326 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.

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 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.

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.

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 present invention relates to a pharmaceutical combination product and a therapeutic use thereof. Specifically, the present invention provides a pharmaceutical combination product comprising a first pharmaceutically active ingredient and a second pharmaceutically active ingredient, wherein the first pharmaceutically active ingredient is a KRAS inhibitor. The present invention also provides a use for treating tumors, comprising administering the pharmaceutical combination product of the present invention to a subject in need.

The invention discloses a drug activity prediction method and system based on multi-modal medical big data, and relates to the technical field of artificial intelligence. The method comprises the steps of obtaining multi-modal medical big data, and performing multi-modal coverage collection based on the multi-modal medical big data to obtain a multi-modal data set; carrying out biological feature recognition based on the multi-modal data set and carrying out clustering analysis to determine a plurality of biological feature classes; performing drug activity influence analysis according to the biological characteristic classes, and constructing a characteristic-activity mapping list to screen target candidate drugs; and extracting biological characteristic data prediction activity based on the target candidate drugs, and generating drug activity report feedback optimization data. The technical problems of inaccurate prediction result and poor generalization ability caused by dependence on single-modal data and lack of correlation analysis on complex biological characteristics of a traditional drug activity prediction method are solved, and high-precision prediction of drug activity is realized by utilizing multi-modal fusion and biological characteristic clustering analysis, so that the method is suitable for large-scale popularization and application. And the medicine screening efficiency and the intelligent level are improved.

Use of a bitter melon exosome and an oral medicament prepared therefrom. The bitter melon exosome obtained from the bitter melon juice can be used for preparing a pharmaceutical formulation embedding a protein, a polypeptide, a small molecule peptide, a nucleic acid, or a small molecule compound. The compositions of the oral medicament of the present invention comprise the bitter melon exosome and an active pharmaceutical ingredient encapsulated in the bitter melon exosome. The bitter melon exosome is suitable for preparing a drug that is easily damaged by the gastrointestinal tract and is mostly administered by means of an injection route into an oral agent, and the oral agent can produce a similar therapeutic effect to that of the injection administration route by oral administration, and is convenient to use. The extraction method for the bitter melon exosome is simple and has a low cost. Moreover, the bitter melon exosome has no immunogenicity, has relatively high biocompatibility and biosafety, and has relatively strong tolerance to gastric acid and digestive tract proteolytic enzymes, and intestinal barrier permeability.

The invention belongs to the technical field of medicine synthesis, and particularly relates to a memantine derivative and a synthesis method and application thereof. The memantine derivative comprises an intermediate structural formula I, an intermediate structural formula II, an intermediate structural formula III and a structural general formula, 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 R1 and R2 is N-substituted heterocyclic pentyl or heterocyclic cyclohexyl. According to the memantine derivative provided by the invention, a memantine group is combined with an OAB-14 partial structure to change a parent nucleus structure, so that the drug activity is improved. The invention also provides a synthesis method of the compound, and the obtained compound is used for treating Alzheimer's disease and Parkinson's disease.

This disclosure provides mixtures of beta-cyclodextrin molecules substituted at one or more hydroxyl positions by hydroxypropyl groups, the mixture optionally including unsubstituted beta-cyclodextrin molecules, for use as a pharmaceutically active ingredient; methods of making such mixtures; methods of qualifying such mixtures for use in a pharmaceutical composition suitable for intrathecal or intracerebroventricular administration; pharmaceutical compositions suitable for intrathecal or intracerebroventricular administration comprising such mixtures; and methods of using the pharmaceutical compositions for treatment of Niemann-Pick disease Type C.

A apparatus including: a silicone-based body oriented down a central axis, the silicone-based body comprising: a rigid frame having a top axial surface and a bottom axial surface, an outer surface, and a substantially arcuate inner surface; and a plurality of gas-permeable, flexible film membranes connecting the inner surface about a perimeter of the rigid frame at the top axial surface and the bottom axial surface respectively to define an internal void within the body, wherein the rigid frame has a plurality of corrugations along the top axial surface and the bottom axial surface, and wherein the internal void provides for a medically, biologically, chemically, or pharmaceutically active environment.

This disclosure provides mixtures of beta-cyclodextrin molecules substituted at one or more hydroxyl positions by hydroxypropyl groups, the mixture optionally including unsubstituted beta-cyclodextrin molecules, for use as a pharmaceutically active ingredient; methods of making such mixtures; methods of qualifying such mixtures for use in a pharmaceutical composition suitable for intrathecal or intracerebroventricular administration; pharmaceutical compositions suitable for intrathecal or intracerebroventricular administration comprising such mixtures; and methods of using the pharmaceutical compositions for treatment of Niemann-Pick disease Type C.

