39 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.

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 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 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 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.

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

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.

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 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.

The invention provides a pharmaceutical composition for treating megaloblastic anemia or iron-deficiency anemia. The pharmaceutical composition is prepared from an effective amount of empagliflozin, an effective amount of folic acid, an effective amount of 5-methyltetrahydrofolic acid and pharmaceutically acceptable auxiliary materials.

The invention relates to an empagliflozin pharmaceutical composition and a preparation method thereof. According to the invention, through the specific proportion of the filling agent and the particle size of the raw material medicines, and the direct tabletting process, the commercial complex process is avoided, the reproducibility and stability of the product process are ensured under the condition of safe and efficient production, the quality meets the requirement in a long-term stability test, and better stability is achieved; and in an in-vivo bioequivalence test, clinical equivalence with a reference preparation is shown.

The present invention relates to a bilayer tablet comprising empagliflozin and metformin, 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 bilayer tablet.

The invention discloses a microchannel reaction preparation process of an empagliflozin intermediate, which comprises the following steps: preparing solutions A, B, C and D with corresponding concentrations in advance, mixing the solutions A, B and C by using a static mixer, and introducing the mixed solution into a microchannel reactor I; mixing the solution with the solution D through a static mixer after the micro-channel reaction is completed, introducing the mixture into a micro-channel reactor II, and separating a product after the reaction is completed to obtain a target compound IV. The method has the beneficial effects that the reaction adopts a microchannel reactor technology, the mass transfer and heat transfer efficiency of empagliflozin preparation is remarkably improved, the reaction temperature is ensured to be constant and free of fluctuation, the temperature runaway risk is thoroughly avoided, the generation of byproducts is effectively inhibited, the production safety is greatly enhanced, and the method is mild in process reaction condition, simple to operate and suitable for industrial production. The reaction speed is high, the production period is remarkably shortened, the catalytic effect of the catalyst is good, the reaction selectivity is high, byproducts are few, and post-treatment of products is facilitated.

The invention provides a purification method of empagliflozin, which is characterized in that an empagliflozin crude product to be purified is crystallized by adopting a good solvent-poor solvent crystallization system, and the good solvent is a mixed solvent of tetrahydrofuran (THF) and water. According to the purification method provided by the invention, THF and water are used as a crystallization system of a good solvent, impurities can be effectively removed, a high-purity product can be obtained, the yield can be greatly improved, the process loss is reduced, in addition, the purification method does not need expensive reagents or raw materials, the process is simple and convenient, the operability is high, and the purification method is very suitable for large-scale production and application.

The invention provides a pharmaceutical composition containing effective medicinal dose of enalapril folic acid and empagliflozin. The invention also provides application of the composition in preparation of medicines for treating heart failure.

The present invention relates to a composition, a combination, and a combination therapy for treating type 2 diabetes mellitus. The composition, combination, and combination therapy effectively reduce blood glucose level by administering 10 mg or 25 mg of empagliflozin to a patient with type 2 diabetes mellitus whose blood glucose level is not adequately controlled by a combination therapy of metformin and sitagliptin, and maintains the controlled blood glucose level for a long period of time with symptoms mostly confirmed to be moderate or lower, and most of the adverse drug reactions are known adverse reactions that have been previously reported in previous clinical trials of clinical trial drugs, and therefore, a new three-drug composition, a combination, and a combination therapy with ensured safety may be provided.

The present invention is directed to methods for treating diabetic macular edema (DME), proliferative diabetic retinopathy (PDR), wet age-related macular degeneration (AMD) and / or retinal vein occlusion (RVO) in a patient or subject in need comprising administering an effective amount of at least one anti-DME agent selected from the group consisting of desipramine, protriptyline, cyclosporin A, crisaborole, empagliflozin, nitroxolone, suprofen, sulfisoxazole, methapyrilene, phentolamine, naphazoline or a pharmaceutically acceptable salt thereof, preferably at least one agent selected from the group consisting of desipramine, nitroxolone, methapyriline, phentolamine, napthazoline and their pharmaceutically acceptable salts.

The invention provides a pharmaceutical composition. The pharmaceutical composition is prepared from metformin, empagliflozin, folic acid substances and a pharmaceutically acceptable carrier, wherein the metformin, the empagliflozin and the folic acid substances are in effective medicinal dose. The invention also provides an application of the pharmaceutical composition in preparation of a medicine for improving and / or delaying senescence.

The present invention relates to a stable ready to use suspension of empagliflozin Particularly, the present invention relates to a stable, taste-masked, ready to use suspension of empagliflozin and the process for preparing it. The present invention also relates to a method for treating patients with diabetes, type 1 or type 2 by administering a stable, taste-masked, ready-to-use suspension comprising empagliflozin and pharmaceutically acceptable excipients.