884 results about "Pharmacometrics" patented technology

According to the invention, there is provided a solid pharmaceutical composition formulation for nasal delivery of an opioid antagonist, comprising a pharmacologically-effective amount of an opioid antagonist and a pharmaceutically-acceptable carrier. The compositions are preferably in the form of a powder produced by spray-drying, which are subsequently loaded into single use nasal applicators. Preferred pharmaceutically-acceptable carriers in this regard include disaccharides (e.g. lactose or trehalose) and dextrins (e.g. cyclodextrins or maltodextrins), preferably spray-dried together in combination. Compositions may further comprise an alkyl saccharide, preferably a sucrose ester, such as sucrose monolaurate. The compositions and applicators may be employed in the treatment of opioid overdose in subjects.

A computer-implemented system for personalized health optimization constructs a confidence-weighted personal health knowledge graph (PHKG) from heterogeneous data, including wearable sensors, medical devices, lab results, medication logs, and conversational inputs. A multi-stage causal-inference stack identifies modifiable drivers of outcomes using layered methods (e.g., MI, GAM, Neural Granger, DAG-GNN), and simulates candidate interventions. A recommendation engine ranks lifestyle or pharmacologic actions using a benefit-to-friction score, selecting a personalized intervention aligned with user readiness and clinical safety constraints. Interventions may include a minimum effective dose (MED), optimal level, adaptive low-dose, or behavioral challenge. Optional modules include reinforcement learning for timing adaptation and privacy-preserving on-device inference. The system operates across domains including metabolic, cardiovascular, renal, sleep, stress, and medication response, enabling cross-condition synergy evaluation. The architecture is modular, supports runtime plug-in targets, and adapts in real time with or without continuous clinical oversight, depending on deployment.

Veterinary pharmaceutical compositions for direct systemic introduction, also known as DSI pharmaceutical compositions. One veterinary pharmaceutical composition for direct systemic introduction includes about 10-17 dry mass % bovine gelatin; about 10-17 dry mass % mannitol; about 0-1 dry mass % of a surfactant; and about 65-80 dry mass % of the active pharmaceutical ingredient which is a proton pump inhibitor. A method of manufacturing a veterinary pharmaceutical composition for direct systemic introduction includes combining one or more pharmacologically inactive compounds to form a first solution; using one or more surfactants to form a second solution; adding an active pharmaceutical ingredient to the second solution to form a first mixture; adding the first solution to the first mixture to form a pre-formulation; freezing the pre-formulation; and lyophilizing the pre-formulation.

Compounds of formula (II) and formula (I) which are inhibitors of QPCTL and QPCT: (II) and (I) are provided herein. Also provided are pharmaceutical compositions containing this compound, as well as compounds for use in methods of treating cancer, neurodegenerative, inflammatory or autoimmune diseases. Exemplary compounds are, for example, 3-(6-fluoropyridin-3-yl)-2-[4-(4-methyl-4H-1,2,4-triazol-3-yl)piperidin-1-yl]benzonitrile (Example 1): (1), and pharmacological data are provided. TIFF2025524039000368.tif70128

The present invention addresses the problem of providing a novel compound that has a thyroid-stimulating hormone receptor antagonistic activity and is useful for the treatment of thyroid-related diseases. The present invention relates to a nitrogen-containing condensed ring compound represented by formula (A-I) or a pharmacologically acceptable salt thereof. The present invention relates to a nitrogen-containing condensed ring compound represented by formula (A-I) or a pharmacologically acceptable salt thereof. The compound or the pharmacologically acceptable salt thereof according to the present invention has an antagonistic activity against thyroid-stimulating hormone receptors and is therefore useful as a therapeutic agent for thyroid-related diseases (e.g., hyperthyroidism, Graves' disease, thyroid eye disease, and thyroid cancer) and others.

