715 results about "Pharmacokinetics" patented technology

Disclosed herein are compositions comprising an NSAID such as meloxicam and / or rizatriptan in combination with a cyclodextrin and / or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the NSAID for the treatment of pain such as migraine, arthritis, and other conditions. Also disclosed herein are methods of treating pain, such as migraine, comprising administering meloxicam and rizatriptan to a human being suffering from pain, such as migraine. For migraine, these methods may be particularly useful when the meloxicam and rizatriptan are administered while the human being is suffering from an acute attack of migraine pain or migraine aura. In some embodiments, the combination of meloxicam and rizatriptan may be administered in a manner that results in a Tmax of meloxicam of 3 hours or less.

Disclosed herein are compositions comprising an NSAID such as meloxicam and / or rizatriptan in combination with a cyclodextrin and / or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the NSAID for the treatment of pain such as migraine, arthritis, and other conditions. Also disclosed herein are methods of treating pain, such as migraine, comprising administering meloxicam and rizatriptan to a human being suffering from pain, such as migraine. For migraine, these methods may be particularly useful when the meloxicam and rizatriptan are administered while the human being is suffering from an acute attack of migraine pain or migraine aura. In some embodiments, the combination of meloxicam and rizatriptan may be administered in a manner that results in a Tmax of meloxicam of 3 hours or less.

Disclosed herein are compositions comprising an NSAID such as meloxicam and / or rizatriptan in combination with a cyclodextrin and / or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the NSAID for the treatment of pain such as migraine, arthritis, and other conditions. Also disclosed herein are methods of treating pain, such as migraine, comprising administering meloxicam and rizatriptan to a human being suffering from pain, such as migraine. For migraine, these methods may be particularly useful when the meloxicam and rizatriptan are administered while the human being is suffering from an acute attack of migraine pain or migraine aura. In some embodiments, the combination of meloxicam and rizatriptan may be administered in a manner that results in a Tmax of meloxicam of 3 hours or less.

The invention relates to the technical field of medical information, in particular to an intelligent prediction model and method for postoperative complications of anesthetized patients, and the method comprises the steps: collecting preoperative to postoperative complete-cycle clinical data of a patient through a medical data interface; analyzing operation codes to generate risk features, extracting vital sign dynamic features, and establishing a complication probability mapping relation through a multi-modal fusion network; combining the complication probability and pharmacokinetic parameters to construct an optimization model, and solving an individualized anesthetic dosage interval by using a gradient descent algorithm; vital signs are dynamically monitored in the operation, a dose re-optimization mechanism is triggered, the infusion rate is adjusted, and a closed-loop control link is formed; and generating a visual decision report. According to the method, through deep integration of complete-cycle clinical data and multi-modal feature modeling, preoperative physiological parameters, operation coding semantic information and intraoperative vital sign dynamic modes are subjected to fusion analysis, a nonlinear mapping relation between dosage and complication probability is constructed, and the risk prediction precision and individualized adaptability are remarkably improved.

Disclosed in the present invention are a quinazoline compound, and a pharmaceutical composition thereof and the use thereof. Provided in the present invention is a compound as represented by formula I, a stereoisomer thereof or a pharmaceutically acceptable salt thereof. The compounds of the present invention have a good degradation effect on the KRAS protein with a G12D mutation, have a good inhibitory activity against the proliferation of tumor cells with a KRAS G12D mutation, and exhibit good pharmacokinetic properties.

Disclosed herein are compositions comprising an NSAID such as meloxicam and / or rizatriptan in combination with a cyclodextrin and / or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the NSAID for the treatment of pain such as migraine, arthritis, and other conditions. Also disclosed herein are methods of treating pain, such as migraine, comprising administering meloxicam and rizatriptan to a human being suffering from pain, such as migraine. For migraine, these methods may be particularly useful when the meloxicam and rizatriptan are administered while the human being is suffering from an acute attack of migraine pain or migraine aura. In some embodiments, the combination of meloxicam and rizatriptan may be administered in a manner that results in a Tmax of meloxicam of 3 hours or less.

