860 results about "Drug activity" patented technology

Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.

Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.

The present invention provides combination therapy that includes an KRASG12C inhibitor, such asor a pharmaceutically acceptable salt thereof, and one or more additional pharmaceutically active agents, particularly for the treatment of cancers. The invention also relates to pharmaceutical compositions that contain an KRASG12C inhibitor and one or more additional pharmaceutically active agents for the treatment of cancers.

The invention relates to application of a combined pharmaceutical composition in preparation of a medicine for resisting transforming follicular lymphoma. Active components in the combined pharmaceutical composition comprise a first component and a second component, the first component is selected from any one or a combination of at least two of sitagliflozin, pharmaceutically acceptable salt, isomer, solvate and metabolite of sitagliflozin; and the second component is selected from any one or a combination of at least two of chidamide, pharmaceutically acceptable salts, isomers, solvates and metabolites of the chidamide. Research finds that the combined use of the two active components not only can reduce the dosage of each drug and improve the medication safety, but also has the effect of improving or treating convertible follicular lymphoma more remarkably than that of a single drug active component, and plays a role in synergistic promotion. The invention provides an effective drug combination strategy for improvement or treatment of convertible follicular lymphoma, and has very significant significance.

The invention relates to a drug delivery carrier based on extracellular vesicles and application thereof.The drug delivery carrier contains extracellular vesicle scaffold protein and recombinant membrane fusion protein, the recombinant membrane fusion protein comprises a first fragment and a second fragment, the amino acid sequence of the first fragment is shown as SEQ ID NO: 5, and the amino acid sequence of the second fragment is shown as SEQ ID NO: 6; the second fragment has n amino acids, the sequence of the second fragment is the sequence of the first n amino acids at the N end of the amino acid sequence as shown in SEQ ID NO: 7, and n is an integer between 50 and 200. According to the drug delivery carrier disclosed by the invention, the efficiency of releasing drug active molecules before reaching lysosome is remarkably improved, and the drug effect of extracellular vesicle drugs can be improved.

The invention relates to hydrogel for treating ischemic brain injury and a preparation method thereof. The hydrogel is prepared from the following raw materials: methylacryloylated hyaluronic acid, methylacryloylated gelatin, curcumin loaded HA-PPS (Hydroxypropyl-Polyphenylene Sulfite) nano-micelles and dendrobium polysaccharide loaded sodium alginate microspheres. Through combination of a nanotechnology and an intelligent response material, HA-PPS is adopted to load curcumin and sodium alginate microspheres are adopted to encapsulate dendrobium polysaccharide, so that the drug activity can be more effectively protected, the drug is protected to penetrate through a blood brain barrier and be accurately delivered to a brain injury area, and targeted release of the drug is realized; the anti-oxidation and anti-inflammatory effects are better under the combined action of the curcumin and the dendrobium polysaccharides, and meanwhile, a slow release function is also achieved.

Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.

This disclosure relates to administration of a combination of: 1) about 100-110 mg, about 104-106 mg, or about 105 mg or less of bupropion hydrochloride, or a molar equivalent amount of the free base form or another salt form of bupropion; and 2) about 40-50 mg, about 44-46 mg, or about 45 mg or less of dextromethorphan hydrobromide, or a molar equivalent amount of the free base form or another salt form of dextromethorphan in human patients for treating neurological and psychiatric conditions, such as agitation associated Alzheimer's disease and / or reducing relapse of agitation in Alzheimer's disease.

Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.

The invention discloses a hollow skeleton type drug-loading rod core as well as a preparation method and application thereof. The raw material composition comprises the following components in parts by weight: 1-1000 parts of active pharmaceutical ingredients; 100 parts of R-vinyl silicone rubber; 0.45 to 20 parts of hydrogen-containing silicone oil; more than or equal to 0.000002 parts of a catalyst; the content of vinyl in the R-vinyl silicone rubber is 0.1-0.5 mol%; the content of Si-H groups in the hydrogen-containing silicone oil is 0.18 to 1.6 mol%; the molar ratio of the Si-H group to the vinyl group is (0.5-20): 1. According to the invention, methyl vinyl silicone rubber, hydrogen-containing silicone oil, a platinum catalyst and other components are taken as a basic prescription of silicone rubber, and a model drug and the silicone rubber are mixed by using an extrusion technology to prepare the hollow skeleton type drug-loaded rod core. Advantages of traditional storage type implants and skeleton type implants are integrated, the production process is simple, the medicine application range is wide, the release amount is stable, and the release amount is large.

Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.

The invention discloses a drug-loaded rod core, a raw material composition thereof, an implant, preparation and application. The raw material composition of the drug-loaded rod core comprises the following components in parts by weight: 1-1000 parts of active pharmaceutical ingredients; 100 parts of R-vinyl silicone rubber; 0.45 to 20 parts of hydrogen-containing silicone oil; the content of a catalyst is greater than or equal to 0.000002 part, preferably 0.000002-1 part; wherein the average particle size of the active pharmaceutical ingredients is 1-1000 nm. According to the invention, the drug active ingredients with the average particle size of 1-1000nm are adopted, so that the solubility of the drug can be obviously improved; the compatibility with silicon rubber is better, the release speed of the obtained skeleton type implant and storage type implant is obviously improved, and the drug release behavior is stable; meanwhile, the application range is wide, the preparation method is suitable for various drugs, and large-dose stable release is achieved.

Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.

The invention discloses nano-composite hydrogel based on active oxygen removal as well as a preparation method and application of the nano-composite hydrogel, and relates to the technical field of biomedicine. The nano composite hydrogel based on active oxygen removal comprises a three-dimensional network skeleton structure formed by cross-linking oxidized chondroitin sulfate and carboxymethyl chitosan, and melatonin-loaded mesoporous polydopamine nanoparticles are encapsulated in the three-dimensional network skeleton structure. According to the invention, a nano material is combined with a three-dimensional network skeleton structure of the hydrogel, a novel nano composite hydrogel is developed, and the nano composite hydrogel has self-healing ability, good biocompatibility, good mechanical properties and long-acting drug release ability; meanwhile, the melatonin is loaded into the nano-composite hydrogel to develop a medicine compound, the medicine activity and the treatment effect are better than those of the melatonin, inflammation and oxidative stress can be relieved more effectively, and symptoms can be improved more effectively.

The invention discloses an antibody-coupled drug combination prediction method based on a virtual graph and multi-scale characteristics, provides a method for constructing initial characteristics of a drug carrier, a linker, an antibody heavy chain and light chain and an antigen target protein, provides a method for extracting drug sequence characteristics by using 1DCNN, and designs a drug characteristic extraction method based on graph virtual nodes. Virtual nodes and virtual edges are introduced into a molecular structure diagram, a Graph Transform is used as a diagram feature extractor, virtual node features are used as drug representation, then protein and drug features are input into a feature fusion module, an attention mechanism and a gating jump connection mechanism are added in feature fusion, and the protein and drug features are fused. And the feature information of different hidden layers is fused while the potential interaction is captured, so that higher-precision affinity prediction is realized. The method can solve the technical problem that the structural features of the antibody-coupled drug are difficult to extract in the prior art and the technical problem that the features of different components are difficult to fuse.

The invention relates to an antidepressant pharmaceutical composition and application thereof, and particularly discloses a pharmaceutical composition for treating depression as well as a preparation method and application thereof. The active pharmaceutical ingredients of the pharmaceutical composition are prepared from the following traditional Chinese medicines in parts by weight: 500 to 600 parts of radix bupleuri, 500 to 600 parts of fructus aurantii immaturus, 500 to 600 parts of radix aucklandiae, 500 to 600 parts of pericarpium citri reticulatae, 500 to 600 parts of rhizoma pinelliae preparata, 750 to 900 parts of herba taraxaci, 500 to 600 parts of scorched fructus crataegi, 300 to 360 parts of scorched semen arecae, 500 to 600 parts of paederia scandens, 300 to 400 parts of radix codonopsis, 300 to 400 parts of rhizoma corydalis and 500 to 600 parts of fried medicated leaven. The pharmaceutical composition has a remarkable curative effect on depression, animal experiments show that the pharmaceutical composition can remarkably enhance the social coefficient (showing that the pharmaceutical composition can improve social fear of depression patients) and improve sweet water preference (showing that the pharmaceutical composition is beneficial to transformation of negative emotions such as interest deficiency of the depression patients), and the pharmaceutical composition is safe to take, free of adverse reaction and toxic and side effects and free of toxic and side effects. And the composition can take effect quickly, and can take effect generally within 1-2 weeks after medication.

