83 results about "Plasma concentration" patented technology

To provide a method and device for predicting plasma concentration transition in combination of multiple drugs, by easily determining Ki, fm in vivo, and making them into a database, since, there has been dynamic prediction using a physiologic medicine speed theory (PBPK) model, as a prediction method of a drug interaction for medical products, however, prediction using an inhibition constant (Ki) of in vitro data and a contribution ratio (fm) of a metabolic enzyme, do not always match increase of clinical AUC.SOLUTION: There is provided a method for determining a parameter of a compartment model from a pharmacokinetic parameter of an interacted drug and interaction drug, then converting the compartment parameter into a PBPK model parameter, then determining by simulation using the PBPK model, a Ki value and fm being AUC increase ratios observed clinically. The acquired parameter is made into a database, and simulation of blood concentration transition of the interacted drug and interaction drug is performed.SELECTED DRAWING: Figure 1

Described herein are dosage forms of enantiomerically enriched (S)-bupropion or enantiomerically enriched (R)-bupropion. The (S)-bupropion or the (R)-bupropion may be deuterium enriched, or may have natural isotopic abundance. These dosage forms may be administered, either fed or fasted, to treat a condition recited herein, to achieve a certain pharmacokinetic parameter of a bupropion or a metabolite of a bupropion, and / or to enhance dextromethorphan plasma levels.

A technique is provided for identifying correct or sufficient doses in a patient being treated with a drug for a neurological deviation condition. A method may include performing a plurality of fright response tests on a user, each test utilizing a device having a camera, a display, and optionally a speaker, and each test occurring at a different time after the user has been administered a medicament. The method may include receiving a plurality of images of at least one eye of the user from a camera during each test, and then calculating a magnitude of eyelid closure based on each image. The method may include determining a value of a correlation between a predetermined plasma concentration of the drug and the determined amplitude, and then determining whether a correct or sufficient dose has been reached based on the value of the correlation.

The present invention relates to the crystalline form of bipyrimidine compounds, as well as methods for preparing the same and their use. In particular, the present invention relates to crystalline form I of 4'-cyclopropyl-5,6'-dimethoxy-N-((4-(1-methyl-4-(trifluoromethyl)-1H-imidazole-2-yl)bicyclo[2.2.2]octan-1-yl)methyl)-[2,5'-bipyrimidine]-4-amine, wherein the X-ray powder diffraction pattern of crystalline form I includes characteristic peaks at diffraction angles (2θ) of 6.378±0.2°, 9.521±0.2°, 15.721±0.2°, 16.379±0.2°, 16.981±0.2°, 17.560±0.2°, 19.080±0.2° and 22.200±0.2°. Crystal form I possesses high stability, high solubility, high plasma concentration, high bioavailability, and excellent pharmacological activity, making it suitable for pharmaceutical preparations.

Provided are intermittent administration methods for reducing toxicity in the treatment of conditions associated with increased 15-hydroxyprostaglandin dehydrogenase (15-PGDH) activity or expression levels in a subject with a 15-PGDH inhibitor. Further, provided herein are methods of treating a condition associated with increased 15-hydroxyprostaglandin dehydrogenase (15-PGDH) activity or expression level in a subject by administering a 15-PGDH inhibitor while maintaining the therapeutic effect of the 15-PGDH inhibitor when the plasma concentration of the 15-PGDH inhibitor in the subject drops below the EC50 of the 15-PGDH inhibitor.

The present invention relates to a syrup containing alectinib or a salt thereof. The present invention provides a syrup containing alectinib or a salt thereof, which is a poorly water soluble agent, and having improved fluidity and / or palatability. The syrup of the present invention has a plasma concentration profile equivalent to or greater than, or is biologically equivalent to, a capsule containing the same amount of alectinib or a salt thereof as the syrup, or has an enhanced oral bioavailability compared to a capsule containing the same amount of alectinib or a salt thereof as the syrup.

