60 results about "Empagliflozin" patented technology

The present invention relates to a film coated tablet comprising empagliflozin and metformin hydrochloride, wherein comprising at least one binder which is hydroxypropyl methyl cellulose or hydroxypropyl cellulose or mixtures thereof, the tablet provides pharmacotechnical properties and the desired dissolution profile. The present invention also relates to a simple, rapid, cost effective, time-saving and industrially convenient method of preparing the tablet.

This application provides a method for improving the mixing uniformity of a compound preparation of metformin and empagliflozin, belonging to the field of pharmaceutical technology. The invention provides a dry granulation and ultrasonic mixing method, which utilizes airflow pulverization, ultrasonically assisted vertical axis planetary mixer mixing, and forced sieving technology to enhance the process. The method utilizes the synergistic effect of ultrasound and the mixer to shorten mixing time, enhance mixing efficiency, and significantly improve the uniformity and dissolution rate of the preparation. This process is short, simple to operate, and easily controllable, making it suitable for large-scale production.

The invention provides application of a sodium-glucose co-transporter 2 inhibitor in preparation of a medicine for preventing or treating senescence. In an aging animal model, it is found that the sodium-glucose co-transporter 2 inhibitor empagliflozin can improve heart aging, enhance heart functions caused by aging and increase the ejection fraction of left ventricle; meanwhile, the memory function caused by senescence can be improved, and the expression levels of senescence factors p16, p21 and p53 are improved. The sodium-glucose co-transporter 2 inhibitor empagliflozin has a prospect of being developed as an anti-aging drug.

The present application relates to a kind of asymmetric catalytic hydrogenation synthesis new method of (S)‑3‑(4‑(5‑bromo / iodine‑2 chlorobenzyl) phenoxy) tetrahydrofuran in engletin intermediate.This method is prepared by acylation, reduction from simple raw material, and formula a-1 compound is obtained.In which formula a-1 compound and formula a compound, through asymmetric catalytic hydrogenation process, and intramolecular dehydration ring-closing reaction synthesis (S)‑3‑(4‑(5‑bromo / iodine‑2 chlorobenzyl) phenoxy) tetrahydrofuran in engletin intermediate.The raw material of this synthesis method is easy to obtain, simple operation, suitable for industrial amplification.

The invention discloses a preparation process of empagliflozin, which comprises the following steps: by taking D-(+)-gluconic acid delta-lactone as a raw material, carrying out condensation reaction on D-(+)-gluconic acid delta-lactone and (R)-3-(4-(5-bromo-2-chlorobenzyl) phenoxy) tetrahydrofuran through a protective reagent under the action of a Grignard reagent; carrying out protonation reaction under the action of sulfuric acid to obtain an intermediate; and removing a protecting group through organic acid to obtain empagliflozin. The reaction route has the advantages of few steps, high selectivity, few byproducts, high product yield, easiness in product separation, convenience in operation, suitability for large-scale industrial production and the like, and is suitable for large-scale popularization and application.

The present invention relates to a pharmaceutical composition for preventing or treating metabolic abnormality-related fatty liver diseases containing empagliflozin and telmisartan. The pharmaceutical composition has no issues of drug-drug interaction and exhibits a synergistic effect in the prevention or treatment of metabolic dysfunction-related fatty liver disease, thereby allowing effective application to patients with metabolic dysfunction-related fatty liver disease.

The present invention discloses a pharmaceutical combination formulation comprising sitagliptin and empagliflozin and a preparation method thereof.

The present invention belongs to the field of pharmaceutical synthesis technology and specifically relates to a method for preparing an empagliflozin intermediate compound. The method uses 2-chloro-5-iodobenzyl bromide and (S)-3-(4-bromophenoxy)tetrahydrofuran as starting materials, reacting them under the catalysis of magnesium and 2,2,6,6-tetramethylpiperidinyl oxide to produce the empagliflozin intermediate compound (S)-3-(4-(2-chloro-5-iodophenyl)phenoxy)tetrahydrofuran. This process eliminates the need for n-butyl lithium, has a short synthetic route, is simple to operate, and is more suitable for large-scale industrial production.