This invention provides anhydrous ethyl carboxylate compound-coated taste-masking granules. The anhydrous taste-masking granules comprise ethyl carboxylate compound-coated microcapsules and a flavoring material. The ethyl carboxylate compound-coated microcapsules are formed by sequentially coating a blank core with a drug-loaded layer, an isolation layer, and a taste-masking layer. The drug-loaded layer includes an active pharmaceutical ingredient, a coating material, an anti-adhesion agent, and an antistatic agent. The isolation layer includes a coating material, an anti-adhesion agent, and an antistatic agent. The taste-masking layer includes a coating material, a plasticizer, an anti-adhesion agent, and an antistatic agent. The active pharmaceutical ingredient is an ethyl carboxylate compound or a pharmaceutically acceptable salt thereof. The structure of the ethyl carboxylate compound is shown below. By using a smaller-sized blank core, a specific amount of talc, and Eutec E100 / EPO as the coating material for the taste-masking layer, smaller-sized coated microcapsules with fewer static electricity and adhesion problems, and anhydrous ethyl carboxylate compound-coated taste-masking granules with a better taste, are obtained.

The application belongs to the field of compound synthesis, and discloses a kind of compound containing seven-membered lactam and pyrone skeleton and its construction and application, and the chemical structure is shown in the following, wherein R1 is selected from any one of hydrogen, alkyl, halogen;R2 is selected from any one of alkyl, aryl;R3 is selected from any one of hydrogen, phenyl.The seven-membered lactam and pyrone skeleton has good drug activity, and can be used for preparing antitumor drugs.The application also discloses a construction method of the seven-membered lactam and pyrone skeleton.The construction method of the seven-membered lactam and pyrone skeleton has the advantages that raw materials and catalysts are cheap and easy to obtain, operation is simple and convenient, and the universality of substrates is wide.

An apparatus including: a core including an annular body defining an internal void oriented down a central axis having a top axial surface and a bottom axial surface; at least one retainer including an annular body adapted to couple to the top axial surface or the bottom axial surface of the core to form a circumferential engagement cavity defined radially between the at least one retainer and the core; at least one ring seal disposed within the engagement cavity; and at least one flexible film membrane partially disposed within the engagement cavity, where the at least one flexible film membrane at least partially encloses the internal void to provide for a medically, biologically, or pharmaceutically active environment within the internal void of the core.

This invention discloses a method, apparatus, and device for predicting the activity of chemically modified siRNA, comprising: acquiring the original base sequence and chemical modification information of the target siRNA, and retrieving the physicochemical properties of the target siRNA; encoding the original base sequence, chemical modification information, and physicochemical properties as features; and generating a prediction result of the silencing efficiency of the target siRNA based on the encoded features using a pre-constructed prediction model; wherein the pre-constructed prediction model includes: a feature fusion sub-model and a classification sub-model; the feature fusion sub-model is used to perform feature fusion on the encoded features based on a cross-attention mechanism; and the classification sub-model is used to generate a prediction result of the silencing efficiency based on the fused features. This method, based on a multi-dimensional, multi-view learning strategy and an attention mechanism fusion model, significantly improves the algorithm's ability to represent chemically modified siRNA data, and, combined with the nonlinear data fitting ability of the deep learning framework, improves the accuracy of the algorithm in predicting the drug activity of chemically modified siRNA.

This invention discloses a chiral [oxyindole-pyrrolidine-β-lactam] bispirocyclic compound containing trifluoromethyl groups, with the following structural formula: The preparation includes the following steps: 1. Sequentially adding a metal catalyst, a chiral ligand, a base, indigo-derived trifluoromethylimine ylide, and 3-methylene β-lactam, followed by the addition of an organic solvent to obtain a mixture. The mixture is stirred at a reaction temperature of 0℃ to 50℃. 2. After the reaction is complete, the chiral [oxyindole-pyrrolidine-β-lactam] bispirocyclic compound containing trifluoromethyl groups is obtained through post-processing. The chiral [oxyindole-pyrrolidine-β-lactam] bispirocyclic compound containing trifluoromethyl groups prepared in this application lays a material foundation for in-depth drug activity research based on new drug development.

The present invention relates to a dual functional domain structure and its uses. The dual functional domain according to the present invention includes a first domain that binds to a disease-site-specific expression protein and a second domain that binds to a disease-specific expression protein. In this case, the first domain serves to mask the drug's function at a non-disease site, thereby enabling disease-site-specific drug delivery. In addition, the first domain is cleaved by a proteolytic enzyme specifically expressed at the disease site to induce drug activity and exhibit drug activity in a disease-site-specific manner. Furthermore, the multispecific fusion protein comprising the dual functional domain structure can be designed in various forms to encompass various functions.Therefore, the dual functional domain structure and the multispecific fusion protein comprising the dual functional domain structure according to the present invention can be used for various applications as an alternative to conventional antibodies.

The present invention relates to means and methods to non-invasive ocular drug delivery technologies, particularly aimed at delivering pharmaceutically active ingredients (APIs) to the posterior segment of the eye.

