49 results about "Nimesulide" patented technology

Low dose pharmaceutical dosage form comprising nimesulide or its pharmaceutically acceptable salts, esters, solvates or hydrates thereof, along with one or more pharmaceutically acceptable excipient(s) are provided. The present invention also provides process of preparing such dosage forms and therapeutic methods of using such dosage forms. The low dose compositions 10 are designed to exhibit such bioavailability, which is effective in the treatment of NSAID indicated disorders particularly, which require long-term treatment regimens such as arthritis. Such compositions reduce the cost of therapy in diseases, which require long-term therapies, are easy to manufacture, and also result in the reduction of dose related side effects associated with nimesulide therapy.

A controlled release composition comprising nimesulide as an active agent formulated as a gastroretentive system, preferably as a solid oral dosage form is provided, wherein the residence time of the active agent is increased in the stomach, duodenum, jejunum or ileum. The present invention also provides process of preparing such dosage form and methods of using such dosage form compositions. The dosage form compositions are preferably administered once-a-day or twice-a-day and are particularly very useful in the prophylaxis or treatment of NSAID indicated disorder(s) such as acute painful conditions like post-operative trauma, pain associated with cancer, sports injuries, migraine headache and the like, or chronic diseases such as arthritis and the like.

The invention provides a nimesulide medicine composition for improving dissolution performance and a preparation method thereof. The medicine composition in the invention comprises the following components in weight percentage: 1%-30% of nimesulide, 5%-30% of dispersing agent (at least one kind of liquid polyethylene glycol), 60%-85% of diluent (one or more of microcrystalline cellulose, lactose and starch), 1%-10% of silicon dioxide, 2%-20% of disintegrating agents (carboxymethyl starch sodium) and 0.1%-5.0% of adhesives (hydroxypropyl methylcellulose). The dissolution degree of the nimesulide medicine composition can reach above 90% within 5-10 minutes, and even 100%, thus the nimesulide medicine composition is different from the conventional solid composition of various medicines; and the nimesulide medicine composition improves the bioavailability of the nimesulide, is beneficial to clinical rapid fever abatement or pain killing and has high application value.

Low dose pharmaceutical dosage form comprising nimesulide or its pharmaceutically acceptable salts, esters, solvates or hydrates thereof, along with one or more pharmaceutically acceptable excipient(s) are provided. The present invention also provides process of preparing such dosage forms and therapeutic methods of using such dosage forms. The low dose compositions 10 are designed to exhibit such bioavailability, which is effective in the treatment of NSAID indicated disorders particularly, which require long-term treatment regimens such as arthritis. Such compositions reduce the cost of therapy in diseases, which require long-term therapies, are easy to manufacture, and also result in the reduction of dose related side effects associated with nimesulide therapy.

The invention belongs to the field of pharmacy and relates to a hot-melt extruded quick release preparation of nimesulide and a hot-melt extruding method thereof. The hot-melt extruded quick release preparation is mainly characterized in that copovidone (PVP-VA64, Kollidon VA64) or povidone (PVPK30) serves as a main dispersing carrier material, and when necessary, a sugar alcohol auxiliary material serving as a plasticizer is added into the main dispersing carrier material, so that the aims of reducing extruding temperature and simplifying an extruding process are fulfilled. And due to the adoption of a nimesulide solid dispersion, the hot-melt extruded quick release preparation has the characteristic of quick dissolution.

A topical pharmaceutical formulation made up of nimesulide or a pharmaceutically acceptable derivative of nimesulide, together with thiocolchicoside or a pharmaceutically acceptable derivative of thiocolchicoside. The present invention more particularly relates to pharmaceutical combinations of nimesulide and thiocolchicoside, in the form of topical gels, ointments, cream, sprays, or lotions with anti-inflammatory, analgesic, and myorelaxant activities.

A slow-release composition of nimesulide is proportionally prepared from nimesulide, hydro-xyproply methylcellulose containing methoxy (19-24), hydro-xyproply methylcellulose containing methoxy (28-30), ethylcellose, lactose, magnesium stearate, and alcohol solution of ethyecellulose.

A controlled release anti-inflammatory nimesulide oral formulation. The formulation comprises 45-65% by weight of nimesulide and 10-30% by weight of hydrophilic polymer as retardant with pharmaceutically acceptable auxiliary agents and / or excipients. The nimesulide is partially or fully dispersed in the hydrophilic polymer. The process for the preparation of the formulation comprises mixing the nimesulide with the hydrophilic polymer and pharmaceutically acceptable auxiliary agents and / or excipients.

