13 results about "Linagliptin" patented technology

To provide a novel polymorph of linagliptin that is stable, and to provide a method for producing a novel polymorph of linagliptin by a safe and simple method that facilitates commercial mass production.SOLUTION: Provided is a novel polymorph of linagliptin that is a compound 1-[ (4-methyl-quinazolin-2- yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine having a peaks at 2θ(°)=6.9, 7.6, 9.2, 14.5, 17.7, 20.9±0.2θ in powder X-ray diffraction. The invention also relates to a method of producing the same.SELECTED DRAWING: Figure 1

To provide a linagliptin-containing pharmaceutical composition, particularly a linagliptin-containing film-coated tablet, and a method for producing the same, which can suppress the delayed disintegration, delayed dissolution, and increase of related substances that occur over time by simpler means. [Solution] The invention provides linagliptin as an active ingredient, along with excipients, disintegrants, binders, and lubricants. The binder used is a polyvinyl alcohol / acrylic acid / methyl methacrylate copolymer or a polyvinyl alcohol / polyethylene glycol / graft copolymer. The uncoated tablets are prepared by a wet granulation method called fluid bed granulation drying. Hypromellose is used as the film coating agent, and the film coating layer does not contain polyethylene glycol, resulting in linagliptin-containing film-coated tablets.

The present invention provides an injectable depot composition comprising linagliptin and low-dose liraglutide. The combination therapy of linagliptin and low-dose liraglutide provides a synergistic effect in the treatment of obesity compared to the administration of each drug alone. In addition, the administration dose of liraglutide can be reduced compared to the administration of liraglutide alone, and thus the direct cause of side effects related to the gastrointestinal system and the cardiovascular system of liraglutide can be reduced. Furthermore, by the combination of linagliptin, it has the advantage of additionally providing an improvement effect on metabolic diseases and cardiovascular diseases related to blood sugar, blood lipids, blood pressure, fatty liver, etc. In addition, compared to the conventional liraglutide dosage form of once-daily subcutaneous injection, the depot composition of linagliptin and liraglutide of the present invention can significantly improve patient convenience and patient compliance by unifying the administration route and improving the administration cycle.

The present invention relates to pharmaceutical compositions of linagliptin, pharmaceutical dosage forms, their preparation, their use and methods for treating metabolic disorders.

The application discloses a key amino acid induced new crystal form of linagliptin based on protein-drug interaction structure mining and a preparation method thereof; and the technical scheme is that key amino acids are introduced into a solvent crystallization system of linagliptin to induce five new crystal forms of linagliptin; the preparation method does not need to use a large amount of organic solvents, has the characteristics of being simple, precise and efficient, has strong crystal form regulation capacity, is energy-saving, environment-friendly and safe, and is easy to realize green industrial production.

The invention discloses a pharmaceutical composition containing linagliptin and metformin hydrochloride and a preparation method thereof.According to the composition, a small amount of meglumine (0.01%-1.0% w / w) is added, a linagliptin mixture and a metformin hydrochloride mixture are separately granulated, the growth of an impurity A, an impurity B and total impurities in an obtained linagliptin and metformin hydrochloride tablet is slow, the content of impurities in the linagliptin and metformin hydrochloride tablet is low, and the content of impurities in the linagliptin and metformin hydrochloride tablet is high. The stability of the composition is obviously improved, and the dissolution effect is not influenced. According to the preparation method of the composition, auxiliary materials in the preparation process are easy to obtain, the price is low, and the composition is suitable for commercial production.

The present application relates to the field of medicine, in particular to the use of POU2F2 gene or protein in screening products for preventing or treating atherosclerosis. The present application first discloses that POU2F2 can be used as a key pathogenic target of atherosclerosis, and on this basis, a candidate drug linagliptin is screened. The experimental results show that in the in vitro atherosclerosis model, linagliptin can significantly inhibit the expression of POU2F2 and down-regulate the levels of inflammatory factors and adhesion molecules. The findings clarify the mechanism of linagliptin in regulating POU2F2 related signal pathways, inhibiting vascular inflammatory response and reducing vascular endothelial damage, and fully show that it has a good clinical application prospect in preparing drugs for preventing or treating atherosclerosis and its related cardiovascular and cerebrovascular diseases.

