12 results about "Olmesartan" patented technology

The application discloses an olmesartan medoxomil and amlodipine besylate pharmaceutical composition and a preparation method thereof, and belongs to the technical field of medicines. The olmesartan medoxomil and amlodipine besylate pharmaceutical composition takes olmesartan medoxomil and amlodipine besylate as active ingredients, and is prepared into antihypertensive tablets by being matched with a disintegrant, a filler and a lubricant; wherein the filler is a mixture of pre-gelatinized starch and a co-processed product of microcrystalline cellulose and colloidal silicon dioxide. The preparation method adopts a direct compression process, and sequentially comprises the steps of mixing, whole-granulating, twice mixing, lubricating, tabletting and stomach-soluble film coating, and is simple in process and suitable for industrialized scale-up production. The application effectively solves the problem of low dissolution rate of the existing olmesartan medoxomil and amlodipine besylate tablets, and the prepared tablets have the advantages of high dissolution rate, similar dissolution curve to commercial preparations, high bioavailability, stable quality and good clinical application value.

The invention discloses an olmesartan medoxomil pharmaceutical co-crystal as well as a preparation, a preparation method and application thereof. The co-crystal is formed by olmesartan medoxomil and a specific co-crystal forming agent through intermolecular force. The invention also particularly provides a compound preparation containing the olmesartan medoxomil pharmaceutical co-crystal and hydrochlorothiazide. Through the eutectic technology, the invention fundamentally overcomes the inherent defects of low solubility and slow dissolution of olmesartan medoxomil as a BCS II drug. Experiments show that the preparation disclosed by the invention can realize rapid and complete drug release in vitro (the dissolution rate within 30 minutes is greater than or equal to 98%), the relative bioavailability of olmesartan in vivo can be improved by at least 180% compared with that of a reference preparation, and meanwhile, the eutectic structure ensures that the preparation has excellent chemical stability under an accelerated test condition. The invention provides an innovative solution for the development of an efficient and stable olmesartan medoxomil preparation.

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).

This invention provides a method for synthesizing triphenylmethylolmesartan medoxomil, an intermediate of olmesartan medoxomil. The method includes hydrolyzing compound 2 in a toluene / C1-C4 lower alcohol mixed solvent under the action of an alkali to obtain a synthesis solution of an intermediate sodium salt; adding a carbonate and a phase transfer catalyst to the synthesis solution of the intermediate sodium salt to carry out a condensation reaction to obtain triphenylmethylolmesartan medoxomil. This invention effectively controls the content of impurity A in the product by using a toluene / C1-C4 lower alcohol mixed solvent system and inhibiting the high-temperature elimination reaction of hydroxyl groups by a protic alcohol solvent. This invention has a short production cycle, a simple process, and does not require changing or adding new solvents during the process, facilitating solvent recovery and reuse in industrial production and effectively reducing production costs. The synthesis method of triphenylmethylolmesartan medoxomil described in this invention has a high overall yield, high production efficiency, simple product purification, and good quality control.

The invention discloses a three-compound composition of olmesartan medoxomil, amlodipine besylate and hydrochlorothiazide and a preparation method of the three-compound composition. The three-compound preparation comprises three active ingredients of olmesartan medoxomil, amlodipine besylate and hydrochlorothiazide, the auxiliary materials comprise pregelatinized starch, silicified microcrystalline cellulose, cross-linked carboxymethyl cellulose, polylactic acid spray-dried powder, tocopherol and the like; an olmesartan medoxomil, amlodipine and hydrochlorothiazide tablet obtained after coating operation of the olmesartan medoxomil, amlodipine and hydrochlorothiazide three-compound composition is stable in dissolution, consistent with an original product, very smooth in surface, free of dents and more stable in quality.

