Resveratrol micelle eye drops and preparation method thereof

A technology of resveratrol and eye drops, applied in the directions of emulsion delivery, metabolic diseases, sensory diseases, etc., can solve the problems of only 3 months of effective stability, limited therapeutic effect, no mitochondrial targeting, etc. Prolonged drug action time, good solubility and good drug stability

Inactive Publication Date: 2015-12-09
滨州医学院烟台附属医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, it has the following disadvantages: (1) The micelles constructed by polyethylene caprolactam-polyvinyl acetate-polyethylene glycol copolymer have no mitochondrial targeting, and the ocular surface administration of antioxidant drugs such as resveratrol can partially correct corneal damage. The redox imbalance in the body, the subcellular organ that acts on is the mitochondria, but because the micelles canno

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  • Resveratrol micelle eye drops and preparation method thereof
  • Resveratrol micelle eye drops and preparation method thereof
  • Resveratrol micelle eye drops and preparation method thereof

Examples

Experimental program
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Example Embodiment

[0020] Example 1:

[0021] Put 50mg resveratrol, 25mg dequinium chloride and 1g polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol (molecular weight 118000) in a 100mL round bottom flask, add 10mL absolute ethanol, after fully dissolving, 40 Dehydrated ethanol was evaporated in a rotary vacuum in a water bath to obtain a uniformly dispersed film of the drug and the copolymer, then distilled water was added, the film was fully washed, and the micellar solution was obtained by ultrasonicating in a water bath with a power of 200w for 15 min. After passing the micelle solution through a 0.22 μm microporous membrane, freeze-drying was performed to obtain micelle powder. Then, use 10 mL of borate buffer to disperse and dissolve the micellar powder, add the preservative benzalkonium chloride, and the isotonicity regulator sodium chloride, adjust the pH to 7.4, and sterile filter and pack. The average particle size of resveratrol micelles measured by laser particle size an...

Example Embodiment

[0022] Example 2:

[0023] Put 50mg resveratrol, 26.7mg dequinium chloride and 1.2g polyvinylcaprolactam-polyvinyl acetate-polyethylene glycol (molecular weight 118000) in a 100mL round-bottom flask, add 10mL absolute ethanol, and dissolve it fully. , 40 ℃ water bath rotary vacuum evaporation of absolute ethanol to obtain a uniformly dispersed film of drug and copolymer, then add distilled water, fully wash the film, 200w power water bath ultrasonic for 15min, to obtain a micelle solution. After passing the micelle solution through a 0.22 μm microporous membrane, freeze-drying was performed to obtain micelle powder. Then, use 10 mL of borate buffer to disperse and dissolve the micellar powder, add the preservative benzalkonium chloride, and the isotonicity regulator sodium chloride, adjust the pH to 7.4, and sterile filter and pack. The average particle size of resveratrol micelles measured by laser particle size analyzer was 97 nm, the dispersion index PDI=0.036, and the d...

Example Embodiment

[0024] Example 3:

[0025] Put 50mg resveratrol, 26.2mg dequinium chloride and 1.1g polyvinylcaprolactam-polyvinyl acetate-polyethylene glycol (molecular weight 118000) in a 100mL round-bottom flask, add 10mL absolute ethanol, fully dissolve , 40 ℃ water bath rotary vacuum evaporation of absolute ethanol to obtain a uniformly dispersed film of drug and copolymer, then add distilled water, fully wash the film, 200w power water bath ultrasonic for 15min, to obtain a micelle solution. After passing the micelle solution through a 0.22 μm microporous membrane, freeze-drying was performed to obtain micelle powder. Then, use 10 mL of borate buffer to disperse and dissolve the micellar powder, add the preservative benzalkonium chloride, and the isotonicity regulator sodium chloride, adjust the pH to 7.4, and sterile filter and pack. The average particle size of resveratrol micelles measured by laser particle size analyzer was 94 nm, the dispersion index PDI=0.035, and the dispersio...

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Abstract

The invention discloses resveratrol micelle eye drops. The resveratrol micelle eye drops are prepared from resveratrol which serves as a main drug, a preservative and an isoosmotic adjusting agent. The resveratrol micelle eye drops are characterized by being further prepared from a polyethylene caprolactam-polyvinyl acetate-polyethylene glycol copolymer which serves as a pharmaceutical necessity, dequalinium which serves as a mitochondrion target modifier and a stabilizer, wherein the mass ratio of the main drug of the resveratrol to the pharmaceutical necessity of the polyethylene caprolactam-polyvinyl acetate-polyethylene glycol copolymer ranges from 1:20 to 1:24, and the mass ratio of the dequalinium to the pharmaceutical necessity of the polyethylene caprolactam-polyvinyl acetate-polyethylene glycol copolymer ranges from 1:40 to 1:45. According to the resveratrol micelle eye drops, the administration concentration can reach 5 mg/ml, the micelle particle size is small, the distribution range is uniform, and the drug stability is good; the administration irritation is reduced, absorption of corneas on the drug is improved, the administration concentration is reduced, the drug acting time is prolonged, the administration times are decreased, the patient compliance is improved, and the good economical efficiency is achieved.

Description

technical field [0001] The invention relates to a resveratrol eye drop, in particular to a resveratrol micelle eye drop 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 economic and mental burden of patients 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 treatment measures f...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/05A61K47/34A61K47/22A61P27/02A61P3/10
Inventor 辛萌童琳
Owner 滨州医学院烟台附属医院
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