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Myricetin micelle eye drops with synergistic effect and preparation method of myricetin micelle eye drops

A synergistic, myricetin technology, applied in non-active ingredients medical preparations, active ingredients-containing medical preparations, pharmaceutical formulas, etc., can solve problems such as strong irritation, improve stability, and prolong corneal retention time. , anti-diabetic neuroprotective effect

Inactive Publication Date: 2018-05-29
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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  • Myricetin micelle eye drops with synergistic effect and preparation method of myricetin micelle eye drops
  • Myricetin micelle eye drops with synergistic effect and preparation method of myricetin micelle eye drops
  • Myricetin micelle eye drops with synergistic effect and preparation method of myricetin micelle eye drops

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Put 50mg myricetin and 900mg rebaudioside A in a 100mL round bottom flask, add 50mL absolute ethanol, after fully dissolving, evaporate absolute ethanol in a 40°C water bath in a rotating vacuum to obtain a uniformly dispersed film of the drug and the copolymer, and 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 myricetin micelles measured by a laser particle size analyzer is 10.1 nm, the dispersion index PDI=0.015, and the dispersion uniformity is good. The myricetin micelle eye drop is stored at room temperature for 3 months, and the leakage of myricetin from the micelle is less than 10%.

Embodiment 2

[0028] Put 20mg myricetin and 300mg rebaudioside A in a 100mL round bottom flask, add 50mL absolute ethanol, after fully dissolving, evaporate absolute ethanol in a 40°C water bath in a rotating vacuum to obtain a uniformly dispersed film of the drug and the copolymer, and 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 myricetin micelles measured by a laser particle size analyzer is 10.7nm, the dispersion index PDI=0.021, and the dispersion uniformity is good. The myricetin micelle eye drop is stored at room temperature for 2 months, and the leakage of myricetin from the micelle is less than 10%.

Embodiment 3

[0030] Put 100mg myricetin and 3000mg rebaudioside A in a 100mL round bottom flask, add 50mL absolute ethanol, after fully dissolving, evaporate absolute ethanol in a 40°C water bath in a rotating vacuum to obtain a uniformly dispersed film of the drug and the copolymer, and 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 myricetin micelles measured by a laser particle size analyzer is 10.5 nm, the dispersion index PDI=0.019, and the dispersion uniformity is good. The myricetin micelle eye drop is stored at room temperature for 2.5 months, and the leakage of myricetin from the micelle is less than 10%.

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Abstract

The invention discloses myricetin micelle eye drops with a synergistic effect. The eye drops take myricetin as a main medicine and are characterized by also comprising rebaudioside A as an auxiliary medicine material, wherein the mass ratio of the main medicine, namely, myricetin to the auxiliary medicine material, namely, rebaudioside A is (1:15)-(1:30); the eye drops are characterized by also comprising the rebaudioside A (CAS register number of58543-16-1, the molecular formula of C44H70O23 and the molecular weight of 967.03) with the purity higher than or equal to 98%. The prepared myricetin micelle eye drops have the administration concentration reaching 10 mg / ml and have small micelle size, uniform distribution range and good medicine stability, the administration irritation is notably reduced, medicine adsorption of cornea is improved, the administration concentration is reduced, the medicine acting time is prolonged, the administration times are reduced, the compliance of patients is improved, meanwhile, rebaudioside A has antidiabetic and anti-inflammatory activities, and accordingly, the myricetin micelle eye drops have good synergetic efficacy for eye treatment of diabetic keratopathy and cornea neuropathy. The myricetin micelle eye drops are very economical.

Description

technical field [0001] The invention relates to a myricetin eye drop, in particular to a myricetin micelle eye drop with a synergistic effect and a preparation method thereof. Background technique [0002] The prevalence of diabetes in my country has increased rapidly in recent years, and diabetes has become a major public health problem in China. The patient's long-term hyperglycemia state leads to lesions in various tissues and organs throughout the body, causing serious diabetes-related complications, including diabetic keratopathy. In addition, diabetic patients are prone to delayed corneal epithelial healing or even non-healing during corneal trauma or corneal surgery. Blindness is difficult to treat, the prognosis is poor, and the patient's economic and mental burden is serious. At present, the clinical treatment methods for diabetic keratopathy are limited. Therefore, it is of great clinical significance to study new therapeutic targets and effective prevention and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/26A61K31/352A61K31/704A61P3/10A61P27/02
CPCA61K47/26A61K9/0048A61K9/1075A61K31/352A61K31/704A61K2300/00
Inventor 吴祥根庄增芳孙凤瑗侯玉真宋开超
Owner QINGDAO UNIV OF SCI & TECH
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