16 results about "Etiracetam" patented technology

The invention discloses a levetiracetam sustained-release granule and a preparation process thereof, and relates to the technical field of pharmaceutical preparations. The preparation method specifically comprises the following steps: S1, preparing levetiracetam active particles; s2, preparing a transition coating solution and a slow-release coating solution; and S3, coating the levetiracetam active particles with a transition layer and a sustained-release layer in sequence to obtain the levetiracetam sustained-release particles. Wherein the transition coating liquid is prepared by mixing the following raw material components in parts by weight: 3-5 parts of sodium alginate, 1-1.5 parts of a plasticizer and 100 parts of purified water; wherein the molecular weight of the sodium alginate is 50000 to 100000; the slow-release coating solution is prepared by mixing the following raw material components in parts by weight: 5-8 parts of silicon dioxide modified chitosan, 3-5 parts of sodium alginate, 1.5-3 parts of a plasticizer and 200 parts of purified water; wherein the molecular weight of the sodium alginate is 150000 to 200000.

The present application relates to a levetiracetam oral solution. Specifically, the present application provides a levetiracetam oral solution comprising levetiracetam, sucralose, polyethylene glycol 400, glycerol, lactose, mannitol, sorbitol, hydroxyethyl cellulose, citric acid, disodium hydrogen phosphate, sodium bisulfite and water. The levetiracetam oral solution of the present application can effectively mask the bitter taste of levetiracetam and its residues, thereby having excellent oral compliance, and the levetiracetam oral solution has excellent stability to light, high temperature and high humidity, can be divided and packed in transparent containers, is convenient for storage and transportation, ensures quality safety, and guarantees medication safety.

The invention relates to the field of pharmacy, and discloses a levetiracetam derivative, and the levetiracetam derivative is a boron dipyrromethene levetiracetam derivative. The structural formula of the BODIPY-L-Racetam derivative is as shown in formula (I), wherein the BODIPY-L-Racetam derivative contains two substituent groups, namely R1 and R2; wherein R1 is any one of straight chain alkyl groups or branched chain alkyl groups of-C6H5,-(4-Me) C6H4,-(4-Cl) C6H5,-(4-Br) C6H4,-(4-F) C6H4,-(3-F) C6H4,-(3-Br) C6H4 and C4-C10; r2 is any one of-H,-Cl,-OCH3,-OCH2CH3,-OC6H5,-O (4-OMe-C6H4),-O (4-Me-C6H4),-O (4-ClC6H4),-O (4-BrC6H4),-O (4-CF3C6H4),-C6H5,-(4-Me) C6H4,-(4-Cl) C6H5,-(4-Br) C6H4,-(4-F) C6H4, CH (CO2CH2CH3) 2 and CH (CO2CH2CH3) 2, and a synthesis method and application thereof. According to the invention, synthesis of the levetiracetam derivative is realized, the characteristic that levetiracetam can treat epilepsy is reserved, and the levetiracetam has a bright color, so that the levetiracetam derivative is favorably applied to research of levetiracetam drug delivery and drug effect monitoring.

This application relates to the field of analytical detection technology, specifically to sample pretreatment methods, kits, and detection methods for the detection of antiepileptic drugs. The sample pretreatment method for the detection of antiepileptic drugs in this application includes one or more of the following antiepileptic drugs: valproic acid, carbamazepine, phenytoin, levetiracetam, lamotrigine, and phenobarbital. The sample pretreatment method includes the following steps: mixing magnetic beads with an activation solution to prepare a magnetic bead suspension; mixing the sample to be tested, the magnetic bead suspension, and an internal standard solution, and separating the supernatant and the magnetic bead complex after magnetic adsorption treatment; adding an eluent to the magnetic bead complex, and collecting the magnetic bead-target complex after elution treatment; adding an elution buffer to the magnetic bead-target complex, and collecting the supernatant after elution treatment for detection. The above sample pretreatment method is simple to operate, time-saving, and low-cost, providing key technical support for the efficient quantitative detection of antiepileptic drugs.

This invention relates to the preparation of high-purity levetiracetam (S)-2-(2-oxo-1-pyrrolidine)butyramide. The preparation of the high-purity levetiracetam begins with 2-(2-oxopyrrolidine-1-yl)butyric acid as the starting material. Through esterification and ammonolysis, a racemic levetiracetam is obtained, which is then resolved by R-mandelic acid to yield high-purity levetiracetam with a chiral content of over 99.9%, a chiral isomer content of less than 0.05%, and no chloride detected. The chiral isomer (R)-2-(2-oxo-1-pyrrolidine)butyramide recovered after resolution can be racemed and further resolved by R-mandelic acid for the preparation of levetiracetam, achieving a total yield of over 90%. The recovered R-mandelic acid can be reused repeatedly, significantly reducing the consumption of resolving agent. This reaction has a short procedure, is easy to operate, and has a stable yield, which significantly reduces the cost of preparing levetiracetam. In addition, it has a very high chiral content, making it suitable for large-scale industrial production.

This invention relates to the field of pharmaceutical analysis technology, specifically to a method for determining the content of L-2-aminobutyric acid (GABA), a degradation impurity, in a concentrated solution of levetiracetam for injection. The method includes the following steps: diluting the concentrated levetiracetam for injection with a 50% acetonitrile aqueous solution, and then determining the content using high-performance liquid chromatography (HPLC) with a UV detector. C0.05 is also used. 18 The chromatographic column uses an aqueous solution of ammonium dihydrogen phosphate and acetonitrile as the mobile phase. This invention provides an accurate method for determining the degradation impurity L-2-aminobutyric acid in levetiracetam, which is highly specific, sensitive, accurate, and easy to operate, effectively controlling the quality of concentrated levetiracetam injection solutions.

