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Astragaloside eye drops with high water solubility and high stability as well as preparation method thereof

An astragaloside IV, water-soluble technology, applied in the field of highly stable astragaloside IV eye drops and preparation thereof, can solve problems such as strong irritation, and achieve the effects of improving stability, enhancing curative effect, and improving stability

Inactive Publication Date: 2018-09-04
QINGDAO UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The concentration of ginsenosides in 15mg / ml rabbit eyes can also show strong irritation after topical eye drops (some literature reports that ginsenosides can cause hemolysis), and it is not suitable as a carrier for ocular drug delivery

Method used

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  • Astragaloside eye drops with high water solubility and high stability as well as preparation method thereof
  • Astragaloside eye drops with high water solubility and high stability as well as preparation method thereof
  • Astragaloside eye drops with high water solubility and high stability as well as preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Put 50mg of astragaloside IV, 900mg of rebaudioside A, and 300mg of glycyrrhizic acid into a 100mL round-bottomed flask, add 50mL of absolute ethanol, and after fully dissolving, evaporate the absolute ethanol in a 40°C water bath in a rotary vacuum to obtain the drug and the copolymer. Disperse the film evenly, then add distilled water, wash the film thoroughly, and ultrasonicate in a 300w water bath for 10 minutes to obtain a micellar solution. After passing the micellar solution through a 0.22 μm microporous membrane, add the preservative benzalkonium chloride and the isotonic regulator sodium chloride, adjust the pH to 6.5, adjust the volume to 10 ml, and then sterile filter and dispense. The average particle diameter of the astragaloside IV micelles measured by the laser particle size analyzer is 10.1 nm, the dispersion index PDI=0.015, and the dispersion uniformity is good. The astragaloside IV micellar eye drops are stored at room temperature for 3 months, and th...

Embodiment 2

[0026] Put 20mg of astragaloside IV, 300mg of rebaudioside A, and 50mg of glycyrrhizic acid into a 100mL round-bottomed flask, add 50mL of absolute ethanol, and after fully dissolving, evaporate the absolute ethanol in a 40°C water bath in a rotary vacuum to obtain the drug and copolymer Disperse the film evenly, then add distilled water, wash the film thoroughly, and ultrasonicate in a 300w water bath for 10 minutes to obtain a micellar solution. After passing the micellar solution through a 0.22 μm microporous membrane, add the antiseptic benzalkonium chloride and the isotonic regulator sodium chloride, adjust the pH to 6.6, adjust the volume to 10 ml, and then sterile filter and dispense. The average particle size of the astragaloside IV micelles measured by the laser particle size analyzer is 10.7nm, the dispersion index PDI=0.021, and the dispersion uniformity is good. The astragaloside IV micellar eye drops are stored at room temperature for 2 months, and the leakage of ...

Embodiment 3

[0028] Put 100mg of astragaloside IV, 3000mg of rebaudioside A, and 1000mg of glycyrrhizic acid into a 100mL round-bottomed flask, add 50mL of absolute ethanol, and after fully dissolving, evaporate the absolute ethanol in a 40°C water bath in a rotary vacuum to obtain the drug and copolymer Disperse the film evenly, then add distilled water, wash the film thoroughly, and ultrasonicate in a 300w water bath for 10 minutes to obtain a micellar solution. After passing the micellar solution through a 0.22 μm microporous membrane, add the antiseptic benzalkonium chloride and the isotonic regulator sodium chloride, adjust the pH to 6.8, adjust the volume to 10 ml, and then sterile filter and dispense. The average particle size of astragaloside IV micelles measured by the laser particle size analyzer is 10.5nm, the dispersion index PDI=0.019, and the dispersion uniformity is good. The astragaloside IV micellar eye drops are stored at room temperature for 2.5 months, and the leakage o...

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Abstract

The invention discloses astragaloside eye drops with high water solubility and high stability. The astragaloside eye drops comprise astragaloside serving as a main medicine, and are characterized by further comprising rebaudioside A and glycyrrhizic acid which serve as medicine auxiliary materials; the mass ratio of the astragaloside to the rebaudioside A ranges from 1:15 to 1:30; and the mass ratio of the glycyrrhizic acid to the rebaudioside A ranges from 1:3 to 1:6. According to the astragaloside eye drops, the administration concentration can reach 10 mg / ml, micelles have small grain diameter and are distributed uniformly, the medicine stability is high, the administration irritation property is obviously reduced, and the medicine absorbed by cornea is increased; moreover, the rebaudioside A and the glycyrrhizic acid have anti-diabetic and anti-inflammatory activities, so that the astragaloside eye drops have a good medicine effect of coordinating eye treatment diabetic cornea lesion and corneal nerve lesion, and the astragaloside eye drops are highly economical.

Description

technical field [0001] The invention relates to astragaloside IV eye drops, in particular to a highly water-soluble and highly stable type of astragaloside IV eye drops and a preparation method thereof. Background technique [0002] Astragaloside IV (Astragaloside IV, CAS No. 83207-58-3), is a cyclopropane-type triterpene saponin isolated from Astragalus membranaceus. It is the main active ingredient of Astragalus membranaceus. , anti-oxidation, anti-virus, anti-hyperglycemia and neuroprotection and other pharmacological activities, has good medicinal value and great potential for development. The latest research shows that astragaloside IV has a wide range of pharmacological activities in the treatment of diabetes, such as lowering blood sugar, lowering blood lipids, improving insulin resistance, and inhibiting inflammation. It has a protective effect, which shows that astragaloside IV has broad application prospects in the treatment of diabetes and its complications, such...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/7048A61K47/26A61K47/28A61P3/06A61P3/10A61P9/10A61P27/02A61P29/00A61P37/02A61K31/704
CPCA61K47/26A61K47/28A61P3/06A61P3/10A61P9/10A61P27/02A61P29/00A61P37/02A61K9/0048A61K9/1075A61K31/704A61K31/7048A61K2300/00
Inventor 吴祥根孙凤瑗张凡
Owner QINGDAO UNIV OF SCI & TECH
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