The method of obtaining anti-inflammatory antipyretic |
|
IPC classes for russian patent The method of obtaining anti-inflammatory antipyretic (RU 2173555):
 
 The method of obtaining derivatives of 2-(phenylamino)phenylacetic acid / 2172309
The invention relates to the field of technology for pharmaceutical preparations, namely, the method of obtaining the derivatives (salts, esters or amides) substituted 2-(phenylamino)phenylacetic acid, which can be used as drugs for various purposes
 The method of obtaining funds that have anti-inflammatory activity / 2171680
The invention relates to medicine
 Solid pharmaceutical compositions containing (s)-2-(4 - isobutylphenyl)-propionic acid as the active ingredient and microcrystalline cellulose and colloidal silicon dioxide as the excipients / 2168980
The invention relates to medicine and relates to solid pharmaceutical compositions
 Derivatives of l-arginine, the retrieval method, the pharmaceutical composition having inhibitory no - synthase activity / 2168493
The invention relates to a derivative of L-arginine, method for their production and pharmaceutical compositions based on them
 1-phenyl-2-dimethylaminomethylene-1-olavie compounds, methods for their preparation and medicinal products based on them / 2167148
The invention relates to 1-phenyl-2 - dimethylaminomethylene-1-alowyn compounds, method of their production and to their use in medicinal products
Medicinal product on the basis of paracetamol / 2166937
The invention relates to the field of medicine and relates to a medicinal product on the basis of paracetamol containing antihypoxic drug in therapeutic doses
 Di - and trivalent small molecule inhibitors of selectin, pharmaceutical composition, method of inhibiting selectin / 2165931
The invention relates to novel di - and trivalent small selectin inhibitors of formula II, where X is selected from the group comprising-CN, -(CH2)nCO2H, -(CH2)nCONHOH, -O(CH2)m-CO2H, -(CH2)nCOZ, -(CH2)nZ, -CH(CO2H), (CH2)mCO2H,
-OH; Y = -(CH2)f; R1, R2independently selected from the group including hydrogen, lower alkyl, halogen, -OZ, -NO2, -NH2; R3selected from the group including hydrogen, lower alkyl, hydroxy-lower alkyl, amino-lower alkyl, lower alkyl-carboxylic acid; f = 1 - 6; n = 0 to 2; b = 0 - 2; m = 1 to 3; Z represents lower alkyl, phenyl, or their pharmaceutically acceptable salts, esters, Amida  How to obtain tramadol / 2165922
The invention relates to the chemistry of aminoalcohols, in particular, to an improved process for the preparation of tramadol - 2-dimethyl aminomethyl-1-(3-methoxyphenyl)cyclohexanol
 A method of producing microparticles ion conjugate continuous selection, the method of making spherical ion conjugate continuous selection / 2173137
The invention relates to a pharmacy and affects the way of receiving and giving of spherical ionic conjugate, which contains a biodegradable polymer containing free carboxyl groups, and the drug containing free amino groups, the polymer and the drug is formed between the ionic bonds
 Balls "biosan" for the treatment of obesity of various origins and treatment of obesity of different genesis / 2172179
The invention relates to pharmacology and about creating convenient for intravaginal application form new, not previously used in gynecological practice antiseptic plant have antibacterial, antifungal, antiviral activity and activates the reparation of damaged mucosa
 Modafinil with a specific particle size / 2171674
 The processing method of the medicinal product, the apparatus for forming drugs and drug / 2170083
The invention relates to techniques for the production of agglomerated powdered drugs
 The processing method of the medicinal product, the apparatus for forming drugs and drug / 2170082
The invention relates to techniques for the production of dispersed powdered drugs
Intersolubility pellets of fluoxetine, composition, gelatin capsule, the way to treat people and the way to obtain intersolubility containing fluoxetine granules / 2164405
The invention relates to medicine, in particular to pharmacology concerns intersolubility composition, including fluoxetine in the form intersolubility of granules, which intersolubility layer includes acetate-succinate the hypromellose
 Pharmaceutical composition containing lamotrigine / 2160106
The invention relates to pharmaceutical drug levels of lamotrigine and its pharmaceutically acceptable salts, formed by joining acid
 9-n-ethenylene derivative 9(s)-erythromycylamine and method of production thereof / 2170739
