Voriconazole-coated carrageenan corneal contact lens and preparation method thereof

A technology of voriconazole and glue cornea, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc. It can solve the problems of the preparation method of entrapped voriconazole that have not been reported, and improve treatment compliance Sex, reduce dosage, improve the effect of treatment effect

Pending Publication Date: 2021-06-22
THE AFFILIATED HOSPITAL OF QINGDAO UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there has been no report on carrageenan contact lenses embedded with voriconazole and its preparation method

Method used

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  • Voriconazole-coated carrageenan corneal contact lens and preparation method thereof
  • Voriconazole-coated carrageenan corneal contact lens and preparation method thereof
  • Voriconazole-coated carrageenan corneal contact lens and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] The components and contents of the voriconazole-embedded carrageenan contact lens involved in this embodiment are as follows: successively add silver salt solution and voriconazole solution to the carrageenan aqueous solution, and the mass volume ratio of the carrageenan aqueous solution to the silver salt solution and the voriconazole solution is: 10 grams: 5-15 microliters: 7-13 microliters, wherein the mass percentage concentration of the carrageenan aqueous solution is 0.99-10%, the voriconazole solution is the voriconazole DMSO solution with a mass concentration of 0.1-5 mg / microliter, silver salt solution Be the silver nitrate aqueous solution that molar concentration is 0.1 mol / liter; Concrete preparation process step comprises:

[0030] (1) Preparation of carrageenan solution: Weigh 0.099-1 gram of κ-carrageenan, add 9-9.901 grams of sterilized deionized water, heat in a water bath to 50-90°C, stir for 0.5-3 hours, and configure the mass percentage concentration ...

Embodiment 2

[0035] The components and contents of the voriconazole-embedded carrageenan contact lens involved in this embodiment are as follows: successively add silver salt solution and voriconazole solution to the carrageenan aqueous solution, and the mass volume ratio of the carrageenan aqueous solution to the silver salt solution and the voriconazole solution is: 10 grams: 5-15 microliters: 7-13 microliters, wherein the mass percentage concentration of the carrageenan aqueous solution is 0.99-10%, the voriconazole solution is the voriconazole DMSO solution with a mass concentration of 0.1-5 mg / microliter, silver salt solution Be the silver nitrate aqueous solution that molar concentration is 0.1 mol / liter; Concrete preparation process step comprises:

[0036] (1) Preparation of carrageenan solution: Weigh 0.3 g of κ-carrageenan, add 9.7 g of sterilized deionized water, heat in a water bath to 70° C., stir for 1 hour, and configure a carrageenan aqueous solution with a mass percentage c...

Embodiment 3

[0041] This example relates to an in vitro release test of a carrageenan contact lens embedded with voriconazole.

[0042] Step 1: draw the absorbance-concentration standard curve of voriconazole: first detect the ultraviolet absorption spectrum of voriconazole in the wavelength range of 200-350nm (such as figure 2 Shown in A), set 255nm as the voriconazole detection peak, then carry out the 255nm ultraviolet absorption peak measurement to the concentration gradient of 0 to 80 mg / liter voriconazole DMSO solution, draw the absorbance-concentration standard curve of voriconazole (such as figure 2 shown in B).

[0043] Step 2: Put 5 corneal contact membranes with a diameter of 14mm prepared in Example 2 into a dialysis bag (MWCO1000Da), completely immerse the dialysis bag in 100mL of PBS buffer solution (PH=7.4), and then rotate at a speed of 37 rpm , shake at a temperature of 37°C, take samples at the time points of shaking 0, 0.25h, 0.5h, 1h, 2h, 3h, 4h, 5h, 6h, 8h, 10h, 12h...

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Abstract

The invention relates to the technical field of ophthalmic dosage forms and medical materials, and relates to a voriconazole-coated carrageenan corneal contact lens which is prepared by the following components according to the content: sequentially adding a silver salt aqueous solution and a voriconazole solution into a carrageenan aqueous solution, wherein the mass volume ratio of the carrageenan aqueous solution to the silver salt aqueous solution to the voriconazole solution is 10 g: (5-15) microliter: (7-13) microliter, the mass percent concentration of the carrageenan aqueous solution is 0.99-10%, the voriconazole solution is a voriconazole DMSO solution with the mass concentration of 0.1-5 mg/microliter, and the silver salt aqueous solution is a silver nitrate aqueous solution with the molar concentration of 0.1 mol/liter; the added silver ions can promote gelation of carrageenan, and the silver elementary substance can kill fungi, so that the dosage of voriconazole is reduced, the drug release time can be prolonged to 24 hours, the frequency of eye administration is reduced, the local eye stimulation symptom is relieved and the treatment effect on fungal keratitis is improved.

Description

Technical field: [0001] The invention relates to the technical field of ophthalmic dosage forms and medical materials, and relates to a voriconazole-embedded carrageenan corneal contact lens and a preparation method thereof, in particular to a corneal contact lens prepared with voriconazole and carrageenan, which has a long drug release time and is safe and non-irritating , with good adhesion to the cornea, for the treatment of fungal keratitis. [0002] technical background: [0003] Fungal keratitis is a disease of the cornea caused by pathogenic fungal infection. my country, as a developing country with industry and agriculture as its main industry, is a high-incidence area of ​​fungal keratitis. Corneal trauma, especially plant trauma during production activities provides opportunities for the occurrence of fungal keratitis. The population continues to expand and some antibiotics and hormones are still being abused clinically. In recent years, the incidence of fungal kera...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/36A61K33/38A61K31/506A61P27/02A61P31/02A61P31/10
CPCA61K47/36A61K33/38A61K31/506A61P27/02A61P31/02A61P31/10
Inventor 赵桂秋李翠李道浩彭旭东宋奎文王谦
Owner THE AFFILIATED HOSPITAL OF QINGDAO UNIV
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