Disclosed herein are compositions comprising an NSAID such as meloxicam and / or rizatriptan in combination with a cyclodextrin and / or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the NSAID for the treatment of pain such as migraine, arthritis, and other conditions. Also disclosed herein are methods of treating pain, such as migraine, comprising administering meloxicam and rizatriptan to a human being suffering from pain, such as migraine. For migraine, these methods may be particularly useful when the meloxicam and rizatriptan are administered while the human being is suffering from an acute attack of migraine pain or migraine aura. In some embodiments, the combination of meloxicam and rizatriptan may be administered in a manner that results in a Tmax of meloxicam of 3 hours or less.

Disclosed herein are compositions comprising an NSAID such as meloxicam and / or rizatriptan in combination with a cyclodextrin and / or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the NSAID for the treatment of pain such as migraine, arthritis, and other conditions. Also disclosed herein are methods of treating pain, such as migraine, comprising administering meloxicam and rizatriptan to a human being suffering from pain, such as migraine. For migraine, these methods may be particularly useful when the meloxicam and rizatriptan are administered while the human being is suffering from an acute attack of migraine pain or migraine aura. In some embodiments, the combination of meloxicam and rizatriptan may be administered in a manner that results in a Tmax of meloxicam of 3 hours or less.

Provided herein are novel cyclic peptides, their synthetic process, compositions, properties including stability and pharmacokinetic profiles, and applications for treating solid tumor cancers.

Disclosed herein are compositions comprising an NSAID such as meloxicam and / or rizatriptan in combination with a cyclodextrin and / or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the NSAID for the treatment of pain such as migraine, arthritis, and other conditions. Also disclosed herein are methods of treating pain, such as migraine, comprising administering meloxicam and rizatriptan to a human being suffering from pain, such as migraine. For migraine, these methods may be particularly useful when the meloxicam and rizatriptan are administered while the human being is suffering from an acute attack of migraine pain or migraine aura. In some embodiments, the combination of meloxicam and rizatriptan may be administered in a manner that results in a Tmax of meloxicam of 3 hours or less.

The invention provides a phosphate of a compound shown in a formula (I) and a polymorphic substance of the phosphate, and the phosphate and the polymorphic substance of the phosphate have excellent hygroscopicity, solubility and stability, have excellent druggability and are suitable for industrial production and storage. In addition, the phosphate and the polymorph thereof have excellent pharmacokinetic properties.

The invention belongs to the technical field of nuclear medicine molecular diagnosis and treatment, and discloses a modified CAIX targeting cyclic peptide, a nuclide marker and application of the modified CAIX targeting cyclic peptide in tumor diagnosis and treatment. According to the CAIX targeted cyclic peptide, a rigid bifunctional chelating agent RESCA is introduced to replace a traditional chelating agent, and a sulfonated or alkylated amino acid connector is combined, so that the enzymolysis resistance and in-vivo stability of the probe are remarkably improved. By optimizing the structure of the connector, the lipophilicity is reduced, liver and gall metabolism and non-specific uptake are reduced, and the high uptake rate of tumor target tissues is maintained. The therapeutic nuclide marker of the cyclopeptide can be used for intratumoral irradiation therapy using DOTA or NOTA in combination with an alkylated amino acid linker or an albumin ligand. Experiments show that the marker has high radiochemical purity, excellent pharmacokinetic characteristics and low kidney retention, and is suitable for precise diagnosis and targeted therapy of CAIX high expression tumors such as kidney cancer, colorectal cancer and brain glioma.

Disclosed herein are dosage forms comprising a combination of: 1) an active pharmaceutical ingredient (API), 2) a cyclodextrin, and 3) a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the drug for the treatment of conditions such as pain.

