341 results about "Pharmacodynamics" patented technology

The invention discloses an optimization analysis system for simulating an anesthesia process, relates to the technical field of anesthesia simulation optimization analysis, and is used for solving the problem of inaccurate anesthesia individualized simulation decision. By constructing an anesthesia simulation system fusing a pharmacokinetic and pharmacodynamic model and a physiological coupling model, dynamic process simulation under individual physiological states and operative characteristics is realized, state evolution trajectories of an induction period, a maintenance period and a resuscitation period can be accurately deduced, and by introducing deep learning calculation and stage continuity constraints, the accuracy of the state evolution trajectories of the induction period, the maintenance period and the resuscitation period is improved. The method comprises the following steps of: establishing a multi-path drug delivery and ventilation strategy, setting a risk-efficiency scoring function, completing state tracking and index evaluation of the whole process, generating a strategy scoring set with confidence information, further supporting an abnormal probability judgment and risk triggering mechanism by the system, and outputting key monitoring parameters and coping strategies, so as to improve the simulation accuracy and stability; therefore, closed-loop control of strategy optimization and risk early warning is realized, and the credibility of the anaesthesia simulation process is improved.

The invention relates to an amido-substituted aromatic heterocycle inhibitor as well as a preparation method and application thereof. Specifically, the compound disclosed by the invention has a structure as shown in a formula (I), and each group is defined in the specification. The invention further discloses a preparation method of the compound and application of the compound as a KRAS mutation inhibitor. The compound has a very good inhibition effect on KRAS mutation and has better pharmacodynamic and pharmacokinetic performance and lower toxic and side effects. # imgabs0 #

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 application belongs to the technical field of biological medicine and immunology, and particularly relates to a single-domain antibody targeting cross binding of human and cynomolgus monkey CD46 and application thereof. The application utilizes alpaca to generate nanoscale antibodies, the molecular weight of which is about 15 kDa, and the nanoscale antibodies can more efficiently penetrate solid tumor tissues or cross blood-brain barrier, and the binding efficiency of the antibodies and target points is as high as possible. The 11 single-domain antibodies prepared by the application have specificity of anti-human and anti-cynomolgus monkey CD46, and in the binding detection with CD46 target proteins and CD46 overexpression cells, the binding efficiency is significantly better than that of Anti-CD46 humanization antibody, and the single-domain antibodies can be used for tumor treatment. Meanwhile, the single-domain antibodies have cross binding ability of cross species, and can be directly used for preclinical pharmacodynamics and safety evaluation, without the need of developing species-specific alternative antibodies, so that the application achieves 'one target and double effect'.

The invention discloses a patient historical state-based anesthetic dose simulation evaluation system, which is characterized by comprising a multi-source data integration and preoperative physiological feature quantification layer, a dose effect relationship simulation layer and a risk evaluation and recommendation output layer. The method has the following advantages and effects that the personalized pharmacokinetics-pharmacodynamics model is constructed by integrating multi-source historical data of a patient, vital sign change tracks under different anesthetic doses are simulated, the recommended dose interval is generated based on multi-objective optimization, the change from experience dependence to accurate quantification is realized, and the accuracy of the recommended dose interval is improved. The problem of inaccurate anesthetic dosage prediction caused by individual differences is effectively solved, and the safety and effectiveness of an anesthesia scheme are remarkably improved.

The present invention relates to a substituted pyrimidine-fused ring inhibitor, a method for preparing same, and use thereof. Specifically, the compound of the present invention has a structure represented by formula (I). Further disclosed are a method for preparing the compound, and use of the compound as a KRAS mutation inhibitor. The compound has a good selective inhibition effect on KRAS mutation and has better pharmacodynamic and pharmacokinetic performance and lower toxic and side effects.

