18 results about "Oxcarbazepine" patented technology

The invention belongs to the technical field of biological culture, and particularly relates to a chlorella extracellular fluid and a preparation method and application thereof.The preparation method of the chlorella extracellular fluid comprises the following steps that a BG11 culture medium is inoculated with a chlorella solution cultured to the logarithmic phase, oxcarbazepine is added, and the chlorella extracellular fluid is obtained; the preparation method comprises the following steps: placing chlorella in an intermittent illumination environment with the temperature of 20-30 DEG C and the rotating speed of 100-200 rpm for growth, centrifuging the chlorella to obtain supernate after the chlorella grows to the 10th-16th day, filtering, sub-packaging, and performing cryopreservation to obtain the chlorella extracellular fluid. By adding oxcarbazepine, the chlorella extracellular fluid prepared in a specific culture medium and a specific growth environment has high oxidation activity, excellent stability and excellent degradation capacity, and a new thought is provided for solving the pollution treatment problem of current environmental pollutants such as pharmaceutical products, polycyclic aromatic hydrocarbons and dyes.

The invention relates to a method for preparing oxcarbazepine impurities, which comprises the following steps of: reacting iminostilbene serving as a raw material with an oxidizing agent N-methylmorpholine-N-oxide under the catalysis of potassium osmate and DABCO to generate a diol intermediate; oxidizing the diol intermediate in the presence of an oxidizing agent 2, 3-dichloro-5, 6-dicyano-1, 4-benzoquinone to obtain an alpha-hydroxy ketone intermediate; oxidizing the alpha-hydroxy ketone intermediate (III) in the presence of ammonium nitrate and copper acetate to obtain a diketone intermediate; and reacting the diketone intermediate (II) with isocyanate chlorosulfonate to obtain the oxcarbazepine impurity 11-ketone oxcarbazepine (I). The preparation method has the advantages of being convenient to operate, high in yield and good in product purity. # imgabs0 #

The present application provides a detection method and quality control method for related substances in dextromethorphan oral solution, which comprises the following steps: dissolving dextromethorphan oral solution in a solvent to obtain a test solution; and performing high performance liquid chromatography detection on the test solution; the mobile phase used in the high performance liquid chromatography detection comprises mobile phase A and mobile phase B, the mobile phase A comprises a phosphate solution, the mobile phase B comprises acetonitrile, and the concentration of the phosphate solution is 0.1 mM-10 mM. The detection method has good linear relationship between dextromethorphan and related substances, good accuracy and sensitivity, strong specificity, high stability, good separation degree and good reproducibility, and is suitable for wide application.

The invention discloses a cyclization continuous flow synthesis process of iminodibenzyl. 2, 2 '-diamino bibenzyl is used as a raw material, polyphosphoric acid is used as a cyclization agent, toluene is used as a dispersion medium, the efficient heat and mass transfer characteristic of the microchannel reactor is utilized, the reaction temperature is controlled within 85 + / -2 DEG C, meanwhile, the material ratio and the retention time are optimized, generation of high-polymer impurities is inhibited from the source, no remarkable high-polymer impurities exist in reaction liquid, a rectification purification process is not needed, and the production cost is reduced. And washing the toluene layer with phosphoric acid, washing with clear water, and crystallizing to obtain a high-purity qualified product. In the product obtained by the process, the content of high polymer impurities is less than or equal to 0.003 wt%, the residue of 2, 2 '-diamino bibenzyl is less than or equal to 0.0002 wt%, the purity of the product is more than or equal to 99.8%, and the molar yield reaches 93.2%; the toluene solvent recycling rate is greater than or equal to 95%, the discharge amount of three wastes is reduced by more than 70% compared with that of a traditional intermittent process, and the method has the advantages of product quality improvement, production efficiency improvement and environmental protection, and can be directly applied to large-scale production of antiepileptic drug oxcarbazepine and carbamazepine intermediates.

The invention relates to the technical field of biological detection, and particularly discloses a method for simultaneously determining serum concentrations of an anti-epileptic drug and active metabolites thereof based on an LC-MS / MS (Liquid Chromatography-Mass Spectrometry / Mass Spectrometry) method. According to the method, the C18 chromatographic column with the filler particle size of 3.0 microns is selected for the first time, efficient separation of lamotrigine, levetiracetam, oxcarbazepine and active metabolites thereof is achieved, and the separation efficiency is equivalent to that of a small-particle-size column; a pretreatment process is simplified by precipitating protein through a single organic solvent, and accurate quantification of four components is completed by only using two isotope internal standard oxcarbazep-d4 and levetiracetam-d6, so that the cost is reduced. In the aspect of the detection range, the lower quantification limit of oxcarbazepine is broken through to 0.04 [mu] g.mL <-1 >, and the technical contradiction between oxcarbazepine and the upper quantification limit (as high as 50 [mu] g.mL <-1 >) of LEV across three orders of magnitude is overcome. According to the scheme, hardware requirements and reagent cost are reduced, and meanwhile, high sensitivity and a wide linear range are achieved.