The present invention addresses the problem of providing a novel compound that has an OX2R agonist activity.　The present invention relates to a substituted sulfonamide compound which is represented by formula (I) or a pharmacologically acceptable salt thereof. A compound according to the present invention, or a pharmacologically acceptable salt thereof, has an agonist activity against OX2R, and is useful as, for example, a therapeutic agent for sleep disorders associated with OX2R (for example, narcolepsy, idiopathic hypersomnia, Kleine-Levin syndrome, hypersomnia associated with a physical disease, hypersomnia associated with a mental disease, hypersomnia associated with a drug or a substance, circadian rhythm sleep-wake disorders, insufficient sleep syndrome, and extended sleep).

A cosmetic containing (A) an alkali metal salt of an alkanoyl N-methyltaurine having an alkanoyl group having 8-20 carbon atoms, (B) a plant extract, (C) one or more compounds selected from the group consisting of compounds represented by general formula (1) and pharmacologically acceptable salts thereof, and (D) water (in general formula (1), R1, R3, R4 and R6 are each independently an alkyl group having 1-3 carbon atoms, R2 is an alkyl group having 1-3 carbon atoms, and R3 is an alkyl group having 1-3 carbon atoms; and R2 and R5 each independently represent a hydrogen atom or an alkyl group having 1-3 carbon atoms. ). # imgabs0 #

The invention relates to the technical field of traditional Chinese medicine research, in particular to a discovery method of a cough relieving and phlegm eliminating quality marker of cough relieving granules and the quality marker. According to the application, the cough-relieving and phlegm-eliminating drug effects of the cough-relieving granules are evaluated by virtue of concentrated ammonia water cough inducing and phenol red excretion tests, plasma pharmaceutical chemistry research of the cough-relieving granules is developed by virtue of a UHPLC-Q-Exactive Plus Orbitrap HRMS technology, and 26 prototype blood-entering components of the cough-relieving granules are analyzed and identified; through network pharmacological analysis of components entering blood, 11 potential active components for relieving cough and eliminating phlegm of the cough-relieving granules are screened, relate to 40 common targets such as IL6, TLR4, STAT3 and the like, and mainly participate in signal channels such as PI3K-Akt, HIF-1, EGFR (epidermal growth factor receptor) and the like; the seven prototype blood-entering components are quantitatively analyzed by utilizing pharmacokinetics. The three compounds of azelaic acid, caffeic acid and vanillin are used as the cough relieving and phlegm eliminating quality markers of the cough relieving granules through effectiveness, transitivity and testability. The research result is of great significance in deeply defining the pharmacodynamic material basis of the cough-relieving granules, optimizing the quality standard and promoting the clinical application of the cough-relieving granules.

The invention pertains to the technical field of biomedical engineering and pharmacology and, without being limited thereto, specifically relates to a composition that enables the healing of full-thickness and chronic wounds (particularly in the foot region) observed in individuals suffering from diabetic disease.

A system and method are herein disclosed. The system and method use a generative AI agent to analyze and identify synergistic blends of natural compounds for combination therapies by leveraging an array of specialized modes to access data from a multitude of sources including patient medical history (including test results, drug history, and imaging) to improve the efficacy of compounds, including traditional medicine, in line with combination therapy principles, aimed at: enhanced efficacy, decreased toxicity, improved dosage, and reduced drug resistance. In this way, the generative AI agent determines cross-therapeutic similarities and / or dissimilarities between pharmaceutical, naturopathic, homeopathic, and nutraceutical compounds along a plurality of compound property vectors such as efficiency, efficacy, toxicity, effects, side-effects, chemistry, pharmacology, pharmacokinetics, mechanisms of action, and pharmacodynamics, thereby enabling the proposition of cross-disciplinary and transdisciplinary therapeutic analyses and the identification of synergistic effects in combination therapies.

