80 results about "Celecoxib" patented technology

The invention belongs to the technical field of biomedical anti-inflammatory gels, and discloses a renewable boundary lubrication natural polyphenol anti-inflammatory hydrogel and a preparation method and application thereof.The hydrogel is of a hydrophilic viscoelastic sea island structure, gallic acid grafted gelatin blended with hyaluronic acid serves as a base material, celecoxib lipidosome is entrapped in the hydrogel, and the hydrogel is prepared from natural polyphenols, an articular cavity is injected through an enzyme crosslinking technology to form gel, hyaluronic acid and lipidosome form a hydrated lubricating layer on a cartilage-gel interface, and after the interface is abraded, internal lipidosome and hyaluronic acid are exposed to supplement lubrication so as to form sustainable lubrication; the liposome responds to friction shear crushing to release celecoxib and cooperates with gallic acid at an interface to resist inflammation progress and repair cartilage, the injectable hydrogel is developed based on gallic acid, hyaluronic acid, gelatin and celecoxib liposome to treat early osteoarthritis, mechanical lubrication and inflammation resistance are combined, and the preparation method has the advantages that the preparation method is simple, the preparation cost is low, and the application prospect is wide. The problems of large-dose toxicity, short lubrication period and the like caused by independent treatment are effectively solved, and the preparation has important clinical application significance.

The invention belongs to the technical field of biology, and particularly relates to a composition for tumor targeted therapy, hydrogel and a preparation method and application thereof. The tumor targeted therapy composition provided by the invention comprises the aging tumor cells and the celecoxib, the immune activation function of the aging tumor cells is that STCs can effectively activate the maturation of dendritic cells and the immune function of T cells and NK cells, SASP of the STCs is regulated through the celecoxib, especially generation of prostaglandin E2 is inhibited, and the tumor targeted therapy effect is improved. And the combined use further enhances the anti-tumor immune effect.

The invention relates to the field of pharmaceutical preparations, and particularly discloses a celecoxib orally disintegrating tablet and a preparation process thereof. The invention relates to a preparation process of a celecoxib orally disintegrating tablet. The preparation method comprises the following steps: adding beta-cyclodextrin into deionized water, dissolving to obtain an emulsion, adding celecoxib into the emulsion, and stirring to obtain a matrix liquid; the preparation method comprises the following steps: adding bacterial cellulose into deionized water, adding ammonium carbonate, and carrying out vacuum filtration to obtain a fiber cake; dipping the fiber cake into an absolute ethyl alcohol solution of tetraethyl silicate, washing, drying and grinding to obtain a carrier; adding the carrier into the matrix liquid, stirring at room temperature, centrifuging, and freeze-drying the centrifugate to obtain an inclusion compound; uniformly mixing the inclusion compound with a filling agent, a slipping agent, an adhesive and a sweetening agent, adding pure water, stirring, emulsifying, vacuumizing, defoaming, sub-packaging into bubble caps, pre-freezing, freeze-drying and sub-packaging. The orally disintegrating tablet prepared by the invention is high in disintegration speed, convenient to take, slightly sweet in taste and high in medication compliance of patients.

The present invention relates to a stable oral liquid pharmaceutical composition of celecoxib or pharmaceutically acceptable salts thereof. The celecoxib present in the compositions as described herein do not show any precipitation when subjected in Fasted-State Simulated Gastric Fluid (FaSSGF) at pH 2.0, temperature of 37° C.±0.5° C. and under stirring at a speed of 50 rpm at least for 60 minutes. It also relates to the process of preparing and method of using said composition of celecoxib.

It is described and claimed a pharmaceutical composition comprising celecoxib and acetaminophen as active ingredients, wherein the pharmaceutical composition is an immediate release coated tablet. The pharmaceutical composition of the invention is particularly stable and allows the oral administration in a single dosage unit of two active ingredients. It is further provided a process for manufacturing the pharmaceutical composition, as well as the use of said pharmaceutical composition for the treatment of pain, it provides analgesia and a reduction of adverse effects.

