of dissolving process and absorption of medicinal agent in stomach.
EFFECT: improved and valuable properties of tablet.
FIELD: pharmaceutical industry.
SUBSTANCE: pharmaceutical composition exhibiting neotropical, antiepileptic, sedative, and antistress activities, normalizing metabolic processes in body, contains aminoacetic acid and pharmaceutically acceptable carrier constituted by mixture of sorbitol and crosslinked carboxymethylcellulose sodium salt at weight ratio between 1:1 and 1:3 with additive selected from vinylpyrrolidone/vinyl acetate, stearic acid, stearic acid sodium salt, and mixtures thereof.
EFFECT: increased bioavailability and active component release velocity.
2 cl, 1 tbl
FIELD: pharmaceutics, medicine.
SUBSTANCE: the present innovation deals with cardiotherapy for treating and preventing coronary deficiency. The preparation is designed as a plate (film) consisted of three layers, each of them is manufactured out of co-polymer of vinyl pyrrolidone, acrylamide and nitroglycerin-containing ethylacrylate; moreover, internal layer additionally contains solid fat - cacao oil, and weight ratio for the sum of external layers to internal corresponds to 1 : 1. The suggested preparation could additionally contain brilliant green dyestuff. The preparation should be manufactured out of pre-obtained mixture of nitroglycerin and copolymer in solution of alcohol and water followed by layer-by-layer forming three-layer film due to spreading the mixture onto solid bottom plate and drying at 30-50 C. The innovation provides higher adhesion to gingival mucosal surface, decreased side action, improved bioavailability and stability of therapeutic effect.
EFFECT: higher efficiency of therapy.
3 cl, 3 ex
FIELD: pharmaceutical industry, medicine.
SUBSTANCE: invention relates to peroral immediate-released drug in solid form, containing low molecular thrombin inhibitor based on peptide with pH-depending solubility. Claimed drug has size particle less than 300 mum and contains combination of microcrystal cellulose and sodium glycolate starch in amount of more than 35 mass % (calculates as preparation mass).
EFFECT: drug with reduced dependence of thrombin inhibitor dissolution from pH and increased releasing rate from tablet.
17 cl, 3 ex, 3 dwg
FIELD: medicinal industry.
SUBSTANCE: the present innovation deals with manufacturing medicinal preparation containing drotaverin hydrochloride to be applied for interrupting spasms of smooth musculature. Mass for tableting should be prepared due to mixing the powder of drotaverin hydrochloride with that of dyed granulate at the ratio of 1:3 to 2:1. One should obtain the dyed granulate by moisturizing inert pharmaceutical filler with binder's solution dyed with quinoline yellow dyestuff. Then comes drying up to 0.1-2.5% followed by granulation and tableting. The innovation enables to obtain tablets of drotaverin hydrochloride upon industrial equipment at its degradability being below 15 min, being stable during manufacturing and at storage. Quality of tablets meets all the requirements of pharmacopoeic article.
EFFECT: higher efficiency of manufacturing.
2 cl, 4 ex, 3 tbl
FIELD: medicine, hygiene.
SUBSTANCE: the present tablets are designed in solid form and contain the substance of purifying action in the form of finely dispersed insoluble abrasive components, SAS, aromatizing agents, dyestuffs, thickening agents, moreover, the content of water in components should be decreased by 35-37%. The suggested tablets should be prepared due to mixing the components with water to form solid forms out of obtained homogeneous plastic material at the room temperature to be then dried up and packed. Tablets for disposable intake provide great consumer's latitude being very convenient at usage.
EFFECT: higher efficiency of application.
FIELD: medicine, pharmaceutics.
SUBSTANCE: the suggested composition includes therapeutically efficient quantity of para-aminosalicylic acid (PASA) as an active substance and target additives as sorbitol, polyvinyl pyrrolidone, salt of stearic acid, talc and citric acid. Pharmaceutical composition is designed as tablets covered with a membrane. The latter contains either "Acryl-iz" of Calarcon firm or composition consisting of copolymer of methacrylic acid with ethylacrylate, titanium dioxide, talc, propylene glycol and iron oxide. The suggested PASA-based antitubercular preparation meets all normative requirements of the State Pharmacopoeia, XI publication and has expiry terms of 2 yr.
EFFECT: higher efficiency of application.
6 cl, 3 ex, 1 tbl
FIELD: pharmaceutical industry.
SUBSTANCE: invention relates to porous quick-breaking active ingredient-containing granules based on chitosan or basic derivative thereof prepared by drop-by-drop technique, wherein aqueous solution or dispersion of chitosan or basic derivative thereof, one or several active substances, optional secondary active substances, and acid are dropwise added to cooling fluid at maximum temperature -5°C. As a result, solution or dispersion is solidified in the form of drops, which are then separated and dried. Such procedure is used to prepare therapeutical or diagnostic agents.
EFFECT: avoided use of gelatin or collagen as carrier.
FIELD: medicine, pharmacy.
SUBSTANCE: invention relates to a pharmaceutical composition for oral administration in treatment or prophylaxis of obesity or hyperlipidemia. The composition comprises orlistat and at least one ester of fatty acids and polyols. Melting point of fatty acid ester exceeds the body temperature and polyol is taken among group including glycerol, sugars, derivatives of sugars and their mixtures. Also, invention relates to a method for preparing above described composition and to a method for treatment or prophylaxis of obesity. Invention enhances effectiveness and activity of orlistat by reducing variability of effectiveness and/or activity of orlistat between patients and frequency and severity of adverse effects.
EFFECT: improved and valuable pharmaceutical properties of compositions.
24 cl, 1 tbl, 10 ex
FIELD: medicine, pharmacy.
SUBSTANCE: invention relates to nootropic, cerebroprotective medicinal agents as tablets. Tablet of a medicinal agent comprises thiotriazoline and piracetam as active components and accessory components used for formation of core and applying an envelope on it. Invention provides elevating rate and power of a medicinal agent effect on the brain blood supply, expanding spectrum of its pharmacological effect and excludes negative adverse effects.
EFFECT: improved and valuable medicinal properties of agent.
FIELD: organic chemistry, biochemistry.
SUBSTANCE: invention relates to epothilones with modified thiazole substituent, methods for production thereof and pharmaceutical composition capable of cell growth inhibiting containing the same. Claimed compounds have general formula I , wherein P-Q represents double carbon bond or epoxy; R represents H, C1-C6-alkyl; G represents ; R1 represents and ; G1 and G2 represent hydrogen; G3 represents O, S, and NZ1; G4 represents H, optionally substituted C1-C6-alkyl, OZ2, Z2C=O and Z4SO2; G5 represents halogen, N3, CN, NC, heteroaryl containing nitrogen or oxygen, and heterocycle; G6 represents H, C1-C6-alkyl, or OZ5, wherein Z5 represents H, C1-C6-alkyl; G9 represents oxygen; Z1 represents H, optionally substituted C1-C6-alkyl, optionally substituted acyl; Z2 represents optionally substituted C1-C6-alkyl or aryl; Z4 represents optionally substituted aryl.
EFFECT: new epothilones capable of cell growth inhibiting.
19 cl, 39 ex