267 results about "Celecoxib" patented technology

Pharmaceutical compositions are provided comprising one or more orally deliverable dose units, each comprising particulate celecoxib in an amount of about 10 mg to about 1000 mg in intimate mixture with one or more pharmaceutically acceptable excipients. The compositions are useful in treatment or prophylaxis of cyclooxygenase-2 mediated conditions and disorders.

Celecoxib, a COX-2 specific non-steroidal anti-inflammatory agent, is provided in combination with DFMO for the prevention and/or treatment of cancers. Provided with the present invention are pharmaceutically acceptable compositions that include a non-steroidal anti-inflammatory agent, celecoxib, together with an effective amount of difluoromethylornithine.

The invention relates to a solid dispersion containing celecoxib as well as a preparation method and application thereof. The invention needs to solve the technical problems of difficult pulverization of raw materials and difficult preparation of solid oral preparation of celecoxib. The solid dispersion is a solid dispersion containing the celecoxib and polyethylene glycol which are in the weight ratio of 1:0.5-10. The preparation method comprises the following steps of: melting solid polyethylene glycol by heating, adding the celecoxib and dissolving to obtain a clear solution; or mixing and heating the solid polyethylene glycol and the celecoxib, and melting to obtain a clear solution; and then rapidly cooling to obtain the solid dispersion. The solid dispersion can be prepared into various oral preparations after being pulverized.

The invention belongs to the field of pharmaceutical preparations and provides a Celecoxib nanosuspension and a preparation method thereof. Celecoxib is a novel non-steroidal anti-inflammatory drug, inhibits cyclooxygenase -2(COX-2) is through specificity, has anti-inflammatory and pain-easing effects and is clinically used for treating osteoarthritis and rheumatoid arthritis. However, the Celecoxib has very low solubility and in-vivo bioavailability. In order to increase the dissolution and the bioavailability of the drug, a high-speed shearing combined high-pressure homogenizing method is adopted to prepare the Celecoxib nanosuspension, the particle size and the polydispersion index PI are used as indicators for formulation technology optimization, a laser particle analyzer and a transmission electron microscope are adopted to study the particle size and form of the drug, the dissolution of the drug is evaluated through in-vitro dissolution experiments, and rat in-vivo pharmacokinetic study is conducted. Measurement results prove that the drug particle size of the nanosuspension is 50-500 nm, and the dissolution and the in-vivo bioavailability of the drug are increased obviously.

The invention provides celecoxib and a preparing method thereof. The preparing method of the celecoxib comprises the following steps: mixing 5- (4-methylphenyl) -3-trifluoromethyl-1H-pyrazole and 4-halogen benzene sulfonamide, then dissolving the mixture in the second organic solvent, and then adding alkali and catalyst to obtain the celecoxib after coupling reactions. The 5-(4-methylphenyl) -3-(trifluoromethyl)- 1H-pyrazole:(1) is prepared according to the following procedures: mixing dissolving 1-(4- methylphenyl) -4, 4, 4-trifluoro1, 3-butanedione and hydrazine hydrate in the second organic solvent, then obtaining 5-(4-methylphenyl)-3-(trifluoromethyl)-1H-crude pyrazole after heating and dehydration cyclization reaction; (2), obtaining 5-(4-methylphenyl) -3- (trifluoromethyl)-1H-pyrazole by purifying the crude pyrazole. The preparing method provide by the invention can effectively reduce the content of regional isomers in celecoxib, and dramatically improve the quality of products. The productivity can reach 81.3%, and the content of the regional isomer is 0.01%.

The invention provides a celecoxib solid composition with high dissolution, a preparation method and an application. The amorphous composition of celecoxib is obtained by dissolving the celecoxib into one or more pharmaceutically acceptable solvents and adsorbing and drying with pharmaceutically acceptable auxiliary materials. The composition can be further prepared into various solid preparation forms such as tablets, capsules and granules according to the actual requirement. Through the prepared celecoxib composition and preparations thereof, the dissolution of the celecoxib can be greatly improved, and the defects of low dissolution and low bioavailability of the celecoxib are overcome.

A pharmaceutical dosage form comprising celecoxib and a pharmaceutically acceptable carrier, the dosage form when initially administered to at least 12 human patients in the fasted state in a crossover study providing: (a) a mean blood plasma concentration of celecoxib within 0.5 hour after administration (C_0.5) of at least about 0.9 ng/ml per mg of celecoxib dosed; (b) a mean blood plasma concentration of celecoxib 12 hours after administration (Ci2) of at least about 0.6 ng/ml per mg of celecoxib dosed; (c) a mean area under the blood plasma concentration versus time curve for the 12 hour period following administration (AUC₁₂) of at least 19 ng-hr/mL per mg of celecoxib dosed; and (d) a mean maximum blood plasma concentration (C_max) of celecoxib of less than about 4.9 ng/ml per mg of celecoxib dosed.