The invention relates to a new 9-N-ethenylene derivative 9 (S)-erythromycylamine General formula I, where R1and R2the same or different and represent a nitrile group, a carboxyl group of the formula COOR3where R3represents a C1-C4is an alkyl group, or ketogroup formula COR4where R4represents a C1-C4is an alkyl group, or of pharmaceutically acceptable salts of the accession of inorganic or organic acids, as well as to the method of production thereof
|
(57) Abstract: According to the new method of training materials, separate successive granulating components of the medicinal product by the hydration of each component of the binder solution with simultaneous drying to obtain a coating on the granules. The granules are dried to a moisture content of 0.1 to 2.2%, mixed and packaged. The means are in the form of a granulated powder. To obtain the use, g/packing: acetylsalicylic acid or paracetamol - 0,18-0,58; ascorbic acid - 0,08-0,22; calcium gluconate - 0,08-0,22; diphenhydramine and/or rutin - 0,018-0,058; binder - 0,002-8,982; flavors of 0.002 to 1.00. As a binder, the use of starch and/or polyvinylpyrrolidone, and/or glucose and/or sucrose and/or lactose and/or gelatin. The method provides receiving anti-inflammatory antipyretic stable quality within 12 months. 3 C.p. f-crystals, 4 PL. The invention relates to the medical industry, namely the production of medicines, containing four, pathcomponent mixture of acetylsalicylic acid, paracetamol, ascorbic acid, organic salts of calcium, Dimedrol, and(or) routine, primenyaemoi number of complex anti-inflammatory antipyretics, containing acetylsalicylic acid, paracetamol, caffeine, ascorbic acid, known under the trade names: argolin, aspisol, aspirin+C, Coldrex, aspirin P, askofen and others (Reference Vidal. Drugs in Russia.- M: Astra Pharm Service, 1996). Drug Antigrippin (powder for oral administration, contains 0.5 g of acetylsalicylic acid and 0.2 g of ascorbic acid) has the advantage over the above-mentioned drugs associated with the presence of 0.05 g Dimedrol (antiallergic and sedative effect), 0.2 g of calcium gluconate and 0.05 g of rutin (tonic). A method of obtaining Antigrippin providing separate granulation of each component of a 5% solution of methylcellulose in 70% alcohol, a mixture of the obtained granules, tableting. The implementation of this method allows to obtain the drug in pill form, stable in storage during the year (Zakrzewska T. N., Shatilo centuries, Kachalova N. A., Korobeinikova O. N. , E. Nikulina Century of Research on technology of tablets neostigmine methylsulfate and "Antigrippin" replacement medicines dry concentrates//Increase the quality of medical assistance outpatient and inpatient patients on the basis of which OAB., 1986, Kazan, 1986, S. 272). The disadvantage of this method of obtaining drugs is ineffective dosage form of the drug - tablets, which are used by patients without prior grinding. Once in the stomach, they slowly decompose with the formation of insoluble crystals of acetylsalicylic acid, causing irritation to the mucous membranes and as a consequence complications (gastritis, ulcer) (Kudrin A. N. Pharmacology: A Tutorial.- M.: Medicine, 1991. - C. 131). The closest analogue to the invention, the nature and properties of the final product is a method of obtaining anti-inflammatory antipyretic in powder form for oral administration containing aspirin and ascorbic acid, calcium gluconate, diphenhydramine and(or) routines involving a sequence of technological operations:1. Preparation of raw materials. 2. The mixture of drug substances in a ratio which provides the content, g/packing: acetylsalicylic acid, and 0.5, ascorbic acid 0.2, calcium gluconate 0.2 and Dimedrol 0.05 and(or) routine of 0.05. 3. Adding Aerosil. 4. Packing the mixture powder in packages of laminated paper (the prototype). The aim of the present invention is to improve the stability, quality and expanding the range of action of anti-inflammatory antipyretic under the conditions: - stability of quantitative and qualitative characteristics of the drug for more than 12 months; - solubility of drugs in hot water (except routine) for 3 min; exceptions to the irritation of the gastric mucosa crystals of acetylsalicylic acid. This objective is achieved in that a method of obtaining anti-inflammatory antipyretic, containing acetylsalicylic acid or paracetamol, ascorbic acid, calcium gluconate, diphenhydramine and(or) rutin, including the preparation of raw materials, application of