497 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.

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.

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 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.

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 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 present invention relates to a pamoate drug sustained-release microsphere and a preparation method therefor. A sustained-release microsphere formulation for injection prepared according to the preparation method of the present invention has a relatively narrow microsphere particle size distribution, and the release time of active pharmaceutical ingredients of a drug can last for about three to four months. In addition, the microsphere formulation prepared by the present invention can maintain stable plasma concentration in an animal body, and has no relatively large plasma concentration fluctuation within three to four months, thereby better avoiding the occurrence of toxic and side effects.

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.

The invention provides a cell-targeted drug preliminary screening model training method, a drug preliminary screening method and equipment, and the method comprises the steps: obtaining molecular fingerprint feature data corresponding to each compound sample with label information to form a corresponding original data set, and carrying out the data screening of the original data set in a distance measurement mode, and training a regression model based on a graph neural network to learn the structural topology of each compound sample, and training the model as a cell-targeted drug preliminary screening model for predicting whether the compound has potential cell-targeted drug activity or not. According to the application, the comprehensiveness of molecular characterization can be effectively improved in the training process of the cell-targeted drug preliminary screening model, and the generalization ability of the trained cell-targeted drug preliminary screening model can be effectively improved, so that the application universality of the trained cell-targeted drug preliminary screening model can be effectively improved; and the accuracy and the reliability of a potential cell targeted drug activity prediction result predicted by the model can be 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 delayed timed release pharmaceutical composition, a preparation method therefor, and use thereof. The pharmaceutical composition comprises a tablet core. The tablet core comprises a drug-containing layer and a boosting layer stacked on the drug-containing layer. The drug-containing layer comprises a drug active ingredient. The drug active ingredient is levodopa or a derivative thereof, or a mixture of levodopa or a derivative thereof and a DOPA decarboxylase inhibitor, and accounts for 5-72.5 wt% of the content of the drug-containing layer. The pharmaceutical composition is a capsule-shaped tablet, can realize the effects of 1-3 h delayed release of the drug active ingredient and reaching a peak concentration at 6-10 h, can be used for reducing morning stiffness in patients with Parkinson's disease, and has good application prospects.

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.

A preserved liquid aqueous pharmaceutical composition includes one or more etherified cyclodextrin derivatives, at least one water-soluble preservative, and at least one pharmaceutically active compound which is poorly water-soluble, very poorly water-soluble or water-insoluble. The liquid aqueous pharmaceutical composition provides an acceptable solubility of the pharmaceutically active compound, such as pimobendan, in aqueous solution whereby the water-soluble preservatives retain their effectiveness in the presence of the etherified cyclodextrin derivatives allowing the use in an oral administration form.

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.