559 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 paclitaxel ganoderma lucidum spore oil self-nanoemulsion composite particles with ganoderma lucidum spores as a carrier and a preparation method of the paclitaxel ganoderma lucidum spore oil self-nanoemulsion composite particles, and belongs to the technical field of medicines. Pretreated Ganoderma lucidum spores (GLS) are obtained through process screening and serve as a drug carrier, and paclitaxel-loaded Ganoderma lucidum spore oil self-nanoemulsion (PGS) is loaded into the Ganoderma lucidum spores (GLS) to obtain paclitaxel-loaded composite particles (PGS (at) GLS). An in-vitro release curve shows that the PGS-atGLS has the characteristic of slow release after reaching the intestinal tract; in-vivo pharmacodynamic experiments show that PGS-atGLS can significantly inhibit development and metastasis of mouse colorectal cancer; tumor tissue slice immunofluorescence analysis shows that PGS-atGLS can effectively play a role in treating colon cancer. The paclitaxel self-nanoemulsion-loaded ganoderma lucidum spore composite particles synergistically promote cancer immune circulation by inducing immunogen cell death and immunoregulation, significantly improve the treatment effect of colon cancer, and have good biological safety.

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 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.

The present invention provides anticancer agents comprising as an active ingredient a bispecific antibody that comprises a domain comprising a glypican 3-binding antibody variable region, a domain comprising a T cell receptor complex-binding antibody variable region, and common L chains that can enhance the affinity for the two antigens, as well as pharmaceutical compositions comprising the bispecific antibody as an active ingredient, the compositions being for use in combination with other anticancer agents. The bispecific antibodies are novel molecules which are produced with high efficiency and have strong anti-tumor activity as well as safety and excellent pharmacodynamics. The bispecific antibodies can be expected to be applied to various cancers.

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 discloses a salt of ponabulin and application thereof, relates to the field of medicinal chemistry, and solves the problem that the curative effect is influenced by poor water solubility of ponabulin in the prior art. The invention provides a plurality of ponabulin salts, the salts are formed by ponabulin and inorganic acid or organic acid, and the structure of the ponabulin is shown as a formula I. The invention further provides a preparation method of the ponabulin salt. In addition, the invention finds that the solubility of p-toluenesulfonate and 1, 5-naphthalene disulfonate of ponabulin in water is remarkably improved by more than 2000 times compared with free alkali, so that the requirement that a solubilizer is not added or a few solubilizers are added in the injection preparation process can be met, and potential harm to human health in the long-term use process of the solubilizers can be prevented. Pharmacodynamic tests show that the salt of the ponabulin has good anti-tumor activity and an effect of relieving neutropenia, and is suitable for preparing anti-tumor drugs. # imgabs0 #

The invention relates to application of VBIT-4 or pharmaceutically acceptable salt thereof in preparation of drugs for preventing or treating vitiligo and complications thereof. A large number of modern pharmacological scientific researches and in-vivo pharmacodynamic tests prove that VBIT-4 has a treatment effect on a leucoderma mouse model and inhibits synthesis of inflammatory factors and chemotactic factors in a leucoderma mouse skin lesion area. The mechanism of the invention is that VBIT-4 inhibits the expression of inflammatory factors and chemotactic factors in skin tissues so as to treat leucoderma, compared with the existing treatment means, VBIT-4 can promote the compound color of pigments in a skin lesion region on the back of a leucoderma mouse, has no obvious toxicity, and reduces the expression level of inflammatory factors (IL-1beta, IL-6 and IFN-alpha) and chemotactic factors (CXCL9 and CXCL10). In conclusion, the VBIT-4 is clear in action mechanism, remarkable in effect and free of obvious side effects, and has remarkable advantages and progress compared with existing drugs.

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 invention provides a human amylin polypeptide analogue containing non-natural amino acid and a derivative of the human amylin polypeptide analogue. According to the present invention, the human amylin polypeptide derivative obtained by introducing the non-natural amino acid to the N-terminal of the human amylin and modifying with the albumin binding residue can effectively prevent enzymatic degradation and prolong the half-life period, and has characteristics of improved solubility and / or physical stability and / or bioavailability and / or pharmacokinetic properties, the compound can be used for treating obesity and obesity-related diseases.