The invention belongs to the technical field of food functional ingredient nutriology research, and discloses application of narirutin in improving the intestinal flora homeostasis of food allergy organisms. The narirutin can adjust the relative abundance value of certain intestinal flora by adjusting the diversity of the intestinal flora of a food allergy body, improve the relative abundance of beneficial bacteria and harmful bacteria, and can influence the metabolism of short-chain fatty acid of the intestinal flora of the food allergy body, so that the food allergy body is improved. Further, the application of the narirutin in improving the intestinal flora homeostasis of food allergy organisms is realized. The application of narirutin in the research fields of nutriology, biology and pharmacology is expanded.

The invention discloses a traditional Chinese medicine composition for treating skin diseases and a preparation method of the traditional Chinese medicine composition. The traditional Chinese medicine composition is prepared from the following raw materials in parts by weight: 6-12 parts of radix notoginseng, 8-15 parts of radix salviae miltiorrhizae, 10-20 parts of rhizoma chuanxiong, 8-15 parts of rhizoma curcumae longae, 15-35 parts of radix angelicae sinensis, 3-8 parts of sandalwood, 3-8 parts of fructus aurantii immaturus, 40-60 parts of ramulus cinnamomi, 8-15 parts of rhizoma corydalis, 8-15 parts of rhizoma curcumae, 2-5 parts of flos carthami, 5-12 parts of radix puerariae, 8-15 parts of radix rehmanniae, 3-8 parts of pericarpium citri reticulatae and 8-15 parts of spica prunellae. The traditional Chinese medicine composition is prepared from 3-8 parts of radix trichosanthis, 15-35 parts of tribulus terrestris, 15-35 parts of cicada slough, 5-12 parts of stiff silkworm and 8-15 parts of rhizoma drynariae. According to a multi-target collaborative mechanism, network pharmacology proves that 12 pathological pathways such as IL-17A and the like can be regulated and controlled, and the TNF-alpha inhibition rate is 89% and the barrier repair speed is increased by 2.3 times through key component combination. According to a transdermal synergistic technology, the specific surface area of the medicine reaches 8.5 m < 2 > / g through superfine grinding, a Franz test shows that the penetration amount of tanshinone is increased by 3.7 times, and the onset time is shortened to 8.3 minutes. Dual scar regulation and control: the thickness of scars in 12 weeks is reduced by half through TGF-beta3 up-regulation and alpha-SMA inhibition, and the collagen order degree is improved by 3.2 times.

The invention relates to application of periplocin in anti-lung adenocarcinoma drugs and a target screening method of periplocin. Periplocin can be used for preparing anti-cancer drugs for treating lung adenocarcinoma, and can inhibit proliferation, invasion and metastasis of lung adenocarcinoma cells and induce apoptosis of the lung adenocarcinoma cells. Meanwhile, the invention also provides a method for screening anti-lung adenocarcinoma related targets of periplocin by combining transcriptomics with network pharmacology, which comprises the following steps: firstly, searching effective active components and prediction action targets of periplocin through a TCMSP database, constructing network pharmacology to screen key components and targets, and then constructing and analyzing a regulatory network. Intersection genes are determined in combination with transcriptomics, and a new thought is provided for lung adenocarcinoma treatment and drug research and development.

The invention provides a micro-fluidic organ chip for three-dimensional cell culture. The micro-fluidic organ chip comprises a cell model loading and culturing unit, a liquid inflow-outflow unit with height difference, and an embedded inverted cone compression ring sealing unit, the cell model loading and culturing unit is constructed by overlapping at least three layers of chips up and down; and the liquid inflow-outflow unit with the height difference is constructed and formed by respectively forming liquid circulation holes which are hermetically connected through the embedded inverted conical compression ring sealing unit on at least three layers of chips. According to the invention, the cell culture space is expanded through the cell model loading and culture unit, high compatibility of cell culture is realized, and the problem of non-uniform concentration of a test substance is eliminated through the liquid inflow-outflow unit with height difference; and high-reliability miniaturized sealing design is realized through the embedded inverted cone pressing ring sealing unit, and the device can be widely applied to culture of cell models and test substance treatment and effect index detection taking toxicological and pharmacological researches as target scenes.