The present application relates to the biomedical field, specifically relates to a glucose-responsive empagliflozin microneedle delivery system and application thereof.The glucose-responsive empagliflozin microneedle delivery system of the present application is characterized in that the microneedle delivery system is a microneedle patch, comprising a substrate and a microneedle array arranged on the substrate; the microneedle in the microneedle array contains glucose-responsive empagliflozin nanoparticles CB@E or PCB@E.The present application has the following technical effects: the empagliflozin nanoparticles of the present application have precise glucose-responsive drug release performance.The microneedle drug delivery system of the present application has the effect of long-term control of blood glucose.In a T2DM rat model, MN@CB@E exhibits long-acting blood glucose control effect, can reduce blood glucose to normal level within 4h and maintain for 24h, and the hypoglycemic duration is significantly better than that of subcutaneous injection of free empagliflozin (only maintains for 6h), and there is no risk of hypoglycemia after administration to healthy rats.

The present invention belongs to the field of pharmaceutical synthesis technology, and specifically relates to a one-pot method for preparing empagliflozin. The preparation method comprises the following steps: using 4-(5-bromo-2-chlorobenzyl)phenol as a starting material, nucleophilic addition reaction with sugar occurs under the action of a Grignard reagent; then adding a methanolic solution of hydrogen chloride to undergo methyl etherification; then undergoing a nucleophilic substitution reaction with (R)-3-tetrahydrofuryl p-toluenesulfonate; and finally adding Et3SiH3 / AlCl3 to undergo a reduction reaction to obtain a crude product of empagliflozin. The one-pot method for preparing a crude product of empagliflozin provided by the present invention does not require the removal of intermediates during the reaction process, thus avoiding centrifugation and drying operations, and greatly shortening the production cycle. The preparation method is simple to operate, easy to operate in post-processing, and easy to recover the solvent; and it greatly improves production capacity. The purity of the refined finished product is above 99.5%, the total product yield can reach 40%, impurities are easy to control, and it is suitable for industrial production.

The invention provides a pharmaceutical composition. The pharmaceutical composition is prepared from amlodipine, empagliflozin, folic acid substances and a pharmaceutically acceptable carrier, wherein the amlodipine, the empagliflozin and the folic acid substances are in medicinal effective dose. The invention also provides application of the pharmaceutical composition in preparation of medicines for treating lower limb artery occlusion diseases.

The invention discloses a pharmaceutical composition for reducing blood sugar and application thereof, and belongs to the technical field of preparation of drugs for reducing blood sugar. The pharmaceutical composition is prepared from the following components in parts by weight: 5 to 7 parts of empagliflozin, 30 to 40 parts of cortex cinnamomi extract, 500 to 700 parts of metformin, 60 to 80 parts of microcrystalline cellulose, 10 to 15 parts of polyvinylpolypyrrolidone, 100 to 120 parts of HPMC K100M, 50 to 60 parts of ethyl cellulose, 40 to 50 parts of Eudragit FS30D, 40 to 50 parts of soybean phospholipid and 10 to 20 parts of poloxamer 188. The composition is applied to preparation of sustained-release tablets for reducing blood sugar, and can reduce loss of islet cells and protect kidney functions and gastric mucosa.

To provide methods for treating chronic heart failure, in particular in patients with HFrEF or HFpEF, with a good efficacy, with regard to disease modifying properties and with regard to reduction of risk of mortality or hospitalization while at the same time showing a good safety profile.SOLUTION: The present invention relates to methods for preventing or treating acute or chronic heart failure and for reducing the risk of cardiovascular death, hospitalization for heart failure and other conditions in patients with preserved or reduced ejection fraction by administering empagliflozin to the patient.SELECTED DRAWING: None

The present invention relates to a pharmaceutical combination preparation, which comprises all of ezetimibe, rosuvastatin and empagliflozin as active ingredients, and thus can be administered as a single drug, and not through co-administration, in the simultaneous treatment of dyslipidemia and diabetes, thereby increasing patient dosing convenience, minimally affecting dissolution between drugs, ensuring biological equivalence, and providing excellent stability of the active ingredients.