The invention relates to the technical field of separation and purification of radix arnebiae seu lithospermi, in particular to a naphthoquinone compound in radix arnebiae seu lithospermi, a preparation method of the naphthoquinone compound and application of the naphthoquinone compound in preparation of drugs for treating cervical carcinoma, the naphthoquinone compound in radix arnebiae seu lithospermi is chemically named as (Z)-2-ethoxy-5, 8-dihydroxy-3-(4-methyl-1, 3-pentadiene-1-yl) naphthalene-1, 4-diketone, and the structural formula of the naphthoquinone compound is shown in the description. The naphthoquinone compound in the lithospermum is disclosed for the first time, in-vitro anti-tumor pharmacodynamic experiments are carried out on the naphthoquinone compound in the lithospermum, and the experiments show that the naphthoquinone compound in the lithospermum has a certain inhibition effect on human Hela cells; therefore, the naphthoquinone compound in the radix arnebiae seu lithospermi can be applied to preparation of drugs for preventing / treating cervical cancer.

The invention relates to the technical field of cell biology, in particular to application of a composition containing a mesenchymal stem cell secretor in pulmonary fibrosis. A systematic pharmacodynamic experiment verifies that the composition can remarkably reduce the content of a key fibrosis promoting factor TGF-beta1 in the blood of a pulmonary fibrosis model rat and effectively improve the blood-gas exchange function at the same time, and the blood oxygen saturation (SaO2) is remarkably increased, and the partial pressure of carbon dioxide (pCO2) is remarkably reduced. The improvement of the key indexes proves that the composition has a definite anti-fibrosis effect and a lung function protection effect, and a brand new treatment strategy is provided for pulmonary fibrosis diseases which lack special-effect treatment clinically at present. The technology not only has a remarkable clinical transformation value, but also develops an innovative research thought for the lung disease treatment field based on the action mechanism of the stem cell secretor, and has important scientific significance and market development prospect.

The invention belongs to the technical field of biological medicine and immunology, and particularly relates to a single-domain antibody targeting cross binding of human and cynomolgus monkey CD46 and application of the single-domain antibody. The alpaca is utilized to generate the nanoscale antibody, the molecular weight of the nanoscale antibody is about 15 kDa, the nanoscale antibody can more efficiently penetrate solid tumor tissues or cross a blood brain barrier, and the binding efficiency of the antibody and a target spot is improved as much as possible. The 11 single-domain antibodies prepared by the invention have the specificity of resisting human and cynomolgus monkey CD46, the binding potency of the 11 single-domain antibodies is remarkably superior to that of an Anti-CD46 humanization antibody in the binding detection of CD46 target protein and CD46 overexpression cells, and the 11 single-domain antibodies can be used for treating tumors. Meanwhile, the single-domain antibody disclosed by the invention has cross-species cross binding capacity, can be directly used for preclinical pharmacodynamics and safety evaluation, does not need to develop a species-specific substitution antibody, and realizes'one target and double effects'.

The present invention relates to an ambroxol-ibuprofen cocrystal dry powder inhaler, a preparation method and application thereof, and belongs to the professional field of pharmaceutical preparations. The dry powder inhaler is mainly composed of ambroxol, ibuprofen and lactose, the molar ratio of ambroxol to ibuprofen is 1:1, and the mass ratio of lactose to ambroxol-ibuprofen cocrystal is 5-35%. The results of the rat lung tissue distribution experiment showed that the administration method of dry powder inhalation can significantly enhance the drug delivery efficiency in the lungs and greatly prolong the drug retention time in the lungs compared with the traditional intravenous administration. Pharmacodynamic experiments further revealed that the ambroxol-ibuprofen cocrystal dry powder inhaler can effectively inhibit the active expression of inflammatory factors in model animals, and reduce the accumulation of hydroxyproline (HYP) in lung tissue and serum, improve anti-fibrosis and anti-inflammatory capabilities, improve oxidative stress capabilities, thereby helping to delay the pathological process of pulmonary fibrosis, showing great development potential as an anti-pulmonary fibrosis drug.

