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Pterostilbene nano eye drops and preparation method thereof

A technology of pterostilbene and eye drops, applied in the field of highly stable pterostilbene nano-eye drops and its preparation

Pending Publication Date: 2021-09-07
BINZHOU MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

And the above-mentioned deficiency of pterostilbene severely limits its development into aqueous solution type eye drops

Method used

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  • Pterostilbene nano eye drops and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Put 10mg of pterostilbene and 150mg of glycosyl hesperidin in a 100mL round bottom 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, and then Add distilled water, fully wash the membrane, 300w power water bath ultrasonic 10min, get 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 pterostilbene micelles measured by laser particle size analyzer is 10.1nm, the dispersion index PDI=0.015, and the dispersion uniformity is good. The pterostilbene micelle eye drop is stored at room temperature for 3 months, and the leakage of pterostilbene from the micelles is less than 10%.

Embodiment 2

[0017] Put 10mg of pterostilbene and 300mg of glycosyl hesperidin in a 100mL round bottom flask, add 50mL of absolute ethanol, after fully dissolving, evaporate the absolute ethanol in a rotating vacuum at 40°C 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 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 pterostilbene micelles measured by the laser particle size analyzer is 10.7nm, the dispersion index PDI=0.021, and the dispersion uniformity is good. The pterostilbene micelle eye drop is stored at room temperature for 2 months, and the leakage of pterostilbene from the micelles is less than 10%.

Embodiment 3

[0019] Put 2mg of pterostilbene and 30mg of glycosyl hesperidin in a 100mL round bottom 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, and then Add distilled water, fully wash the membrane, 300w power water bath ultrasonic 10min, get 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 pterostilbene micelles measured by the laser particle size analyzer is 10.5nm, the dispersion index PDI=0.019, and the dispersion uniformity is good. The pterostilbene micelle eye drop is stored at room temperature for 2.5 months, and the leakage of pterostilbene from the micelles is less than 10%.

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Abstract

The invention discloses a pterostilbene nano eye drop and a preparation method thereof, which adopts pterostilbene as a main drug, glycosyl hesperidin as a pharmaceutical excipient, the mass ratio of the pterostilbene to the glycosyl hesperidin is 1: 15-1: 30, and the purity of the glycosyl hesperidin (the CAS registration number is 161713-86-6, the molecular formula is C34H44O20, and the molecular weight is 772.7) is greater than or equal to 96%. According to the prepared pterostilbene nano eye drops, the administration concentration can reach 1 mg / ml, the micelle particle size is small, the distribution range is uniform, the medicine stability is good, the eye local safety is good, meanwhile, the glycosyl hesperidin has the anti-inflammatory activity and the like, so that the pterostilbene eye drops have the good synergistic effect on treating diabetic keratopathy and corneal neuropathy of eyes, and the pterostilbene nano eye drops disclosed by the invention have very good economical efficiency.

Description

technical field [0001] The invention relates to a pterostilbene eye drop, in particular to a highly stable pterostilbene nano-eye drop and a preparation method thereof. Background technique [0002] Pterostilbene (Pterostilbene, CAS No. 537-42-8), is an active ingredient derived from plants such as red sandalwood, blueberry, grape and flower palm wood, which has anti-cancer, anti-inflammatory, antioxidant and analgesic effects. At present, a large number of studies have shown that pterostilbene has a good effect in the treatment and protection of skin diseases, especially in the fields of anti-oxidation. Pterostilbene has a variety of pharmacological activities such as preventing and treating cardiovascular diseases, anti-tumor, and anti-oxidation. It has good medicinal value and great potential for development. The latest research shows that pterostilbene has a wide range of pharmacological activities such as significant anti-oxidation, anti-inflammation, and free radical ...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/09A61K31/7048A61K47/26A61P3/10A61P25/02A61P27/02
CPCA61K31/09A61K31/7048A61K9/1075A61K9/0048A61K47/26A61P3/10A61P27/02A61P25/02A61K2300/00
Inventor 辛萌
Owner BINZHOU MEDICAL COLLEGE
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