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a medicament microsphere and a preparation method thereof. The medicament microsphere comprises medicinal materials, a high polymer material and a surfactant, wherein the ratio of the medicament to the high polymer material is 1:(1-3); the medicament preferably is celecoxib, ketoprofen, dipyridamole and nimodipine. The medicament microsphere is prepared by adopting an O/W emulsified solvent diffusion-volatilization method. The O/W emulsified solvent diffusion-volatilization method comprises the following steps: respectively weighing the medicinal materials, the high polymer material and a release regulator according to the prescription amount, and then adding the weighted materials to an organic solvent; ultrasonically or mechanically stirring and dissolving as a disperse phase; taking a surfactant solution as a continuous phase; warming and stirring after low-temperature emulsification under an agitation state, so as to remove an organic solvent; and then carrying out solid separation, washing by distilled water, and drying, so as to obtain the medicament microsphere. Thus, the prepared microsphere is high in encapsulation efficiency and high in yield.

The invention provides a celecoxib composition. The celecoxib composition contains one or more types of dose units which can be orally released, and each of the dose units contains 50-500mg of celecoxib D95 particles and one or more types of mixtures of pharmaceutical excipients. The composition can be used for treating or preventing diseases caused by COX-2.

The invention relates to a synthesis method of celecoxib, which comprises the following specific steps of: 1, carrying out claisen condensation on p-methylacetophenone and trifluoroacetic acid ethyl esters in an aprotic organic solvent under the catalysis of alkali to obtain 1-(4-methylphenyl)-4,4,4-trifluoro-1,3-butanedione; and 2, reacting the obtained 1-(4-methylphenyl)-4,4,4-trifluoro-1,3-butanedione with sulfonamide-phenylhydrazine hydrochloride to obtain celecoxib, wherein in the step 1, the alkali for catalysis is selected from one or more of sodium hydride, potassium hydride, lithium hydride and calcium hydride. The synthesis method of celecoxib provided by the invention is easy to operate, high in yield, high in product purity and easy for industrial production.

Parenteral (injectable) celecoxib emulsions and nanoemulsions are disclosed as are their use to treat pain in patients so afflicted. The emulsions are generally oil in water emulsions often comprised of an oil phase including an oil and a lecithin wherein the mean droplet size of the discontinuous oil phase is about 200 nanometers or less.

The invention relates to a novel composition of celecoxib and glucosyl-cyclodextrin or sulfobutyl-beta-cyclodextrin as well as a preparation method of the composition and application in medicine preparations. According to the invention, the prepared composition of celecoxib and glucosyl-cyclodextrin or sulfobutyl-beta-cyclodextrin has the advantages of improving the water solubility and the stability and has no adverse effect of hemolysis, so that the composition can serve as a starting material or a constituent for preparing intestinal-administration preparations or non-intestinal-administration preparations for treating tumors or rheumatoid arthritis; and the solid preparations have high bioavailability and the freeze-dried powder injections meet the requirements on the aspect of pH value and have no adverse effect of hemolysis.

The invention provides a preparation method of celecoxib. The preparation method provided by the invention can improve the yield and the purity and save the cost by using an amide solvent.

The invention relates to a celecoxib-containing capsule, which contains 40wt%-70wt% of celecoxib, 22wt%-50wt% of a water-soluble filler, 0.5wt%-25wt% of low substituted hydroxypropyl cellulose, and 0.5wt%-10wt% of sodium dodecyl sulfate. The celecoxib capsule with a prescription provided by the invention has no special requirement for the particle size of celecoxib, the celecoxib bulk drug directly synthesized by a conventional synthesis method can be taken as a preparation raw material, and no special treatment is needed. The preparation process is simple, the product quality is uniform and stable, and has effective bioavailability.

Belonging to the field of pharmacy, the invention relates to a lactose celecoxib pharmaceutical composition and a preparation method. The composition is characterized in that lactose and celecoxib form solid dispersions by means of coprecipitation.

The invention specifically relates to a celecoxib solid dispersion and a preparation method and application thereof. The celecoxib solid dispersion is prepared from celecoxib and poloxamer 188 at a mass ratio of 1:(1-20) by a melting process and a solvent process. The dispersion provided by the invention has good dispersity and high stability; the solubility and dissolution rate of the medicine are increased; the solubility of the medicine in water is 5-200 times higher than that of the raw medicines; with good dissolution rate in water, the in-vivo absorption of the medicine can be enhanced so as to improve the bioavailability. The solid dispersion also can be made into multiple clinically acceptable dosage forms which are used as new dosage forms of celecoxib.