The invention discloses an application of DL-3-phenyllactic acid in treatment of cardiac mucinoma. Based on metabonomics, it is found that the level of endogenous DL-3-phenyllactic acid in serum of a patient is remarkably reduced, pharmacodynamic verification is conducted by means of a cardiac mucinoma tissue-derived cardiac mucinoma organ model of the patient, it is proved that DL-3-phenyllactic acid can inhibit proliferation of cardiac mucinoma organs in a dose-dependent mode, and the half inhibitory concentration IC50 value of DL-3-phenyllactic acid is 95.52 mu M. The DL-3-phenyllactic acid can inhibit proliferation of cardiac mucinoma organs in a dose-dependent mode. Network pharmacological analysis indicates that the drug action mechanism may involve key targets such as AKT1 and SRC. The invention discloses the therapeutic efficacy of the DL-3-phenyllactic acid on the cardiac mucinoma for the first time, and provides a solid preclinical experimental basis for developing the DL-3-phenyllactic acid into the medicine for treating the cardiac mucinoma. The invention has non-obvious and important clinical application value.

The invention discloses a pharmaceutical composition and application thereof in preparation of a medicine for treating sudden deafness, pharmacodynamic data shows that all components of the composition have a synergistic effect, the solubility and bioavailability of the composition in water can be remarkably improved, and the pharmaceutical composition can be used for treating sudden deafness. Through an oral administration mode, the hearing threshold of cochlear ischemia reperfusion model animals can be remarkably reduced, release of inflammatory factors such as serum IL-1beta and TNF-alpha is inhibited, oxidative stress is relieved (the malondialdehyde level is reduced), so that multi-target synergistic treatment of sudden deafness is realized, the effect is remarkable, the defects that an existing drug is single in target and inconvenient to administrate are overcome, and the application prospect is wide. The important clinical application value is realized.

The application discloses application of Xintong preparation in preparation of a medicine for treating diabetes and a preparation method thereof, and belongs to the field of traditional Chinese medicines. The Xintong preparation is prepared from 13 raw medicinal materials of Huangqi, Gegen, Danshen, Dangshen, Maidong, Heshouwu, Yinyanghuo, Dangui, Zaokesheng, Haizao, Kelp, Muli and Zhishi, has the effects of benefiting qi and activating blood, reducing phlegm and dredging collaterals. Pharmacodynamic experiments show that the Xintong preparation has the effect of reducing blood sugar, can effectively improve the physical conditions of polydipsia, polyphagia, polyuria and emaciation and lack of strength of an animal model of diabetes, significantly reduces the fasting blood sugar and serum insulin level, improves the oral glucose tolerance, has a definite treatment effect on type II diabetes, and expands the clinical application range of the Xintong preparation, and has a wide market application prospect.

The application discloses a LYTAG-Gem compound for enhancing the anti-tumor effect of gemcitabine and application thereof, relates to the technical field of biological medicine, and particularly relates to a gemcitabine (Gem) targeted delivery system based on a lysosome targeting chimera (LYTAC) and application thereof in enhancing the anti-tumor process. 2+ The system is assembled from heavy chain ferritin, Ni 2+ , NTA-PEG5000-DBCO and a targeting ligand TPP-1-N3 in a specific mass percentage, can efficiently load Gem and form a nano compound with a particle size of about 59-79 nm, the system targets tumor cells through heavy chain ferritin, and realizes site-specific release of Gem in cells by means of an endocytosis-lysosome pathway mediated by the LYTAC structure, in-vivo pharmacodynamic experiments show that the LYTAC-Gem compound can significantly inhibit the tumor growth of a KPC pancreatic cancer mouse model, molecular mechanism research further reveals that the LYTAC-Gem compound can down-regulate the expression of PD-L1 protein in tumor tissues, and it is indicated that the LYTAC-Gem compound has the potential to activate an anti-tumor immune response, and the application provides a novel targeted delivery strategy for overcoming the toxic side effects and tumor drug resistance of gemcitabine.