The present invention addresses the problem of providing a novel compound that has a thyroid-stimulating hormone receptor antagonistic activity and is useful for the treatment of thyroid-related diseases. The present invention relates to an N-substituted cyclic amide compound represented by the formula or a pharmacologically acceptable salt thereof. The compound or the pharmacologically acceptable salt thereof according to the present invention has a thyroid-stimulating hormone receptor antagonistic activity and is useful as a therapeutic agent for thyroid-related diseases (e.g., hyperthyroidism, Graves' disease, thyroid eye disease, and thyroid cancer) and others.

The present invention relates to an ionic complex comprising a cationic polypeptide and an anionic excipient selected from: a PEG-carboxylic acid; a fatty acid having 10 or more carbon atoms; an anionic phospholipid; and a combination thereof. The invention also relates to a pharmaceutical composition comprising the ionic complex of the invention and a pharmaceutically acceptable carrier. The cationic polypeptide of the ionic complex has pharmacological activity and the complex can provide a more desirable pharmacokinetic profile for the cationic polypeptide of the complex as compared to the cationic polypeptide alone following administration. As such, the invention also relates to the use of the ionic complex and pharmaceutical composition comprising same to treat a subject suffering from a disease or disorder that is responsive to the cationic polypeptide of the ionic complex.

Provided herein are compounds of Formula (II) and Formula (I), which are inhibitors of QPCTL and QPCT: (II) and (I). # imgabs0 # also provides a pharmaceutical composition comprising said compound, as well as said compound for use in a method of treating cancer, a neurodegenerative disease, an inflammatory disease, or an autoimmune disease. Exemplary compounds are, for example, 3-(6-fluoropyridin-3-yl)-2-[4-(4-methyl-4H-1, 2, 4-triazol-3-yl) piperidin-1-yl] benzonitrile (embodiment 1): (1). Pharmacological data is provided.

The invention discloses a uric acid reducing composition and a preparation method and application of plant extracts of the uric acid reducing composition, and belongs to the technical field of traditional Chinese medicine formulas and preparation. The uric acid reducing composition is prepared from the following raw materials in parts by mass: 3 to 27 parts of corn stigma, 3 to 27 parts of pericarpium citri reticulatae and 3 to 27 parts of white kidney beans. The preparation method of the plant extract comprises the following steps: pretreating the raw materials, extracting effective components, compounding according to different proportions, evaluating the in-vitro xanthine oxidase inhibition effect by using the plant extract, determining the formula compatibility of the raw materials according to quantitative pharmacology, and further determining the formula compatibility of the uric acid reducing composition. The corn stigma is treated by adopting a steam wall breaking technology, so that the extraction rate of effective components of the corn stigma is remarkably improved, and the uric acid reducing effect of the product is enhanced; the uric acid reducing food prepared on the basis of the uric acid reducing composition is safe, free of side effects and suitable for being eaten by people with high uric acid for a long time.

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 discloses a method for analyzing a mechanism of treating leucopenia by using a Shengbai oral liquid by using a network pharmacology mode, and the method is based on an HITS algorithm, and identifies key regulation and control nodes through hub and authority scores of nodes. An analysis result shows that PPBP, ALOXE3 and CCR1 are hub genes ranked in the first three, and PPBP not only has the highest hub score, but also shows the most significant expression change. In a bone marrow microenvironment, PPBP / CXCL7 may affect differentiation and maturation of hematopoietic stem cells and promote generation of specific types of leukocytes.

Increase of energy expenditure as an effective treatment of obesity and related disorders is a target for drug research and development. A 15% increase of energy expenditure is believed to be sufficient to achieve significant weight and fat mass reduction while providing meaningful improvement of metabolic parameters. Disclosed herein is a method for pharmacological inhibition of miR-22-3p, which represents a new therapeutic approach for treating human obesity, diabetes, and hypercholesterolemia.

