422 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 a deep learning method-based pharmacokinetics-pharmacodynamics and reinforcement learning-based propofol administration method and application thereof, a PKPD model is used for simulating the metabolic process of propofol in a human body, and a time dependency relationship and dynamics continuous information are extracted through LSTM and Neural OED; then a nonlinear relation between the propofol drug effect concentration and a clinically observed anesthesia depth index BIS is established through a Kan network, mapping between monitoring information and the anesthesia depth in an operation is rapidly established, a strategy is adjusted in time according to environment changes, and the method is suitable for processing non-standardized complex problems and has good application prospects. And the dosage and the administration scheme of the medicine are individually adjusted, so that the treatment effect is improved.

Provided are immediate or prolonged administration of certain potassium ATP (KATP) channel openers, optionally in combination with growth hormone, to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of KATP channel openers that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are methods of co-administering KATP channel openers with other drugs (e.g., in combination with growth hormone) to treat diseases of humans and animals (e.g., Prader-Willi Syndrome (PWS), Smith-Magenis syndrome (SMS), and the like.

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 #

The invention relates to the technical field of ferula asafoetida endophytic fungi separation and purification, in particular to alkaloid compounds in ferula asafoetida endophytic fungi as well as a preparation method and application of the alkaloid compounds in the ferula asafoetida endophytic fungi. And extracting with dichloromethane to obtain dichloromethane part extract, and purifying and separating the dichloromethane part extract by adopting silica gel column chromatography and high performance liquid chromatography to obtain the alkaloid compounds in the endophytic fungi of ferula sinkiangensis. The alkaloid compound in the ferula sinkiangensis endophytic fungi is disclosed for the first time, the compound is subjected to an in-vitro anti-tumor pharmacodynamic experiment, and according to the experiment result, the alkaloid compound has a certain inhibition effect on MCF-7 cells; therefore, the alkaloid compound can be used for preparing the medicine for preventing and treating the breast cancer, and a new medicine is provided for preventing and treating the breast cancer.

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 relates to the technical field of indole alkaloid compounds, in particular to indole pleurotus nebrodensis alkali A, a preparation method thereof and application of the indole pleurotus nebrodensis alkali A to preparation of drugs for preventing and resisting tumors. Pleurotus nebrodensis sporocarp is smashed, ethyl alcohol is added, heating reflux preparation and concentration are conducted, obtained pleurotus nebrodensis total extract is dispersed into suspension with water, and then the suspension is placed in a drying oven to be dried to obtain the indole pleurotus nebrodensis alkali A. The indole pleurotus nebrodensis alkali A is obtained. The method comprises the following steps: sequentially extracting with petroleum ether, dichloromethane and ethyl acetate, concentrating an extracting solution to obtain ethyl acetate part extract, carrying out gradient elution separation on the ethyl acetate part extract by silica gel column chromatography, carrying out gradient elution on the obtained third fraction by high performance liquid chromatography, purifying and separating, and collecting eluate to obtain the indole pleurotus nebrodensis alkali A at 16.3 minutes. The indole pleurotus nebrodensis alkali A is disclosed for the first time, and it is found through in-vitro antitumor pharmacodynamic experiments that the indole pleurotus nebrodensis alkali A has a certain inhibition effect on human HGC-27 gastric cancer cells, so that the indole pleurotus nebrodensis alkali A can be used for preparing drugs for preventing and resisting gastric cancer.

A GLP-1R agonist compound and the use thereof, specifically a compound represented by formula Ⅰ, or an isotope marker, a stereoisomer or a pharmaceutically acceptable salt thereof, and the use thereof as a drug. The compound shows a good agonistic effect and pharmacodynamic property on GLP-1R, can be used as a regulator for preparing a drug for treating, ameliorating or preventing metabolic diseases and related diseases, and has broad application prospects.

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 invention discloses a traditional Chinese medicine composition for treating breast cancer complicated with anxiety disorder as well as a preparation method and application of the traditional Chinese medicine composition. The traditional Chinese medicine composition is mainly prepared from the following raw material medicines: astragalus membranaceus, herba epimedii, ligusticum wallichii, semen boitae, acanthopanax, rhizoma drynariae, selfheal, arisaema cum bile, turtle shell, nigrum fruit, salvia chinensis and artemisia apiacea. The invention further discloses a preparation method of the traditional Chinese medicine composition, a pharmaceutical preparation and application. Pharmacodynamic experiments prove that the traditional Chinese medicine composition can remarkably inhibit tumor growth of anxiety tumor-bearing mice and improve anxiety behavioral indexes, achieves dual treatment targets of tumor resistance and emotion regulation, and is particularly suitable for middle and advanced breast cancer combined anxiety patient groups needing long-term treatment.