The application relates to the technical field of pharmaceutical analysis, and discloses a pharmacokinetic analysis method of Tongwei Xiaozheng medicinal liquid, which adopts Q-Orbitrap high-resolution liquid chromatography-mass spectrometry to analyze the concentration of Jasmonic acid in blood components of the Tongwei Xiaozheng medicinal liquid in rat plasma, establishes a plasma concentration determination method for the blood original component Jasmonic acid, carries out methodological verification such as specificity, precision and accuracy, and then calculates pharmacokinetic parameters. In the Tongwei Xiaozheng medicinal liquid, 92 blood components are identified, 17 of which are original components and 75 of which are metabolites, the application firstly determines that Jasmonic acid is one of the blood original components of the Tongwei Xiaozheng medicinal liquid, and reveals the pharmacokinetic characteristics of the Jasmonic acid in normal and model rats. The method has strong specificity, high sensitivity and good reproducibility, and can provide a scientific basis for the research on the pharmacodynamic material basis of the Tongwei Xiaozheng medicinal liquid, the establishment of quality control standards and the clinical rational use of drugs.

The present invention relates to an oral extended-release dosage form of 7-methylxanthine (7-MX) or a pharmaceutically acceptable salt thereof. The dosage form is designed for twice-daily administration and provides controlled release of the active agent, achieving pharmacokinetic characteristics including sustained plasma concentrations and reduced fluctuation compared to immediate-release formulations. The invention further relates to the use of such dosage forms in the treatment of myopia, wherein the extended-release characteristics enhance therapeutic effectiveness in myopia.

An oral dosage form of an antidiabetic pharmaceutical composition comprises a metformin-containing core portion, an outer portion that comprises a non-biguanide antidiabetic agent such as sitagliptin, and a controlled membrane film sandwiched therebetween. The controlled membrane film is provided with at least one passageway allowing core-residing metformin to release out when the oral dosage form is in an aqueous environment, such as in the gastrointestinal (GI) tract of a subject. The oral dosage form has a dissolution profile such that upon dissolving in a medium with a pH of approximately 6.8 at approximately 37° C., less than 15% of the metformin is released at approximately 1 hours, and approximately 45-99% of the metformin is released at approximately 12 hours. The oral dosage form can provide a maximum plasma concentration of the metformin from approximately 7.5 to 15 hours after single-dose oral administration.

A bremelanotide pharmaceutical composition, a formulation thereof, a preparation method therefor, and use thereof. The bremelanotide pharmaceutical composition comprises bremelanotide as a pharmaceutically active ingredient, a solvent, and a polymer. The solvent includes one or more of N-methylpyrrolidone, polyethylene glycol, dimethyl sulfoxide, and benzyl benzoate and enables the plasma concentration of bremelanotide to be stably greater than 0.1 ng / mL at 120-168 h, thereby achieving the target sustained release. The bremelanotide pharmaceutical composition can be directly injected and does not require the addition of a thickener, a gel-forming agent, or other excipients.

The invention relates to the technical field of biological medicine, in particular to centipeda minima extracellular vesicle nose drops and a preparation method and application thereof.The centipeda minima extracellular vesicle nose drops comprise active ingredients, plant extracellular vesicles (Cm-EVs) derived from centipeda minima, the concentration of the plant extracellular vesicles (Cm-EVs) is 1 * 10 < 10 >-5 * 10 < 11 > particles / ml; the key active substances are as follows: the content of the Cm-EVs naturally encapsulated sesquiterpene lactone compound centipederin is more than or equal to 50 micrograms per milliliter (detected by HPLC-MS); the pharmaceutical auxiliary materials comprise 0.05 to 0.2 percent (w / v) of sodium hyaluronate, 0.8 to 1.0 percent (w / v) of NaCl and 0.005 to 0.02 percent (v / v) of polysorbate 80; the method has the beneficial effects that the targeted enrichment capability is realized: mucous membrane adhesion is enhanced through surface pectin protein, and the nasal cavity residence time is prolonged to 6 hours (the free medicine is less than 1 hour); the nano-scale particle size (80-200nm) can efficiently penetrate through the mucous layer, and the nasal mucosa drug concentration reaches 20 times of the plasma concentration (rat pharmacokinetic data); the long-acting slow-release property is as follows: the active ingredients are protected by the lipid bilayer, the cumulative release rate of the centipederin within 72 hours reaches 82%, and the free medicine can be completely released within 24 hours.