This invention relates to the application of frog seeds and their extracts in the preparation of sleep-improving products, belonging to the field of sleep health technology. Specifically, it relates to the application of frog seeds in the preparation of drugs, health products, or special diets with sleep-improving functions, and the application of frog seed extract in the preparation of drugs, health products, or special diets with sleep-improving functions. The frog seed extract is frog seed oil, obtained from frog seeds through supercritical CO2 extraction or cold pressing. The advantage is that animal pharmacodynamic experiments have confirmed that the frog seeds and their extracts of this invention can improve sleep. The sleep-improving functions specifically include one or more of the following aspects: shortening sleep onset time and alleviating sleep anxiety; improving sleep onset efficiency; prolonging sleep duration and increasing total sleep volume; reducing the number of nighttime awakenings and improving sleep continuity; improving the quality of deep sleep, increasing the proportion of deep sleep, and promoting bodily recovery.

The present invention belongs to the technical field of veterinary preparations, and specifically relates to a veterinary enrofloxacin compound gel ear drops and its preparation method and application. The compound gel ear drops include four active substances: enrofloxacin, triamcinolone acetonide, gentamicin sulfate, and pulegone. The preparation method is to add poloxamer, L-cysteine, and carbomer to water, stir and add benzyl alcohol to obtain solution A, dissolve low-erucic acid rapeseed oil in ethanol of more than 85%, add enrofloxacin, triamcinolone acetonide, pulegone, and gentamicin sulfate to obtain solution B; slowly add solution B to the gel matrix of solution A to obtain solution C, and then filter to obtain the compound gel. Pharmacodynamic experiments have confirmed that it has a good therapeutic effect on inflammation of the external ear canal of pets; accelerated experiments have confirmed that the compound gel is stable in nature, can be stored for a long time, and is suitable for further expansion of production.

The invention provides a traditional Chinese medicine delivery system of temperature-sensitive gel for allergic rhinitis based on a fructus xanthii formula, belongs to the technical field of pharmaceutical preparations, and solves the technical problems that the existing allergic rhinitis medicines are mainly hormone, have repeated effects and the like. Comprising the following preparation steps: S1, initially preparing a traditional Chinese medicine formula of the cocklebur fruit powder for treating rhinitis; s2, performing raw material level network pharmacology prediction; s3, trial production of a raw material grade temperature-sensitive gel product; s4, carrying out raw material grade experiment testing; s5, carrying out pharmacological prediction on the monomer-level network; s6, carrying out preliminary trial production on the monomer-grade temperature-sensitive gel product; s7, carrying out monomer-level preliminary experiment testing; s8, upgrading the formula; s9, carrying out trial production on the monomer-grade temperature-sensitive gel product again; and S10, carrying out experimental test on the monomer level again to confirm the most effective traditional Chinese medicine formula. According to the invention, a set of closed-loop iteration system of clinical experience-network pharmacology prediction-response surface process optimization-multi-level pharmacodynamic verification is constructed, and a traditional Chinese medicine delivery product which is controllable in quality, clear in mechanism and excellent in curative effect and is used for effectively treating allergic rhinitis can be prepared.

A method and system for predicting a set of linking parameters that relate pharmacokinetic and pharmacodynamic effects. One or more processors receive a population dataset that comprises a population pharmacokinetic (PK) dataset and a population pharmacodynamic (PD) dataset. The one or more processors transform the population dataset into a plurality of data density images that includes a PK data density image and a PD data density image. The one or more processors predict the set of linking parameters using the plurality of data density images.