The invention provides a Nimesulide sustained-release tablet and a preparation method thereof. The Nimesulide sustained-release tablet is prepared by Nimesulide, skeleton sustained-release material, a bond and a lubricant. The invention is characterized in that the skeleton sustained-release material is a mixture of compressible starch and hydroxypropyl methylcellulose with the weight ratio of 1 : 1; moreover, the weight ratio of the Nimesulide : the compressible starch : the hydroxypropyl methylcellulose is 2 : 1 : 1; wherein, the preferable viscidity range of the hydroxypropyl methylcellulose is 20 to 4000 mpa.s. The Nimesulide sustained-release tablet can be slowly released to maintain more stable blood medicine concentration and longer action time; the Nimesulide sustained-release tablet taken before sleeping can appear peaking effect in the morning, achieve the best clinic treatment target and have better medicament economy advantage.

The invention discloses a nimesulide suspension and a preparation method thereof, relating to the field of medicine, in particular to the technical field of pharmacy by taking nimesulide as a raw material. Firstly, cane sugar, a preservative and purified water are mixed and heated to be prepared into simple syrup; the nimesulide is evenly mixed with Tween-80 to be prepared into particles with the particle diameter less than or equal to 10 micrometers; after the purified water is added into a suspending agent for swelling, the mixture is mixed with glycerol; and after the above three materials are mixed, and pigment, Stevioside and essence are added to be evenly stirred. The invention has simple process, easy production and operation, is favorable for quick adsorption after being taken and can quickly reach the treatment purpose, and the medicine has favorable curative effect and is convenient to carry and store.

The invention relates to a drug compound playing the role of diminishing inflammation, alleviating pain and eliminating fever and being used for treating arthritis, odynolysis and pyrexia caused by upper respiratory tract infection, and particularly relates to a drug compound oral pharmaceutical formulation adopting nimesulide as the ingredient and being prepared jointly with the medicinal carrier used as the stroma. The drug compound aims to supplement the deficiency of the prior oral nimesulide pharmaceutical formulation and provide a drug compound oral formulation, sustained-release nimesulide dropping pill which has high bioavailability, controllable release time, long-acting effect, reduced frequency of drug taking for a patient, low cost and absence of contamination during the production. The sustained-release nimesulide dropping pill adopts nimesulide as the chemical ingredient and is prepared jointly with the medicinal carriers of hydrophilic frame ingredients and hydrophobic frame ingredients used as the stroma.

The present invention relates to the use of nimesulide and structurally related compounds in the prevention and / or treatment of neurodegenerative conditions. It is based, at least in part, on the discovery that nimesulide exhibits a neuroprotective effect against &bgr.-amyloid induced cell death Without being bound to any particular theory, it appears that nimesulide inhibits a non-inflammatory mechanism of neurodegeneration

This invention relates to compositions of nimesulide for topical application.

The administration to a mammal of a combination of compounds, at least one of which is an a2d calcium channel subunit (A2d) ligand and at least one of which is a non-steroidal anti-inflammatory drug (NSAID), provides a surprising and potent inhibition of the micturition reflex, superior to that obtained by treatment with an A2d ligand or NSAID alone. Combinations of A2d ligand and NSAIDs are thus useful for treatment of lower urinary tract disorders and symptoms thereof. Preferred A2d ligands are gabapentin and pregabalin. Preferred NSAIDs are celecoxib, diclofenac, diflunisal, flurbiprofen, naproxen, nimesulide or sulindac.

The invention relates to a preparation method and application of a boron and nitrogen co-doped carbon dot. The preparation method comprises the following steps: putting diammonium hydrogen citrate andpinacol diboron into a lining polytetrafluoroethylene reaction kettle; then adding ultrapure water; heating the solution at 160 to 240 DEG C for 6 to 12 h; at the end of the reaction, naturally cooling the solution to room temperature, and performing high-speed centrifugation, filtration and freeze drying on the solution to obtain yellow solid powder which is the carbon dot. When the boron and nitrogen co-doped carbon dot is used for detecting nimesulide, the fluorescence intensity, at 408 nm, of a solution is prepared from a solution prepared from the carbon dot, a nimesulide-containing sample solution to be tested and a B-R buffer solution with the pH of 10 is measured by using a fluorescence spectrophotometer, and the concentration of the nimesulide is calculated according to a standard curve; extremely high selectivity is achieved.

The invention discloses a double-bag packaged nimesulide dry suspension. The double-bag packaged nimesulide dry suspension is prepared by the following steps: uniformly mixing 10 to 200 weight parts of nimesulide, 300 to 1,500 weight parts of filling agent, 100 to 500 weight parts of viscosity agent, 10 to 200 weight parts of flow aid, 5 to 10 weight parts of sweetener, and 1 to 3 weight parts of essence; crashing the mixture; screening the mixture with a screen of 30 to 40 meshes; mixing the mixture uniformly; placing the mixture in a novel powder feed device; and performing heat-sealing on the novel powder feed device with a powder-packing double-sealing device. Compared with the prior production technology, the nimesulide dry suspension prepared by the invention is convenient to administrate according to dose, has accuracy dose, and overcomes the defects that the quality is easy to change after single-bag package is unsealed and that the secondary pollution is easily caused by repeatedly sampling.

