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Hydroxytyrosol eye drops for effectively targeting trigeminal ganglion and preparation method thereof

A technology of hydroxytyrosol and trigeminal nerve, applied in medical preparations of non-active ingredients, nervous system diseases, active ingredients of hydroxyl compounds, etc., can solve the problem of corneal nerve/epithelial repair and pathological state of trigeminal ganglion. Correct other problems to achieve the effect of improving trigeminal ganglion targeting, controllable micellar particle size, good solubility and stability

Active Publication Date: 2016-08-31
QINGDAO UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This reminds us that the ocular surface drug commonly used in ophthalmology mainly treats the "treetops" with drugs, but the effective transfer of drugs to the "tree roots" through the damaged "treetops" is limited, especially in the case of trauma, ophthalmic surgery, etc. In the case of "treetop" injury, the absorption and transport of the drug after ocular surface administration to the trigeminal ganglion through the corneal nerve is limited, and the pathological state of the trigeminal ganglion cannot be effectively corrected, which will further affect the repair of the corneal nerve / epithelium

Method used

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  • Hydroxytyrosol eye drops for effectively targeting trigeminal ganglion and preparation method thereof
  • Hydroxytyrosol eye drops for effectively targeting trigeminal ganglion and preparation method thereof
  • Hydroxytyrosol eye drops for effectively targeting trigeminal ganglion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022]Put 50mg of hydroxytyrosol and 900mg of polyethylene caprolactam-polyvinyl acetate-polyethylene glycol (molecular weight: 118,000) into a 100mL round bottom flask, add 20mL of absolute ethanol, after fully dissolved, evaporate the absolute ethanol in a 40°C water bath in a rotary vacuum To obtain a uniformly dispersed film of drug and copolymer, dissolve 50 mg of lidocaine in 10 mL of phosphate buffer, then pour the phosphate buffer into a round-bottomed flask, wash the film thoroughly, and ultrasonicate in a 300w water bath for 10 minutes to obtain a gel Continue to incubate at 40°C for 30 minutes, add preservative benzalkonium chloride to make the final concentration 0.005%~0.02%, add isotonic regulator sodium chloride until the osmotic pressure of the solution reaches 270~330mOsm / kg, use hydrochloric acid or hydrogen Use sodium oxide to adjust the pH to 6.8~7.4, pass the micellar solution through a 0.22µm microporous membrane, and then aseptically dispense it. The ave...

Embodiment 2

[0024] Put 50mg of hydroxytyrosol and 900mg of polyethylene caprolactam-polyvinyl acetate-polyethylene glycol (molecular weight: 118,000) into a 100mL round bottom flask, add 20mL of absolute ethanol, after fully dissolved, evaporate the absolute ethanol in a 40°C water bath in a rotary vacuum To obtain a uniformly dispersed film of drug and copolymer, dissolve 10 mg of lidocaine in 10 mL of phosphate buffer, then pour the phosphate buffer into a round-bottomed flask, wash the film thoroughly, and ultrasonicate in a 300w water bath for 10 minutes to obtain gel Continue to incubate at 40°C for 30 minutes, add preservative benzalkonium chloride and isotonic regulator sodium chloride, adjust the pH to 7.4, pass the micellar solution through a 0.22 μm microporous membrane, and then aseptically dispense it. The average particle size of hydroxytyrosol micelles measured by laser particle size analyzer is 50.3nm, the dispersion index PDI=0.052, and the dispersion uniformity is good. T...

Embodiment 3

[0026] Put 50mg of hydroxytyrosol and 900mg of polyethylene caprolactam-polyvinyl acetate-polyethylene glycol (molecular weight: 118,000) into a 100mL round bottom flask, add 20mL of absolute ethanol, after fully dissolved, evaporate the absolute ethanol in a 40°C water bath in a rotary vacuum To obtain a uniformly dispersed film of the drug and the copolymer, dissolve 25 mg of lidocaine in 10 mL of phosphate buffer, then pour the phosphate buffer into a round-bottomed flask, wash the film thoroughly, and ultrasonicate in a 300w water bath for 10 minutes to obtain gel Continue to incubate at 40°C for 30 minutes, add preservative benzalkonium chloride and isotonic regulator sodium chloride, adjust the pH to 7.4, pass the micellar solution through a 0.22 μm microporous membrane, and then aseptically dispense it. The average particle size of hydroxytyrosol micelles measured by the laser particle size analyzer is 49.8nm, the dispersion index PDI=0.048, and the dispersion uniformity...

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Abstract

The invention discloses hydroxytyrosol eye drops for effectively targeting trigeminal ganglion and a preparation method thereof. The eye drops comprise hydroxytyrosol used as a main drug and a preservative, an isoosmotic adjusting agent, a polyethylenecaprolactam-polyvinyl acetate-polyethylene glycol copolymer and lidocaine or its pharmaceutically acceptable salts. Mass ratio of the hydroxytyrosol main drug to the polyethylenecaprolactam-polyvinyl acetate-polyethylene glycol copolymer drug excipient is 1: 18. Mass ratio of lidocaine to the polyethylenecaprolactam-polyvinyl acetate-polyethylene glycol copolymer drug excipient is 1: 18-1: 90. The eye drops of the invention have good solubility and stability, and micelles have controllable particle size, uniform distribution range and good storage stability. Through ocular surface administration, the eye drops effectively target and are absorbed by trigeminal ganglion, thus raising safety and effectiveness of the medicine in treating diabetic keratopathy and nervous lesion.

Description

technical field [0001] The invention relates to an eye drop, in particular to a hydroxytyrosol eye drop capable of effectively targeting the trigeminal ganglion 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 effect...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/05A61K47/18A61K47/32A61P3/10A61P27/02A61P25/00
CPCA61K9/0048A61K9/08A61K31/05A61K47/18A61K47/32
Inventor 陈豪郑洲王斌陈鹏吴祥根
Owner QINGDAO UNIV
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