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Dihydromyricetin medicament taking biocompatible micro-emulsion as carrier, preparation method and application

A dihydromyricetin, biocompatible technology, applied in pharmaceutical formulations, medical preparations with inactive ingredients, medical preparations containing active ingredients, etc., can solve problems such as the limitation of the ability to form aggregates, and achieve good compatibility performance , the effect of small viscoelasticity and good compatibility

Inactive Publication Date: 2018-06-08
SHANDONG NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to its special rigid surface structure, it is limited in the ability to form aggregates.

Method used

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  • Dihydromyricetin medicament taking biocompatible micro-emulsion as carrier, preparation method and application
  • Dihydromyricetin medicament taking biocompatible micro-emulsion as carrier, preparation method and application
  • Dihydromyricetin medicament taking biocompatible micro-emulsion as carrier, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] 1.995g sucrose stearate, 0.855g sodium deoxycholate, 1.9g isopropanol and 0.25g isopropyl myristate are placed in a stoppered colorimetric tube, and they are mixed evenly with a vortex mixer, and Stir fully in a constant temperature water bath at 50-60°C to dissolve it. Then, 5 g of twice distilled water was added dropwise to the colorimetric tube, placed in a water bath, stirred and mixed, and finally left to stand in a constant temperature water bath at 40°C to achieve phase equilibrium, and the microemulsion obtained was the drug-loaded microemulsion, denoted as B 1 .

Embodiment 2

[0053] Place 1.89g sucrose stearate, 0.81g sodium deoxycholate, 1.8g isopropanol and 0.5g isopropyl myristate in a colorimetric tube with a stopper, and mix it evenly with a vortex mixer, Stir fully in a constant temperature water bath at 50-60°C to dissolve it. Then, 5 g of twice distilled water was added dropwise to the colorimetric tube, placed in a water bath, stirred and mixed, and finally left to stand in a constant temperature water bath at 40°C to achieve phase equilibrium, and the microemulsion obtained was the drug-loaded microemulsion, denoted as B 2 .

Embodiment 3

[0055] 1.785g sucrose stearate, 0.765g sodium deoxycholate, 1.7g isopropanol and 0.75g isopropyl myristate are placed in a stoppered colorimetric tube, and they are mixed evenly with a vortex mixer, and Stir fully in a constant temperature water bath at 50-60°C to dissolve it. Then, 5 g of twice distilled water was added dropwise to the colorimetric tube, placed in a water bath, stirred and mixed, and finally left to stand in a constant temperature water bath at 40°C to achieve phase equilibrium, and the microemulsion obtained was the drug-loaded microemulsion, denoted as B 3 .

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Abstract

The invention discloses dihydromyricetin medicament taking biocompatible micro-emulsion as a carrier, a preparation method and application. According to the preparation method, the biocompatible micro-emulsion which is constructed by taking sucrose stearate and sodium deoxycholate as surfactants, isopropyl alcohol as a cosurfactant, and isopropyl myristate as an oil phase to serve as the carrier of an oil soluble medicament. Bicontinuous micro-emulsion with an oil-in-water structure is prepared; the micro-emulsion has a very good sustained releasing effect on a DMY medicament; a releasing process conforms to a first order kinetic equation; good anti-oxidation activity of the medicament can still be maintained in the micro-emulsion, and the medicament has very good cleaning activity on ABTS.+. The change of the composition and the environment of the micro-emulsion has certain influence on the cumulative release rate and the anti-oxidation activity; along with the increment of oil content and water content, the cumulative release rate and the anti-oxidation activity of dihydromyricetin are increased; when the mixed surfactant and oil are in the ratio of 9:1 and the water content is 65 percent, the DMY / micro-emulsion has the highest anti-oxidation activity and cumulative release rate.

Description

technical field [0001] The invention belongs to the technical field of medicament preparation, and in particular relates to a preparation method and application of a dihydromyricetin medicament with a biocompatible microemulsion as a carrier. Background technique [0002] Dihydromyricetin (DMY) is a natural polyphenolic flavonoid that exists in large quantities in grape plants. It has been widely concerned due to its antibacterial, antioxidative, blood fat lowering and hangover and other physiological effects. However, due to its poor stability, low water solubility (0.2mg / mL), and easy absorption and metabolism, its utilization is low, which limits its practical application. In recent years, these shortcomings of dihydromyricetin can be improved by chemical structure modification (chemical modification by branching other groups on the hydroxyl group of DMY), but the preparation process is generally more complicated. The protection and solubilization of drugs and the impro...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61K47/26A61K47/28A61K47/14A61P39/06
CPCA61K31/352A61K47/14A61K47/26A61K47/28
Inventor 王仲妮董爽爽周玉芳梁净净
Owner SHANDONG NORMAL UNIV
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