a coating on cgem spray solutions of binders, each particle of drugs simultaneously with drying. Thus according to the invention it is proposed to use the ingredients in the following proportions, g/packing: Acetylsalicylic acid or paracetamol - 0,18 - 0,58 Ascorbic acid - 0,08 - 0,22 Calcium gluconate - 0,08 - 0,22 Diphenhydramine and(or) rutin - 0,018 - 0,058 Binder - 0,002 - 8,982 Flavors of 0.002 to 1.0 Also in the method of obtaining the specified funds proposed: as a solution of the binder to use 3-10% solution of starch paste or 5-25% solution of gelatin, or 5-25% solution of the polyvinylpyrrolidone, or 20-67% sugar or glucose syrup, 20-40% solution of lactose; - drying the obtained granules to a moisture content of 0.1 to 2.2%; - use as a binder starch and / or polyvinylpyrrolidone, glucose, sucrose, lactose, gelatin, flavorings - essences of citrus, lemon or other fruit concentrates. It is known that in 100 ml of hot water dissolve about 0.5 g of acetylsalicylic acid or paracetamol, 0.2 g of calcium gluconate, more than 1 g Dimedrol and ascorbic acid. In that case there is the possibility of developing more effective drug dosage form powder for solution preparation (hot PIEE irritating to the mucous membrane of the stomach, to reduce the probability of complications and to improve the effectiveness of treatment, to expand the range of application, including for children half dosage when replacing acetylsalicylic acid paracetamol. Thus, the claimed method of the technological process provides reception of medicines in the form of crystals of medicinal substances coated. This allows you to separate incompatible components from each other and, ultimately, to obtain the product of stable quality in the past 12 months (inactivation of drugs less than 10%) (see example 4). The increase or decrease of parameters of the process aside from the stated limits leads to lower quality assets or makes it difficult to obtain (see examples 1-3). The method of obtaining anti-inflammatory antipyretic, containing acetylsalicylic acid or paracetamol, ascorbic acid, calcium gluconate, diphenhydramine and(or) rutin, as follows: acetylsalicylic acid or paracetamol, ascorbic acid, calcium gluconate, diphenhydramine, rutin sift through a sieve. Medicinal substance load in the m include the spraying of the solution of the binder (starch, gelatin, polyvinylpyrrolidone, sucrose, lactose and glucose) in the layer of drugs. The amount of feed solutions is carried out in a ratio which is necessary and sufficient to cover each crystal of the drug by the shell, sustainably protecting mutually incompatible substances from the contact (see examples 1 and 2). The feed rate of the solutions is determined by the design parameters of the installation, the properties of medicinal substances, provided a stable fluidized bed and the absence of particle aggregation. After submitting the required quantity of binder solution obtained granules are dried to a moisture content of 0.1 to 2.2% of necessary and sufficient for the stability of quality characteristics of the drug during storage for 12 months (see example 3). Then the granules are mixed in a ratio designed to obtain drugs specified structure, and Packed in packages of gas-tight material. Example 1. To select the optimum binder and its amount in the composition of the medicinal product conducted experiments in which a constant number of medicinal substances (50.0 g) was loaded in a laboratory setting is the R substances by spraying through the air injector solutions 1-10% starch paste, 3-25% polyvinylpyrrolidone or gelatin, 10-67% glucose or sucrose, 10-40% lactose. The process was performed under continuous stirring and drying with heated air at 30-50oC. In the process of coating samples were taken, was determined by the number of shell, in % by weight of loaded drugs. The samples were mixed in the calculated ratios and controlled the stability of the obtained mixtures during storage. Optimal were the cases in which there was no change in color and moisture of the drug for 1 year. In the experiments was determined by calculation of the minimum (according to the stability of the drug within 1 year) and the maximum number of binding (when the increase of the shell does not lead to increase shelf life). It is established that the optimal ratio of the binder is in the range from 0.002 to 8,982 g/packaging, including: starch 0,002 - 0,017, gelatin 0,003 - 0,078, polyvinylpyrrolidone 0,004 - 0,035, sucrose 0,114 - 8,952, lactose 