20 results about "Ilaprazole" patented technology

The invention relates to the technical field of biological medicine, in particular to an ilaprazole enteric-coated tablet and a preparation method thereof. The ilaprazole enteric-coated tablet sequentially comprises a tablet core, an isolating layer and an enteric-coated layer from inside to outside, the tablet core at least comprises an active ingredient ilaprazole or a pharmaceutically acceptable salt thereof, the particle size D90 of the ilaprazole or the pharmaceutically acceptable salt thereof is less than or equal to 10 microns, and a solvent used in a coating process of the isolating layer is water. By controlling the particle size D90 of the ilaprazole to be less than or equal to 10 microns and controlling the preparation method of the tablet core, the tablet core with relatively good content uniformity and appearance state is prepared, the problem that the tablet core is easy to generate spots is solved, and the problem that the intestinal tract is stimulated by over-high local drug concentration when the ilaprazole enteric-coated tablet is released and dissolved out is avoided. In the coating process of the isolating layer, solvent purified water is used for replacing traditional ethanol, so that the problems of pressure for removing an organic solvent in the preparation process of the tablet and environmental pollution in the preparation process are avoided under the condition of ensuring the quality of the tablet.

The invention discloses a method for detecting the dissolution rate of ilaprazole. The invention provides a method for detecting the dissolution rate of ilaprazole. The dissolution rate of ilaprazole is detected by adopting an ultraviolet-visible spectrophotometric method. The detection method disclosed by the invention has the advantages of simplicity and convenience in operation, good repeatability, more stable dissolution rate data, better dissolution amount, convenience and rapidness, easiness in automation, more accurate and stable detection result and more suitability for industrial production.

The invention belongs to the technical field of injection production processes, and particularly relates to a famotidine injection and a preparation method thereof. According to the famotidine injection disclosed by the invention, dendrobium nobile is fermented by using lactic acid bacteria ATCC 8008 and saccharomycetes ATCC 918, and chlorogenic acid and ilaprazole are added to prepare the famotidine injection. According to the method for fermenting by using the lactic acid bacteria ATCC 8008 and the saccharomycetes ATCC 918, not only can the curative effect of famotidine be improved, but also the effect of the dendrobium is enhanced due to the modification of the dendrobium, and more beneficial substances in the dendrobium are obtained. The Chinese yam and the lotus seeds used in the famotidine have good body building effects, have the advantages of tonifying the spleen and nourishing the stomach and can also enter the heart and the spleen, and the medicine effect of the prepared famotidine is enhanced. The famotidine prepared by the invention can be used for treating peptic ulcer, and has a great development prospect in the field of first aid.

The invention discloses a novel ilaprazole crystal form. The X-ray diffraction spectrum of crystal powder of the crystal form has the following characteristic peaks expressed by angle 2 theta: 6.7 degrees + / -0.2 degrees, 6.9 degrees + / -0.2 degrees, 12.6 degrees + / -0.2 degrees, 15.8 degrees + / -0.2 degrees, 18.1 degrees + / -0.2 degrees, 21.2 degrees + / -0.2 degrees, 22.1 degrees + / -0.2 degrees, 23.6 degrees + / -0.2 degrees and 25.6 degrees + / -0.2 degrees. The invention also discloses a preparation method of the novel ilaprazole crystal form, which comprises the following steps: dissolving an ilaprazole crude product in a mixed solution of dichloromethane, methanol and triethylamine, decolorizing with activated carbon, adding isopropyl ether for crystallization, centrifuging the obtained solid, and pulping with ethanol and n-heptane. The crystal form of ilaprazole can exist stably and is not prone to moisture absorption, and the crystal form is good in thermal stability, facilitates purification of ilaprazole and is beneficial to storage.

The present application provides a method for quantitatively analyzing acid-suppressing drugs by a high-performance liquid chromatography-tandem mass spectrometry device, comprising: preparing a sample solution containing the acid-suppressing drug; injecting the sample solution into the high-performance liquid chromatography-tandem mass spectrometry device to obtain a mass chromatogram; and quantitatively analyzing the acid-suppressing drug using an internal standard method according to the mass chromatogram, wherein the acid-suppressing drug is selected from: esomeprazole, rabeprazole, ilaprazole, lansoprazole, pantoprazole and vonoprazan fumarate; using a mixed mobile phase consisting of mobile phase A and mobile phase B for gradient elution in the high-performance liquid chromatography, wherein mobile phase A is an acetonitrile solution containing formic acid or a water-acetonitrile mixture containing ammonia and ammonium acetate (water: acetonitrile volume ratio: 1:99-10:90); and mobile phase B is selected from an aqueous solution containing ammonium acetate, an aqueous solution containing formic acid and ammonium acetate, an aqueous solution containing ammonia and ammonium acetate, and an aqueous solution containing ammonia and ammonium formate.

The invention discloses a preparation method of an ilaprazole degradation impurity A, and belongs to the field of medicine preparation. According to the method, the ilaprazole degradation impurity A is obtained through high-yield conversion of ilaprazole under the catalysis of copper trifluoromethanesulfonate, and the compound can be used for medicine research of ilaprazole bulk drugs or related preparations.