The present invention provides a tetrazole compound, a pharmaceutical composition thereof and a use thereof. The compound of the present invention has a brand-new structure, a low clearance rate, high plasma exposure, good oral bioavailability, and good pharmacokinetic properties, and is conducive to drug development. The compound of the present invention or a pharmaceutically acceptable salt thereof can be used for preventing and / or treating pain, including neuropathic pain, etc.

A conjugate of the formula (I) wherein F is a ligand (radical thereof) that binds fibroblast activation protein alpha (FAPα); L is a functionalized linker that binds with F, A, and X; A is a pharmacokinetic extender that binds or associates or binds with a protein in the blood of an animal; and X is chelator; a method of imaging cancer-associated fibroblasts (CAFs) and activated myofibroblasts in a subject; and a method of treating a disease characterized by upregulation of FAPα, such as cancer, in a subject.

The invention discloses an alpha nuclide drug in-vitro cellular response prediction method and system based on multi-module mathematical modeling and a medium, and the method comprises the steps: constructing a basic parameter input module, a pharmacokinetic prediction module, a cell absorbed dose calculation module and a biological effect prediction module which are connected in sequence; a three-compartment dynamical model and a micro-dose learning point kernel convolution and DNA damage repair dynamical model are integrated, and full-chain and quantitative simulation from drug distribution, microscopic energy deposition to cell survival is achieved. The method overcomes the defects that an existing empirical model cannot accurately reflect the high LET characteristic of alpha particles, neglects the bystander effect and repair dynamics and the like, and the prediction precision is remarkably improved. According to the method, the curative effects of different drugs, cell lines and dosage schemes can be quickly simulated on a computer, the research and development cost and period are greatly reduced, and an efficient theoretical tool is provided for new drug screening and dosage optimization.

The invention belongs to the field of medicines, and relates to a heterocyclic compound as shown in formula (I), which can be used as a voltage-gated sodium channel inhibitor, especially has an excellent inhibition effect on Nav1.8, has excellent selectivity and pharmacokinetic properties, and can be applied to prevention, alleviation and / or treatment of voltage-gated sodium channel related diseases.

The invention discloses a sedation depth monitoring method based on a graph convolutional neural network, and relates to the technical field of sedation monitoring, and the method comprises the steps: collecting a multi-source biomarker of a patient, carrying out the filtering and artifact removal of an electroencephalogram signal, and generating preprocessed electroencephalogram data; performing attention pooling processing on the node-level feature tensor, calculating a sedation depth index, and generating a pain interference factor according to a connection edge weight of the dynamic function connection graph; and when the pain interference factor exceeds a preset pain threshold value and the sedation depth index meets a preset condition, generating a sedation optimization instruction, and when the virtual pharmacokinetic node displays metabolic abnormality, generating an infusion rate adjustment instruction. According to the method, through a dynamic function connection diagram construction link, the time-varying intensity of the skin conductance reaction signal and the rugosa electromyographic signal is used as a dynamic weight, and accurate quantification of the pain-sedation coupling effect is achieved.

The invention provides a salt of an aza-aryl compound, and a crystal form, a preparation method and application of the salt. The invention provides p-toluenesulfonate or hydrochloride of a compound as shown in a formula (I). The salt of the compound shown in the formula (I) is higher in AUC and Cmax, the in-vivo peak reaching time is shorter, the exposure amount is higher, and the pharmacokinetic property is good. # imgabs0 #

The invention discloses a meta-learning-based small sample pharmacokinetic property prediction method and related equipment, and relates to the field of pharmacokinetics. The method comprises the following steps: acquiring multi-dimensional feature data of candidate compounds, wherein the multi-dimensional feature data comprises atomic-scale features, molecular descriptors and molecular structure features; inputting the multi-dimensional feature data into a preset pharmacokinetic property prediction model to obtain a preliminary prediction result, the pharmacokinetic property prediction model being pre-trained through meta-learning based on small samples, the model comprising a first machine learning model and a second machine learning model, the preliminary prediction result comprises a first prediction result output by the first machine learning model and a second prediction result output by the second machine learning model; and determining a pharmacokinetic property prediction result of the candidate compound according to the first prediction result and the second prediction result. According to the method, the problem of low accuracy of a pharmacokinetic property prediction result can be relieved in a small sample scene of early drug research and development.