0,167 - 4,075, glucose 0,061 - 8,982. In the experiments investigated the influence of the solution concentration of the binder on the quality of the shell. Determined that the optimum binder solutions are: 2-10% starch Kleist is entrale solution of the binder is lower than the stated limits complicates the process of applying a coating on the granules, reduces their strength and as a consequence reduces the yield of the target fraction. The increase in the concentration of the binder in the solution above the stated limits of the limited solubility of these components in water. Example 2. In an installation for coating Glatt (USA) were loaded with 50 kg of drug substances (acetylsalicylic acid or paracetamol, or ascorbic acid, or calcium gluconate, or Dimedrol, or routine, or powdered sugar). Included the supply air to get a stable fluidized bed. The temperature in the chamber was maintained at a level of 50-60oC. Then included the submission of a 3% aqueous solution of starch paste and sprayed 30 kg of 3% solution of starch paste at a rate of 10 kg/h After the end of the process of applying the membrane pellets were finally dried at a temperature of 50-60oC to a moisture content of not more than 2.2%. Before completing the coating of powdered sugar in mass was injected 0.5 kg essences of citrus. The resulting powders were analyzed on the content of active substances, and then mixed in the calculated ratio. The drug was Packed up in bags made from laminated paper 5 g using a universal filling machine TOO. The term hengliang medicinal substances was carried out in experiments, in which sample preparation obtained by the method shown in example 3, was moistened with water to a moisture content of 2.0 and 2.2, 2.8 per cent, were Packed up to 5 g in packages of laminated paper and laid on storage under natural conditions. Once a month was determined by qualitative and quantitative characteristics of the listed options. Indicator in determining the retention period, served as data on the degree of destruction of at least one component more than 10%. It is established that the increase in humidity over 2.2% dramatically reduces the retention period (see tab. 3). Example 4. In the experiments conducted a comparative study of quality characteristics of the preparation obtained in accordance with the claimed method (see example 2), in comparison with the prototype when stored in a cool (12-15oC) dark place. To get the prototype was mixed in a mortar weighed 200 g sucrose, 50 g of acetylsalicylic acid, 20 g of calcium gluconate, 20 g of ascorbic acid, 5 g of rutin, 5 g Dimedrol and 3 g of Aerosil. The resulting mixture was Packed up by 3.0 g in packages of laminated paper. The appearance definition, fluctuations in the mass of individual packages and raspadaemosti conducted in accordance with For reactions of authenticity and quantitative determination of paracetamol, calcium gluconate, ascorbic acid, Dimedrol used methods respectively FS 42-3292-96, FS 42-2668-89, FS 42-3019-94 (Guide to laboratory exercises in pharmaceutical chemistry/Ed. by P. L. Senova. M.: Medicine, 1978, c. 266). It is established that the application of the inventive method allows to increase the shelf life up to 1 year in comparison with the prototype - 2 months (see table. 4). 1. The method of obtaining anti-inflammatory antipyretic in the form of a granulated powder containing acetylsalicylic acid or paracetamol, ascorbic acid, calcium gluconate and/or rutin, binders and flavors, namely, that provide training materials, separate successive granulating components of the medicinal product by the hydration of each component of the binder solution with simultaneous drying to obtain a coating on the pellets, then the pellets are dried to a moisture content of 0.1 to 2.2%, mixed and Packed, and the components are taken in the following ratio, g/packing:Acetylsalicylic acid or paracetamol - 0,18 - 0,58 Ascorbic acid - 0,08 - 0,22 < / BR> Flavors of 0.002 to 1.00 2. The method according to p. 1, in which as a binder, the use of starch, and/or polyvinylpyrrolidone, and/or glucose and/or sucrose and/or lactose and/or gelatin. 3. The method according to p. 2, in which the binder solution using 3 - 10% solution of starch paste, or 5 - 25% solution of gelatin, or 5 - 25% solution of the polyvinylpyrrolidone, or 20 - 67% sugar or glucose syrup, or 20 to 40% solution of lactose. 4. The method according to p. 1, in which the flavorings used essences of citrus, lemon or other fruit concentrates.
|