The invention relates to a preparation method of a high-purity ilaprazole sodium anhydride crystal form (C crystal). The ilaprazole sodium anhydride crystal form (C crystal) prepared by the invention is high in purity, low in impurity content and low in solvent residue, and meets the requirements of medicinal bulk drugs. The preparation method disclosed by the invention is simple, simple and convenient to operate, small in solvent dosage, mild in reaction condition, easy to control and low in preparation cost; and the target product crystal form can be obtained very definitely with good reproducibility.

The invention discloses a method for detecting related substances in ilaprazole, which comprises the following steps: high performance liquid chromatography is adopted, the test conditions are as follows: an octadecylsilane chemically bonded silica chromatographic column is adopted, eluents are a mobile phase A and a mobile phase B for online mixed gradient elution, the mobile phase A is a solution of a phosphate solution and an organic solvent, the mobile phase B is a solution of a phosphate solution and an organic solvent, and the mobile phase C is an octadecylsilane chemically bonded silica chromatographic column. The organic solvent is an alcohol solvent; the mobile phase A is an organic solvent, the mobile phase B is an alcohol solvent, and the related substances are IM-A, IM-C, IM-E and IM-O. According to the method, the ilaprazole raw material medicine and the four impurities can be rapidly and effectively separated under the same chromatographic condition, baseline separation can be achieved between a main peak and adjacent impurity peaks and between the impurity peaks, and the minimum separation degree reaches 5.6. The analysis method disclosed by the invention is strong in specificity, high in sensitivity, good in precision, high in accuracy and good in separation degree, the quality of an ilaprazole product can be effectively controlled, and the effectiveness and the safety of a medicine are finally ensured.

The invention belongs to the technical field of tumor treatment medicines, and particularly discloses a novel combined therapy for treating drug-resistant breast cancer by using abelsilib and ilaprazole. The new application of the ilaprazole in enhancing the drug-resistant breast cancer treatment effect of the abelsiril is found for the first time by applying the abelsiril and the ilaprazole in combination or synergistically in preparing the drug for treating the drug-resistant breast cancer. Compared with the single use of the abesilib, the combined application of the ilaprazole can significantly inhibit the growth and proliferation of the abesilib drug-resistant breast cancer cells, and shows a better anti-tumor effect. Therefore, the invention not only provides a theoretical basis for the application of ilaprazole in breast cancer treatment, but also provides a new treatment strategy and means for clinically overcoming the abelsiril drug-resistant breast cancer.

The present invention relates to a pharmaceutical composition containing ilaprazole or a salt thereof, and a preparation method therefor. The pharmaceutical composition contains or consists of ilaprazole or a salt thereof, and a ilaprazole derivative, wherein the amount of the ilaprazole derivative in the pharmaceutical composition is not higher than 1.3 wt % (less than or equal to 1.3 wt %). The composition can be used for treating peptic ulcer bleeding and stress ulcer and preventing upper gastrointestinal hemorrhage caused by severe diseases.

The present invention relates to an oral immediate-release formulation comprising ilaprazole with improved stability as an active ingredient and a method for preparing same, wherein the present invention relates to an oral immediate-release formulation and a method for preparing same, the oral immediate-release formulation comprising ilaprazole and a stabilizer in an inner core portion thereof and an antacid in an outer layer portion thereof, in which the oral immediate-release formulation has improved compounding stability by suppressing contact between the inner core portion and the outer layer portion through coating on the inner core portion, has excellent stability by minimizing the amount of related substances generated, and has a fast drug effect (the time to reach maximum blood concentration (Tmax) ranges from 0.3 hours to 0.8 hours) and excellent stability, through the rapid antacid effect of the antacid.

The invention belongs to the technical field of medicine and chemical production, and particularly relates to a method for preparing ilaprazole sodium by a continuous flow method. The preparation method comprises the following steps: (1) adding ilaprazole thioether, a sodium hydroxide solution and an iron catalyst into acetone to obtain ilaprazole thioether alkali liquor; (2) respectively introducing the ilaprazole thioether alkali liquor and oxygen into the tubular reactor through a flow meter for reaction; and (3) evaporating the organic phase obtained in the step (2) to dryness, adding ethyl acetate, pulping, filtering and drying to obtain the ilaprazole sodium solid. A continuous flow reaction process is adopted to replace a traditional kettle type process, oxygen is adopted as an oxidizing agent for oxidation reaction, conditions are mild, process parameters are easy to control and adjust, the safety is improved, the reaction time is greatly shortened, the reaction heat transfer effect is good, the whole experimental operation is simpler and more convenient, and the method is suitable for industrial continuous production.

The invention discloses an ilaprazole sodium freeze-dried preparation as well as a preparation method and application thereof. The invention provides an ilaprazole sodium freeze-dried preparation which comprises the following components: ilaprazole sodium, an excipient, cycleanine tetraacetic acid and a pH (Potential of Hydrogen) regulator, and does not contain ethylenediamine tetraacetic acid. The ilaprazole sodium freeze-dried preparation is good in stability, lower in impurity content, good in solubility, safer, simple to prepare and suitable for industrial production.

