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Preparation method of injectable hydrogel for controlled release of voriconazole intraocular drug

A voriconazole ophthalmic and drug-controlled release technology, which is applied in the field of injectable hydrogel preparation, can solve the problems of increased patient pain, economic burden, poor biocompatibility of the voriconazole sustained-release system, and poor long-term controlled release effect. To achieve the effect of long-acting drug controlled release, pain relief and economic burden

Active Publication Date: 2020-02-18
QINGDAO UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] The purpose of the present invention is to solve the problems of rapid metabolism of existing voriconazole preparations, need for repeated administration, increased patient pain and economic burden, poor biocompatibility of existing voriconazole slow-release systems, and poor long-acting controlled-release effects

Method used

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  • Preparation method of injectable hydrogel for controlled release of voriconazole intraocular drug
  • Preparation method of injectable hydrogel for controlled release of voriconazole intraocular drug
  • Preparation method of injectable hydrogel for controlled release of voriconazole intraocular drug

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specific Embodiment approach 1

[0047] Embodiment 1: This embodiment is a preparation method of an injectable hydrogel for controlled release of voriconazole intraocular drug, which is specifically completed according to the following steps:

[0048] 1. Preparation of white flocculent polyaldehyde dextran:

[0049] ①. Dissolve dextran in distilled water at a temperature of 50°C to 60°C to obtain a dextran solution; cool the dextran solution to 20°C to 25°C, then dissolve sodium periodate into the dextran In the solution, react at a temperature of 20°C to 25°C for 2 hours, add ethylene glycol, react at a temperature of 20°C to 25°C for 2 hours, and finally stand at room temperature for 4 hours to obtain an orange solution;

[0050] The volume ratio of the mass of dextran described in step 1. to distilled water is (3g~6g): 100mL;

[0051] The volume ratio of the amount of the substance of sodium periodate described in step 1. and distilled water is (18.52mmol~37.04mmol): 100mL;

[0052] The mol ratio of the ...

specific Embodiment approach 2

[0076] Embodiment 2: The difference between this embodiment and Embodiment 1 is that the molecular weight of the dextran described in step ① is 40,000. Other steps are the same as in the first embodiment.

specific Embodiment approach 3

[0077] Embodiment 3: The difference between this embodiment and Embodiment 1 or 2 is that the dialysis bag described in Step 1 ② is MD44 imported from the United States, with a molecular weight cut-off of 8,000-14,000. Other steps are the same as those in Embodiment 1 or 2.

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Abstract

The invention discloses a preparation method for injectable hydrogel for controlled release of a voriconazole intraocular drug, and relates to the preparation method for injectable hydrogel. The preparation method aims to solve the problems that an existing voriconazole preparation is fast in metabolism and needs to be repeatedly supplied, the body pain and economic burden of a patient are increased, and an existing voriconazole sustained release system is poor in biocompatibility and poor in long-acting controlled-release effect. The method comprises the following steps of 1, preparing whiteflocculent polyaldehyde dextran; 2, preparing water-soluble linear poly-beta-cyclodextrin; and 3, firstly preparing a PBS solution of the water-soluble linear poly-beta-cyclodextrin with voriconazoleloaded in a cyclodextrin molecular cage, and then dissolving carboxymethyl chitosan into the PBS solution so as to obtain the injectable hydrogel for controlled release of the voriconazole intraoculardrug. According to the preparation method, the half-life of the prepared injectable hydrogel for controlled release of the voriconazole intraocular drug in a vitreous cavity is 30-60 days; and the injectable hydrogel for controlled release of the voriconazole intraocular drug can be obtained.

Description

technical field [0001] The invention relates to a preparation method of injectable hydrogel. Background technique [0002] Fungal endophthalmitis is a fungal infection of the eye. In recent years, the incidence rate has been on the rise. The onset is hidden, early diagnosis is difficult, the course of the disease is long, and it is easy to relapse. It often causes vision loss and eyeball atrophy. It is reported that 24% of exogenous endophthalmitis and 16% of endogenous endophthalmitis end with enucleation or enucleation of eye contents, and severe cases may die from sepsis, thus improving the cure of fungal endophthalmitis rate and prognosis are critical. [0003] Voriconazole (Voriconazole, UK.109,496), chemical name: (2R,3S)-2-(2,4-difluorophenyl)-3-(5-fluoropyrimidin-4-yl)-1-(1H -1,2,4-Triazole-1-yl)-2-butanol is a second-generation triazole broad-spectrum antifungal drug developed by American Rising Company and approved by the US FDA in June 2002. It was first listed...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/06A61K47/36A61K47/69A61K31/506A61P31/10A61P27/02
CPCA61K9/0048A61K9/06A61K31/506A61K47/36A61K47/6951A61P27/02A61P31/10
Inventor 杨超丛海林马修彬迟晓东
Owner QINGDAO UNIV
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