A kind of repaglinide chitosan sustained and controlled release microspheres and preparation method thereof

Abstract

The invention discloses a preparation of repaglinide chitosan sustained and controlled release microspheres and a preparation method thereof. The core-shell microsphere preparation is formed in the capsule material formed by condensation and cross-linking of polysaccharides. The preparation has slow and controlled release of drugs, and significantly improves the stability of repaglinide. The capsule material prepared by natural cross-linking agent and chitosan has good biocompatibility without any cytotoxicity, and can promote the absorption of drugs , improve the bioavailability of the drug. The invention is used for preparing repaglinide chitosan sustained and controlled release microspheres, and the medicine in dosage form is mainly used for preventing and treating type Ⅱ diabetes mellitus with high blood sugar.

Description

technical field [0001] The invention belongs to the field of medicine and chemical industry, and relates to a slow and controlled release microsphere and a preparation method thereof, in particular to a repaglinide chitosan slow and controlled release microsphere and a preparation method thereof. Background technique [0002] Repaglinide, the chemical name is S(+)-2-ethoxy-4-{2-[(3-methyl-1-(2-(1-piperidinyl)phenyl)butyl) Base) amino] -2-oxoethyl} benzoic acid, which belongs to insulin secretagogue, is clinically used for the treatment of type Ⅱ diabetes mellitus whose hyperglycemia cannot be effectively controlled by diet control and exercise. However, because the half-life of repaglinide is very short, usually only 1-2 hours, the existence time in the gastrointestinal tract is short, and the bioavailability is very low. [0003] Chitosan (CS) is a good bioorganic carrier currently used in drug sustained and controlled release preparations. It can solubilize drugs, promote...

AI Technical Summary

Problems solved by technology

[0002] Repaglinide, the chemical name is S(+)-2-ethoxy-4-{2-[(3-methyl-1-(2-(1-piperidinyl)phenyl)butyl) Base) amino] -2-oxoethyl} benzoic acid, which belongs to insulin secretagogues, is clinically used for the treatment of type Ⅱ diabetes mellitus whose hyperglycemia cannot be effectively controlled by diet control and exercise

However, due to the short half-life of repaglinide, usually only 1-2h, the existence time in the gastrointestinal tract is short, and the bioavailability is very low.

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