621 results about "Drug activity" patented technology

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.

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.

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 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 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.

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.

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 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.

The invention discloses a drug-loaded polygonatum kingianum extracellular vesicle, a preparation method and an application of the drug-loaded polygonatum kingianum extracellular vesicle in preparation of an anti-photoaging product, and aims to provide a drug-loaded polygonatum kingianum extracellular vesicle which has relatively high encapsulation efficiency and drug loading rate and good stability and biocompatibility, can effectively treat skin UVB inflammation, solves the problem that a drug is insoluble in water, improves the curative effect, and can be used for preparing an anti-photoaging product and a preparation method of the drug-loaded polygonatum kingianum extracellular vesicle. According to the technical scheme, the drug-loaded polygonatum kingianum extracellular vesicles comprise the polygonatum kingianum extracellular vesicles and drug active components loaded in the polygonatum kingianum extracellular vesicles, and the drug-loaded polygonatum kingianum extracellular vesicles comprise the drug-loaded polygonatum kingianum extracellular vesicles and the drug active components loaded in the drug-loaded polygonatum kingianum extracellular vesicles. The pharmaceutical active component is at least one of resveratrol, glutathione, astaxanthin and vitamin C. The invention further discloses a preparation method of the pharmaceutical composition. The invention belongs to the technical field of biological medicine.

The invention discloses a system and a method for rapidly detecting trace active ingredients of a medicine, belongs to the technical field of medicine detection, and relates to cross application of surface enhanced Raman spectroscopy and artificial intelligence. The system comprises a sample preparation module, a micro-fluidic enrichment module, a Raman spectrum acquisition module, a self-adaptive spectrum analysis module, a multi-component identification module and an intelligent report generation module, and efficient enrichment and nanogram-level detection of drug molecules are realized through an enhanced surface Raman scattering micro-fluidic chip. Intelligent identification and accurate quantification of complex spectral characteristics are realized by adopting a deep learning algorithm and a self-adaptive weight calculation method, synchronous detection of 5-10 active pharmaceutical ingredients is supported, the detection sensitivity reaches nanogram / milliliter level, the quantification error is less than 5%, the detection time of the whole process is 5-10 minutes, and the detection accuracy is high. The sensitivity, the accuracy and the efficiency of medicine quality detection are obviously improved.

The invention provides application of sulfasalazine and a combined drug thereof in drug-resistant head and neck malignant tumors, which comprises the following steps: when the sulfasalazine is independently used, the sulfasalazine has a treatment effect on the drug-resistant head and neck malignant tumors and can delay the growth of the drug-resistant head and neck malignant tumors; combined use of sulfasalazine and chemotherapeutic drugs has a synergistic effect, and the sulfasalazine can be used for treating drug-resistant head and neck malignant tumors. The technical problem to be solved by the invention is to explore the drug activity of sulfasalazine in the treatment of drug-resistant head and neck malignant tumors and solve the limitation of drug resistance to treatment in the drug treatment process.

The application provides application of grass aconite in preparation of anti-epilepsy drugs and a mechanism analysis method, relates to the technical field of anti-epilepsy drugs, and discloses a "drug active ingredient-key target point-disease-pathway" network diagram of the grass aconite anti-epilepsy by starting from the chemical structure of the effective component of the grass aconite, applying network pharmacology and molecular docking technology, revealing how the active component of the grass aconite plays the drug efficacy through "multi-target point, multi-pathway and multi-pathway" combined regulation, predicting the anti-epilepsy target point and mechanism of the grass aconite, and providing certain theoretical reference for research and development of the grass aconite as an anti-epilepsy drug and a functional food.

The invention belongs to the technical field of pharmaceutical preparations, and relates to a compound I patch composition, a compound I patch and a preparation method thereof. The patch composition comprises the following components in parts by weight: 0.5-12 parts of a pharmaceutical active component, 10-30 parts of a penetration enhancer, 15-56 parts of a crystal inhibitor and 35-57 parts of an acrylic acid pressure-sensitive adhesive, the patch composition also comprises solvent dimethyl sulfoxide and absolute ethyl alcohol, and the residual quantity of the dimethyl sulfoxide is not less than 2.0%; wherein the active pharmaceutical ingredient is a compound I, and the structural formula of the compound I is shown in the specification. According to the patch composition containing the compound I, the medicine stability is high, medicine crystallization and impurity generation are effectively avoided or reduced, and the patch containing the compound I has higher stability and safety; the patch composition containing the compound I has more appropriate drug permeability, so that the patch containing the compound I has higher drug effectiveness.