Provided herein are novel cyclic peptides, their synthetic process, compositions, properties including stability and pharmacokinetic profiles, and applications for treating solid tumor cancers.

The invention discloses a deuterated 2-(azetidine-3-yl) ethanone compound as well as a pharmaceutical composition and application of the deuterated 2-(azetidine-3-yl) ethanone compound. The deuterated 2-(azetidine-3-yl) ethanone compound has the structural characteristics of a formula (I), and the definition of each group in the formula (I) is shown in the specification. The compound shown in the formula (I) can be used as a muscarinic M4 receptor positive allosteric modulator, and compared with Emraclidine (CV-231), the compound shown in the formula (I) has better pharmacokinetic characteristics and higher safety. # imgabs0 #

The disclosed device, system and method manages medication delivery failures. An effective therapeutic range of a patient physiological property is determined based on a pharmacokinetic profile of a medication. During an administration of the medication to the patient, an expected trend in the measured physiological property is determined based on sensor data, the pharmacokinetic profile of the medication, a dose of the medication provided to the patient, and the at least one physical property of the patient, and an infusion device is caused to adjust the dose of the medication to cause the physiological property to follow the expected trend. Responsive to determining that a current trend in the physiological property has deviated from the expected trend, and will fall outside the effective therapeutic range within a predetermined time period, a delivery failure is determined and an alarm is provided.

The invention relates to the technical field of biological medicines, and discloses a polypeptide for treating osteoarthritis by aiming at AHR (Aryl Hydrocarbon Receptor), the amino acid sequence of the polypeptide is GFQQSDVIHQSVYELISINHTEDRA, and the amino acid sequence of the polypeptide is GFQQSDVIHQSVYELISINHTEDRA, and the amino acid sequence of the polypeptide is GFQQSDVIHQSVYELISINHTEDRA. The polypeptide is prepared by a solid-phase polypeptide synthesis method; the solid-phase polypeptide synthesis method specifically comprises the following steps: synthesizing from a C end to an N end, connecting a carboxyl group of a first amino acid to insoluble resin, then adding other amino acids one by one to form a peptide chain, and carrying out protection and deprotection reactions of a side chain in each step. The polypeptide is composed of natural amino acids and has good biocompatibility and degradability, and experimental results show that no obvious toxic reaction occurs in the cell level and the animal level, so that the polypeptide has conditions for further development of pharmacokinetic research and preclinical tests, and a feasible basis is provided for conversion to clinical application.

The invention discloses a multi-technology combined medication analysis platform of an oligonucleotide drug, which relates to the technical field of drug analysis and is technically characterized by comprising an oligonucleotide drug delivery technology module, a liposome, a polymer nanoparticle or an exosome is selected as a delivery carrier, the surface of the delivery carrier is modified with hydrophilic polyethylene glycol or a targeting ligand, and the oligonucleotide drug delivery technology module is connected with the oligonucleotide drug delivery module. The performance of the material is represented by dynamic light scattering and a transmission electron microscope; the multi-technology platform analysis module integrates RT-qPCR, LC-FL, LC-MS / MS and LC-HRMS technologies, is respectively used for target gene expression quantification, drug distribution tracking, drug principal component quantification and metabolite structure analysis, establishes a cross validation rule, and requires a correlation coefficient R2gt of an LC-MS / MS quantitative result and RT-qPCR expression data; 0.95%, 0.95%; the pharmacokinetic evaluation module constructs a PBPK model to predict human pharmacokinetic parameters, and draws a drug metabolism network diagram in combination with an LC-HRMS metabolite identification result; by integrating various advanced analysis technologies, the problems of low sensitivity, poor specificity and difficult metabolite analysis in the prior art are solved.