The application provides a preparation method of crystalline form B of ilaprazole. The application provides a preparation method of crystalline form B of ilaprazole, which comprises the following steps: mixing a solution or slurry of ilaprazole raw materials and a good solvent with an anti-solvent, and crystallizing to obtain the crystalline form B of ilaprazole. The preparation method of the application has the advantages of good stability, high yield, good purity, low solvent residue, compliance with the standard of raw materials, and suitability for industrial production.

The invention provides an ilaprazole freeze-dried enteric-coated tablet and a preparation method thereof. The ilaprazole freeze-dried enteric-coated tablet comprises a plain tablet core and a coating layer, the plain tablet core comprises ilaprazole, a disintegrating agent, a freeze-drying protective agent and a medicinal excipient, the plain tablet core subjected to freeze-drying treatment forms a loose porous structure, and the moisture content of the plain tablet core is 1t; 5%. According to the ilaprazole freeze-dried enteric-coated tablet, the plain tablet core subjected to freeze drying treatment forms a loose porous structure, and the moisture content of the plain tablet core is 1t; the long-term storage stability of the tablet core can be improved, and the growth of related substances in the long-term storage process is effectively avoided, so that the drug effect and the drug safety of ilaprazole are improved; the quick release of the tablet core in the intestinal tract can be accelerated, and the absorption efficiency of the intestinal tract on ilaprazole is improved, so that the curative effect of the medicine is enhanced.

The invention relates to a preparation method of an ilaprazole crystal form B. The preparation method comprises the following steps: dissolving ilaprazole sodium salt in a mixed solution of an organic solvent and water, adding a certain amount of acid for dissociation, separating out salt, adding a seed crystal for crystallization, pulping the obtained solid with water, and washing with leacheate to obtain the target crystal ilaprazole crystal form B. A single solvent is used for crystallization, the method has the advantage of low cost, distillation is not needed, the working hours and energy consumption are shortened, and the operation process is simplified; the use of dangerous solvent ethers is avoided, and industrialization is easy; the problem that the residual solvent is easy to exceed the standard is solved, and the purity and yield of the target product are improved.

The invention is applicable to the technical field of drug synthesis, and provides a preparation method of ilaprazole, which comprises the following steps: adding ilaprazole sodium into a mixed solution of purified water and triethylamine to obtain a first mixed solution; adding dichloromethane and a tartaric acid aqueous solution into the first mixed solution for free extraction, and collecting an organic phase; washing the obtained organic phase, adding purified water and n-heptane for crystallization treatment, and filtering and drying to obtain ilaprazole. The process is simple and easy to operate, ilaprazole sodium is dissolved in a mixed solution of purified water and triethylamine, dichloromethane and a tartaric acid aqueous solution are added for free extraction, purified water and n-heptane are added into an obtained organic phase for crystallization treatment, and ilaprazole is obtained. Tartaric acid is creatively used for acidification, water and n-heptane are added for two-phase crystallization during crystallization, firing residues of the product are reduced on the premise that the yield is improved, and the obtained product is high in purity and excellent in color.

The present disclosure provides a kind of ilaprazole freeze-dried enteric-coated tablets and its preparation method.The above-mentioned ilaprazole freeze-dried enteric-coated tablets include tablet core and coating layer, tablet core includes ilaprazole, tablet core also includes disintegrating agent, freeze-drying protective agent and pharmaceutical excipient, the tablet core after freeze-drying treatment is formed with loose porous structure, and the moisture content of tablet core is <5%.The above-mentioned ilaprazole freeze-dried enteric-coated tablets, since the tablet core after freeze-drying treatment is formed with loose porous structure, and the moisture content of tablet core is <5%, both can improve the long-term storage stability of tablet core, effectively avoid the increase of related substances in long-term storage process, to improve the efficacy of ilaprazole and the safety of drug;It can also speed up the rapid release of tablet core in the intestine, improve the absorption efficiency of ilaprazole in the intestine, to enhance the curative effect of drug.

The application discloses a preparation method of ilaprazole, and belongs to the field of drug synthesis. The ilaprazole is synthesized from 5-(1H-pyrrol-1-yl)-2-mercaptobenzimidazole and 3-methyl-4-methoxy-2-chloromethylpyridine hydrochloride through two-step reaction. The preparation method is mild in process condition, good in quality, high in yield, and suitable for large-scale production.

The present invention relates to a pharmaceutical combination preparation comprising ilaprazole, an antacid, and an alkalizing agent and, more specifically, to a pharmaceutical combination preparation and a method for preparing same, wherein decomposition of ilaprazole in the stomach is prevented without enteric coating to improve stability, thereby increasing bioavailability, and the quality and productivity of pharmaceutical products are improved due to uncomplicated manufacturing processes and excellent storage stability of the preparation.