13 results about "Irbesartan" patented technology

The invention belongs to the technical field of biological medicines, and particularly relates to application of an angiotensin II receptor antagonist in preparation of a medicine for preventing and treating renal tubular injury caused by triptolide. According to the invention, the upstream key target protein of the TPL-induced renal tubule injury is determined to be HSPA1 through experiments for the first time, and the problem that the key target spot of TPL toxicity is not determined in the prior art is solved. Based on a key target spot of TPL toxicity, through molecular screening and parallel pharmacodynamic verification on various sartan drugs such as irbesartan, losartan, olmesartan and valsartan, it is determined that the angiotensin II receptor antagonist has a general protection effect on TPL toxicity. Wherein the protective efficacy of irbesartan as a preferable embodiment is obviously superior to that of losartan of the same kind (the efficiency slope is 2.451 to 1.584).

The invention discloses application of irbesartan in preparation of a medicine for preventing or treating osteoarthritis, and belongs to the technical field of biological medicine. Osteoarthritis single cell transcriptome data are integrated and analyzed, differential expression genes are screened, and irbesartan is screened by using a relocation method and Mendel randomization analysis to serve as a medicine for treating osteoarthritis; analysis results show that irbesartan can significantly reduce the risk of osteoarthritis. An irbesartan administration experiment is carried out by using a zebra fish bone arthritis model, and the experiment result shows that irbesartan obviously increases the joint gap of anal fins of zebra fish and has an obvious protection effect on articular cartilage; a transcriptome sequencing result shows that irbesartan plays the role by inhibiting the MAPK signal channel. The invention provides the effect of irbesartan in the development of osteoarthritis for the first time, provides a new strategy for prevention and treatment of osteoarthritis, and has a wide application prospect.

The present application relates to a preparation method of an intermediate of an irbesartan isomer, which comprises Step 1: reacting 4-formylphenylboronic acid with o-halobenzonitrile to obtain a compound 2 in the following formula; Step 2: reacting the compound 2 with 1-amino-1-cyclopentanecarboxamide to obtain 1-[2'-cyano-(1,1'-biphenyl)-4-ylmethylamino]cyclopentane-1-carboxamide, the structure of which is shown as a compound 3 in the following formula; reacting 1-[2'-cyano-(1,1'-biphenyl)-4-ylmethylamino]cyclopentane-1-carboxamide with trimethyl orthobutyrate to obtain a compound 4. The present application has the effects of reducing the operation difficulty of preparing the irbesartan isomer and its intermediate and improving the yield. #imgabs0#

The application discloses irbesartan and hydrochlorothiazide tablets and a preparation method thereof. The tablet comprises irbesartan granules and hydrochlorothiazide granules. The irbesartan granules comprise irbesartan, hydroxyphenyl cellulose, glycerophosphoric acid calcium, a disintegrant and a binder. The hydrochlorothiazide granules comprise hydrochlorothiazide, a diluent, a disintegrant and a binder. The tablet can solve the problems of easy agglomeration of irbesartan and hydrochlorothiazide, and difficulty in controlling the content uniformity due to the great difference in the dosage. Meanwhile, the tablet can effectively overcome the poor solubility of irbesartan and hydrochlorothiazide, and good dissolution effect is obtained.

The present invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a pharmaceutical composition containing irbesartan and amlodipine besylate and a preparation method thereof. The pharmaceutical composition comprises an irbesartan layer, an amlodipine besylate layer and a coating layer; the raw materials of the irbesartan layer include irbesartan, croscarmellose sodium and hydroxypropyl cellulose; the raw materials of the amlodipine besylate layer include amlodipine besylate, croscarmellose sodium and hydroxypropyl cellulose; the model of the hydroxypropyl cellulose is HPC-M. The present invention granulates irbesartan with suitable excipients by wet granulation to solve the problems of small bulk density and poor fluidity of irbesartan itself. Granulates amlodipine besylate with suitable excipients by fluidized bed granulation to solve the problems of poor mixing uniformity and low content and improve the stability of the product, and has good application prospects.

The invention discloses a method for recovering an irbesartan intermediate 4 '-((4-oxo-2-propyl-1, 3-diazaspiro [4.4] nonyl-1-ene-3-yl) methyl)-[1, 1'-biphenyl]-2-nitrile from an irbesartan mother solution. According to the method, after the mother liquor is washed with the alkali liquor, crystallization is conducted in ethyl acetate or ethyl alcohol under the low-temperature condition, the irbesartan intermediate is recycled from the irbesartan mother liquor, the obtained product is high in purity and can be directly recycled for synthesis of irbesartan, and the production cost and environmental protection pressure are reduced.

