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Dihydromyricetin eye drop with synergistic effect and high aqueous solution stability and preparation method thereof

A technology of dihydromyricetin and high aqueous solution, which is applied in the directions of non-active ingredient medical preparations, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve problems such as strong irritation, improve stability and improve curative effect. , the effect of improving stability

Inactive Publication Date: 2018-04-24
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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  • Dihydromyricetin eye drop with synergistic effect and high aqueous solution stability and preparation method thereof
  • Dihydromyricetin eye drop with synergistic effect and high aqueous solution stability and preparation method thereof
  • Dihydromyricetin eye drop with synergistic effect and high aqueous solution stability and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Put 50mg of dihydromyricetin and 900mg of rebaudioside A in a 100mL round-bottomed flask, add 50mL of absolute ethanol, after fully dissolving, evaporate the absolute ethanol in a 40°C water bath in a rotating vacuum to obtain a uniformly dispersed film of the drug and the copolymer , then add distilled water, fully wash the membrane, 300w power water bath ultrasonic 10min, get micellar solution. After the micellar solution is passed through a 0.22 μm microporous membrane, the preservative benzalkonium chloride and the isotonic regulator sodium chloride are added, the pH is adjusted to 7.4, and the sterile filter is then dispensed. The average particle diameter of the dihydromyricetin 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 dihydromyricetin micelle eye drop is stored at room temperature for 3 months, and the leakage of dihydromyricetin from the micelle is less than 10%. ...

Embodiment 2

[0026] Put 20mg of dihydromyricetin and 300mg of rebaudioside A in a 100mL round-bottomed flask, add 50mL of absolute ethanol, after fully dissolving, evaporate the absolute ethanol in a 40°C water bath in a rotating vacuum to obtain a uniformly dispersed film of the drug and the copolymer , then add distilled water, fully wash the membrane, 300w power water bath ultrasonic 10min, get micellar solution. After the micellar solution is passed through a 0.22 μm microporous membrane, the preservative benzalkonium chloride and the isotonic regulator sodium chloride are added, the pH is adjusted to 7.4, and the sterile filter is then dispensed. The average particle size of the dihydromyricetin micelles measured by the laser particle size analyzer is 10.7nm, the dispersion index PDI=0.021, and the dispersion uniformity is good. The dihydromyricetin micelle eye drop is stored at room temperature for 2 months, and the leakage of dihydromyricetin from the micelle is less than 10%.

Embodiment 3

[0028] Put 100mg of dihydromyricetin and 3000mg of rebaudioside A in a 100mL round-bottomed flask, add 50mL of absolute ethanol, after fully dissolving, evaporate the absolute ethanol in a 40°C water bath in a rotating vacuum to obtain a uniformly dispersed film of the drug and the copolymer , then add distilled water, fully wash the membrane, 300w power water bath ultrasonic 10min, get micellar solution. After the micellar solution is passed through a 0.22 μm microporous membrane, the preservative benzalkonium chloride and the isotonic regulator sodium chloride are added, the pH is adjusted to 7.4, and the sterile filter is then dispensed. The average particle diameter of the dihydromyricetin micelles measured by the laser particle size analyzer is 10.5nm, the dispersion index PDI=0.019, and the dispersion uniformity is good. The dihydromyricetin micelle eye drop is stored at room temperature for 2.5 months, and the leakage of dihydromyricetin from the micelle is less than 10...

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Abstract

The invention discloses a dihydromyricetin micelle eye drop with a synergistic effect and high aqueous solution stability. The dihydromyricetin micelle eye drop comprises dihydromyricetin as a main medicine, is characterized by further comprising rebaudioside A as a medicinal auxiliary material, wherein the mass ratio of the dihydromyricetin as the main medicine to the rebaudioside A as the medicinal auxiliary material is 1:15 to 1:30, is characterized by further comprising rebaudioside A (CAS registration number of 58543-16-1, a molecular formula of C44H70O23 and the molecular weight of 967.03) with the purity being higher than or equal to 98%. The dihydromyricetin micelle eye drop prepared by a preparation method provided by the invention has the medicine administering concentration as high as 10mg / ml, is small in micelle particle size, uniform in distribution range and good in medicinal stability, significantly reduces the medicine administering irritation, improves medicine absorption of corneae, decreases the medicine administering concentration, prolongs the acting time of medicines, reduces the medicine administering times and improves patient compliance; meanwhile, the rebaudioside A has anti-diabetic and anti-inflammatory activities and the like, so that the dihydromyricetin micelle eye drop has a very good synergistic medicinal efficacy of treating diabetic keratopathy and corneal neuropathy of eyes; the dihydromyricetin micelle eye drop is very economical.

Description

technical field [0001] The invention relates to a dihydromyricetin eye drop, in particular to a dihydromyricetin micelle eye drop with synergistic effect and high aqueous solution stability and a preparation method thereof. Background technique [0002] Dihydromyricetin (Dihydromyricetin, CAS No. 27200-12-0) is a polyphenolic hydroxyl dihydroflavonol widely present in natural plants, also known as snake grapevine and dihydromyricetin, belonging to flavonoids , Dihydromyricetin has various pharmacological activities such as prevention and treatment of cardiovascular diseases, anti-tumor, anti-oxidation, etc., has good medicinal value, and has great potential for development. The latest research shows that because dihydromyricetin has a wide range of pharmacological activities such as significant anti-oxidation, anti-inflammation, and free radical scavenging, it has broad application prospects in the treatment of diabetes and its complications, such as diabetic keratopathy. B...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/352A61K47/26A61K31/704A61P3/10A61P27/02A61P25/00
CPCA61K47/26A61K9/0048A61K9/1075A61K31/352A61K31/704A61K2300/00
Inventor 吴祥根孙凤瑗汝绍刚金宏
Owner QINGDAO UNIV OF SCI & TECH
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