Solid dispersion and preoral combination of glibenclamide and preparation method

Abstract

A dispersed solid or orally taken composition of gliben clamide clamide is prepared from glibenclamide and dispersing medium proportionally through mixing, grinding and fusing or spray drying.

Description

technical field

[0001] The invention relates to a solid dispersion of glibenclamide (Glibenclamide), an oral pharmaceutical composition of the dispersion and a preparation method of the dispersion, belonging to the technical field of medicine. Background technique

[0002] Glibenclamide is a second-generation sulfonylurea oral antidiabetic drug, also known as glibenclamide, and its chemical name is N-[2-[4-[[[(cyclohexylamino)carbonyl]amino]sulfonyl] Phenyl]ethyl]-2-methoxy-5-chlorobenzamide has the characteristics of small dosage and strong efficacy, and is widely used in clinical practice. Its main function is to lower blood sugar by intensely stimulating the pancreas to secrete insulin, which depends on the function of the functional β cells in the islets.

[0003] However, glibenclamide is weakly acidic, and only a small amount dissolves in water medium (the solubility in water at 25°C is 0.1mg / ml, which is insoluble according to the definition of Chinese Pharmacopoeia)...

Examples

Embodiment 1

[0035] Glyburide 10g and microcrystalline cellulose 20g were ground and mixed for 20 minutes to obtain the glibenclamide solid dispersion of the present invention.

Embodiment 2

[0037] Glibenclamide 15g, lactose 35g, grind and mix for 25 minutes to obtain.

Embodiment 3

[0039] Glibenclamide 10g, mannitol 20g, grind and mix for 25 minutes to obtain.

technical field

[0001] The invention relates to a solid dispersion of glibenclamide (Glibenclamide), an oral pharmaceutical composition of the dispersion and a preparation method of the dispersion, belonging to the technical field of medicine. Background technique

[0002] Glibenclamide is a second-generation sulfonylurea oral antidiabetic drug, also known as glibenclamide, and its chemical name is N-[2-[4-[[[(cyclohexylamino)carbonyl]amino]sulfonyl] Phenyl]ethyl]-2-methoxy-5-chlorobenzamide has the characteristics of small dosage and strong efficacy, and is widely used in clinical practice. Its main function is to lower blood sugar by intensely stimulating the pancreas to secrete insulin, which depends on the function of the functional β cells in the islets.

[0003] However, glibenclamide is weakly acidic, and only a small amount dissolves in water medium (the solubility in water at 25°C is 0.1mg / ml, which is insoluble according to the definition of Chinese Pharmacopoeia)...

Examples

Embodiment 1

[0035] Glyburide 10g and microcrystalline cellulose 20g were ground and mixed for 20 minutes to obtain the glibenclamide solid dispersion of the present invention.

Embodiment 2

[0037] Glibenclamide 15g, lactose 35g, grind and mix for 25 minutes to obtain.

Embodiment 3

[0039] Glibenclamide 10g, mannitol 20g, grind and mix for 25 minutes to obtain.

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