The invention provides a Nimesulide liposome solid preparation and a preparation method of the drug composite thereof. For the Nimesulide liposome solid preparation of the invention, the active ingredient Nimesulide is prepared into liposome and then prepared into Nimesulide solid preparation with other ingredients, wherein the liposome is prepared by the following ingredients according to parts by weight: 1 part of Nimesulide, 3-10 parts of lauric acid glycerol monolaurate, 0.5-4 parts of cholesterol, and 0.1-2 parts of poloxamer188. Compared with the existing Nimesulide liposome solid preparation, the Nimesulide of the invention has high dissolution rate and improved bioavailability, and overcomes the detect that the bioavailability of the Nimesulide liposome solid preparation in the prior art is low.

A chitosan-containing fibroin tissue repair material is a fibroin-containing membranoid substance. Internal average pore density is 1-3000 per mm2, average pore size is 1-500um, and the membranoid substance comprises, by weight, 105-150 parts of fibroin solution, 9-10 parts of fibroin nanofiber solution, 2-3 parts of chitosan acetic acid solution and 1-2 parts of nimesulide. The invention relates to the field of biomaterials and fibroin. The biomaterials for repairing damaged large tissue and complex organs must be capable of promoting blood vessel formation to enable the large tissue and the complex organs to have biological functions. However, in the prior art, pure silk fibroin repair materials are in the majority and are difficult to realize ideal functions in promoting blood vessel formation and tissue repair, and that the chitosan-containing fibroin tissue repair material has better tissue repair effect.

The invention discloses a Nimesulide enteric preparation combination and a preparation method thereof. The Nimesulide enteric preparation combination is mainly prepared from Nimesulide bulk drugs and suitable auxiliary materials. The improvement of the invention on the existing Nimesulide oral preparation is effective and obviously safe; compared with the common Nimesulide oral preparation, the Nimesulide enteric preparation combination has the advantages that the combination is less irritant to stomachs, thereby reducing the adverse reactions; and the Nimesulide enteric preparation combination is particularly suitable for patients with stomach-upset diseases, such as the active hemorrhage of digestive tract, active digestive ulcer and the like. The invention provides a Nimesulide preparation having the advantages of higher safety, equivalent curative effect and higher quality controllability and stability of the preparation process.

Use of a substance which is COX-2 selective and which can reduce prostaglandin levels of cerebrospinal fluid in a method for reducing the perception of pain in a subject is described. A preferred COX-2 selective inhibitor is nimesulide. Use of a COX-2 selective inhibitor as described has particular application in the relief of pain following surgery, especially following thoractotomy and also in the treatment of chronic post-thoracotomy pain.

The invention relates to a bioactive glass composite biological tissue repairing material and a preparation method thereof, and belongs to the field of a composite biological material. The bioactive glass composite biological tissue repairing material consists of the following raw materials in percentage by mass: 35 to 45 percent of a bioactive glass precursor solution, 35 to 45 percent of tetrahydrofuran, 5 to 10 percent of a fibroin solution, 5 to 10 percent of a fibroin nano-fiber solution, 2 to 3 percent of nimesulide, 2 to 3 percent of polyglycollide, 1 to 2 percent of a green tea extract, 1 to 2 percent of sodium hyaluronate and 1 to 2 percent of allantoin. The bioactive glass composite biological tissue repairing material prepared by the method has high mechanical property and excellent medicinal adhesiveness.

A slow-release composition of nimesulide is proportionally prepared from nimesulide, hydro-xyproply methylcellulose containing methoxy (19-24), hydro-xyproply methylcellulose containing methoxy (28-30), ethylcellose, lactose, magnesium stearate, and alcohol solution of ethyecellulose.

The invention relates to a method for preparing a Nim-PLLA (nimesulide-poly-l-lactic acid) composite microsphere with a supercritical anti-solvent crystallization technology. The nimesulide sustained-release microsphere with a sustained-release effect is prepared. The grain size of the drug composite microsphere can be effectively controlled through change of the drug solvent variety, the solution concentration, the crystallization pressure, the crystallization temperature, the flow velocity of the introduction of a solution sample and the like, and the grain size of the prepared microsphere is in a range from 1 mu m to 10 mu m. According to the drug sustained-release microsphere prepared with the method, the drug solubility and the drug sustained-release property are effectively improved.