The invention discloses an application of an epoxidase type II inhibitor, the application is the application in preparation of drugs for treating liver injury, hepatitis, hepatic fibrosis, or liver function decline or complications thereof, and the application discovers that the existing COX-2 selective inhibitors such as celecoxib and the like and a novel efficient COX-2 selective inhibitor 6, 7, 8, 9, 10, 11, 12, 13, 14, 16, 17, 17, 17, 17, 17, 17, 17, 17, 17, 17, 17, 17, 17, 17, 17, 17, 17, 17, 17, the 2, 8-deuterated dimethyl-2-(trifluoromethyl)-2H-benzopyran-3-carboxylic acid disclosed by the invention has the effects of remarkably relieving liver injury, reducing necrosis focus and inflammatory cell infiltration of liver cells and resisting cholestatic hepatic fibrosis; in addition, hepatocyte lipid accumulation and ballooning induced by high fat diet can be reduced, and the progress of lipid hepatitis is remarkably inhibited; it is found for the first time that the traditional Chinese medicine composition can significantly reduce the concentration of serum bilirubin and play a role in relieving hyperbilirubinemia caused by liver injury or liver insufficiency; the traditional Chinese medicine composition can be used for treating neonatal jaundice, congenital bile duct atresia, cholestatic cirrhosis, acute toxic hepatic failure, bilirubin increase caused by acute attack of chronic hepatitis, chronic hepatic failure or hepatic encephalopathy and the like; therefore, the method has obvious economic benefit and clinical application value.

The application relates to a celecoxib capsule composition and belongs to the technical field of pharmaceutical preparations. The celecoxib capsule composition is prepared from the following components in percentage by weight: celecoxib 74.1%, lactose monohydrate 16.4%-17.4%, arginine 1.0%-2.0%, sodium dodecyl sulfate 3.0%, povidone (K30) 2.5%, cross-linked sodium carboxymethyl cellulose 1.0%, and magnesium stearate 1.0%. The problem that the dissolution curve of the celecoxib capsule is significantly slowed down during storage is solved by adding appropriate arginine in the prescription.

The invention discloses a celecoxib capsule and a preparation method thereof, and relates to the technical field of sustained-release capsules. Sorbitol is added into medicine particles to serve as a filling agent, the particles can easily form a porous network structure after being dried, and the surface porosity is increased; the porous particles can improve the release rate of the medicine. However, the sorbitol is high in hygroscopicity and can cause caking of the medicine particles, and the nano silicon dioxide absorbs moisture, so that direct contact between the sorbitol and the environment is reduced, and the particles are prevented from being bonded and clustered after moisture absorption. Therefore, the nano silicon dioxide is added to improve the stability and reduce the moisture absorption rate. In order to accelerate dissolution, polyvinyl alcohol is used for accelerating dissolution, and meanwhile, the polyvinyl alcohol can reduce the moisture absorption rate; the polyvinyl alcohol is subjected to amination treatment, and the aminated polyvinyl alcohol can improve the hydrophilicity of the capsule, so that the transmittance of the medicine is improved, and the release rate of the medicine is improved.

The application belongs to the technical field of wound dressings, and discloses a water-based gel dressing with antibacterial and scar prevention effects and a preparation method, wherein 3-fluoro-4-carboxyphenylboronic acid is introduced to graft chitooligosaccharide, a large number of catechol structures in tannic acid solution are combined with the phenylboronic acid bond to form a dynamic boron ester bond, and a network gel structure is formed by responding to the supermolecular forces such as hydrogen bonds, wherein the boron ester bond can be broken in response to the high ROS level of the wound microenvironment and the acidic environment caused by bacterial infection, so as to efficiently release celecoxib, a selective non-steroidal anti-inflammatory drug of cyclooxygenase-2, and the liposome of verteporfin is limited in volume and stays in the dressing for a longer time, so that the sustained and stable release can be maintained in the whole wound healing process, thereby achieving the effects of on-demand inflammation regulation and long-acting mechanical response regulation.

The invention provides a substrate-free anti-inflammatory hydrogel microneedle particle and a preparation method thereof. The microneedle particle comprises an anti-inflammatory active component and a microneedle substrate used for wrapping the anti-inflammatory active component, the anti-inflammatory active component is selected from any one of curcumin, celecoxib and aesculin; the hydrogel is prepared from hyaluronic acid. A substrate of a traditional microneedle is abandoned, and the problems of displacement and falling caused by sweat or skin deformation are avoided. The raw materials of the microneedle particles are safe, no chemical cross-linking agent is used during preparation, and the risks of inducing local allergy and aggravating oxidative stress are avoided. The substrate-free microneedle particles have higher flexibility and contact area, and can be better attached to the skin, so that the delivery efficiency of drugs can be improved.

