14 results about "Metoclopramide" patented technology

The invention discloses a preparation method of metoclopramide tablets, which comprises the following steps: uniformly mixing a metoclopramide tablet raw material main drug, a filler and a lubricant to prepare premixed powder; performing dry granulation on the premixed powder in a dry granulator to obtain dry granules of metoclopramide tablets; uniformly mixing the dry metoclopramide tablet particles with an external lubricant to prepare intermediate particles; and tabletting the metoclopramide tablet intermediate particles to prepare the metoclopramide tablet. The composition is simple, only contains the main drug, the filler and the lubricant, is safe to use, and does not increase the burden of a patient. The preparation process is simple and convenient to operate, is a dry granulation process, and is white tablets in drug character.

The invention provides a metoclopramide intermediate and a preparation method and application thereof, the molecular formula of the metoclopramide intermediate is C9H10ClNO3, and the metoclopramide intermediate can be used for quality detection and control in the synthesis process of metoclopramide and can also be used for formulating a central control standard of a metoclopramide ammonolysis reaction product.

The invention relates to the field of medicinal chemistry, and provides a preparation method of metoclopramide intermediate methyl 2-methoxy-4-acetamidobenzoate, which comprises the following steps: mixing methyl 2-methoxy-4-acetamidobenzoate and acetic anhydride in a molar ratio of 1: (1.2-2.0) in the absence of a solvent, and reacting at the temperature of 50-80 DEG C; and after the reaction, adding methyl tert-butyl ether for crystallization, cooling and filtering to obtain a product. The method has the advantages that acetic anhydride is used as an acylation reagent; on one hand, compared with acetyl chloride, the reaction is more stable, the reaction controllability is better, and the product purity is high; on the other hand, acetic anhydride is liquid and can serve as a solvent, no extra solvent needs to be added, and cost is saved; meanwhile, no solvent is added, so that the post-treatment process is simplified, the operation is simple, and the yield is higher. The 2-methoxy-4-acetamidobenzoic acid methyl ester prepared on the basis of the method has the purity of 99.8% or above and the yield of 90% or above, and is suitable for industrial production.

Metoclopramide is administered for the treatment of moderate to severe gastroparesis, in some embodiments, severe gastroparesis.

The application provides a use of a combination of metoclopramide and latanoprost for preparing an anticoagulant drug, and belongs to the technical field of biological medicines. It is accidentally found that the anticoagulant effect of patients with deep vein thrombosis combined with high intraocular pressure is improved after long-term continuous oral administration of metoclopramide. Thanks to this beneficial discovery, the application realizes good anticoagulant effect by applying the latanoprost liniment in a topical manner on the basis of oral administration of metoclopramide. The application is convenient to administer, has definite and sustained curative effect, and is safe and reliable. The application expands the optional range of anticoagulant drugs, and realizes better curative effect at the same time, and has outstanding technical advantages and wide popularization prospect.

Nasal formulations of metoclopramide, which remain stable and / or colorless upon storage over a period of time, are provided. Also provided are methods of treating disorders treatable with metoclopramide, comprising administering the nasal solutions to patients in need thereof.

Described herein are methods for treating gastroparesis with intranasally-administered compositions comprising metoclopramide. The methods include periods of time in which a patient is not administered a composition comprising metoclopramide.

The invention discloses application of a compound containing a dibenzofuran structure in preparation of a medicine for preventing and / or treating nausea and vomiting, and relates to the technical field of medicinal chemistry. The invention provides application of a compound containing a dibenzofuran structure in preparation of a medicine for preventing and / or treating nausea and vomiting, the molecular formula of the compound is C19H11ClN2O4, and the CAS number is 328255-08-9. The compound can effectively reduce the number of times of canine retching and vomiting caused by cis-platinum, has an effect superior to that of metoprazole, has the potential of preventing and / or vomiting caused by chemotherapy, and has an application prospect in development of drugs for treating vomiting caused by chemotherapy drugs.

Described herein are methods for reducing healthcare resource use by patients treated with metoclopramide.

The invention relates to a preparation method of metoclopramide. Specifically, the invention discloses a method for preparing high-purity metoclopramide with higher yield by taking 2-ethanolamine as a raw material in an organic solvent through a three-step reaction. The 2-ethanolamine is wide in source, the selectivity of the 2-ethanolamine serving as a starting material and suppliers is higher, the cost is lower, the 2-ethanolamine is more economical, the public route is novel, the cost is obviously reduced, and the total yield is slightly increased.

This invention belongs to the field of pharmaceutical material synthesis technology, specifically relating to a preparation process of metoclopramide. The invention first hydrolyzes 4-acetamido-5-chloro-2-methoxybenzoate to obtain the hydrolysate 4-amino-5-chloro-2-methoxybenzoic acid. Then, dichloromethane, the hydrolysate, and N,N'-carbonyldiimidazole are added to a reaction vessel, and the mixture is heated to 40-50°C and maintained at this temperature. After the reaction, N,N-diethylethylenediamine is added dropwise to the reaction solution, controlling the temperature inside the reaction vessel to not exceed 43°C during the addition. After the addition is complete, the mixture is kept under reflux and the reaction is maintained at this temperature. Crude metoclopramide is obtained after the reaction, which is then purified to obtain metoclopramide. This invention achieves a high yield and improved purity of metoclopramide through the optimization of various conditions, such as screening and determining the raw material ratio and controlling the type and amount of solvent.

Metoclopramide is administered for the treatment of moderate to severe gastroparesis, in some embodiments, severe gastroparesis.

The invention provides a method for detecting the dissolution rate of domperidone tablets, and relates to the technical field of analytical chemistry. According to the method, high performance liquid chromatography is adopted for determination, mobile phases comprise a mobile phase A and a mobile phase B, the mobile phase A is methanol-ionic liquid, the mobile phase B is an acetonitrile-glacial acetic acid solution, a gradient elution procedure is adopted, effective separation of domperidone and a large number of other auxiliary materials and impurities is achieved, the number of main peak theoretical plates of domperidone is larger than 3000, and the detection wavelength is 250nm. The domperidone component is exclusively and precisely measured, the quality evaluation of the dissolution rate of the domperidone tablet is greatly improved, and the detection method has high specificity and high sensitivity, and meanwhile, meets the green and environment-friendly requirements.

The invention provides a preparation method of metoclopramide, which comprises the following steps: mixing 5-chloro-4-amino-2-methoxybenzoic acid methyl ester hydrochloride and N, N-diethylethylenediamine, and heating to react, so as to obtain a metoclopramide crude product reaction solution; dissociating the metoclopramide crude product reaction solution by using a sodium hydroxide solution, filtering, washing a filter cake to be neutral by using water, and drying to obtain a metoclopramide crude product. According to the method, the methyl 5-chloro-4-amino-2-methoxybenzoate hydrochloride is used as the raw material to prepare the metoclopramide, so that the reaction impurities are reduced, the conversion rate is increased, and the relative peak area of the methyl 5-chloro-4-amino-2-methoxybenzoate is only 0.11% in the prepared crude product reaction liquid of the metoclopramide.