4 results about "Vildagliptin" patented technology

This invention belongs to the field of pharmaceutical technology, and specifically relates to a vildagliptin-valsartan co-amorphous compound, its preparation method, and its application. The co-amorphous compound comprises vildagliptin and valsartan; the molar ratio of vildagliptin to valsartan in the co-amorphous compound is 1:0.5-3. In this invention, vildagliptin and valsartan interact to form hydrogen bonds. This interaction not only prevents solvent-mediated drug recrystallization but also accelerates the dissolution and exudation of valsartan. Compared to the valsartan raw material, the solubility and dissolution rate of valsartan in this co-amorphous compound are significantly improved, while the solubility and dissolution rate of vildagliptin are reduced. This is beneficial for improving the bioavailability of valsartan, delaying the release and absorption of vildagliptin in vivo, and the co-amorphous compound exhibits good stability.

This application provides a method for the efficient recovery of vildagliptin from vildagliptin mother liquor, belonging to the field of medicinal chemistry technology. Using vildagliptin mother liquor containing disubstituted impurities as the treatment target, an N-dealkylation reaction is used to selectively remove additional alkyl substituents from the disubstituted impurities, directionally converting the impurities into the target product vildagliptin, thus achieving waste resource utilization. This application requires no complex equipment, uses mild reaction conditions, achieves a disubstituted impurity conversion rate ≥90%, increases the total vildagliptin yield by 5-8%, and does not generate new process impurities. Hydrogen peroxide, as a commonly used industrial oxidant, is inexpensive, and the only byproduct is water, significantly reducing environmental pressure. It is fully compatible with existing industrial production processes and has outstanding economic value and environmental significance.

This application provides a method for preparing a high-purity vildagliptin intermediate and its disubstituted impurities, belonging to the field of medicinal chemistry. L-proline is weighed, added to solvent one and heated, stirred until dissolved, to obtain solution one; chloroacetyl chloride is weighed, added to solvent two and stirred until homogeneous, to obtain solution two; solutions one and two are added dropwise to solvent three and reacted; after the reaction is complete, the temperature is lowered, cyanuric chloride is added, the reaction is followed by further cooling and quenching, filtration, washing, and separation. The aqueous phase is extracted, the combined organic phases are concentrated, dried, and crystallized to obtain the vildagliptin intermediate. The dual titration method of this application allows for the control of impurity content in the vildagliptin intermediate to below 0.1%.

The invention provides application of combination of vildagliptin and naringin in preparation of a preparation for preventing and / or treating radiation-induced lung injury, and belongs to the technical field of biological medicine. Combined application of vildagliptin and naringin is found for the first time, the vildagliptin and naringin show a remarkable synergistic interaction effect in prevention and / or treatment of radiation-induced lung injury, the whole pathological process of radiation-induced lung injury can be intervened through multi-target and multi-channel cooperation, the defects that a single drug is single in action target and limited in prevention and treatment effect are overcome, and the vildagliptin and naringin are applied to prevention and / or treatment of radiation-induced lung injury. The outstanding clinical application value is realized. The combination of the two can significantly reduce the effective action dose of each single drug, reduce potential adverse reactions caused by long-term application of a high-dose single drug, and improve the medication safety. Wherein vildagliptin is a mature drug which is already marketed in clinic, naringin is a bioactive component of a natural source, the biocompatibility is good, the administration route is convenient, and the vildagliptin and the naringin can be flexibly prepared into various clinically applicable preparation forms.