The present disclosure relates to methods of diseases and / or conditions associated with Covid-19 infection, including long COVID, comprising administration of a COX-2 inhibitor, an antiviral compound, and one or more additional active ingredients, such as a combination of nirmatrelvir and ritonavir, molnupiravir, BCG vaccine, or ivermectin.

The invention discloses a high-drug-loading-capacity celecoxib solid dispersion with solubilizing performance and a preparation method thereof. The solid dispersion is prepared from the following components in percentage by mass: 50% of celecoxib, 40-47% of a carrier material and 3-10% of a crystal inhibitor, the total percentage of all the components is 100%. Wherein the carrier material is polyacrylic resin; the crystal inhibitor is selected from one or more of copovidone VA64, povidone K30, hydroxypropyl methylcellulose E5 and hydroxypropyl methylcellulose E50; the solid dispersion provided by the invention has high dissolution rate and good stability, and can effectively inhibit recrystallization of a drug in a supersaturated solution and maintain the supersaturation degree of the drug in the solution; according to the present invention, the carrier-crystal inhibitor binary polymer combination is adopted to achieve the complete release of the drug, and the new idea is provided for the preparation or the process innovation of the high drug loading capacity celecoxib preparation.

The invention provides a lipidosome preparation capable of performing brain-targeted drug delivery in a depression model, a preparation method of the lipidosome preparation and application of the lipidosome preparation in improving the anti-depression effect of fluoxetine, and belongs to the technical field of pharmaceutical preparations. The composition disclosed by the invention consists of DOPG, DSPE-PEG2000-PGP, DSPE-PEG2000, cholesterol, fluoxetine and celecoxib, and can be used for improving the anti-depression effect of fluoxetine. The double-drug-loading liposome with high entrapment efficiency and uniform particle size is prepared through a film hydration-film extrusion method, has good stability and biocompatibility, has an obvious targeting drug delivery effect in a chronic social contusion stress model, is suitable for a combined treatment strategy of depression, and has a good clinical application prospect.

The present invention provides a celecoxib cream and a preparation method thereof, and belongs to the technical field of pharmaceutical preparations, the celecoxib cream comprises, by mass, 0.5%-2% of celecoxib, 1%-20% of an oily matrix, 1%-20% of an emulsifier, 0.1%-10% of a transdermal absorption enhancer, 1%-20% of a thickener, 2%-15% of a humectant, 0.1%-2% of a preservative, 0.1%-10% of a pH regulator, and the balance of deionized water. The prepared celecoxib cream is good in stability and high in bioavailability, and gastrointestinal reaction and oral first pass effect of a traditional oral dosage form are avoided. The celecoxib cream disclosed by the invention is also added with a transdermal absorption enhancer, so that medicine molecules can be helped to penetrate through a skin barrier and directly reach a focus part; the metabolism loss of the medicine on the skin surface can be reduced, more active ingredients enter blood circulation or deep tissues, the local treatment effect is enhanced, and the important clinical value is achieved.

The invention belongs to the technical field of wound dressings, and discloses a hydrogel dressing with antibacterial and scar-preventing effects and a preparation method thereof.3-fluoro-4-carboxyphenylboronic acid grafted chitosan oligosaccharide is introduced, phenylboronic acid bonds are matched with a large number of catechol structures in a tannic acid solution to form dynamic boron ester bonds, and the dynamic boron ester bonds are grafted to the chitosan oligosaccharide; the preparation method comprises the following steps: carrying out joint response with supramolecular forces such as hydrogen bonds to form a network gel structure, enabling boron ester bonds to respond to a high ROS level of a wound microenvironment and an acidic environment caused by bacterial infection to break, so as to efficiently release cyclooxygenase-2 selective non-steroidal anti-inflammatory drug celecoxib, and enabling the vinipofen liposome to be limited by a relatively large volume, so that the vinipofen liposome has a good anti-inflammatory effect. The time of staying in the dressing is longer, and continuous and stable release can be maintained in the whole wound healing process range, so that the effects of on-demand inflammation regulation and control and long-acting mechanical response regulation and control are achieved.

The present disclosure describe a simple optimized method that allows the combined manufacture of five active substances: cyanocobalamin, pyridoxine, thiamine, pregabalin and celecoxib in a single solid, stable, immediate release pharmaceutical form for pain. The combined use of drugs that act at distinct levels is associated with greater pain relief and, as they can be used at lower doses, with a reduced risk of adverse effects. In this context, the combined use of B vitamins plus pregabalin and celecoxib would be associated with greater analgesic activity through complementary action mechanisms.