The invention discloses a colorectal cancer radiotherapy sensitization medicine and application thereof, belongs to the field of biological medicine, and particularly relates to a colorectal cancer radiotherapy sensitization medicine which comprises active pharmaceutical ingredients and a solvent, the active pharmaceutical ingredients comprise doxorubicin and a nitrogen-containing compound, the nitrogen-containing compound comprises quinoline-6-carbohydrazide and N-benzyloxymethyl-4-nitroimidazole, and the nitrogen-containing compound comprises quinoline-6-carbohydrazide and The colorectal cancer radiotherapy sensitization medicine disclosed by the invention focuses on a key driving gene FOXP4 for colorectal cancer radiotherapy resistance, and FOXP4 protein is degraded through a ubiquitin-proteasome way, so that not only can the sensitivity of tumor cells to radiotherapy be remarkably improved and tumor growth be inhibited, but also damage to normal tissues is reduced; moreover, the problem of drug resistance easily generated by a traditional method is effectively avoided, the research and development cost is greatly reduced, clinical transformation is accelerated, and the method has a good clinical application prospect.

The invention provides a meibomian gland dysfunction treatment composition based on chlorella, the composition comprises sodium hyaluronate gel and drug-loaded chlorella powder, and the drug-loaded chlorella powder comprises chlorella and loaded drug components. The invention also provides a preparation method of the meibomian gland dysfunction treatment composition based on chlorella, which comprises the following steps: (1) dispersing a chlorella suspension in a sodium hydroxyethyl cellulose solution, and adding the medicinal components in the stirring process; (2) carrying out ultrasonic treatment and freeze drying to obtain drug-loaded chlorella powder; and (3) resuspending the drug-loaded chlorella powder, and adding sodium hyaluronate to form the gelatinous composition. The invention also provides application of the composition in preparation of medicines for treating meibomian glands. The composition not only can deliver active ingredients of the medicine in a targeted manner, but also can supplement lipid components lacking in meibomian glands, so that meibomian gland dysfunction is effectively treated.

The invention provides a preparation composition of a glucagon-like peptide-1 receptor agonist for nasal mucosa administration, and particularly relates to the technical field of biological medicine materials. The preparation composition mainly comprises a glucagon-like peptide-1 receptor stimulant, alkyl glycoside and phospholipid, wherein the ratio of the glucagon-like peptide-1 receptor stimulant to the alkyl glycoside to the phospholipid is (0.25-17.5): (0.25-10): (0.1-10) by mass. The active pharmaceutical ingredients in the preparation composition provided by the invention are delivered through nasal mucosa, directly enter blood circulation from an absorption part, can take effect quickly, have higher bioavailability, and improve the compliance of patients.

The present disclosure provides a delivery system for a pharmaceutically active ingredient, as well as a preparation method and use of the delivery system. The delivery system comprises lipid nanoparticles and extracellular vesicles, and the lipid nanoparticles and the extracellular vesicles form a chimeric structure through fusion polypeptide. The delivery system disclosed by the invention has the characteristics of high delivery efficiency, low immunogenicity, capability of efficiently loading mRNA and the like.

A drug sustained-release microsphere for injection and a preparation method therefor. A sustained-release microsphere preparation for injection prepared by means of the preparation method has a relatively narrow particle size distribution with regard to microspheres, and the release time of the active ingredients of a drug can last about four weeks to six weeks. The small molecule sustained-release microsphere has a stable blood concentration, can maintain the blood concentration within 4-6 weeks relatively well, and has no significant fluctuation in blood concentration, which better avoids the occurrence of toxic side effects.

