12 results about "Rebamipide" patented technology

To provide a technology that suppresses the strong bitter taste of rebamipide in various dosage forms of formulations. [Solution] A pharmaceutical composition containing rebamipide, an organic acid (excluding amino acids), and an amino acid.

A solubilizing composition for the poorly soluble drug rebamipide, its preparation method and application, and the solubilizing method, by combining rebamipide with a phosphorylated drug in a specific ratio, effectively improves the solubility of rebamipide in PBS. The solubilizing composition prepared by this invention significantly improves the bioavailability of rebamipide, providing a new approach for the development of oral and ophthalmic formulations of rebamipide.

The application belongs to the field of medicine, and discloses a rebamipide volorabine salt, which has a structure shown in formula (I), wherein the structure of formula (I) is as follows: the application discloses a preparation method of the rebamipide volorabine salt and application of the rebamipide volorabine salt in preparation of a medicine for treating and / or preventing a gastric acid related disease or a helicobacter pylori infection disease.

The invention discloses hollow adhesive microspheres loaded with rebamipide as well as a preparation method and application of the hollow adhesive microspheres, and belongs to the technical field of improvement of pharmaceutical dosage forms. The preparation method of the rebamipide-loaded hollow adhesive microspheres comprises the following steps: mixing ethyl cellulose, an acrylic resin material and rebamipide in a mixed solvent prepared from a chloralkane solvent and an alcohol solvent to obtain an oil phase solution; mixing polyvinyl alcohol and an oil-in-water surfactant in water to obtain a water phase solution; adding the oil phase solution into the water phase solution, mixing and volatilizing under a stirring condition, and forming a porous cavity structure with a fiber interpenetrating network through liquid-liquid phase separation in a stirring process, so as to obtain the rebamipide hollow microspheres; and carrying out adhesion coating on the rebamipide hollow microspheres to obtain the rebamipide-loaded hollow adhesion microspheres. The rebamipide-loaded hollow adhesive microspheres prepared by the invention can be detained in the stomach for a long time to realize controllable release, so that the bioavailability and the treatment effect of rebamipide are improved.

The invention belongs to the field of medicines, and discloses a rebamipivonoprazan salt, which has a structure as shown in a formula (I), or an optical isomer or a deuterated compound of the structure as shown in the formula (I), and the structure of the formula (I) is as shown in the specification. The invention discloses a preparation method of the rebamipivonoprazine salt and application of the rebamipivonoprazine salt in preparation of drugs for treating and / or preventing gastric acid related diseases and helicobacter pylori infection diseases.

The invention provides a preparation method of a rebamipide-polypeptide conjugate and application of the rebamipide-polypeptide conjugate in xerophthalmia treatment, and belongs to the field of medicinal chemistry. The rebamipide-polypeptide conjugate synthesized by the invention is composed of three modules, namely a hydrophobic drug rebamipide, a beta-sheet self-assembly motif and a hydrophilic fragment. The medicine is connected with the polypeptide through a breakable disulfide bond. The obtained rebamipide-polypeptide conjugate can be self-assembled in water to form a nano structure, and a hydrophobic drug is contained in the nano structure. Under the action of ocular surface reductive glutathione, the disulfide bond connected with the medicine is broken, so that the release of the medicine is realized. According to the strategy, the drug is used as a molecular building block for building a delivery carrier of the drug, the solubility of the hydrophobic drug is obviously improved, the precorneal retention time of the drug is prolonged, and a better treatment effect is achieved. The method is simple and convenient in synthesis and high in repeatability, provides a foundation for application in the fields of drug delivery, biomedical engineering and the like, and has a good application prospect.

The present invention provides a pharmaceutical composition that, despite containing rebamipide, exhibits excellent transparency and high stability. [Solution] A pharmaceutical composition containing rebamipide, amino sugar, a solubilizer, a buffer, and an organic acid.

The invention relates to the technical field of pharmaceutical analysis, in particular to a method for detecting bromoacetoacetanilide and aniline in a rebamipide tablet, impurities are detected by using a liquid chromatography-mass spectrometry technology, adopting an Agilent C18 chromatographic column and taking a 0.1% formic acid solution-acetonitrile mixed solution as a mobile phase, and the content of the impurities is calculated by adopting an external standard method. According to the method for detecting bromoacetoacetanilide and aniline in the rebamipide tablet, a liquid chromatography-mass spectrometry technology is adopted, quantitative detection of bromoacetoacetanilide and aniline is achieved, and the method is high in specificity, high in sensitivity, good in stability, high in sensitivity, high in sensitivity and high in reliability. According to the method, the content of bromoacetoacetanilide and aniline in the rebamipide tablet can be effectively measured, the quality control of the rebamipide tablet is perfected, the product quality is controllable, and the safety and effectiveness of the product are ensured.

This invention relates to the field of pharmaceutical formulation technology, and discloses a rebamipide tablet formulation and its preparation process. The formulation, by weight, mainly comprises 100 parts rebamipide, 5 to 15 parts L-arginine, 2 to 8 parts poloxamer 188, 10 to 20 parts hydroxypropyl cellulose, and excipients such as low-substituted hydroxypropyl cellulose and microcrystalline cellulose. The preparation process includes: preparing a composite binder solution containing L-arginine, poloxamer 188, and hydroxypropyl cellulose at 10°C to 15°C; adding rebamipide and cold-curing to obtain a suspension; subsequently, during fluidized bed granulation, by adjusting the absolute humidity and temperature of the inlet air in stages, sequentially performing high-humidity delayed drying and spreading followed by dehumidification and temperature-increasing curing. This invention prevents hydrophobic drug agglomeration and nozzle clogging through low-temperature processing; the in-situ crystallization of L-arginine creates a weakly alkaline microenvironment, significantly improving the drug dissolution rate in acidic media; and achieving high granulation yield and batch-to-batch uniformity of content.

The present invention relates to an ophthalmic composition comprising rebamipide as an active ingredient, and comprising polyoxyl 40 stearate and hydroxypropylmethylcellulose as solubilizers in order to improve the stability of the active ingredient. In addition, the present invention relates to an ophthalmic composition further comprising at least one selected from the group consisting of poloxamer and povidone, and thus is to be administered twice a day or three times a day by delaying the release of rebamipide.

The invention relates to the technical field of chemical synthesis, and particularly discloses a method for synthesizing a rebamipide intermediate through a one-pot method. According to the method, after the condensation reaction is finished, the alcohol solvent in the system is immediately removed, so that the superposition expansion effect of solvent steam and bubbles during subsequent carbon dioxide release is avoided, and the blasting boiling phenomenon can be obviously reduced; the problem that the low-temperature decarboxylation efficiency is low is solved by means of the catalytic action of SBA-15-SO3H subsequently, CO2 is slowly escaped in a boiling-free and solvent-interference-free environment, the explosion boiling problem is avoided, the industrial production stability is guaranteed, SBA-15-SO3H can be recycled, the material cost is reduced, and the method is suitable for industrial production. A safe, efficient, economical and sustainable solution is provided for industrial production of the rebamipide intermediate, and the method has a relatively high application prospect.

The invention belongs to the technical field of pharmaceutical preparations, and relates to a rebamipide tablet and a preparation method thereof. The rebamipide tablet comprises rebamipide, at least one penetration enhancer and at least one biological adhesive, and the penetration enhancer and the biological adhesive are added to effectively promote penetration and absorption of rebamipide in gastrointestinal tracts, so that the bioavailability is improved. The rebamipide tablet is simple in preparation process, high in dissolution rate, good in dissolution uniformity and suitable for industrial mass production.