The invention belongs to the technical field of specific therapeutic activity of pharmaceutical preparations, and relates to a liposome containing an active component celecoxib, a preparation and application. The liposome disclosed by the invention is prepared by adopting a film dispersion method and is prepared from celecoxib, sauchinone, phospholipid, cholesterol and a polyvinyl alcohol-sodium alginate blend. Celecoxib and sauchinone are wrapped by lipidosome, the water solubility of the lipidosome is improved, and the drug loading capacity and the encapsulation efficiency of the lipidosome are higher through a specific formula and a specific method; in addition, the combined use of the celecoxib and sauchinone has a synergistic effect, and the effect of treating rheumatoid arthritis is superior to that of single use of the celecoxib.

An embodiment relates to a tablet comprising celecoxib, and ciprofloxacin or a pharma- ceutically acceptable salt thereof, and a low viscosity hydroxypropyl methylcellulose having a viscosity of less than 150 cP when measured as a 2% solution in water at 20°C.

The invention provides application of a CD5-targeting reagent in the aspects of reducing the drug resistance of tumor cells and improving the anti-tumor curative effect of drugs, and clarifies for the first time that CD5 molecules can promote high expression and cell nucleus displacement of transcription factors FOXO3a and FOXO4 in a forkhead cassette O signal channel; therefore, expression increase of the ABC drug-resistant protein family in diffuse large B-cell lymphoma tumor cells is mediated, and drug resistance of tumor cells to various chemotherapeutic drugs is promoted. Further, it is found that the celecoxib can significantly inhibit expression of CD5 molecule mediated ABC drug-resistant protein in B-cell lymphoma cells, then the celecoxib and chemotherapeutic drugs are combined for application, the killing effect of traditional chemotherapeutic drugs on diffuse large B-cell lymphoma tumor cells is significantly enhanced, and the chemotherapeutic drug resistance of diffuse large B-cell lymphoma is overcome. The anti-drug-resistant tumor strategy can overcome the problems of low treatment response rate and poor prognosis of the CD5-positive diffuse large B-cell lymphoma to the existing chemotherapy regimen due to multidrug resistance, and significantly improves the anti-tumor treatment effect.

The present invention relates to a pharmaceutical composition which comprises the synergistic combination of a selective inhibitor of cyclooxygenase-2, such as the active ingredient: celecoxib and its pharmaceutically acceptable salts, and a carbamate derived from guaifenesin, such as the active ingredient: methocarbamol and its pharmaceutically acceptable salts, which are formulated with pharmaceutically acceptable excipients and / or carriers and / or additives in a single dosage unit to be orally, dermally or transdermally or topically administered, which is also indicated in the treatment of pain, inflammation and muscular contractions, wherein said combination has a triple analgesic, anti-inflammatory and muscle-relaxing effect, and is better tolerated and has less side effects in patients with pain, inflammation and muscular contraction.

The present disclosure relates to methods of treating Alzheimer's disease, diseases and / or conditions associated with Covid-19 infection, including long COVID, a post-acute infection syndrome, or symptoms of orthostatic intolerance comprising administration of a therapeutically-effective combination of a COX-2 inhibitor and an antiviral compound.

The invention discloses a pharmaceutical composition containing gramine and application thereof.The pharmaceutical composition comprises gramine and celecoxib, and the mass ratio of gramine to celecoxib is 1: 1. The pharmaceutical composition with the effect of relieving ulcerative colitis (UC) has the advantages that the effect of relieving the ulcerative colitis (UC) is achieved, and the pharmaceutical composition can be used for treating the ulcerative colitis; a preclinical experiment result shows that the pharmaceutical composition provided by the invention has a good effect of treating ulcerative colitis. In the in-vivo and in-vitro UC morbidity process, 3% DSS induces a mouse UC model and LPS stimulates NCM460 cells to trigger an inflammatory reaction along with the increase of the inflammatory factor level; the pharmaceutical composition can inhibit the expression of inflammatory factors PTGS2, TNF-alpha, IL-1beta and IL-6, can protect the intestinal barrier, and significantly increases the expression of Occludin, Claudin-1 and ZO-1 proteins. The pharmaceutical composition is convenient and simple in administration route, has no obvious adverse reaction, can be developed into a new generation of medicine for relieving the ulcerative colitis, and is expected to become a good prescription for treating the ulcerative colitis.