The application discloses a kind of hierarchical response intelligent drug-loading units and its controlled-release system, including A type drug-loading microbubble and B type phase change droplet, A type drug-loading microbubble includes gas core and rigid shell, the first drug active substance is loaded in the rigid shell, and the A type drug-loading microbubble has first burst threshold;B type phase change droplet includes low-boiling liquid perfluorocarbon core and phospholipid shell, the second drug active substance is loaded in the phospholipid shell, and the B type phase change droplet has phase transition threshold and second burst threshold;Wherein, first burst threshold>Second burst threshold>Phase transition threshold.The application realizes the precision and intelligent controlled-release of drug, significantly improves curative effect and reduces toxic side effect, benefits from the core structure design of hierarchical response drug-loading unit and programmable ultrasonic excitation sequence, and the application completely changes the extensive release mode of traditional one-time blasting.

This disclosure provides mixtures of beta-cyclodextrin molecules substituted at one or more hydroxyl positions by hydroxypropyl groups, the mixture optionally including unsubstituted beta-cyclodextrin molecules, for use as a pharmaceutically active ingredient; methods of making such mixtures; methods of qualifying such mixtures for use in a pharmaceutical composition suitable for intrathecal or intracerebroventricular administration; pharmaceutical compositions suitable for intrathecal or intracerebroventricular administration comprising such mixtures; and methods of using the pharmaceutical compositions for treatment of Niemann-Pick disease Type C.

The present application provides a drug-loaded microsphere for loading polypeptide drugs, the polypeptide drug delivery drug-loaded microsphere is W1 / O / W2 structure, which is composed of polypeptide drug active substance and hydrophilic gel as the inner water phase (W1), organic solvent of water-insoluble polymer as the oil phase (O), and solution containing emulsifier as the outer water phase (W2). The sustained-release microsphere of the present application introduces hydrophilic temperature-sensitive gel and water-insoluble polymer to co-load drugs, increases the hydrophilicity of the carrier, and reduces the solubility of polypeptide drugs by preparing metal ion-polypeptide drug active substance insoluble complex, thereby controlling the drug release behavior. Compared with the conventional microsphere, the sustained-release microsphere of the present application has the advantages of reducing drug burst release, shortening the drug release platform period, making the overall drug release behavior of the drug tend to zero-order release, releasing more stably, and improving the compliance of the microsphere preparation.

A camptothecin conjugate and a preparation method thereof. The camptothecin conjugate has excellent drug activity and kinetic characteristics, and is suitable for preparing a drug for treating tumor-related diseases.

The invention provides an injection for inducing mesenchymal stem cells. The induced mesenchymal stem cell injection is prepared from induced mesenchymal stem cells modified by hepatocyte growth factors with the cell density being 1.0 * 10 < 5 >-2.0 * 10 < 7 > / ml, HSA with the mass concentration being 0.25%-6%, DMSO with the mass concentration being 5%-10%, glucose with the mass concentration being larger than 0 and smaller than 1%, compound amino acid with the concentration being 0.5-5 mg / mL and the balance compound electrolyte injection. And the induced mesenchymal stem cell injection has a pH value of 6.8 to 7.5. The induced mesenchymal stem cell injection is good in homogeneity, small in batch difference and stable in curative effect, can effectively promote damaged tissue repair, can be directly intravenously injected after cryopreservation and recovery, keeps high cell viability and drug activity, achieves an excellent treatment effect, has good room-temperature stability, is convenient to transport and store, and is suitable for clinical application. The method is suitable for different clinical application occasions, and the clinical application range of the mesenchymal stem cells is expanded.

The invention relates to the technical field of medicines, in particular to application of aspiramycin and / or imiquimod in preparation of a medicine for treating VACV. Aspiramycin and imiquimod which are screened from medicines on the market have antiviral activity, and experimental data show that the Aspiramycin and the imiquimod have anti-VACV medicine activity. Aspiramycin and imiquimod (especially combined application) are used for preparing the medicine for treating VACV, so that the time and cost of preclinical research can be greatly reduced. As the action mechanism of the pox viruses is not unique to the VACV, the combined strategy has the potential to be expanded to infection treatment of other pox viruses (such as monkey pox virus MPXV) and even other DNA (Deoxyribose Nucleic Acid) viruses.

The invention belongs to the technical field of medicines, and relates to a compound as shown in a formula I, a stereoisomer, a prodrug and a pharmaceutically active metabolite thereof, pharmaceutically acceptable salt, a solvate and a hydrate thereof, a pharmaceutical composition containing the compound, and application of the compound in preparation of medicines for preventing and / or treating diseases or symptoms related to virus infection.

A Lac‑Phe‑based composition, a health care supplement, and a use thereof. The composition comprises propylene glycol, glycerol, Lac-Phe and a synergist in a mass ratio of (0.1-100):(0.1-100):(0.1-10):(0.1-2). The solubility of Lac-Phe is improved and the absorption rate of active pharmaceutical molecules in the body is optimized, thereby enhancing the bioavailability and helping to improve the efficacy of Lac-Phe in preventing and treating obesity.