921 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.

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.

A compound as an LPAR1 antagonist, a pharmaceutical composition thereof and a use thereof. A compound represented by formula (I), as well as a racemate, stereoisomer, tautomer, nitrogen oxide, or pharmaceutically acceptable salt thereof. The compound of the LPAR1 antagonist has a good inhibitory effect on LPAR1, has excellent pharmacokinetic properties, and has good druggability.

Modified release formulations of gamma-hydroxybutyrate having improved dissolution and pharmacokinetic properties are provided, and therapeutic uses thereof.

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 drug screening, and provides a multi-target drug screening and optimizing method based on machine learning, which comprises the following steps: S1, carrying out feature screening on compound molecular descriptors by utilizing a machine learning algorithm, and determining the molecular descriptor which has the most significant influence on biological activity; s2, constructing a quantitative structure-activity relation model, and predicting the biological activity of the compound; s3, based on a multi-objective optimization algorithm, combining absorption, distribution, metabolism, excretion and toxicity properties of the compound; according to the method, feature screening is carried out on compound molecule descriptors by utilizing a machine learning algorithm, a QSAR model is constructed to predict the biological activity, ADMET property classification prediction is combined, the biological activity, ADMET properties and pharmacokinetic characteristics of drugs are comprehensively considered, and the accuracy and accuracy of drug activity prediction are improved. The method can efficiently and accurately screen and optimize drug candidate compounds with potential drug effects and good pharmacokinetic characteristics, so that the success rate of drug research and development is increased, and the research and development cost and time are reduced.

The present disclosure provides prodrug compounds of MDMA, MDA, and derivatives thereof having an improved pharmacokinetic profile suitable for the treatment of various neurological diseases.

According to various embodiments, machine learning techniques for determining a pharmacokinetic parameter of a radiotracer in a patient are presented. The techniques include: obtaining a time sequence of positron emission tomography (PET) scans of a target tissue of the patient, where the time sequence of PET scans includes images of a radiotracer in the target tissue; providing the time series of the PET scans to a first neural network system, which provides features extracted from the time series of the PET scans; providing the features extracted from the time series of the PET scans to a second neural network system, which provides an estimated arterial input function; modeling the pharmacokinetic parameter of the radiotracer based on the estimated arterial input function and the time sequence of PET scans; and outputting an estimate of the pharmacokinetic parameter of the radiotracer based on the modeling.

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 crystal form of a neuroactive steroid derivative and application thereof, and belongs to the technical field of medicines. The crystal form of the neuroactive steroid derivative (with the structure as shown in the formula I) provided by the invention is radiated by Cu-K alpha, and characteristic diffraction peaks of an X-ray powder diffraction pattern expressed by a 2 theta angle comprise 11.450 + / -0.200 degrees, 15.724 + / -0.200 degrees, 19.040 + / -0.200 degrees, 22.955 + / -0.200 degrees and 24.975 + / -0.200 degrees. The crystal form provided by the invention has the advantages of good fluidity, no electrostatic phenomenon, high stability and almost no hygroscopicity, and can stably exist under the conditions of high temperature, high humidity and illumination; the compound has a relatively strong positive regulation effect on a GABAA receptor, has relatively good pharmacokinetic properties and oral absorption rate, and can be applied to preparation of oral and other dosage form medicines for efficiently resisting diseases such as postpartum depression. # imgabs0 #

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.

The invention belongs to the field of medicine, and particularly discloses a deuterated tetrahydrofuran NaV1.8 inhibitor and application thereof, and the NaV1.8 inhibitor comprises a compound shown as a formula I or pharmaceutically acceptable salt and solvate thereof; wherein R1 and R2 are respectively and independently selected from H and deuterated C1-3 alkyl groups. The NaV1.8 inhibitor adopts a deuterated tetrahydrofuran medicine, the pharmacokinetic property of the NaV1.8 inhibitor can be remarkably improved, the administration dosage and toxic and side effects can be reduced, specifically, the channel activity IC50 of the NaV1.8 is lower than 0.1 nmol / L, the inhibitory activity IC50 of the NaV1.8 is lower than 43 nmol / L, the oral pharmacokinetic parameter t1 / 2 is 5.2 + / -1.2 h, and the NaV1.8 inhibitor is remarkably superior to a commercially available VX-548 preparation. # imgabs0 #

Modified release formulations of gamma-hydroxybutyrate having improved dissolution and pharmacokinetic properties are provided, and therapeutic uses thereof.

The present invention relates to the field of medicine, and in particular to a PRMT5 inhibitor, as well as a preparation method therefor and a use thereof. The PRMT5 inhibitor is a compound as shown in formula (I), an enantiomer, a diastereoisomer, a racemate, a solvate, a hydrate, a polymorph, a prodrug, an isotope variant, or a pharmaceutically acceptable salt thereof. The present invention has better activity, selectivity, pharmacokinetic characteristics, safety or a wider treatment window.

The invention relates to the technical field of traditional Chinese medicine research, in particular to a discovery method of a cough relieving and phlegm eliminating quality marker of cough relieving granules and the quality marker. According to the application, the cough-relieving and phlegm-eliminating drug effects of the cough-relieving granules are evaluated by virtue of concentrated ammonia water cough inducing and phenol red excretion tests, plasma pharmaceutical chemistry research of the cough-relieving granules is developed by virtue of a UHPLC-Q-Exactive Plus Orbitrap HRMS technology, and 26 prototype blood-entering components of the cough-relieving granules are analyzed and identified; through network pharmacological analysis of components entering blood, 11 potential active components for relieving cough and eliminating phlegm of the cough-relieving granules are screened, relate to 40 common targets such as IL6, TLR4, STAT3 and the like, and mainly participate in signal channels such as PI3K-Akt, HIF-1, EGFR (epidermal growth factor receptor) and the like; the seven prototype blood-entering components are quantitatively analyzed by utilizing pharmacokinetics. The three compounds of azelaic acid, caffeic acid and vanillin are used as the cough relieving and phlegm eliminating quality markers of the cough relieving granules through effectiveness, transitivity and testability. The research result is of great significance in deeply defining the pharmacodynamic material basis of the cough-relieving granules, optimizing the quality standard and promoting the clinical application of the cough-relieving granules.

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 relates to a silybin derivative as well as a preparation method and application thereof, and belongs to the technical field of chemistry. According to the invention, a hydrophilic sodium sulfonate group is introduced into the silibinin, and the silibinin is sulfonated to prepare a novel compound, namely the silibinin sodium sulfonate with good water solubility, so that the solubility of the silibinin sodium sulfonate in water is enhanced, the pharmacokinetic characteristics of the silibinin are improved from the pharmacokinetic aspect, the affinity and biological activity of the silibinin to organisms are improved, and the application prospect of the silibinin sodium sulfonate is widened. The silybin can be prepared into an injection for clinical treatment, provides a more excellent administration route, has the superiority incomparable with that of silybin, and has wide significance and huge treatment value in clinical application.