1. The name of the design product: packaging box (empagliflozin tablets). 2. The use of the design product: for product packaging. 3. The design points of the design product: in the combination of shape and pattern. 4. The picture or photo that best indicates the design points: perspective view 1.

To provide a new pharmaceutical composition containing empagliflozin in which the solubility of empagliflozin in water is relatively high.SOLUTION: The present invention includes, for example, a pharmaceutical composition mainly comprising empagliflozin and a polymeric carrier, wherein the content ratio of empagliflozin to the polymeric carrier is within the range of 1:1 to 1:40 (empagliflozin: polymeric carrier) by mass, and empagliflozin is solid-dispersed in an amorphous state.SELECTED DRAWING: Figure 1

The application discloses a chiral synthesis process of an empagliflozin intermediate, and the process comprises the following steps: dissolving a reactant I in an organic solvent to perform chiral oxidation to alcohol, adding a protecting agent to protect, further reducing a carbonyl in an ester group in a product, and then performing deprotection to obtain a target product, a chiral intermediate compound (S)-(+) 3-hydroxytetrahydrofuran. The application has the advantages that: the chiral alcohol compound is obtained through the oxidation reaction of the relatively cheap raw material under the action of the chiral reagent, the chiral product can be obtained at a high yield, the reaction selectivity is good, the yield is high, the loss of the raw material is reduced, the expensive chiral compound (S)-(+) 3-hydroxytetrahydrofuran is avoided to purchase, the production cost is effectively reduced, meanwhile, the steps are simple, the operation is easy, the raw material is easy to obtain, the product is easy to process, and the application is suitable for industrial large-scale production.

The invention relates to an empagliflozin tablet and a preparation method thereof. The empagliflozin tablet comprises an empagliflozin tablet and a coating layer, the coating layer contains any one or a combination of at least two pigments selected from amaranth, sunset yellow, lemon yellow, new red, allura red or carmine. The pigment is used for replacing titanium dioxide and / or iron oxide yellow in the gastric-soluble film coating of the empagliflozin tablet, so that the safety and the quality of the gastric-soluble film coating are improved. The empagliflozin tablet prepared by the method has a relatively good dissolution behavior, meets the requirement of consistency of imitated medicines, has excellent stability, and is safer and more reliable.

A combined pharmaceutical composition and a formulated pharmaceutical composition comprising empagliflozin or a pharmaceutically acceptable salt thereof and a small molecule GLP-1 receptor agonist or a pharmaceutically acceptable salt thereof, and use of the compositions in the treatment of metabolic diseases and / or kidney diseases.

Provided herein are compositions and methods for reducing or preventing ovarian aging comprising: administering to a subject in need of a reduction or prevention of ovarian aging an effective amount of an SGLT2 antagonist. Examples of SGLT2 antagonists include canagliflozin, bexagliflozin, dapagliflozin, empagliflozin, ertugliflozin, sotagliflozin, phlorizin, or combinations thereof.

A pharmaceutical composition comprising an endothelin A (ETA) receptor antagonist and an SGLT-2 inhibitor and use thereof in the preparation of a drug for preventing and / or treating a disease selected from nephropathy and hypertension, wherein the ETA receptor antagonist is a compound of formula (I) or a salt thereof, and the SGLT-2 inhibitor is selected from dapagliflozin, empagliflozin, canagliflozin, and ertugliflozin, and salts thereof. (I)

The invention belongs to the field of pharmaceutical chemicals, and particularly relates to an amorphous substance of an empagliflozin intermediate and a preparation method thereof, the synthetic route is that the obtained amorphous substance of the empagliflozin intermediate is high in purity, good in stability and easy to store, and the preparation method is simple to operate and suitable for industrial production.

The present invention relates to a film coated tablet comprising empagliflozin and metformin hydrochloride, wherein comprising at least two fillers and the amount of fillers is 10.0% to 60.0% by weight in the total composition, the tablet provides the desired stability and pharmacotechnical properties and the desired dissolution profile. The present invention also relates to a simple, rapid, cost effective, time-saving and industrially convenient method of preparing the tablet.