A method and formulations are developed for enhancing solubility and improving the permeability of bumetanide across a mucosal membrane. The formulation includes bumetanide in various water-cosolvent mixtures, which include at least one of an alcohol, polyether, glyceride, pyrrolidone, or any combination thereof. In some embodiments, the formulation has a pH of about 3.5 to about 8.0. In some embodiments, the formulation enhances the solubility and permeability of the bumetanide. Also disclosed is a use of the formulation for rapidly achieving effective bumetanide plasma concentration leading to diuresis. In some embodiments, the formulation can be administered to a subject conveniently without injection in the treatment of edema associated with heart failure or other conditions.

The invention belongs to the field of biological medicines, and particularly relates to a medicine for treating meningeal metastasis of malignant tumors with NTRK and / or ROS1 mutations and a preparation method, and the medicine is a freeze-dried powder preparation or injection for subarachnoid space injection of NTRK / ROS1-TKIs. The invention also provides an application of the NTRK / ROS1-TKIs in preparation of a medicine for treating meningeal metastasis of malignant tumors with NTRK and / or ROS1 mutation. The prepared NTRK / ROS1-TKIs injection can be directly injected into the subarachnoid space of a patient, the drug concentration in cerebrospinal fluid of the patient is greatly improved, the cerebrospinal fluid / plasma concentration ratio can reach 20 times or more, the problem of insufficient dosage caused by the blood-brain barrier after the targeted drug is orally taken can be completely solved, and the drug has the advantages of fast effect taking, no toxic or side effect and no toxic or side effect. The treatment effect on meningeal metastasis of malignant tumors such as lung cancer can be obviously improved.

Provided herein are tablet(s) comprising N-acetylcysteine amide (NACA) and a NACA-acceptable, biocompatible excipient and optionally one or more pharmaceutically acceptable additives, binders, or fdlers. Also provided are pharmaceutical composition(s) in the form an oral tablet comprising N-acetylcysteine amide (NACA), wherein the composition has a pharmacokinetic (PK) profile comprising mean plasma concentrations of NACA range from about 200 to 1200 ng / mL after administration of the pharmaceutical composition to a human.

The present invention is directed to novel neuro-attenuating norketamine (NANKET) compounds according to any one of formulas (I—shown below), (I-A) and (I-B), or any of the compounds described in Tables A-D, or in any of the Examples provided herein, and pharmaceutically acceptable salts thereof, novel pharmaceutical formulations and novel methods of uses thereof. The present invention also features novel oral neuro-attenuating ketamine (NAKET) and neuro-attenuating norketamine (NANKET) modified-release pharmaceutical formulations, and novel methods of administration thereof, which ensure the steady release of a therapeutically effective amount of ketamine, norketamine, or derivatives thereof from the oral modified-release pharmaceutical formulations without neurologically toxic spikes in plasma concentration of the ketamine, norketamine, or derivatives during the release periods.

The utility model belongs to the technical field of centrifugal equipment, and particularly relates to an auxiliary PRP extraction device. Comprising a base, a connecting rod is connected to the top of the base, and a support is arranged at the top of the connecting rod; a lower mounting groove and an upper mounting groove which are coaxial in the vertical direction are respectively formed in the base and the support, and injectors with conventional sizes can be accommodated in the lower mounting groove and the upper mounting groove; the device further comprises a spiral push rod capable of moving up and down in the vertical direction relative to the upper mounting groove. The auxiliary PRP extraction device provided by the utility model can be directly matched and applied to a specific centrifugal machine, a spiral pushing means is adopted, the pushing pressure impact force can be reduced, and the damage of pressure to active cell components is reduced, so that the extraction dosage is effectively controlled, the extraction rate can be ensured, and the extraction efficiency is improved. The concentration of platelet-rich plasma is accurately controlled, and the treatment effect is finally guaranteed.