The invention belongs to the technical field of biological medicine and immunology, and particularly relates to a single-domain antibody targeting PD-L1 cross binding of human and cynomolgus monkeys and application of the single-domain antibody. The single-domain antibody disclosed by the invention has the specificity of resisting PD-L1 of human and cynomolgus monkeys, and shows relatively strong binding efficacy in the binding detection of PD-L1 target protein or PD-L1 overexpression cells; in the detection of blocking PD-1 / PD-L1 functions, a part of the single-domain antibodies even show a blocking effect which is obviously superior to that of Atezolizumab, so that the single-domain antibodies prepared by the invention can be used for diagnosis, treatment and prognosis detection of PD-L1 positive tumors. Meanwhile, the single-domain antibody disclosed by the invention has cross-species cross binding capacity, can be directly used for preclinical pharmacodynamics and safety evaluation, does not need to develop a species-specific substitution antibody, and realizes'one target and double effects'.

The invention discloses a deuterium labeled gibberellin GA3 compound with high isotope abundance. The molecular formula of the deuterium labeled gibberellin GA3 compound is C19H20D2O6. The invention also discloses a preparation method and application of the compound. According to the deuterium-labeled gibberellin GA3 compound with high isotope abundance, the isotope abundance of deuterium exceeds 99%, a relatively cheap standard sample with higher sensitivity is provided, and an important support is provided for researches on metabolic pathways, pharmacodynamics, pharmacokinetics and the like of the gibberellin GA3 compound.

The invention discloses a preparation rich in polygonatum sibiricum polypeptide and application of the preparation in diabetes mellitus. The composition is prepared from rhizoma polygonati polypeptide, semeglutide, astaxanthin, an active agent and a ferroptosis mixture. Pharmacodynamic experiments show that in a diabetic mouse model, fasting blood glucose can be remarkably reduced, the serum insulin level can be increased, renal function indexes can be improved, and expression of NLRP3 inflammation pathway related proteins (NLRP3, Caspase-1 and IL-1beta) in pancreatic tissue can be remarkably inhibited. By integrating multiple mechanisms of blood glucose reduction, oxidation resistance, inflammation resistance, ferroptosis resistance and the like, multi-target collaborative intervention is realized, the pharmaceutical composition is remarkably superior to a single component in the aspects of blood glucose reduction, pancreas islet function protection and complication alleviation, and a new clinical strategy is provided for treatment of diabetes mellitus, especially type 1 diabetes mellitus.

The invention relates to a GLP-1R agonist compound and application thereof, in particular to a compound as shown in a formula I, or an isotope label, a stereoisomer and pharmaceutically acceptable salt thereof, and application of the compound as a medicine. The compound shows excellent agonistic action and pharmacodynamic performance on GLP-1R, can be used as a regulator for preparing drugs for treating, improving or preventing metabolic diseases and related diseases, and has wide application prospects.

The invention relates to a composition with fat burning accelerating and weight losing effects and application thereof, and belongs to the technical field of traditional Chinese medicine. The technical problems that an existing classic prescription, namely the three-kernel decoction, is laggard in process and large in dosage are solved. The composition consists of the following traditional Chinese medicine extracts in parts by mass: 1-5 parts of a traditional Chinese medicine extract A, 4-7 parts of a traditional Chinese medicine extract B, 6-8 parts of a traditional Chinese medicine extract C and 3-9 parts of a traditional Chinese medicine extract D. According to the composition disclosed by the invention, the classical prescription of the Sanjing decoction is applied, the effective components are extracted and separated through modern science and technology to obtain an effective extract, the curative effect is exerted through a corresponding proportion, and pharmacodynamic research shows that the traditional Chinese medicine composition disclosed by the invention can achieve the effects of accelerating fat burning and losing weight through the effects of diminishing swelling, clearing damp, draining water and expelling toxin. And the related process is advanced, and the dose is not large.

The present application relates to a kind of ganoderma lucidum spore as carrier paclitaxel ganoderma lucidum spore oil self-nanoemulsion composite microparticle and its preparation method, belong to medical technology field.The pretreated ganoderma lucidum spore (GLS) is obtained by process screening, and it is used as drug carrier, and the paclitaxel ganoderma lucidum spore oil self-nanoemulsion (PGS) is loaded therein, and paclitaxel composite microparticle (PGS@GLS) is obtained.Release curve in vitro shows that PGS@GLS has the characteristics of slow release after reaching intestinal tract;In vivo pharmacodynamics experiment shows that PGS@GLS can significantly inhibit the development and metastasis of colorectal cancer in mice;Tumor tissue section immunofluorescence analysis shows that PGS@GLS can effectively exert the therapeutic effect on colon cancer.Paclitaxel self-nanoemulsion ganoderma lucidum spore composite microparticle promotes cancer immune cycle by inducing immunogenic cell death and immune regulation, significantly improves the treatment effect of colon cancer, and has good biological safety.

