233 results about "Pharmacodynamics" patented technology

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 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 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 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 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 invention discloses an application of a P4HA1 inhibitor in preparation of a medicine for treating congenital megacolon-related enterocolitis, deeply clarifies an immune metabolic axis of 'P4HA1-hydroxyproline-eIF5A-IRF4-IL17', and discloses a new mechanism that metabolite hydroxyproline regulates the activity of eIF5A and promotes nuclear translocation of IRF4 so as to enhance TH17 cell mediated inflammatory response. Therefore, a brand new perspective is provided for understanding metabolic immune regulation of intestinal inflammation. By using the P4HA1 inhibitor (such as 1, 4-DPCA), secretion of IL-17 can be effectively inhibited, intestinal inflammation injury of HAEC model mice can be remarkably relieved, and a clear pharmacodynamic basis is achieved.

A method and system for predicting a set of linked parameters associated with pharmacokinetic and pharmacodynamic effects includes: one or more processors receiving a population dataset including a population pharmacokinetic (PK) dataset and a population pharmacodynamic (PD) dataset; the one or more processors converting the population dataset into a plurality of data density images including a PK data density image and a PD data density image; and the one or more processors predicting the set of linked parameters using the plurality of data density images.

The invention relates to a composition for reducing blood fat and blood sugar and improving blood pressure and application thereof, and belongs to the technical field of traditional Chinese medicines. The technical problems that in the prior art, the technology of thirst quenching decoction and gastrodia elata and uncaria decoction prescriptions is backward, and the dosage is large are solved. The composition consists of the following traditional Chinese medicine extracts in parts by mass: 3-9 parts of a traditional Chinese medicine extract A, 2-4 parts of a traditional Chinese medicine extract B, 5-7 parts of a traditional Chinese medicine extract C and 2-6 parts of a traditional Chinese medicine extract D, according to the invention, classic prescriptions of diabetes decoction and gastrodia elata and uncaria drink are applied, effective components are extracted and separated through modern science and technology, effective extracts are obtained, and the curative effect is exerted through a corresponding proportion. Pharmacodynamic research shows that the traditional Chinese medicine composition can achieve the effects of reducing blood fat and blood sugar and improving blood pressure through the effects of clearing stomach heat and nourishing kidney yin. And the related process is advanced, and the dose is not large.

This invention relates to the field of rose separation and purification technology, specifically a novel benzofuran compound from rose petals, its extraction method, and its application. The method involves extracting the total rose extract obtained by heating and reflux of dried rose petals, then extracting the petroleum ether fraction. After elution and separation, the third fraction is further eluted with silica gel, the second fraction is eluted again, and the third fraction is purified by elution. The novel benzofuran compound from rose petals is obtained at 21.0 minutes. This invention discloses for the first time the extraction and isolation of a benzofuran compound from rose petals, and its antibacterial pharmacodynamic effects were tested. The experiments clearly showed that the compound has a strong inhibitory effect on Staphylococcus aureus and Escherichia coli, thus enabling its application in the preparation of antibacterial drugs and antibacterial health products.

The invention provides a method for evaluating the efficacy of treating climacteric hectic fever, which comprises the following steps: collecting literature data of climacteric hectic fever according to a predetermined standard, constructing a data set, and evaluating the quality of the data set; constructing a pharmacodynamic model based on a quality evaluation result and a predetermined curative effect index in the data set, and evaluating the constructed pharmacodynamic model; and performing quantitative analysis processing on time effect distribution and covariable influence factors of drug treatment based on the evaluated pharmacodynamic model so as to simulate and predict result data of drug efficacy parameters and covariable influence degrees of drugs to evaluate time-effect characteristics of drug treatment. The evaluation method can assist in determining the optimal clinical medication treatment strategy of the medicine, and can also provide a diachronic standard curative effect scale reference for the development of a new medicine for treating female climacteric hectic fever.