The invention provides a method for predicting microorganism-drug interaction through a double hypergraph contrast learning framework based on hierarchical attention, and solves the problems that the graph structure is simple, the interpretable analysis is increased, and the prediction precision is improved. The method consists of three modules: S1, data preprocessing: carrying out nonlinear fusion on similarity data of microorganisms and drugs to obtain comprehensive similarity of the microorganisms and the drugs, and forming a double hypergraph by combining an original incidence matrix and the comprehensive similarity with KNN and K-means algorithms; s2, feature extraction: sending the double-hypergraph obtained in the step S1 into a hierarchical attention and hypergraph convolutional network to obtain feature embedding, updating features based on comparison learning of the double-hypergraph, and fusing the double-hypergraph features through an integration network. And S3, result prediction: mapping the microorganism and drug characteristics obtained in the step S2 by using a full connection layer to obtain final characteristics, and performing dot product to obtain a prediction score. And outputting the obtained prediction score in combination with specific literature verification and a network pharmacology verification model.

The invention discloses an application of a pharmaceutical composition of erianin (ERI) and sorafenib (SOR) in preparation of an anti-liver cancer drug. The invention further discloses a pharmaceutical composition which comprises ERI and SOR, and the specific molar ratio of ERI to SOR is optimized and determined through an in-vitro experiment. The composition is developed based on multi-mode screening (network pharmacology prediction, molecular docking and molecular dynamics simulation) of STAT3 targets, and in-vitro experiments prove that the composition has synergistic anti-tumor activity and can be used for preparing anti-liver cancer drugs. The invention further discloses a development method of the ERI-SOR composition integrated with multi-mode computational simulation. Experiments prove that ERI and SOR both show a remarkable synergistic effect (combination index (CI) lt, 1) at the concentration of 0.5-16 [mu] M, CI at the optimal ratio (1: 1, 4 [mu] M + 4 [mu] M) reaches 0.617, the cell proliferation inhibition effect is remarkable compared with that of a single drug, and the excellent synergistic effect is shown.

The invention discloses a screening method of application of a mysorethorn cold mixture to treatment of respiratory syncytial virus. According to the method, network pharmacology and a molecular docking technology are combined, and active ingredients, action targets and action mechanisms of the mysorethorn cold mixture for treating respiratory syncytial virus diseases are explored; an experimental basis is provided for treating the respiratory syncytial virus disease by the mysorethorn cold mixture, and the mysorethorn cold mixture is of great significance in promoting clinical application of traditional Chinese medicines in treating the respiratory syncytial virus disease.

The present invention addresses the problem of providing a novel compound that has OX2R agonist activity.　The present invention relates to a substituted sulfonamide macrocyclic compound represented by formula (I) or a pharmacologically acceptable salt thereof. This compound, or a pharmacologically acceptable salt thereof, has agonist activity against OX2R, and is useful as a treatment agent, etc., for sleep disorders involving OX2R (e.g., narcolepsy, idiopathic hypersomnia, Kleine-Levin syndrome, hypersomnia associated with a physical disease, hypersomnia associated with a mental disease, hypersomnia associated with a drug or a substance, circadian rhythm sleep-wake disorder, insufficient sleep syndrome, and extended sleep).

The invention provides a loxoprofen sodium double-release capsule micro-tablet and a preparation method of the loxoprofen sodium double-release capsule micro-tablet. Through the synergistic effect of the quick-release micro-tablet and the sustained-release micro-tablet, the quick-release micro-tablet can realize quick release and absorption, and the sustained-release micro-tablet can maintain relatively stable blood concentration for a long time. The administration frequency is reduced, the coordination of the postprandial administration requirement and the dietary habit is ensured, and the occurrence of gastrointestinal tract adverse reactions is reduced. The preparation provided by the invention conforms to the dosage form design of the hour pharmacology, can quickly take effect through administration twice every day, can maintain the blood concentration in the high-incidence time period of night diseases, avoids the disadvantage of taking medicine after meal when the night diseases attack, guarantees the sleep quality, and improves the overall treatment effect. The micro tablet is small in size and easy to swallow, and the medication compliance of patients with dysphagia is obviously improved. Through dosage form design and improvement, unmet clinical requirements are expected to be met by virtue of obvious advantages of the traditional Chinese medicine composition.