The present invention relates to compositions, systems, and methods for treating a subject with an eye condition (e.g., topically) using a composition comprising an ACE-2 receptor antagonist (also known as Angiotensin II Receptor Blocker or “ARB”) (e.g., losartan, telmisartan, valsartan, olmesartan, candesartan, irbesartan, eprosartan, azilsartan, or losartan metabolite EXP3174). In certain embodiments, the eye condition is selected from: i) a corneal scarring fibrosis, ii) a transforming growth factor beta-induced (TGFBI) corneal dystrophy, iii) a conjunctival fibrotic disease, iv) an intraocular fibrotic disease, and v) a conjunctival bleb scarring and / or shunt encapsulation (e.g., following glaucoma surgery).

The invention provides an irbesartan solid dispersion and a preparation method of a preparation thereof, and belongs to the technical field of pharmaceutical preparations, the irbesartan solid dispersion is prepared from 10-30% by weight of irbesartan, 60-90% by weight of copovidone and 5-15% by weight of a plasticizer by adopting a twin-screw hot melt extrusion process, and the irbesartan solid dispersion is prepared from the preparation method of the irbesartan solid dispersion and the preparation of the irbesartan solid dispersion. And mixing the solid dispersion with a filling agent, a disintegrating agent and a lubricating agent which are conventional in pharmaceutics to prepare irbesartan unilateral tablets, or additionally adding hydrochlorothiazide and mixing to prepare irbesartan compound tablets. According to the irbesartan tablet and the preparation method thereof, irbesartan is prepared into the solid dispersion and then prepared into the tablet, so that the electrostatic agglomeration of irbesartan is improved to improve the mixing uniformity of the preparation, the dissolution performance of irbesartan is remarkably improved, and the bioavailability of the medicine is improved; therefore, the problems of insufficient subsequent mixing uniformity caused by electrostatic agglomeration in irbesartan preparation preparation and poor dissolution performance and low bioavailability caused by low solubility are effectively solved.

The invention belongs to the technical field of pharmaceutical analysis, and particularly relates to a method for determining related substances of irbesartan and levoamlodipine compound tablets. According to the method, high performance liquid chromatography is adopted for detection, a chromatographic column is YMC-Triart C18, a 0.55% phosphoric acid aqueous solution with the pH value of 3.0-3.5 is used as a mobile phase A, methanol is used as a mobile phase B, and gradient elution is performed. According to the method, known impurities and various unknown impurities including amlodipine impurities A, B, D, E, F, G and H, irbesartan impurities I and the like can be measured under the same chromatographic condition, the separation degree of each chromatographic peak and a main peak or other impurity peaks meets the requirements, the peak shape is good, the method is high in specificity, good in reproducibility and high in accuracy, the sensitivity meets the analysis and detection requirements, and the method is suitable for industrial production. And a reliable detection method is provided for related substances of the irbesartan-levoamlodipine compound.

The invention provides a novel preparation method of an irbesartan composition, and belongs to the technical field of pharmaceutical preparations, the irbesartan composition comprises irbesartan and silicon dioxide, the irbesartan and the silicon dioxide are subjected to wet grinding in a planetary ball mill, and the mass ratio of the irbesartan to the silicon dioxide is (50: 1)-(100: 1); the particle size of irbesartan is not greater than 50 microns; the composition can also comprise one or more of a filler, a disintegrating agent, an adhesive, a lubricant and a flow aid. According to the irbesartan composition, amorphous silicon dioxide is used as a hydrophilic porous carrier to increase the specific surface area of a medicine and promote the wettability of the medicine, and irbesartan is ground into nano-scale particle size by adopting a wet grinding process and is embedded into silicon dioxide, so that the irbesartan composition is prepared. According to the irbesartan tablet, the dissolution rate and oral bioavailability of irbesartan under a low-acid condition can be remarkably improved, an organic solvent and a solubilizer do not need to be used, the medicine storage stability can be improved, the raw material cost is low, the compatibility of existing production equipment is good, and the irbesartan tablet is suitable for industrial mass production.

The application provides a preparation method of an intermediate of irbesartan, adopts DMTMM as a condensing agent and TEMPO / sodium hypochlorite as an oxidizing agent, saves production cost, greatly reduces the security risk possibly introduced in the drug production process, and is more simple, safer, higher in yield, higher in product purity and more suitable for industrial production compared with the prior art.

This invention provides a method for treating irbesartan production wastewater, the main steps of which are: (1) removing irbesartan-related substances from the wastewater; (2) removing residual solvents from the wastewater using a stripping tower; and (3) introducing the remaining wastewater into a biochemical system for degradation. This method can avoid the precipitation of solids that may occur during the treatment of irbesartan production wastewater, and can effectively reduce the COD value at the end of the wastewater treatment, thus reducing the difficulty of treating irbesartan production wastewater.

The invention discloses irbesartan granules and a preparation method thereof. The method comprises the following steps: pulping an irbesartan raw material medicine with an organic solvent or a mixed solution of the organic solvent and water, centrifuging or filtering to obtain a wet product, drying the wet product for the first time, crushing and granulating the wet product for the first time, drying the wet product for the second time, and optionally crushing and granulating the wet product for the second time to obtain irbesartan spherical particles. In addition, the invention also provides a pharmaceutical composition containing the particle.