The invention belongs to the field of biological medicine, and particularly relates to a medicine for treating EGFR mutation non-small cell lung cancer meningeal metastasis, application, a medicine box and a preparation method of the medicine, the medicine is a freeze-dried powder preparation or injection of EGFR-TKIs for subarachnoid space injection, the amount of EGFR-TKIs per person in the medicine is 0.01-5 mg, and the amount of EGFR-TKIs in the medicine is 0.01-5 mg. The injection method comprises any one of lumbar puncture, bridge forebay indwelling catheter injection and Ommaya capsule injection. The prepared EGFR-TKIs injection can be directly injected into the subarachnoid space, the drug concentration in cerebrospinal fluid of a patient is greatly improved, the cerebrospinal fluid / plasma concentration ratio of the EGFR-TKIs injection is increased from far less than 1 to more than 2 times and even can reach more than 10 times, and the EGFR-TKIs injection can completely solve the problem of insufficient dosage caused by a blood-brain barrier after oral administration of a targeted drug and has a good application prospect. The medicine takes effect quickly, and the treatment effect on lung cancer meningeal metastasis can be remarkably improved.

Provided herein are tablet(s) comprising N-acetylcysteine amide (NACA) and a NACA-acceptable, biocompatible excipient and optionally one or more pharmaceutically acceptable additives, binders, or fillers. Also provided are pharmaceutical composition(s) in the form an oral tablet comprising N-acetylcysteine amide (NACA), wherein the composition has a pharmacokinetic (PK) profile comprising mean plasma concentrations of NACA range from about 200 to 1200 ng / ml after administration of the pharmaceutical composition to a human.

Disclosed herein is a method for predicting whether a subject with cancer will exhibit a beneficial response to arginine deficiency therapy. The method includes the step of determining the plasma concentration of arginine in the subject, followed by administering arginine deficiency therapy to the subject alone or in combination with an anticancer agent, based on the determined plasma concentration of arginine. According to some embodiments of this disclosure, the anticancer agent is selected from the group consisting of FOLFOX, docetaxel, cisplatin, pemetrexed, pembrolizumab, and combinations thereof.

The invention discloses application of polyphenol in sleep improving medicine, and particularly relates to the technical field of medicine, the sleep improving medicine is included, and the sleep improving medicine is a medicine composition containing an oral preparation and an external preparation; the oral preparation contains a polyphenol component, and the polyphenol component is selected from at least one of a purple leaf lettuce extract, tea polyphenol, flavonoids and resveratrol. The polyphenol components in the oral and external preparations form a synergistic effect, the basic sleep-aiding effect is achieved by oral administration, the sleep-aiding effect is enhanced by external application, and the combined effect of the two preparations is far better than that of schizophyllan in single oral and external preparations under the action of a penetration enhancer, so that the transdermal efficiency of the polyphenol components can be remarkably improved; and the action duration is superposed with the plasma concentration peak time of the oral polyphenol, so that the sleep aiding effect can be continuously exerted, a favorable nerve environment is created for good sleep, the positive influence on intestinal flora is realized, and the number of effective flora is increased.

Embodiments of the invention are broadly drawn to methods for determining an optimum dose of an antiarrhythmic drug, for example sotalol. In particular, the method involves titrating the dose of the drug gradually to determine the optimum plasma concentration for a patient, whether the patient has normal or abnormal renal function.