The present invention relates to the treatment of an executive function disorder, such as attention deficit hyperactivity disorder (ADHD) and / or autism with both lacosamide and oxcarbazepine.

A composition for the treatment of chronic pain and mixed pain sites may include a serotonin and norepinephrine reuptake inhibitor; a non-steroidal anti-inflammatory agent; optionally acetaminophen; optionally oxcarbamazepine; optionally an oral opioid antagonist; optionally an antacid; optionally an anti-epileptic; and optionally an opioid. A method for treating chronic pain and mixed pain sites may include administering, to a patient in need, a therapeutically effective dosage of the composition.

The invention relates to a method for detecting antiepileptic drugs in serum based on polarity conversion UPLC-MS / MS. The antiepileptic drugs (AEDs) are respectively levetiracetam, pregabalin, gabapentin, lamotrigine, phenobarbital, oxcarbazepine, phenytoin sodium, carbamazepine, clonazepam, diazepam and sodium valproate. Simplifying sample pretreatment by adopting a methanol (containing formic acid) one-step extraction method; in the chromatographic analysis, C18 is used as a chromatographic column and a pre-column, a 5% methanol aqueous solution (containing formic acid)-95% methanol aqueous solution (containing formic acid) is used as a mobile phase, gradient elution is carried out, and the mass spectrum adopts an MRM mode. The method has the advantages of being high in sensitivity, good in precision and accuracy, easy to operate, free of matrix interference and the like, can be used for measuring serum AEDs of different species, and provides technical support for the prevention and treatment mechanism of epilepsy drugs, clinical AEDs blood concentration monitoring, individualized drug delivery scheme formulation and pharmacokinetic research.

The application provides a synthesis process of an ocinaplon intermediate. S1, petroleum ether, methanol and ethyl formate are mixed to obtain a mixed system, ortho-phenyltoluene and sodium methoxide are added, and reaction is carried out to obtain intermediate 1; S2, intermediate 1 is added into methanol, a palladium-carbon catalyst is added, hydrogen is introduced, and reaction is carried out to obtain intermediate 2; S3, phosphoric acid and a supported catalyst are added into intermediate 2, and reaction is carried out to obtain iminodibenzyl. The problem of low iminodibenzyl yield in the prior art is solved.

1. Name of the designed product: medicine packaging set (Oxcarbazepine). 2. Use of the designed product: for medicine packaging. 3. Design points of the designed product: combination of shape and pattern. 4. Picture or photo best indicating the design points: set 1 perspective view 1. 5. Other circumstances needing to be explained: set 1 is an inner packaging box; set 2 is an outer packaging box; set 3 is a packaging bottle.

The present invention belongs to the technical field of biological culture, and particularly relates to a Chlorella extracellular fluid, a preparation method thereof and an application. The preparation method of the Chlorella extracellular fluid comprises the following steps: inoculating the Chlorella algal solution cultured to the logarithmic growth phase into the BG11 medium, adding oxcarbazepine, and growing it in an intermittent light environment at a temperature of 20-30 °C and a rotation speed of 100-200 rpm. When the Chlorella grows to the 10th to 16th day, centrifuge the Chlorella to obtain the supernatant, filter and subpackage it, and then store it frozen to obtain the Chlorella extracellular fluid. By adding oxcarbazepine, the Chlorella extracellular fluid prepared under specific culture medium and specific growth environment in the present invention has strong oxidation activity, excellent stability and excellent degradation ability, providing a new idea for the treatment of current environmental pollutants such as pharmaceutical products, polycyclic aromatic hydrocarbons and dyes.

The invention discloses a method for synthesizing a key intermediate of oxcarbazepine. The method uses compound 2 as a raw material, undergoes acetic acid hydrolysis to obtain compound 3, and then performs serial hydrolysis to obtain a hydroxyl compound, namely compound 4. The hydroxyl compound is subjected to copper-catalyzed air oxidation to obtain a carbonyl compound, namely compound 5, thereby obtaining the key intermediate of oxcarbazepine. The reaction formula is as follows: the process of the invention has a short synthesis process, uses inexpensive and readily available materials, has mild conditions in each step, and has a high yield; compared with a traditional process for direct hydrolysis of bromides, the process for acetic acid hydrolysis followed by hydrolysis of the bromide can effectively inhibit the alkaline elimination of the bromide, and significantly improves the selectivity of the hydrolysis reaction; and the step for oxidizing the hydroxyl compound to prepare the carbonyl compound uses oxygen as an oxygen source, which has clear advantages in terms of economy and safety compared with a traditional sodium hypochlorite / TEMPO oxidation process.