The invention belongs to the field of biological medicine, and particularly relates to an information rhzomorph array for resisting small cell lung cancer and application of the information rhzomorph array. The invention provides polypeptides with amino acid sequences as shown in SEQ ID NO: 1-30. The invention also provides a medicine for resisting small cell lung cancer. The medicine comprises fusion protein obtained by respectively connecting the channel structural domain of the coliform and the polypeptide with the amino acid sequence shown as SEQ ID NO: 1-30. Pharmacodynamic experiments prove that in each growth cycle, a mouse tumor-bearing model always cannot get rid of the recognition and killing of an information rhzomorph array composed of thirty fusion proteins on tumors. A guinea pig model experiment proves that no toxic or side effect is generated in an animal model when the information rhzomorph array is continuously used for 30 days. The information rhzomorph array can be used as an effective small cell lung cancer treatment medicine.

The invention belongs to the technical field of medicines, and particularly relates to an artificial toad venom composition and application thereof, and the core component of the composition comprises one or more of toad cardiotonic steroids, toad tryptamine or toad polypeptides. The invention designs a key raw material, a formula and a preparation method of artificial venenum bufonis, and particularly develops a method for effectively obtaining toad cardiotonic steroid components from plants. Pharmacodynamic evaluation proves that the artificial venenum bufonis composition prepared by the method has the effect equivalent to or close to that of natural venenum bufonis, and has the value for preparing natural venenum bufonis substitutes. According to the invention, sustainable resource guarantee is provided for Chinese patent medicines containing venenum bufonis, and support is provided for wild toad resources and ecological protection in China. The invention also comprises the design and development of a new medicine taking the artificial venenum bufonis composition or the raw materials thereof as components.

The present disclosure relates to the field of molecular virology, including nucleic acid molecules comprising a modified viral genome or self-replicating RNA, pharmaceutical compositions containing said nucleic acid molecules, and the use of such nucleic acid molecules and compositions for producing a desired product in a cell culture or in vivo. Also provided are methods for eliciting a pharmacodynamic effect in a subject in need thereof, as well as methods for preventing and / or treating a variety of health conditions.

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 provides a preparation method and application of polygonatum cyrtonema acidic polysaccharide, and belongs to the technical field of polygonatum cyrtonema polysaccharide extraction. According to the invention, a separation and purification method combining anion exchange chromatography with gel chromatography is adopted, and finally the polygonatum cyrtonema acidic homogeneous polysaccharide (PCPA) with relatively high purity is obtained. An in-vivo pharmacodynamic experiment shows that the prepared PCPA can remarkably relieve intestinal mucosa injury and has relatively high intestinal immune regulation activity. The preparation method provided by the invention is stable in process, and the prepared polygonatum cyrtonema acidic polysaccharide is high in purity, is a homogeneous polysaccharide and has the effect of regulating intestinal immunity.

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 present disclosure relates to a GLP-1R agonist compound and use thereof, and specifically provides a compound represented by Formula I, or an isotope-labelled compound, a stereoisomer, or a pharmaceutically acceptable salt thereof, and use thereof as a medicament. The compound exhibits excellent agonistic effects and pharmacodynamic properties on GLP-1R and, as a modulator, is useful for manufacturing a medicament for the treatment, amelioration, or prevention of metabolic diseases and related diseases, thus having broad application prospects.

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 invention discloses a marine galactooligosaccharide lipid as well as a preparation method and application thereof, and belongs to the field of marine biological resource utilization and drug development. According to the invention, a marine red algae polysaccharide degradation technology and high efficiency of reductive amination aliphatic chain modification are combined together for the first time, and modification of saturated aliphatic chains with different lengths of marine galactooligosaccharides with different polymerization degrees is realized. Cellular level pharmacodynamic evaluation proves that the marine galactooligosaccharide lipid can significantly inhibit release of nitric oxide in microglial cells and expression of inflammatory factors such as interleukin-6 and tumor necrosis factor alpha, and has neuroinflammation inhibition activity; meanwhile, proliferation of tumor cells U87MG and GL261 can be remarkably inhibited, and the compound has certain anti-tumor potential and can be used for preparing drugs for preventing and / or treating neuroinflammation and anti-tumor related diseases. Therefore, the marine galactooligosaccharide lipid prepared by the invention has relatively high clinical application value and development prospect.

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.