The invention discloses a method for adjusting constant plasma concentration, which comprises the following steps of: 1, setting parameters, 2, acquiring data, 3, processing the data, calculating a compensated heating module control PWM (Pulse Width Modulation) signal Hcomp, calculating the compensated plasma concentration n, 4, scanning the frequency of an ion tube, determining a resonance point through a full-bridge current, and calculating the plasma concentration n. The ion tube and the transformer resonate at a resonance point to adjust the working frequency of the full-bridge circuit; and 5, adjusting the temperature of the heating module according to the data collected by the temperature and humidity module to adjust the plasma concentration generated by the ion tube, and / or adjusting the full-bridge amplitude of the full-bridge circuit through the booster circuit to adjust the plasma concentration generated by the ion tube. The plasma concentration value after compensation is obtained in real time through the plasma sensor, and the generator MCU can adjust the working frequency of the full-bridge circuit, so that the ion tube can output plasma constantly, and automatic adjustment of the plasma concentration is achieved.

The invention discloses a compound paracetamol and amantadine hydrochloride capsule containing caffeine microcapsules, which relates to the technical field of medicines and comprises paracetamol, amantadine hydrochloride, calculus bovis factitius, pharmaceutic adjuvants and functional microcapsule units. The functional microcapsule unit has a three-layer structure: a core material taking caffeine and microcrystalline cellulose as a core, an ethyl cellulose controlled release layer and a quick release layer containing chlorpheniramine maleate. According to the structure, time sequence controlled release of drugs is achieved by synthesizing a polymer coating material, chlorpheniramine maleate is quickly released when encountering gastrointestinal fluid to quickly resist allergy, and caffeine starts to be slowly released after being effectively delayed to the intestinal environment, so that the time when the plasma concentration reaches the peak tends to be synchronous with the time when chlorpheniramine maleate reaches the peak; the drowsiness side effect can be effectively resisted.

This invention relates to the interdisciplinary field of biomedical detection and Internet of Things (IoT) sensing technology, specifically disclosing a platelet-rich plasma concentration detection system based on IoT biosensors. The system includes a microfluidic sensor chip, a multi-frequency electrochemical impedance spectroscopy (MES) acquisition unit, a cell morphology identification module, an IoT communication unit, and a remote data processing server. It monitors platelet dynamic aggregation in real time through a three-electrode system, and combines high-dimensional features of broadband impedance spectroscopy with a pre-trained convolutional neural network model to accurately distinguish between simple platelet aggregates, platelet-leukocyte complexes, and microthrombus structures. Furthermore, it leverages the IoT architecture to complete encrypted data upload, remote model optimization, and intelligent coagulation risk assessment. Through the above technical solutions, this invention improves the sensitivity, specificity, and clinical applicability of the detection, constructing a closed-loop blood monitoring system from bedside detection to cloud-based decision support.

The application discloses a method for evaluating environmental risks of drugs in a water environment based on a fish plasma model, and belongs to the technical field of environmental toxicology and ecological risk assessment. The fish plasma-water distribution coefficient is calculated by a drug lipophilicity parameter (Log Dow), the fish steady-state plasma concentration is obtained by combining the measured / predicted environmental concentration, the fish treatment plasma concentration is converted by the difference between the half-inhibitory concentrations of the drug on fish and human, the pharmacological effect risk of the drug on fish is quantitatively evaluated by a risk quotient, and thus high-risk drugs are screened. Compared with the traditional risk quotient method, the application has the advantages of being in line with the drug action mechanism, taking into account the in-vivo enrichment effect, being high in evaluation accuracy, and not needing to rely on a large amount of acute / chronic toxicity data, and can efficiently support the priority control and risk management of drug pollutants in the water environment.

The invention provides a ceftiofur injection as well as a preparation method and application thereof, and belongs to the technical field of veterinary drug preparations. The ceftiofur injection prepared by the invention takes propylene glycol as a solvent, and every 1000 mL of the ceftiofur injection is prepared from the following components: 80 to 120 g of ceftiofur hydrochloride, 50 to 80 g of hydroxypropyl-beta-cyclodextrin, 180 to 220 mL of polyethylene glycol 400, 40 to 60 mL of medicinal glycerol, 2 to 5 mL of laurocapram and 0.8 to 1.2 g of ascorbyl palmitate. The ceftiofur injection prepared by the invention has the advantages that the plasma concentration peak reaching time is obviously shortened, the drug concentration of an infected part is obviously improved, the drug action time is effectively prolonged, the drug resistance risk of bacteria is reduced, the survival rate of piglets can be obviously improved, and the death risk caused by bacterial infection is effectively reduced; the method is suitable for prevention and control of secondary bacterial infection of the porcine reproductive and respiratory syndrome in large-scale pig