The application discloses a genetic polymorphism-based oxcarbazepine quantitative pharmacological model and a construction method thereof, and belongs to the field of pharmacokinetics. The model construction method is characterized by the following steps: collecting steady-state blood drug concentration data and clinical data of epilepsy children patients, adopting a nonlinear mixed effect model method to establish a population pharmacokinetic model of an active metabolite of oxcarbazepine, and quantitatively investigating the influence of physiological factors, combined medication and genetic factors on pharmacokinetic characteristic parameters of the drug; and finally, the final model is internally verified and evaluated by using a goodness-of-fit diagram, a bootstrap method and an intuitive prediction test. The quantitative pharmacological model constructed by the application has stable and accurate prediction performance; the body weight and the genetic polymorphism ABCC2rs2273697 are determined as effective covariates influencing MHD CL / F; and an oxcarbazepine dose optimization scheme is established based on the body weight and the genotype of the patients, so that the treatment effect of the oxcarbazepine is improved, and the occurrence of adverse reactions is avoided.

The invention discloses a synthesis method of oxcarbazepine and analogues thereof, which comprises the following steps: dissolving a dibenzo [b, f] azepine analogue as shown in a formula (I) in an organic solvent under an illumination condition, and carrying out oxidation reaction in an air or oxygen atmosphere under the action of a photocatalyst. And after the reaction is completed, carrying out post-treatment on the reaction liquid to obtain oxcarbazepine shown in the formula (II) and the analogue thereof. The reaction formula is as follows. The method takes light as reaction energy, and has the advantages of high safety, low cost, mild conditions, simplicity and convenience in operation and the like.

The invention discloses a preparation method of oxcarbazepine, and belongs to the technical field of drug synthesis, 2-bromophenylacetyl chloride and N-phenyl cyanamide are subjected to a Friedel-Crafts reaction, and the temperature is controlled at 0-20 DEG C, so that the occurrence of side reactions can be effectively reduced, and the conversion rate of raw materials can be improved. According to the preparation method disclosed by the invention, only a palladium catalyst needs to be used in the synthesis process of the 10-oxo-10, 11-dihydro-5H-dibenzo [b, f] azepine-5-carbonitrile, so that the synthesis cost is effectively reduced, and the post-treatment process is simple; in the hydrolysis reaction, water or dichloromethane is used as a solvent, and 10-oxo-10, 11-dihydro-5H-dibenzo [b, f] aza-5-formamide is obtained under the catalysis of an acidic reagent. The preparation method provided by the invention has the advantages of easily available raw materials, low cost, mild process conditions and simple post-treatment process, and is more beneficial to realization of industrial production.

The invention discloses a preparation method of an oxcarbazepine intermediate, and relates to the technical field of medicine synthesis. The preparation method comprises the following steps: dissolving acyl chloride iminodibenzyl in an aprotic organic solution to obtain a reaction solution, then adding bromine into the reaction solution in stages, and carrying out reaction and purification to obtain the oxcarbazepine intermediate 10, 11-dibromo-10, 11-dihydro-5H-dibenzo [b, f] azacyclopentene-5-carbonyl chloride. Wherein the reaction temperature of each bromine adding stage is subjected to staged control, so that the purity and the yield of the oxcarbazepine intermediate can be improved, the volatilization of bromine can be reduced, and the cost is reduced. According to the method for synthesizing the oxcarbazepine intermediate by the one-pot method, purification of iminostilbene formyl chloride and redissolution by replacing a solvent are not needed, the operation is simple, the production cost is saved, and the method is suitable for industrial large-scale application.

The invention relates to the technical field of pharmaceutical preparations, in particular to oxcarbazepine tablets and a preparation method thereof. The oxcarbazepine tablet comprises the following components in percentage by weight: 70-75% of oxcarbazepine, 15-20% of a filler, 1.8-2.3% of a first adhesive, 0.5-1% of a second adhesive, 5-7% of a disintegrating agent and 0.8-1.2% of a lubricant, wherein the first adhesive is selected from povidone; the second binder is selected from polyethylene glycol. The oxcarbazepine tablet disclosed by the invention has good dissolution performance and stability, by using the combination of povidone and polyethylene glycol adhesive and combining with screening of types and dosages of other auxiliary materials, the use of colloidal silicon dioxide as a flow aid is avoided, the risk of dust inhalation injury of the flow aid is reduced, the flowability of total mixed particles is improved, and the stability of the tablet is improved. And smooth discharging of materials in the tabletting process is ensured, and the tabletting requirement of mass production is met.

This invention relates to the treatment of chronic pain and mixed pain sites. Previously, treatment options for patients with chronic pain and mixed pain sites included switching to different pain medications and used of non-opioid alternatives. Embodiments of the present invention use a serotonin and norepinephrine reuptake inhibitor, a non-steroidal anti-inflammatory agent, optionally acetaminophen, optionally oxcarbamazepine, optionally an oral opioid antagonist, optionally an antacid, optionally an anti-epileptic, and optionally an opioid.