The invention discloses a lung organ chip based on a stretchable biological membrane and a preparation method of the lung organ chip, and belongs to the field of biomedicine and pharmacology. The chip comprises a top cell culture layer, a bottom vacuum negative pressure layer and a stretchable porous membrane layer, the top cell culture layer comprises a cell culture chamber, a fluid micro-channel and a fluid micro-channel outlet / inlet, and the cell culture chamber, the fluid micro-channel and the fluid micro-channel outlet / inlet are communicated with one another; the bottom vacuum negative-pressure layer comprises a vacuum negative-pressure chamber, a gas micro-channel and a gas micro-channel outlet / inlet, and the vacuum negative-pressure chamber, the gas micro-channel and the gas micro-channel outlet / inlet are communicated with one another; the stretchable porous film layer is a deformable single-layer elastic film, and a plurality of through round holes simulating the alveolar structure are formed in the middle of the stretchable porous film layer. The method has the characteristics of low cost, easiness in manufacturing, easiness in operation and the like, and application and popularization of the lung organ chip are facilitated.

The invention relates to the technical field of biomedical engineering and pharmacology and relates to, but is not limited to, a method for the composition and production of a wound dressing for the healing of complete and chronic skin wounds.

The invention discloses a pseudomonas aeruginosa InA protein and application thereof, and relates to the technical field of biological detection, the InA protein is InAS2, InAAP41 or InAS8, the amino acid sequences of the InA protein are respectively shown as SEQ ID NO.1-3, and the nucleotide sequences for coding the InAS2, the InAAP41 and the InAS8 are shown as SEQ ID NO.4-6. Compared with the prior art, the InA protein can improve the solubility of target protein, in addition, the InA protein and pseudomonas aeruginosa immune protein also have ultrahigh affinity, a biosensing chip with regeneration reversibility is developed based on the InA protein, the chip can capture fusion protein with the InA protein, and the biosensing chip has the advantages that the biosensing chip can be used as a biosensing chip with regeneration reversibility, so that the biosensing chip can be applied to biosensing of pseudomonas aeruginosa. The chip can be used for detecting the affinity between the fusion protein with the InA tag and a candidate drug, drug screening is realized, and meanwhile, the protein-drug affinity kinetics detected by the chip can also be used for pharmacological research of drugs.

The invention belongs to the technical field of food nutrition, and discloses application of an artemisia selengensis extract in preparation of a medicine for improving neurodevelopmental disorder and the medicine. The artemisia selengensis extract has the following advantages and effects: the research finds that the artemisia selengensis extract has the effect of improving neurodevelopmental disorders, which is specifically embodied in that the artemisia selengensis extract can effectively increase the activity of acetylcholin esterase, lower the content of ROS (reactive oxygen species), up-regulate antioxidant indexes (GSH (glutathione) content and sod1 and cat gene expression) and relieve oxidative stress injury of zebrafish caused by NP (natriuretic peptide); meanwhile, the artemisia selengensis extract can also up-regulate the expression of a neural development gene (alpha 1-tubulin, mbp) so as to improve the neural development disorder of the zebrafish; besides, the mechanism of improving the zebrafish neurodevelopmental disorder by the artemisia selengensis extract is mainly realized through a p38 / 5-HT / Wnt / beta-catenin signal channel, expression of p38a is down-regulated (network pharmacology finds that p38 in MAPHK is a main mechanism channel), and expression of htr1aa, maoa, wnt4a and beta-catenin is down-regulated.