The invention discloses an application of celecoxib or a pharmaceutical salt thereof in preparation of an antifungal drug synergist. An antifungal drug is selected from an azole antifungal drug, an allylamine antifungal drug or an echinocandin antifungal drug. The azole antifungal drug is selected from the group consisting of fluconazole, voriconazole, itraconazole, posaconazole and isavuconazole; the allylamine antifungal drug is selected from terbinafine; the echinocandin antifungal drug is selected from caspofungin. In-vivo and in-vitro experiments prove that when the celecoxib is combined with the azole antifungal drug and the allylamine antifungal drug terbinafine, a synergistic antifungal effect is shown, and when the celecoxib is combined with the echinocandin antifungal drug caspofungin, an additive effect is shown. Celecoxib and fluconazole are combined for use, so that the survival rate of fungal infected animals can be increased, and toxicity to wax moth larvae and mammalian cells is low.

The present application relates to a celecoxib-vitamin E prodrug. The celecoxib-vitamin E prodrug is prepared by connecting celecoxib with vitamin E by means of a dithio-bis-acetic acid. The catalysts used include: dicyclohexyl carbodiimide (DCC), 4-dimethylaminopyridine (DMAP). The prodrug has some characteristics: uniform distribution in a spherical shape, the average particle size is about 700 nm, the drug loading can reach 4 mg•mL ‑1 The prodrug can improve the bioavailability of celecoxib, and the preparation method thereof is disclosed.

The utility model discloses specific gravity detection alarm equipment for celecoxib production, which comprises a detection cylinder, an installation disc is fixed on the detection cylinder, an alarm box is arranged on the installation disc, a controller and an audible and visual alarm are arranged on the alarm box, a floating ring and a floating cylinder are arranged in the detection cylinder, the floating ring is sleeved outside the floating cylinder, and the controller is connected with the audible and visual alarm. A distance measuring sensor is installed on the floating ring and used for detecting the distance between the floating ring and the floating cylinder, the floating ring and the floating cylinder are supported through a bracket, the edge of the bracket extends out of a strip groove in the surface of the detection cylinder and is provided with a sliding sleeve, a screw penetrates through the sliding sleeve and is in threaded connection with the sliding sleeve, and one end of the screw is connected with a motor. The floating ring and the floating cylinder can directly extend into the reaction kettle for easy specific gravity detection, the trouble of repeated sampling detection is saved, and the floating ring and the floating cylinder can lift and move under the control of the sliding sleeve and the screw rod, so that the floating ring and the floating cylinder can be lifted to be away from a solution during stirring reaction in the reaction kettle, and the solution is prevented from overturning the floating ring and the floating cylinder.

The present invention discloses a ROS-enhanced liposome and its preparation method and application, which relates to the technical field of biomedical polymer materials and new dosage forms of pharmaceutical preparations. The liposome is composed of egg yolk lecithin, cholesterol and DSPE-mPEG. 2K The liposome is a membrane material prepared by a thin film dispersion extrusion method to encapsulate different drugs; wherein the drug is a ROS-responsive celecoxib dimer prodrug (CTC); or a combination of a ROS-responsive celecoxib dimer prodrug (CTC) and sinomenine hydrochloride (SIN); or a combination of a ROS-responsive celecoxib dimer prodrug (CTC), sinomenine hydrochloride (SIN) and L-butionine-(S,R)-sulfoximine (L-BSO). The liposome not only has the advantages of good stability and long circulation time, but also can target and enrich RA tissues through ELVIS, release celecoxib in a high ROS environment, and then combine with sinomenine hydrochloride to achieve a combined therapeutic effect.

This invention provides a biodegradable microsphere, wherein the microsphere (i) has a diameter of from 1 μm to 500 μm; (ii) comprises a polylactic-co-glycolic acid copolymer (PLGA) matrix; (iii) carries pharmaceutical celecoxib; and (iv) when present in a suitable joint-related tissue, releases celecoxib for at least one month. This invention also provides related injectable formulations, methods for treating joint-related disorders, and kits.

This disclosure relates to methods for treating diseases and / or conditions (including long COVID) associated with Covid-19 infection, the methods comprising administering a COX-2 inhibitor, an antiviral compound, and one or more additional active ingredients, such as a combination of nematvir and ritonavir, monorapvir, a BCG vaccine, or ivermectin.