This invention relates to a highly active effective fraction of the Epiglottis-Clearing Decoction and its application in the preparation of antitussive drug compositions, belonging to the field of traditional Chinese medicine extract technology. The effective fraction contains hydroxysaffron yellow A, paeoniflorin, naringin, and neohesperidin, with the total content of these four components not less than 20% of the total mass of the effective fraction. The effective fraction of this invention is prepared by purification with macroporous resin. Compared with the freeze-dried powder of the traditional Epiglottis-Clearing Decoction, the total content of the four active ingredients is increased from 3.32% to 20.87%, achieving a more than 6-fold high-efficiency enrichment. Animal pharmacodynamic experiments show that the antitussive effect of a low dose (275.5 mg / kg) of this effective fraction is comparable to that of the freeze-dried powder of the original decoction (1928 mg / kg), reducing the dosage to about 1 / 7 of the original formula, demonstrating a significant "synergistic effect with reduced dosage" technical effect. The effective active ingredients provided by this invention have a clear content and stable quality, and can be made into modern preparations such as tablets, capsules or granules, solving the problems of large volume, inaccurate dosage and poor patient compliance of traditional decoctions.

The invention discloses an emblic leafflower fruit milk processing technology optimization method based on a single factor and pharmacodynamic experiment, and belongs to the technical field of traditional Chinese medicine processing, and the method comprises the following steps: screening out optimal technological parameters through the single factor experiment: mixing emblic leafflower fruit and raw milk according to a material-liquid ratio of 1: 15, soaking at 45 + / -5 DEG C for 12 hours, cleaning milk stains, naturally air-drying for 2 hours, and drying at 50 DEG C for 24-48 hours until the water content is less than 6%. A liquid chromatography-tandem high-resolution mass spectrometry technology is adopted for analysis and displaying that the content of gallic acid, ellagic acid and corilagin in a processed product is remarkably reduced. Pharmacodynamic experiments prove that the toxicity of the processed product to WRL68 hepatocytes and 293T renal cells is weakened, the survival rate of the hepatocytes and the renal cells is increased along with reduction of the concentration of the components, and the toxicity reduction effect is achieved. The technological parameters are clear, the quality is stable, and a scientific basis is provided for standardized production and clinical safe medication of emblic leafflower fruit milk processing.

The invention discloses a terbinafine hydrochloride spray and a preparation method thereof, and relates to the technical field of pharmaceutical preparations. The terbinafine hydrochloride spray comprises the following components in percentage by weight: 0.5%-2% of terbinafine hydrochloride, 30%-60% of ethanol, 10%-20% of a solubilizer, 1%-5% of an absorption enhancer, 0.05%-0.2% of a pH regulator, 0.01%-0.05% of a preservative and the balance of water. In-vitro transdermal experiments show that the steady-state transdermal rate and the skin drug retention volume of the composition are obviously superior to those of a single absorption enhancer group and an enhancer-free group. Animal pharmacodynamic experiments prove that the spray disclosed by the invention has a remarkable improvement effect on skin lesion symptoms caused by fungal infection. The preparation process is simple, the preparation stability is good, the antifungal curative effect is remarkable, and the preparation has a good application prospect.

The application discloses a kind of bispecific anti-CD3 / CD20 antibodies and its application in B cell lymphoma, belong to the field of biological medicine technology.The bispecific antibody uses "tandem type" molecular structure, by the single-chain antibody (scFv) of anti-CD20 and the nanometer antibody (VHH) of anti-CD3 are fused by flexible connecting peptide.The high-purity bispecific antibody BsAb-20S3V is obtained by CHO cell stable expression system, and it has nanomolar level affinity to CD20+ and CD3+ cells.Experiments in vitro prove that the antibody can effectively mediate T cell specific killing to Raji cell, and the maximum killing rate can reach 75%-90%.In vivo pharmacodynamic evaluation shows that in tumor-bearing mouse model, high-dose group can significantly inhibit tumor growth and induce tumor negative growth.The antibody has good potential to prepare B cell lymphoma treatment drugs.