A double-stranded siRNA for inhibiting PNPLA3 expression and a conjugate comprising same. The double-stranded siRNA comprises a sense strand and an antisense strand, wherein one or more nucleotide residues in a nucleotide sequence of the sense strand and / or the antisense strand are replaced with r1 represented by formula I: formula (I). The introduction of a non-natural nucleotide monomer into the double-stranded siRNA improves the target selectivity and activity of the siRNA sequence, reducing the off-target risk while maintaining high drug activity. Also provided is a tetravalent GalNAc, making it easier to scale up synthesis and reduce costs.

The invention relates to pamoate drug sustained release microspheres and a preparation method thereof. According to the sustained-release microsphere preparation for injection prepared by the preparation method disclosed by the invention, the particle size distribution of the microspheres is relatively narrow, and the release time of active pharmaceutical ingredients can last for about three months to four months. Besides, the microsphere preparation prepared by the invention can maintain stable blood concentration in an animal body, has no large fluctuation of the blood concentration within 3-4 months, and better avoids the occurrence of toxic and side effects.

The invention discloses a multilevel liver targeting drug delivery system based on ionizable amino lipid and a preparation method thereof, the system comprises the following components: target modified ionizable amino lipid, ionizable amino lipid, auxiliary lipid and structural lipid in a molar ratio of (10-30): (30-60): (5-40): (15-55), according to the system, nano lipid particles exist in a water-in-oil-in-water nano emulsion form; wherein the ionizable ammonia lipid is a compound with a structure as shown in a formula (I). The system is suitable for delivering nucleic acid, protein and other active pharmaceutical ingredients to the liver so as to improve the accuracy and treatment effect of drug delivery and reduce the side effects of non-target organs.

Disclosed are a deuterated camptothecin compound represented by formula II and a pharmaceutically acceptable salt thereof, a preparation method thereof, a pharmaceutical composition containing the deuterated camptothecin compound or the pharmaceutically acceptable salt thereof, and uses thereof in the treatment of tumor-related diseases. The deuterated camptothecin compound has excellent pharmaceutical activity and pharmacokinetic characteristics, and has reduced in-vivo toxicity and improved in-vivo safety.

The invention relates to an antibody drug conjugate as well as a preparation method and application thereof, the preparation method of the antibody drug conjugate comprises the following steps: S10, obtaining a wild type antibody, and carrying out hydrolysis reaction on galactose at the tail end of a sugar chain of the wild type antibody to obtain an antibody of which the tail end is four GlcNAc sugar types; s20, obtaining B4GALT1 (Y286L), mixing the UDP-GalNAz, the B4GALT1 (Y286L) and the antibody, and carrying out an enzymatic reaction so as to transfer the azido galactose to the tail end of a carbohydrate chain of the antibody, so as to obtain a carbohydrate chain modified antibody; and S30, mixing a target drug with the carbohydrate chain modified antibody, and carrying out a one-step click chemical reaction to obtain the antibody drug conjugate. The galactose hydrolase can retain four GlcNAc sites, and after the galactose hydrolase is connected with GalNAz, four target drug molecules can be combined, the DAR value of the antibody drug conjugate is increased, and the drug activity of the antibody drug conjugate is improved.

The invention discloses a method for predicting the stability of a protein co-prescription preparation, which is characterized in that when the second virie coefficients of the proteins of all active pharmaceutical ingredients in the co-prescription preparation are positive values and the cross virie coefficients of the proteins of different active pharmaceutical ingredients are also positive values, the co-prescription preparation has good long-term stability; when the second virie coefficient of the protein of at least one medicine active ingredient is a negative value and at least one cross virie coefficient of the protein of each heterogeneous medicine active ingredient is a negative value, the long-term stability of the co-prescription preparation is poor; according to the method, the stability of the co-prescription preparation is predicted through the second Wirie coefficient and the cross Wirie coefficient of the active pharmaceutical ingredient protein of the co-prescription preparation, and the prediction result is accurate; the second Virie coefficient and the cross Virie coefficient are measured by using the component gradient multi-angle light scatterometer, the sample does not need to be marked or subjected to other treatment, sample preparation and instrument operation are simple, and the detection speed is high.