The present invention is directed to novel neuro-attentuating norketamine (NANKET) compounds according to any one of formulas (I—shown below), (I-A) and (I-B), or any of the compounds described in Tables A-D, or in any of the Examples provided herein, and pharmaceutically acceptable salts thereof, novel pharmaceutical formulations and novel methods of uses thereof. The present invention also features novel oral neuro-attenuating ketamine (NAKET) and neuro-attenuating norketamine (NANKET) modified-release pharmaceutical formulations, and novel methods of administration thereof, which ensure the steady release of a therapeutically effective amount of ketamine, norketamine, or derivatives thereof from the oral modified-release pharmaceutical formulations without neurologically toxic spikes in plasma concentration of the ketamine, norketamine, or derivatives during the release periods.

The invention provides a diamond growth distributed bias voltage regulation and control method and system based on spectrum diagnosis, and relates to the technical field of microwave plasma chemical vapor deposition diamond preparation. Spectral distribution of key precursor substances is captured in real time through emission spectra, 'on-demand distribution 'of bias voltage is achieved, the growth rate difference of all areas of a large-size substrate (the diameter is larger than or equal to 50 mm) is reduced to be within 1 micrometer / h and is superior to 1.5 micrometers / h of traditional distributed bias voltage, and the thickness uniformity and crystal form consistency of a diamond film are greatly improved. A quantitative association rule of spectral intensity-bias adjustment amount is established, the bias adjustment amount of 5V corresponds to the concentration exceeding a threshold value by 1%, dependence on artificial experience is avoided, the process repeatability error is smaller than or equal to + / -5%, and industrial batch production is facilitated. The plasma concentration fluctuation can also be responded in real time, the core defect that static presetting cannot be adapted to dynamic change in traditional bias voltage regulation and control is overcome, the quality stability in the growth process is improved by 30% or above, and deterioration of later growth uniformity is effectively avoided.

A topiroxostat pharmaceutical composition, a preparation method and a use. The dissolution release profile of the topiroxostat pharmaceutical composition has the following characteristics: 1) dissolution of no more than 30% of a pharmaceutically active ingredient within 1 hour; 2) dissolution of 20%-70% of the pharmaceutically active ingredient within 8 hours; and 3) dissolution of no less than 70% of the pharmaceutically active ingredient within 24 hours. The topiroxostat pharmaceutical composition has good sustained-release performance and a 24-hour cumulative release rate of 70% or more; the drug exhibits stable plasma concentration, good stability and few adverse effects, requires less frequent administration, and has good patient compliance; and the preparation process is simple and stable, process parameters are adjustable and controllable, which is conducive to production scale-up, and the market prospect is good.

The invention provides an application of terazosin or a pharmaceutically acceptable salt thereof in preparation of a medicine for preventing and / or treating hepatic fibrosis, relates to the technical field of biological medicines, and finds that the terazosin or the pharmaceutically acceptable salt thereof can be used for preventing and treating hepatic fibrosis for the first time. It is revealed that terazosin or a pharmaceutically acceptable salt thereof can improve the degree of hepatic fibrosis by improving the liver function, reducing the content of a marker alpha-SMA of activated hepatic stellate cells in liver tissue, reducing the content of Col1a1 in the liver tissue and reducing collagen deposition in the liver tissue. The liver-targeted sustained-release drug provided by the invention can reduce the peak value of the plasma concentration of terazosin and prolong the plasma half-life period of terazosin, has the same treatment effect as that of repeated low-dose injection of terazosin, and has a wide application prospect.