The invention discloses a traditional Chinese medicine monomer composition derived from chrysanthemum plants and used for treating diabetic retinopathy as well as a preparation method and application of the traditional Chinese medicine monomer composition. The traditional Chinese medicine monomer composition prepared from the chrysanthemum plant as the raw material is high in safety, small in side effect and definite in component and is prepared according to a specific ratio, and pharmacodynamic experiments prove that compared with an ethanol extract, the traditional Chinese medicine monomer composition is more remarkable in curative effect on diabetic retinopathy, and the curative effect of the traditional Chinese medicine monomer composition on diabetic retinopathy is better than that of a traditional Chinese medicine composition on diabetic retinopathy. The composition can improve the pathological state of diabetic retinopathy from multiple targets and multiple ways, specifically can inhibit body mass increase caused by high glucose, reduce blood glucose level, improve retinal tissue structure damage, recover retinal tissue thickness, inhibit retinal cell apoptosis and inflammatory response, reduce the expression level of HIF-1alpha and VEGF protein in retinal tissue, and can be used for treating diabetic retinopathy. Scientific basis and technical support are provided for research and development of novel drugs for treating the diabetic retinopathy, and important clinical significance and market application prospects are achieved.

The invention relates to a composition for invigorating qi and blood and improving deficiency of qi and blood and application thereof, and belongs to the technical field of traditional Chinese medicines. The technical problems that an existing peach kernel and safflower four-ingredient decoction is laggard in process and large in dosage are solved. The composition consists of the following traditional Chinese medicine extracts in parts by mass: 2-6 parts of a traditional Chinese medicine extract A, 1-3 parts of a traditional Chinese medicine extract B, 8-12 parts of a traditional Chinese medicine extract C and 3-7 parts of a traditional Chinese medicine extract D. According to the composition disclosed by the invention, based on a classic prescription of peach kernel and safflower four-ingredient decoction, effective components are extracted and separated through modern science and technology to obtain an effective extract, the curative effect is exerted through a corresponding proportion, and pharmacodynamic research shows that the traditional Chinese medicine composition disclosed by the invention can achieve the effects of invigorating qi and blood and improving deficiency of qi and blood through the effect of nourishing primordial qi. And the related process is advanced, and the dose is not large.

Provided herein is a method of monitoring the change of the alpha-4 integrin activities in an individual by correlating with the soluble vascular cell adhesion molecule (sVCAM) and / or soluble mucosal addressin cell adhesion molecule (sMAdCAM) levels. Particularly, this method can be used, for example, to evaluate the pharmacokinetics and pharmacodynamics (PK / PD) of an alpha-4 integrin inhibitor used to treat a disease associated with pathological or chronic inflammation.

The present invention discloses the use of piperine or its derivatives, relating to the field of pharmaceutical technology. The present invention utilizes natural piperine as a precursor compound and chemically modifies it to obtain a series of novel piperine derivatives. Pharmacodynamic evaluations in leukemia, ovarian cancer, and pancreatic cancer cell models in vitro and in vivo revealed that several novel piperine derivatives inhibit tumor cell proliferation, induce tumor cell apoptosis, and promote leukemia cell differentiation. The present invention provides a group of compounds with novel structures. The synthetic route employed utilizes green chemistry reactions, making them more environmentally friendly and more economical in terms of raw materials. These compounds can be used to develop new drugs for the treatment of leukemia, ovarian cancer, and pancreatic cancer.