Disclosed herein are compositions comprising an NSAID such as meloxicam and / or rizatriptan in combination with a cyclodextrin and / or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the NSAID for the treatment of pain such as migraine, arthritis, and other conditions. Also disclosed herein are methods of treating pain, such as migraine, comprising administering meloxicam and rizatriptan to a human being suffering from pain, such as migraine. For migraine, these methods may be particularly useful when the meloxicam and rizatriptan are administered while the human being is suffering from an acute attack of migraine pain or migraine aura. In some embodiments, the combination of meloxicam and rizatriptan may be administered in a manner that results in a Tmax of meloxicam of 3 hours or less.

The invention belongs to the technical field of nuclear medicine, and relates to a CAIX-targeted cyclic peptide and a preparation method and application thereof, the CAIX-targeted cyclic peptide structure is shown as a formula 1, Linker is a cyclization connexon, and Chenator is a nuclide chelating group. The CAIX-targeted cyclic peptide provided by the invention has high affinity with CAIX, and has low affinity with isoenzyme CAII of CAIX, so that the CAIX-targeted cyclic peptide has high selective affinity with CAIX; the nuclide-labeled radioactive probe has high labeling rate and excellent in-vitro stability, has excellent pharmacokinetic characteristics in tumor-bearing model mice of human renal clear cell carcinoma, and has extremely high tumor uptake, tumor-muscle ratio and tumor-kidney ratio which can meet diagnosis requirements; due to the long-time retention characteristic in tumors, the polymer has a relatively high tumor treatment application value.

The invention relates to the technical field of biological medicines, and particularly discloses a dimer bicyclic peptide nuclide ligand and application thereof. The dimer bicyclic peptide nuclide ligand disclosed by the invention has a structure as shown in a formula I: # imgabs0 # formula I. The dimer bicyclic peptide nuclide ligand disclosed by the invention can be prepared into a nuclide probe targeting Nectin-4 after being labeled by radionuclide, the dimer bicyclic peptide nuclide ligand is good in radiation stability and ideal in pharmacokinetics, a tumor overexpressed by the Nectin-4 is high in uptake of the dimer bicyclic peptide nuclide ligand, and the tumor and muscle uptake ratio and in-vivo metabolic performance are good.

The present invention relates to a compound binding to an endogenous receptor, said compound comprising (i) an oligopeptide comprising a dipeptide with Trp being the C-terminal amino acid of said dipeptide, wherein said Trp is replaced with an α-amino acid Xaa2, whereby the stability in serum or plasma of the peptide bond connecting Xaa2 to the N-terminally adjacent amino acid is increased as compared to the peptide bond connecting Trp to the N-terminally adjacent amino acid in an otherwise identical compound; and (ii) a moiety capable of generating therapeutically effective radiation, said moiety being covalently bound to said oligopeptide.

The invention discloses a small animal in-vivo multi-parameter dynamic monitoring method based on photoacoustic imaging, and relates to the technical field of biomedical imaging, and the method comprises the steps: obtaining a photoacoustic signal generated by a small animal under the excitation of pulse laser output by an optical excitation module through an acoustic detection module; reconstructing a photoacoustic image of the photoacoustic signal through a filtering back projection algorithm; calculating the similarity between adjacent images in the photoacoustic image, identifying the image of which the similarity is lower than a set frame threshold value as a cross section slice polluted by respiratory motion artifacts and removing the cross section slice, and replacing the removed image frame by using the interpolation of an adjacent artifact-free image so as to obtain an updated photoacoustic image; selecting a region of interest in the photoacoustic image, and carrying out oxygenation kinetics monitoring, pharmacokinetics monitoring, perfusion kinetics monitoring or nanoparticle in-vivo kinetics monitoring; according to the monitoring method, motion artifacts caused by breathing of the small animals are effectively inhibited, and in-vivo multi-parameter dynamics monitoring of the small animals is achieved.