The present invention relates to certain SGLT-2 inhibitors for the treatment and / or prevention of oxidative stress, for example in patients with type 1 or type 2 diabetes, as well as the use of such SGLT-2 inhibitors in the treatment and / or prevention of cardiovascular disease in patients, for example in patients with type 1 or type 2 diabetes. The present invention also relates to certain SGLT-2 inhibitors for the treatment and / or prevention of a metabolic disorder and for preventing, reducing the risk of or delaying the occurrence of a cardiovascular event in patients with type 1 or type 2 diabetes.

The present invention relates extended-release tablet compositions comprising empagliflozin or pharmaceutically acceptable salt thereof, metformin or pharmaceutically acceptable salt thereof.

The application discloses a preparation method of an empagliflozin chiral intermediate. A reactant I is subjected to a Davis oxaziridine oxidation reaction to obtain a chiral alcohol compound II, then the chiral alcohol compound II is subjected to a reaction with a compound III fluorobenzene to obtain a compound IV, and the compound IV is reduced to obtain a compound V. The application has the advantages that the chiral alcohol compound is obtained through the oxidation reaction, the chiral product can be obtained at a high yield, the reaction selectivity is good, the yield is high, and the loss of raw materials is reduced; the expensive chiral compound (S)-(+) -hydroxytetrahydrofuran can be avoided through the reaction, the production cost is effectively reduced, the synthesis process is simple, the synthesis steps of (S)-(+) -hydroxytetrahydrofuran are effectively reduced, and the problem that the cost is excessively high due to too many synthesis steps of (S)-(+) -hydroxytetrahydrofuran is avoided.

The invention discloses a catalytic synthesis process of an empagliflozin intermediate compound, which comprises the following steps: dissolving a compound I in an organic solution, adding a catalyst, stirring and mixing at low temperature for 1-2 hours, then adding a compound II, reacting at low temperature, monitoring the reaction by HPLC (High Performance Liquid Chromatography), and separating a product after the reaction is finished to obtain a compound III. The preparation method has the beneficial effects that TMPMgCl.LiCl is used for carrying out oriented metallization on para-position of chlorine atoms and meta-position of benzyl to generate an aryl magnesium reagent, and then the aryl magnesium reagent and hydroxyl-protected glucolactone are subjected to nucleophilic addition reaction to obtain an intermediate compound; a huge TMP (2, 2, 6, 6-tetramethylpiperidyl) group ensures that deprotonation only occurs on a specific C-H bond which is accessible in space and strongest in acidity, extremely high regioselectivity is achieved, and compared with traditional strong bases such as n-butyllithium, the regioselectivity of the method is improved; and diastereoselectivity; therefore, the reaction selectivity is high, and the specificity is strong.

The invention discloses a controlled release preparation and application thereof in preparation of a medicine for treating diabetic osteoporosis. The controlled release preparation consists of the following components: empagliflozin, alendronate sodium, an isolation coating material, an enteric controlled release coating material, a filling agent, a disintegrating agent and a lubricating agent. The enteric controlled release coating material comprises a pH sensitive regulator. The invention also discloses a preparation method of the alendronate sodium enteric-coated pellet, which comprises the following steps: preparing the alendronate sodium enteric-coated pellet, totally mixing, and forming the preparation. The preparation reduces gastrointestinal reaction and has higher stability.

This invention provides a method for purifying empagliflozin. The method comprises (1) extracting a feed solution containing empagliflozin and impurities with an extractant to obtain an extract containing empagliflozin; the impurities include one or more isomers of empagliflozin, esters, and hydrolysis products; the solvent in the feed solution is selected from nonpolar solvents and / or weakly polar solvents; and the extractant includes an ionic liquid or a mixture of an ionic liquid and a polar solvent; (2) the extract containing empagliflozin is back-extracted and concentrated to obtain empagliflozin. This method has advantages such as high separation efficiency, low solvent consumption, low production cost, safety and environmental friendliness, and ease of industrial production.