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Glimepiride hydrogel and preparation method thereof

A hydrogel, glimepiride technology, applied in the field of glimepiride hydrogel and preparation thereof, can solve the problems of limited dissolution of oral drugs, difficult control of drug dosage, poor blood drug durability, and the like, Achieving the effect of avoiding liver first-pass effect, lasting blood drug concentration, and small toxic side effects

Active Publication Date: 2015-05-06
HEBEI UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The purpose of the present invention is exactly to provide a kind of glimepiride hydrogel and preparation method thereof, to develop a new dosage form of glimepiride, to solve the limitation of oral drug dissolution and difficult dosage of existing glimepiride preparations Issues with control, poor biocompatibility, and poor drug persistence in blood

Method used

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  • Glimepiride hydrogel and preparation method thereof
  • Glimepiride hydrogel and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0024] Weigh 100 mg of glimepiride and 400 mg of meglumine co-solvent, heat and dissolve with 5 g of purified water in a water bath at 80°C, stir and let cool to obtain 20 mg / ml glimepiride co-solvent aqueous solution; Add 0.0456g of azone and 0.0446g of oleic acid respectively in this solution, after magnetic stirring evenly, add the ethanol solution of 10% (g / mL) ethylparaben (containing 0.01g ethylparaben) successively , 0.001g EDTA-2Na and 0.652g glycerin, after stirring evenly, it becomes a clear solution, add 50mg carbomer, stir magnetically, make it fully swell and form a gel, add 0.0672g triethanolamine, stir overnight, and obtain a transparent lattice Limepiride hypoglycemic hydrogel.

Embodiment 2

[0026] Weigh 125 mg of glimepiride and 500 mg of meglumine co-solvent, heat and dissolve with 5.04 g of purified water in a water bath at 90°C, stir and let cool to obtain an aqueous solution of glimepiride co-solvent; add 0.107 g of co-solvent to the solution Azone and 0.107g of oleic acid, after magnetic stirring evenly, add 8% (g / mL) ethylparaben ethanol solution (containing 0.018g ethylparaben), 0.0018g EDTA-2Na and 1.071 g glycerin, after stirring evenly, it becomes a clear solution, add 71.4mg carbomer, stir magnetically, make it fully swell and form a gel, add 0.1071g triethanolamine, stir overnight, and obtain transparent glimepiride hypoglycemic hydrogel Glue.

Embodiment 3

[0028]Weigh 75 mg of glimepiride and 300 mg of meglumine co-solvent, heat and dissolve with 4.87 g of purified water in a water bath at 60°C, stir and let cool to obtain an aqueous solution of glimepiride co-solvent; add 0.03 g of co-solvent to the solution Azone and 0.03g of oleic acid, magnetically stirred evenly, then added 5% (g / mL) ethylparaben ethanol solution (containing 0.0006g ethylparaben), 0.061mg EDTA-2Na and 0.60 g glycerin, after stirring evenly, it becomes a clear solution, add 30mg carbomer, stir magnetically, make it fully swell and form a gel, add 0.060g triethanolamine, stir overnight, and obtain transparent glimepiride hypoglycemic hydrogel agent.

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Abstract

The invention discloses glimepiride hydrogel which comprises glimepiride, meglumine, azone, oleic acid, ethylparaben, EDTA-2Na, glycerol, carbomer, triethavolamine and purified water. The glimepiride hydrogel is prepared through the following steps: dissolving glimepiride and meglumine in purified water by heating to obtain a glimepiride cosolvent water solution; and adding azone, oleic acid, ethylparaben, EDTA-2Na and glycerol into the glimepiride cosolvent water solution in sequence, performing stirring uniformly, adding carbomer, performing swelling, adding triethanolamine, and performing stirring uniformly to obtain the glimepiride hydrogel. A prescription provided by the invention is scientific, the process is reasonable, and the prepared glimepiride hydrogel has the characteristics of uniform and exquisite texture, strong adhesive force, good coating performance, easiness in cleaning, good moisture retention, high stability and the like, has good skin permeability, good biocompatibility, a lasting drug effect and small toxic and side effects, is easy to control in dosage, and is suitable for mass diabetic patients (especially for type 2 diabetic patients) to use for a long time.

Description

technical field [0001] The invention relates to a combination preparation for external use, in particular to a glimepiride hydrogel and a preparation method thereof. Background technique [0002] The chemical name of Glimepiride is 1-[4-[2-(3-ethyl-4-methyl-2-oxo-3-pyrroline-1-carboxamido)-ethyl]- Benzenesulfonyl]-3-(trans-4-methylcyclohexyl)-urea is a third-generation sulfonylurea and an oral hypoglycemic agent that can be used in combination with insulin. β - Cells release insulin and inhibit the synthesis of hepatic glucose. Compared with other hypoglycemic drugs of the same class, it has the advantages of quick onset, strong effect, long duration and small dose. [0003] At present, the dosage forms of glimepiride on the market are mainly oral dosage forms such as tablets, dispersible tablets, dropping pills, and capsules. For example, CN103893143A discloses a glimepiride oral tablet, its components are: glimepiride 2%, antioxidant 0.01-0.03%, acid-causing agent 0.3-1....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/64A61K47/32A61K47/26A61P3/10
Inventor 李海鹰杨文智李霞霞潘婷婷申世刚
Owner HEBEI UNIVERSITY
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