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Preparation method of brinzolamide imprinted hydrogel contact lens for sustained and controlled release administration

A contact lens and hydrogel technology, which is applied in the direction of medical formula, glasses/goggles, medical preparations with non-active ingredients, etc., can solve the problems of large side effects and low bioavailability, achieve long residence time and increase flexibility Sex and oxygen permeability, the effect of avoiding environmental pollution and harm to the human body

Active Publication Date: 2020-07-17
TIANJIN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The object of the present invention is to provide a preparation method of brinzolamide imprinted hydrogel contact lens for sustained and controlled release administration; Contact lenses can solve the problems of low bioavailability and large side effects of conventional ophthalmic preparations, so as to better exert the therapeutic effect on eye diseases

Method used

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  • Preparation method of brinzolamide imprinted hydrogel contact lens for sustained and controlled release administration
  • Preparation method of brinzolamide imprinted hydrogel contact lens for sustained and controlled release administration
  • Preparation method of brinzolamide imprinted hydrogel contact lens for sustained and controlled release administration

Examples

Experimental program
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Effect test

Embodiment 1

[0024] Example 1. Preparation of Molecularly Imprinted Hydrogel Contact Lens Using Brinzolamide as a Template

[0025] Preparation of DES hydrophilic monomer:

[0026] Choline chloride (3.75 g) and methacrylic acid (4.2 ml) were added to a glass ampoule, and magnetically stirred in an oil bath at 90°C for 24 hours to form a clear and transparent solution, which was stored at room temperature.

[0027] Preparation of pre-polymerization solution:

[0028]Template brinzolamide (0.0455 g), backbone monomer hydroxyethyl methacrylate (1397.5 μL), functional monomer DES (12.9 μL), cross-linking agent polyethylene glycol dimethacrylate (607.5 μL) were added Put it into a glass ampoule, sonicate for 10 minutes until it is uniform and transparent; then add the initiator AIBN (0.0125 g), and treat it with ultrasonication (40 w) at room temperature for 20 minutes to make it dissolve evenly. Afterwards, nitrogen was purged for 10 minutes, and then the solution was left in the dark for 10...

Embodiment 2

[0033] Embodiment 2, the evaluation of hydrogel contact lens loading capacity

[0034] Carry out according to embodiment 1 step, obtain hydrogel contact lens. Take 10 parts of dried hydrogel lenses, place them in ethanol solution of bulinamide (concentration: 0.1mM-5mM), seal with parafilm, and shake the mixed solution on a constant temperature oscillator for 24h. After equilibrium, centrifuge for 5 minutes in a high-speed centrifuge (5000r / min), take 100 μL of supernatant, and dilute to 10ml with ethanol. The absorbance was then measured with a UV spectrophotometer. according to The adsorption amount was calculated and fitted with the Langmuir-Freundlich model (see image 3 ).

[0035] The detection wavelength is 252nm.

Embodiment 3

[0036] Embodiment 3, the release of brinzolamide drug

[0037] Carry out according to embodiment 1 step, obtain hydrogel contact lens. The obtained lenses were soaked in 100 μg / mL brinzolamide ethanol solution for 3 days, and then washed with distilled water for 5 minutes to remove surface residues. Put the washed lens into a glass bottle containing 10ml of ethanol, put it into the rotor and stir it on a constant temperature magnetic stirrer (rotating speed is 50rp / min), take out 2-3ml from it at regular intervals, and use Measure the absorbance with a UV spectrophotometer (252nm) until there is no significant change in the absorbance. The cumulative release percentage of brinzolamide is plotted against time to obtain the in vitro release curve of the contact lens to the drug (see Figure 4 ).

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Abstract

The invention discloses a preparation method of a molecularly imprinted hydrogel contact lens for sustained and controlled release administration. The method comprises the following steps: mixing choline chloride and methacrylic acid according to a certain proportion, and preparing a hydrophilic functional monomer deep eutectic solvent (DES) in an oil bath at 90 DEG C; taking brinzolamide as a template, hydroxyethyl methacrylate as a framework monomer, DES as a functional monomer, and polyethylene glycol dimethacrylate as a crosslinking agent to perform ultrasonic treatment under action of aninitiator AIBN to obtain a pre-polymerization solution; removing oxygen from the pre-polymerization solution, performing balancing in the dark, then injecting the pre-polymerization solution into a mold, performing ultraviolet polymerization, performing cutting by a round punch, performing eluting to remove unreacted substances, and performing drying to obtain the hydrogel contact lens. The hydrogel contact lens prepared by the preparation method has large drug loading amount, can realize slow release of drugs, and has the advantages of greatly improved bioavailability, good permeability, longretention time, better convenience and higher efficiency compared with a traditional ophthalmic preparation.

Description

technical field [0001] The invention relates to a preparation method of brinzolamide imprinted hydrogel contact lens for sustained and controlled release administration, and the contact lens is obtained by combining molecular imprinting technology with hydrogel. The contact lens can not only be loaded with a therapeutic dose of brinzolamide to treat glaucoma, but also can continuously administer the drug to the eyes to achieve an effective therapeutic effect. Background technique [0002] Glaucoma is the second leading cause of blindness in the world. It is a progressive optic neuropathy caused by pathological high intraocular pressure, characterized by apoptosis of retinal ganglion cells and gradual loss of visual function. At present, the treatment of glaucoma has become a research hotspot in the medical field. The drugs used to treat glaucoma mainly include timolol (C 13 h 24 N 4 o 3 S), carteolol (C 16 h 24 N 2 o 3 ), pilocarpine (C 11 h 16 N 2 o 2 ) and Bri...

Claims

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Application Information

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IPC IPC(8): A61K31/542A61K9/00A61K47/32A61K47/54A61P27/06C08F220/06C08F2/48C08F2/44C08J3/075C08J3/28C08L33/02G02C7/04
CPCG02C7/049C08F220/06C08F2/48C08F2/44C08J3/075C08J3/28A61K31/542A61K9/0048A61K47/32A61K47/554A61K47/542A61P27/06C08J2333/02C08F220/56
Inventor 黄艳萍丰景赵泷刘照胜
Owner TIANJIN MEDICAL UNIV
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