3 results about "Glipizide" patented technology

Relacorilant is useful in the treatment of hypercortisolism and cancer. Many drugs useful in treating hypercortisolism or cancer are metabolized by CYP2C9 enzymes. The effects of concomitant administration of relacorilant and a CYP2C9 substrate are disclosed herein.Relacorilant potently inhibited CYP2C9 in an in vitro test, indicating that co-administration of relacorilant and a CYP2C9 substrate would be expected to increase the CYP2C9 substrate plasma exposure more than five-fold in vivo. Significant reductions in CYP2C9 substrate doses would be expected to be required when administered with relacorilant.Surprisingly, no such increase in plasma exposure was seen in human studies. Applicant discloses that relacorilant may be safely co-administered with unmodified doses of a CYP2C9 substrate such as, e.g., tolbutamide, glimepiride, and glipizide. Relacorilant and unmodified doses of CYP2C9 substrate such as tolbutamide, glimepiride, and glipizide may be co-administered to treat hypercortisolism, or may be co-administered to a cancer patient.

The application provides a preparation process of glipizide, which comprises the following steps: 1) preparing N-nitroso-3-azabicyclo[3.3.0]octane hydrochloride; 2) in the presence of a cerium-based activated carbon catalyst, N-nitroso-3-azabicyclo[3.3.0]octane hydrochloride and hydrazine hydrate are subjected to a reduction reaction in a first organic solvent; after the reaction is completed, filtration is performed, the filtrate is diluted with water, and then extraction, acidification and pH adjustment to 1.5-2.5, low-temperature crystallization, filtration and drying are sequentially performed to obtain N-amino-3-azabicyclo[3.3.0]octane hydrochloride; the cerium-based activated carbon catalyst is prepared by loading a cerium salt on an activated carbon carrier through a precipitation method; and 3) N-amino-3-azabicyclo[3.3.0]octane hydrochloride and p-toluenesulfonylurea are subjected to a heating reflux reaction; after the reaction is completed, post-treatment is performed to obtain glipizide. The whole process does not emit heavy metals, the catalyst can be used repeatedly, and the treatment cost of three wastes is greatly reduced, so that the application provides a green industrialized preparation process chain of glipizide.

The application belongs to the technical field of chemical medicine sustained-release preparation, and proposes a glipizide sustained-release capsule and a preparation method thereof.The glipizide sustained-release capsule is prepared by filling microtablet A with a release time interval of 0-6h and microtablet B with a release time interval of 6-12h in a quantity of 2:3;wherein, the microtablet A comprises glipizide, a skeleton material, a filler, an aqueous binder solution and a lubricant; the microtablet B is prepared by coating the capsule prescription amount of 60% of the microtablet A with a sustained-release coating. By designing two kinds of release microtablets in the sustained-release capsule, the two kinds of microtablets are responsible for their respective release intervals, and are mutually coordinated and supplemented to realize a smooth release curve, and the in-vitro release behavior of the original preparation is highly coincident, and the preparation process of the two kinds of microtablets can be coordinated, and has a greater adjustment space.