The invention relates to the technical field of medicines, and discloses pedunculoside temperature-sensitive injectable hydrogel as well as a preparation method and application thereof. Specifically, the invention provides application of the temperature-sensitive injectable hydrogel with the pedunculoside in preparation of the medicine for treating the cardiovascular diseases, and the temperature-sensitive injectable hydrogel with the pedunculoside comprises the pedunculoside, a lactic acid-glycolic acid copolymer, polyvinyl alcohol and dipolylactic acid-glycolic acid copolymer polyethylene glycol. The microsphere-gel combined delivery preparation PE-M / Ge prepared by the preparation method disclosed by the invention is good in injectability and has a good temperature-sensitive gelling characteristic in vitro; the obvious gel property is realized, and the microspheres are uniformly distributed in the gel; the release of the drug can be effectively reduced, the release curve is closer to zero-order release, the dual controlled release system can more stably release the drug, the toxic and side effects caused by non-characteristic distribution of PE are reduced, and the bioavailability is improved. And the PE-M / Ge has no cytotoxicity to H9c2 cells and HUVECs cells, so that a foundation is laid for in-vivo pharmacodynamic experiments of rats.

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 invention provides a traditional Chinese medicine composition with the effects of warming kidney, supporting yang, promoting blood circulation and relieving pain. The traditional Chinese medicine composition is prepared from the following components: agaric, ligusticum wallichii, radix paeoniae rubra, radix achyranthis bidentatae, dragon's blood, cassia twig, eucommia ulmoides (charcoal), herba pyrolae, radix puerariae, rhizoma corydalis, oyster, radix salviae miltiorrhizae, herba epimedii, fructus psoraleae, trogopterus dung and honey-fried licorice root. The radix salviae miltiorrhizae, the herba epimedii, the fructus psoraleae and the trogopterus dung are added in the formula, so that the effects of nourishing blood, promoting blood circulation, dispersing blood stasis, relieving pain, strengthening muscles and bones, warming and invigorating kidney yang, and promoting blood circulation to relieve pain are improved, and the drug effect is remarkably improved by warming and invigorating, removing blood stasis, promoting blood circulation and relieving pain and blending the medicines with the honey-fried licorice root. Pharmacodynamic experiments prove that the traditional Chinese medicine composition prepared by the invention is remarkable in efficacy, high in bioavailability and stable and reliable in quality, can be prepared into different dosage forms according to the requirements of patients, and is convenient to carry and easy to take.

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 traditional Chinese medicine analysis, and discloses a codonopsis pilosula root traditional Chinese medicine in-blood pharmacodynamic substance mass spectrometry imaging method and application thereof, and the method comprises the following steps: S1, pharmacodynamic research and serum drug chemical analysis of codonopsis pilosula treatment diseases: (1) establishment of an animal model: taking a spleen deficiency model as an example, (2) serum drug chemical analysis, and (3) establishment of an animal model: taking a spleen deficiency model as an example; and S2, researching the distribution of the blood-entering components in the traditional Chinese medicine. Differential distribution of various medicinal effect substances in different tissues of the plant is accurately identified and positioned by utilizing a mass spectrum imaging technology, and deep mass spectrum imaging analysis is quickly performed on the tissues of the target micro-region, so that the type and content information of the components entering the blood is obtained; according to the technology, space metabonomics is added, and the whole action mechanism of the codonopsis pilosula for treating diseases is explored, including codonopsis pilosula pharmacodynamics research and searching of pharmacodynamic substance components and spatial distribution of the pharmacodynamic substance components in codonopsis pilosula roots.

The invention discloses a method for evaluating influence of traditional Chinese medicine on warfarin anticoagulant efficacy based on a PK / PD theory, and belongs to the technical field of medicine evaluation. In order to clarify the material basis and the influence degree of traditional Chinese medicine on warfarin anticoagulation, the method comprises the following steps: carrying out grouped animal experiments, then respectively collecting pharmacodynamic experiment data, drug absorption experiment data, drug metabolism experiment data, drug plasma protein binding rate experiment data and drug excretion experiment data, and constructing a multi-dimensional data set; performing preprocessing, including removing abnormal values and performing data standardization processing to obtain a preprocessed data set; performing dimension reduction analysis by using a principal component analysis (PCA), extracting main components, and generating a score matrix and a load matrix; performing orthogonal partial least square discriminant analysis on the score matrix, and classifying the data based on an orthogonal partial least square discriminant analysis method to obtain a classification result; and obtaining an evaluation result of the influence of the traditional Chinese medicine on the warfarin anticoagulant efficacy based on the obtained classification result. The method is accurate in evaluation.

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.