The invention provides a pharmaceutical composition, a rod core, an implant and a preparation method and application thereof. The pharmaceutical composition comprises the following components in parts by weight: 1-1000 parts of active pharmaceutical ingredients; 100 parts of R-vinyl silicone rubber; hydrogen-containing silicone oil; 0.000002 to 1 part of a catalyst; r in the R-vinyl silicone rubber is substituted or unsubstituted C1-C5 straight-chain alkane or branched alkane, and substituted or unsubstituted C6-C20 aromatic hydrocarbon; the content of vinyl in the R-vinyl silicone rubber is 0.10 to 0.50 mol%; the content of Si-H groups in the hydrogen-containing silicone oil is 0.15 to 1.6 mol percent; the molar ratio of Si-H group in the hydrogen-containing silicone oil to vinyl in the R-vinyl silicone rubber is (0.5-20): 1. The implant provided by the invention can reduce drug loss and sudden release phenomenon, the drug release is more stable, and the production speed is greatly increased.

The present invention relates to a highly concentrated, stable pharmaceutical formulation of a pharmaceutically active anti-HER2 antibody, such as e.g. Trastuzumab (HERCEPTIN™), Pertuzumab or T-DM1, or a mixture of such antibody molecules for subcutaneous injection. In particular, the present invention relates to formulations comprising, in addition to a suitable amount of the anti-HER2 antibody, an effective amount of at least one hyaluronidase enzyme as a combined formulation or for use in form of a co-formulation. The formulations comprise additionally at least one buffering agent, such as e.g. a histidine buffer, a stabilizer or a mixture of two or more stabilizers (e.g. a saccharide, such as e.g. α,α-trehalose dihydrate or sucrose, and optionally methionine as a second stabilizer), a nonionic surfactant and an effective amount of at least one hyaluronidase enzyme. Methods for preparing such formulations and their uses thereof are also provided.

The invention discloses an application of a small molecule compound SFII in preparation of drugs for resisting pyroptosis and GSDMD inhibitors with pyroptosis resisting activity. The small molecule compound Scutellaria flavone II (SII) extracted from Scutellaria baicalensis roots plays an important role in preparation of drugs for inhibiting pyroptosis inflammation so as to prevent or treat atherosclerosis. Experiments prove that the active pharmaceutical ingredient SFII has a definite effect on promoting atherosclerosis by virtue of Gasdermin D and GSDMD mediated macrophage pyroptosis, is convenient to obtain, can be used for preparing drugs for inhibiting GSDMD protein activity to resist pyroptosis and exerting an anti-inflammatory effect so as to prevent or treat atherosclerosis, and has a remarkable effect. The small molecule compound SFII provides a new treatment strategy for atherosclerosis, and has a wide application prospect.

The invention provides an oral cavity soluble film solution based on a nano-carrier and a preparation method of an oral cavity soluble film. According to the method, a nano-carrier technology, microcapsule multilayer coating, a low-temperature electrochemical polymerization method and an ultrasonic dispersion technology are utilized, and uniform distribution and multi-stage slow release of a medicine in an oral instant film are achieved. According to the invention, active pharmaceutical ingredients are firstly wrapped by a nano-carrier, and then a multi-layer composite coating structure is formed by a microcapsule technology, so that drug release effects at different stages are realized. And then, uniformly mixing the microcapsule nano-drug particles with a film-forming substrate, depositing layer by layer to form a film through a low-temperature electrochemical polymerization method, and carrying out low-temperature drying treatment. The soluble film disclosed by the invention has good biocompatibility and mechanical strength, and can be gradually dissolved in an oral cavity, and the medicine is released according to a set stage, so that a long-acting oral care or treatment effect is realized. The method avoids the use of high temperature and organic solvents, is environment-friendly and safe, and is suitable for delivery systems of various oral drugs.