The present invention provides an obesity treatment regimen for reducing side effects by low-dose combination administration of linagliptin and liraglutide. The combination therapy of linagliptin and low-dose liraglutide provides a synergistic effect in obesity treatment compared to administration of each drug alone. Furthermore, the administration dose of liraglutide can be reduced compared to administration of liraglutide alone, and thus the direct cause of side effects related to the gastrointestinal system and the cardiovascular system of liraglutide can be reduced. Furthermore, by the combination of linagliptin, it has the advantage of additionally providing an improvement effect on metabolic diseases and cardiovascular diseases related to blood sugar, blood lipids, blood pressure, fatty liver, etc.

The present invention relates to a pharmaceutical formulation containing three drugs: linagliptin, dapagliflozin, and metformin, and being prepared as a bilayered tablet comprising: an immediate-release layer comprising dapagliflozin and linagliptin as active ingredients; and a sustained-release layer comprising metformin as an active ingredient, wherein the immediate-release layer includes a lipophilic polyphenolic antioxidant as a stabilizer, and the sustained-release layer uses carboxymethylcellulose sodium and hypromellose 2208 together as sustained-release agents. In the pharmaceutical formulation according to the present invention, delamination of the formulation is suppressed, thus enabling the preparation of a high-quality formulation, and the formation of related substances of the active ingredients is suppressed, thus enabling long-term storage. Thus, the pharmaceutical formulation can increase medication compliance as a pharmaceutical composition for improving glycemic control in patients with insufficient glycemic control.

The present invention relates to methods for preventing or treating of metabolic disorders and related conditions, such as in certain patient groups. The present invention relates to treatment of genotyped diabetic patients with DPP-IV inhibitors such as linagliptin. In addition, the present invention relates to pharmaceutical compounds, compositions or combinations, methods of preventing or treating a metabolic disorder in a patient, improving glycemic control, preventing, slowing progression of, delaying or reversing progression to type 2 diabetes mellitus, reducing body weight or preventing an increase in body weight, preventing or treating the degeneration and / or functionality decline of pancreatic beta cells, and uses of the pharmaceutical compositions for preparing pharmaceuticals.

The application provides linagliptin tablets with stable quality, without coating and double aluminum packaging and a preparation method, and belongs to the technical field of pharmaceutical preparations. The linagliptin tablet is composed of drug-containing pellets 50 parts, mannitol 92 parts, pregelatinized starch 18 parts, corn starch 18 parts and magnesium stearate 2 parts. The drug-containing pellets are composed of linagliptin 5 parts, mannitol blank pellet core 29-37 parts, shellac 2-4 parts and kaolin 6-12 parts, and are prepared through a fluidized bed bottom spraying process.

The present invention relates to the technical field of medicine, particularly to a linagliptin synthesis and purification process, which comprises: 1, reacting a compound 1 with 1-bromo-2-butyne in an organic solvent under the condition of sodium bicarbonate at a preset temperature, and carrying out separation and purification to obtain a compound 2; 2, reacting the compound 2 with 2-chloromethyl-4-methylquinazoline in an organic solvent under alkaline conditions, and separating and purifying to obtain a compound 3; 3, the compound 3 and an acidified amino compound react in an organic solvent under the alkaline condition, and a linagliptin product is obtained through separation and purification. In the step 1, sodium bicarbonate is used as alkali, so that generation of a disubstituted impurity A is avoided, and the yield and the purity of the compound 2 are further improved. 30-40% of water is added in the reaction in the step 3, the reaction rate is increased, the position isomer impurity C is controlled to be smaller than or equal to 0.1%, and the purity of 99.9% can be achieved only through one-time crystallization in aftertreatment.