The invention relates to pyridazinone or pyridazine compounds as well as derivatives and pharmaceutical compositions thereof. Specifically, the invention provides a pyridazinone or pyridazine compound as shown in a formula (I) or (Ia) or a stereoisomer, a tautomer, an enantiomer, a diastereoisomer, a resonator, a pharmaceutically acceptable salt, a hydrate, a solvate or a crystal form of the pyridazinone or pyridazine compound. The compound shown in the formula (I) or (Ia) has excellent agonistic effect and pharmacodynamic performance on a thyroid hormone beta receptor.

The application discloses a compound morinda officinalis color-increasing liniment for treating vitiligo and a preparation method thereof, and particularly relates to the technical field of traditional Chinese medicine preparations, wherein the liniment is prepared from morinda officinalis, spilanthes acmella, giant knotweed, caesalpinia sappan, psoralea corylifolia, radix angelicae dahuricae and rhizoma smilacis glabrae as raw medicinal materials. The preparation method comprises the following steps: dynamic reflux extraction, percolation extraction, macroporous adsorption resin purification and preparation molding. Through the classification extraction and purification process, the photosensitive active ingredients are retained, and the photo-toxic impurities are effectively removed, so that the photo-toxicity is completely negative. The pharmacodynamic test shows that the liniment has a significant curative effect on vitiligo. The safety test shows that the liniment has no skin irritation and no allergenicity, and has excellent light safety. The quality research shows that the quality of the liniment is stable and controllable. The liniment has definite curative effect, high safety and stable quality, and has a good clinical application prospect.

The invention belongs to the technical field of medicines, and discloses application of a compound M1 shown as a formula (I) and pharmacodynamically acceptable salt thereof in preparation of medicines for preventing, relieving and / or treating autoimmune demyelination diseases. On a mouse experimental autoimmune encephalomyelitis model, the compound M1 shows a good treatment effect, can effectively prevent and treat pathological changes and disease progression of diseases, relieve the severity of the diseases and inhibit LPS-stimulated microglial BV2 cells from releasing inflammatory mediators, and provides a new drug and a new structure for clinical treatment.

This invention discloses a compound as a TRPA1 inhibitor, its pharmaceutical composition and application, and specifically discloses the compound represented by Formula I, its racemate, its stereoisomer, its tautomer, its nitride, its prodrug, or their pharmaceutically acceptable salts or solvates, which have good inhibitory activity against TRPA1 and excellent pharmacokinetic and pharmacodynamic properties.

The present application relates to a drug protein binding rate prediction method; first, the influence of drug protein binding on protein structure change is characterized by two-dimensional near-infrared correlation spectroscopy, and then a quantitative model is established for predicting the drug protein binding rate by using the characteristic spectrum area related to the drug protein binding. The two-dimensional correlation spectroscopy and machine learning are organically combined to establish a prediction model for the drug protein binding rate in the simulated physiological environment from the aspects of structure characterization signal extraction, separation and quantitative analysis; in actual operation, the sample processing method is simple, the time consumption is less, the cost is low, and the technology is suitable for various related scientific research activities, which can not only realize the protein binding rate prediction of one kind of drug (including acid / alkali type, salt type), but also can distinguish the protein binding rate difference of different products of the same drug, and has important significance for drug in vitro evaluation, generic drug consistency evaluation, pharmacodynamics research and the like.

The invention belongs to the technical field of cosmetics, and particularly relates to a composition for promoting collagen regeneration and inhibiting expression lines for sensitive skin and application of the composition. The invention provides a composition for promoting collagen regeneration and inhibiting expression lines for sensitive skin, the composition is prepared by compounding an Agrocarpus caffeus seed extract, a selaginella tamariscina extract, a lithospermum altaicum extract and acetyl hexapeptide-1, and the four components cooperate through a signal at a pharmacodynamic level, so that the composition has the effects of promoting collagen regeneration and inhibiting expression lines. A complete regulation and control network from inhibition of collagen degradation, promotion of synthesis to barrier repair is formed, the multi-target synergistic effect efficiency is remarkably improved, and full-path regulation and control from inhibition of facial wrinkles and promotion of collagen regeneration to barrier repair are realized; the defects that in the prior art, an action mechanism is single, and a long-term and systematic repairing effect is lacked are effectively overcome, and meanwhile, the mildness and sensitive skin applicability of the formula are remarkably improved.