The application provides a synthesis method of levetiracetam, wherein starting material I is reacted with SOCl2 under the action of a solvent A to generate an intermediate I; the intermediate I is reacted with starting material II under the action of a solvent B to generate an intermediate II; and the intermediate II is reacted with 4-chlorobutyryl chloride under the action of a solvent C to generate levetiracetam. The method is simple in operation, mild in reaction condition, high in yield, low in cost, friendly to the environment and suitable for industrialized mass production of levetiracetam.

The invention relates to the technical field of analysis and detection, in particular to a sample pretreatment method for anti-epileptic drug detection, a kit and a detection method. According to the sample pretreatment method for anti-epileptic drug detection, an anti-epileptic drug comprises one or more of valproic acid, carbamazepine, phenytoin, levetiracetam, lamotrigine and phenobarbital; the sample pretreatment method comprises the following steps: mixing magnetic beads with an activating solution to prepare a magnetic bead suspension; mixing a to-be-detected sample, the magnetic bead suspension and the internal standard solution, performing magnetic attraction treatment, and separating supernate and a magnetic bead compound; leacheate is added into the magnetic bead compound, and after leaching treatment, a magnetic bead-target compound is collected; and adding an eluent into the magnetic bead-target compound, carrying out elution treatment, and collecting a supernatant for detection. The sample pretreatment method is simple to operate, short in time consumption and low in cost, and can provide key technical support for efficient quantitative detection of the anti-epileptic drugs.

There is disclosed an improved process for the racemization of (R)-α-ethyl-2-oxo-1-pyrrolidineacetic acid in a solution of alkali hydroxide. The process comprises heating a crystalline suspension of the racemic (RS)-α-ethyl-2-oxo-1-pyrrolidineacetic acid at a temperature from 100° C. to 250° C. to increase the yield and purity. The racemic (RS)-α-ethyl-2-oxo-1-pyrrolidineacetic acid is optically resolved into(S)-α-ethyl-2-oxo-1-pyrrolidineacetic acid and converted to levetiracetam.

The application discloses a preparation method of levetiracetam, which comprises the following steps: after (S)-alpha-ethyl-2-oxo-1-pyrrolidine acetate is ammoniated in water, excessive ammonia gas in a reaction system is removed, part of water is removed through distillation, and inorganic salt is added before extraction, so that the yield and quality of levetiracetam are improved.

An orodispersible tablet of levetiracetam, comprising: 55-85 %w / w levetiracetam or pharmaceutically acceptable salts thereof; a diluent at 2-35 %w / w (e.g. microcrystalline cellulose (MCC) (1-20 %w / w),

The invention discloses a levetiracetam sustained-release micro-tablet and an application of the levetiracetam sustained-release micro-tablet. The levetiracetam sustained-release micro-tablet core disclosed by the invention has good friability and tabletability, is easy to form in a tabletting processing process, and solves the difficult problems of tabletting formability of the micro-tablet core and friability of the micro-tablet core in a subsequent coating process in the prior art; the successful preparation of the levetiracetam sustained-release micro-tablet core and the sustained-release coated micro-tablet is realized. Compared with an original sustained-release tablet, the levetiracetam sustained-release micro-tablet disclosed by the invention has the advantages that the size and the volume are greatly reduced, the levetiracetam sustained-release micro-tablet is easier to swallow by a patient, and the medication compliance of the patient is greatly improved. And the sustained-release layer coating is coated on the outer layer of the tablet core, so that the levetiracetam sustained-release micro-tablet realizes stable release of a membrane control mechanism, and the long-acting and stable release effect of the sustained-release micro-tablet is achieved.

The invention relates to a crystal form B of (S)-2-aminobutanamide hydrochloride, a preparation method of the crystal form B and a method for preparing levetiracetam by using the novel crystal form. The novel crystal form can improve the reaction yield and product purity of subsequent levetiracetam.

There is disclosed a method for preparing levetiracetam and intermediates from a compound of the formula:wherein CR is selected from the group consisting of cyano, carboxylic acid, carboxamide, alkali carboxylate, alkaline earth metal carboxylate, alkyl carboxylate, and a mixture thereof.

The application discloses a levetiracetam sustained-release granule and a preparation process thereof, and relates to the technical field of pharmaceutical preparations. Specifically, the preparation process comprises the following steps: S1, preparing levetiracetam active granules; S2, preparing a transition coating liquid and a sustained-release coating liquid; and S3, sequentially performing transition layer and sustained-release layer coating on the levetiracetam active granules to obtain the levetiracetam sustained-release granules. The transition coating liquid is prepared by mixing the following raw material components in parts by weight: 3-5 parts of sodium alginate, 1-1.5 parts of a plasticizer and 100 parts of purified water; the molecular weight of the sodium alginate is 50000-100000; the sustained-release coating liquid is prepared by mixing the following raw material components in parts by weight: 5-8 parts of silicon dioxide modified chitosan, 3-5 parts of sodium alginate, 1.5-3 parts of a plasticizer and 200 parts of purified water; and the molecular weight of the sodium alginate is 150000-200000.

There is disclosed a process for the production of levetiracetam by crystallizing levetiracetam in an aqueous solution, optionally in the presence of a water-soluble solvent. The product of levetiracetam contains no residual organic solvent.