The invention relates to the technical field of drug synthesis equipment, in particular to an olmesartan medoxomil phosgene substitution type acylation reaction system, which comprises a reaction container, a reaction kettle, a reaction kettle and a control system, the triphosgene adding device is connected with the reaction container and is used for quantitatively adding triphosgene into the reaction container; the solvent conveying unit is connected with the reaction container and is used for pumping a solvent into the reaction container; the mixed solution feeding unit is connected with the reaction container and is used for slowly adding a mixed solution of 3-hydroxybutanone and a solvent into the reaction container; the temperature control module is connected with the reaction container and is used for accurately controlling the reaction temperature in the reaction container; and the pH adjusting and quenching unit is connected with the reaction container. According to the invention, the triphosgene adding device and the closed system are adopted to completely replace highly toxic gas phosgene, so that major potential safety hazards in the production, storage and transportation processes are fundamentally solved.

A zero-order UV spectrophotometric system for the simultaneous determination of olmesartan medoxomil and metoprolol succinate in tablet form, with analytical wavelengths of approximately 255 nm for olmesartan medoxomil and approximately 215.5 nm for metoprolol succinate using distilled water as solvent.

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 relates to the technical field of pharmacy, and provides a co-amorphous substance containing LBQ657 as well as a preparation method and application of the co-amorphous substance containing LBQ657, the co-amorphous substance containing LBQ657 has a single glass transition temperature and comprises an olmesartan medoxomil-LBQ657 co-amorphous substance or an olmesartan-LBQ657 co-amorphous substance; when the co-amorphous substance containing the LBQ657 is an olmesartan medoxomil-LBQ657 co-amorphous substance, the glass transition temperature Tg1 is 65 + / -5 DEG C; and when the co-amorphous substance containing LBQ657 is an olmesartan-LBQ657 co-amorphous substance, the glass transition temperature Tg2 is 80 + / -5 DEG C. According to the technical scheme, the problems of poor solubility, low inherent dissolution rate and insufficient bioavailability of a traditional drug combination scheme in the related technology are solved.

The application discloses a triple combination of olmesartan medoxomil, amlodipine besylate and hydrochlorothiazide and a preparation method thereof. The triple combination preparation comprises three active ingredients of olmesartan medoxomil, amlodipine besylate and hydrochlorothiazide, and further comprises pre-gelatinized starch, silicified microcrystalline cellulose, cross-linked carboxymethyl cellulose, polylactic acid spray-dried powder and tocopherol as auxiliary materials. The triple combination of olmesartan medoxomil, amlodipine besylate and hydrochlorothiazide is coated to obtain olmesartan medoxomil, amlodipine besylate and hydrochlorothiazide tablets, which have the same dissolution stability as the original research product, a very smooth surface, no indentation and more stable quality.

The invention provides a high-stability and high-bioavailability olmesartan medoxomil tablet and a preparation method thereof, olmesartan medoxomil is coated by a compound with a hydrophobic group and a hydrophilic group at the same time to form an inner hydrophobic-outer hydrophilic composite structure, and a hydrophilic compound is grafted on the outer layer of the composite structure to form the high-stability and high-bioavailability olmesartan medoxomil tablet. The problems that olmesartan medoxomil is easy to crystallize and degrade under high temperature and high humidity, and the bioavailability is low and the olmesartan medoxomil is not easy to store after being prepared into tablets are solved. The preparation method comprises the following steps: granulating by adopting fluidized bed bottom spraying, controlling air inlet temperature, atomizing pressure, spraying rate and material temperature, spraying the main medicine in a clarified solution in a coating form, and granulating; and carrying out vacuum belt type low-temperature drying and tabletting. Compared with the prior art, the olmesartan medoxomil tablet effectively solves the problems that the existing olmesartan medoxomil tablet is low in bioavailability, poor in stability and easy to crystallize and degrade under high temperature and high humidity through the synergistic effect of auxiliary materials and a process, and is suitable for long-term treatment of primary hypertension.

Provided in the present invention is the use of olmesartan medoxomil or a derivative thereof in the preparation of a drug for protecting pancreatic islet β cells, a drug for protecting pancreatic islet β cells against inflammation, a drug for preventing and treating diabetes, and a drug for preventing and treating type 1 diabetes. Further provided in the present invention is the use of a combination therapy of olmesartan medoxomil and sorafenib in the treatment of type 1 diabetes.