The invention provides a nimesulide preparation and a preparation method thereof. The nimesulide preparation is mainly prepared from the following components in percentage by weight by wet granulation: 19.0%-28.0% of nimesulide, 0.07%-0.50% of a surfactant, 1.0%-2.0% of a binder, 4.0%-9.0% of a disintegrant, 30.0%-70.0% of filler, 0.5%-1.2% of a lubricant and the balance of water. The nimesulide preparation is prepared from water as a wetting agent by granulation, possible crystal transformation and toxic and side effects are avoided, safety and efficacy of the preparation are guaranteed, andfaster dissolution is realized.

The invention discloses a heat-clearing antipyretic coating agent for pigs. The heat-clearing antipyretic coating agent comprises the following components: 60-90 g / L nimesulide, 40-60 ml / L radix bupleuri volatile oil, 15-25 g / L ethyl cellulose, 18-22 g / L L-menthol, 15-25 g / L povidone k-30, 5 g / L glyceryl triacetate, 40 ml / L ethanolamine, and alcohol used as a solvent. The invention further discloses the preparation method and application of the heat-clearing antipyretic coating agent. The heat-clearing antipyretic coating agent is good in film-forming property, can slowly release anthelmintic, realizes a quick antipyretic effect, and is long in curative effect and small in stress. The formula and the preparation method of the coating agent are unique, and the curative effect is obvious; a protective film can be formed, medicine on the inner side of the film can be permeated and absorbed, and the outer side of the film plays a protective role; the coating agent can not drop off automatically, and has incomparable advantages compared with water-based liniments and oil pouring agents.

A controlled release pharmaceutical composition for peroral administration including a single unit fast release fraction and a single unit extended release fraction which includes nimesulide as an active drug upto 99% w / w of the composition, one or more release controlling materials from 0.1% to 99% w / w of the composition and pharmaceutical excipients from 0% to 90% w / w of the composition. The nimesulide is present in the fast release fraction and in the extended release fraction.

The present invention provides compositions and methods for inhibiting progressive cognitive impairment in persons at risk of developing dementia, for example patients suffering from MCI. It is based, at least in part, on the discovery that nimesulide, at extremely low concentrations, has a number of anti-amyloid effects, including decreasing the level of Aβ40, inhibiting the activity of secretase-γ, and favoring the formation of sAPPα. As extracellular β-amyloid accumulation is associated with pathologic cognitive deterioration, nimesulide may be used to intervene in amyloid plaque formation and thereby retard cognitive decline.

The invention discloses nimesulide solid dispersion micro-powder. The nimesulide is prepared by using povidone and hydroxypropyl methylcellulose as dispersion carrier materials and carrying out supercritical fluid crystallization. According to the invention, the preparation method of nimesulide solid dispersion micro-powder is operated simply under mild conditions; the controllability is high; andno solvent residue is left. The obtained nimesulide solid dispersion micro-powder is small in particle size, high in dispersity and high in stability; and the saturated solubility can reach over 5 times of that of a nimesulide raw material medicine (pH = 6.8). The micro-powder can be used for preparing solubilizing quick-release particles of nimesulide; the rapid dissolving in the dissolution medium with the pH value of 6.8 is realized; and the equilibrium dissolution rate of the micro-powder is more than two times of those of bulk drugs and nimesulide particles. Besides, the micro-powder canalso be used for preparing nimesulide tablets, capsules or suspensions and the like.

The invention relates to a preparation method of an intermediate of a non-steroidal anti-inflammatory drug, in particular to the preparation method of a nimesulide intermediate of 2-phenoxy-methane-sulfonyl aniline. The preparation method of the nimesulide intermediate of the 2-phenoxy-methane-sulfonyl aniline comprises the following steps: adding o-amino diphenyl ether (I) into a reactor which is provided with a drying and condensing device, adding an organic solvent, continuously adding methanesulfonyl chloride within one hour of heating, filtering and drying mixture, and obtaining 2-phenoxy methanesulfonyl chloride (II).

The invention discloses a preparation method of soluble ampicillin powder for exported poultry. Soluble ampicillin powder is prepared from 10% of ampicillin, deoxyglucose, an anti-inflammatory synergist and nimesulide, wherein ampicillin is semi-synthesized broad-spectrum penicillin, deoxyglucose is a broad-spectrum antiviral agent, the anti-inflammatory synergist can improve the non-specific anti-inflammation effect of a medicine, nimesulide is a novel pain-relieving, anti-inflammatory and antipyretic medicine, and the soluble ampicillin powder is prepared from 10% of ampicillin, deoxyglucose, an anti-inflammatory synergist and nimesulide through mixing. The soluble ampicillin powder for exported poultry has a special effect on low immunity, high fever and inflammation caused by various viruses and toxins, the design is optimized, and the requirements of design are met.