An oral suspension pharmaceutical composition is disclosed for water soluble salts of arylalkanoic acid (NSAID) drugs such as ibuprofen and naproxen. When mixed with glyceryl esters such as glyceryl caprate / caprylate and water, the resulting combination forms a “liquid scaffold” structure that reliably enables the suspension of significant quantities of said arylalkanoic acid drugs. For example, suspensions containing 25% w / w arylalkanoic acid may be obtained using the aforementioned combination. Suspensions comprising further pharmaceutically active agents, in addition to said arylalkanoic acids, may also be prepared. Also disclosed is a binary blend of glyceryl caprate / caprylate and the sodium salt of ibuprofen and a ternary blend of glyceryl caprate / caprylate and the potassium salt of ibuprofen.

Described herein are shock wave catheters and methods of use thereof for delivering an active agent of a drug to the CNS via a body lumen or cavity, such as sinonasal cavity, which can bypass the blood-brain barrier (BBB). The catheters described herein can be advanced through an intranasal passage to the nasal cavity such that at least a portion of the enclosure is disposed in the nasal cavity. The enclosure can be coated with a drug coating. The method can include filling the enclosure with a conductive fluid. At least one shock wave can be generated at a shock wave emitter of the catheter disposed within the enclosure. The at least one shock wave can cause a therapeutically effective amount of the active agent of the drug coating to be delivered to the CNS via tissue of the nasal cavity, in turn, treating central nervous system diseases.

The invention relates to the technical field of medical gel, in particular to gynecological vaginal mucosa repairing gel and a preparation method thereof. Comprising the following raw materials: carbomer, glycerol, sodium hyaluronate, vitamin E, potassium sorbate, a modified nano polylactic acid-glycolic acid copolymer, modified nano collagen, albumin, tea tree essential oil, aloe, astragalus membranaceus, dandelion, stigma croci and ginseng. The modified nano polylactic acid-glycolic acid copolymer, the modified nano collagen and the albumin play a role through a synergistic effect, and the modified nano polylactic acid-glycolic acid is used as a skeleton structure for cell growth and is firmly attached to the active pharmaceutical ingredient-albumin compound; the polyacrylic acid chain on the surface controls the drug release rate by sensing the change of the pH value, the albumin initiates endocytosis through specific binding, and the albumin and the modified nano collagen jointly improve the anti-inflammatory performance, promote cell proliferation and differentiation and promote repair and regeneration of vaginal mucosa tissues.

The invention belongs to the technical field of medical instruments. The invention discloses a drug coating balloon catheter and a preparation method thereof. In one aspect, a drug coated balloon catheter includes a catheter with a balloon; a drug coating at least comprising an inner coating and an outer coating is arranged on the outer wall of the balloon, and the inner coating and the outer coating are provided with drug active ingredients and different carriers respectively; when the balloon is expanded, the inner coating and the outer coating are separated from the balloon through the state change of the temperature-sensitive carrier of the inner coating under the body temperature environment of a patient and the hydration effect, and the outer coating is used for promoting corresponding active pharmaceutical ingredients to be transferred into target tissues through the carrier of the outer coating when the outer coating is separated from the balloon. On the other hand, the invention provides a preparation method of the drug coating balloon catheter. The preparation method has the advantages that the adhesiveness of the drug coating on the balloon can be effectively improved so as to reduce the delivery loss, and the release rate of the drug coating on diseased tissues can be improved so as to improve the drug transfer capacity.

The invention belongs to the technical field of drug synthesis, and particularly relates to an adamantane derivative as well as a synthesis method and application thereof. The adamantane derivative comprises an intermediate structural formula I, an intermediate structural formula II and an intermediate structural formula III, and the structural general formula is as follows: Linker is substituted or unsubstituted C6-C10 aroyl, R1 is hydrogen or C1-C6 alkyl, R2 is hydrogen, C1-C6 alkyl or a nitrogen-containing or nitrogen-free structural fragment, or the integral structure of R1R2 is N-substituted heterocyclic pentyl or heterocyclic cyclohexyl. According to the adamantane derivative provided by the invention, an adamantane structure is combined with part of groups of OAB-14, and a parent nucleus structure is changed, so that the drug activity is improved. The invention also provides a synthesis method of the compound, the obtained compound is screened through cell viability research, and the compound has a potential synergistic effect in the aspects of preventing influenza and treating Alzheimer's disease.