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Dexamethasone in-situ liquid crystal gel preparation for treating diabetic retinopathy and preparation method and application thereof

A technology for diabetic retina and dexamethasone, which is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, metabolic diseases, etc., can solve problems such as short half-life, achieve high long-term stability, improve drug biological Availability, the effect of reducing the number of doses

Pending Publication Date: 2022-01-04
ANHUI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these methods have a short half-life, and all the drug is released within a few hours

Method used

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  • Dexamethasone in-situ liquid crystal gel preparation for treating diabetic retinopathy and preparation method and application thereof
  • Dexamethasone in-situ liquid crystal gel preparation for treating diabetic retinopathy and preparation method and application thereof
  • Dexamethasone in-situ liquid crystal gel preparation for treating diabetic retinopathy and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] A method for preparing dexamethasone in situ liquid crystal gel preparation, comprising the following steps:

[0031] (1) Accurately weigh 65 mg of phytantriol and heat in a water bath at 60° C. as the oil phase.

[0032] (2) Precisely weigh 1 mg of dexamethasone, 30 mg of PEG400, and 5 μL of water for injection and heat in a water bath until the drug dexamethasone is dissolved as the water phase.

[0033] (3) Add the water phase to the oil phase, and quickly vortex it until it is colorless and transparent after adding, to obtain the dexamethasone in-situ liquid crystal gel preparation. Liquid crystal gels are liquid and semi-solid gels before and after in-situ (phase transition).

Embodiment 2

[0035] Phase inversion properties of dexamethasone in situ liquid crystal gel

[0036] Minimum artificial tear volume for phase inversion (V m ) and time (T g )

[0037] Take the dexamethasone in situ liquid crystal gel prepared in Example 1 for the experiment of phase inversion properties. Determination of the V of the formulation using the tube inversion method m and T g . Accurately weigh 200 mg of dexamethasone in-situ liquid crystal gel in a centrifuge tube. In order to simulate the human body environment, place the sample in a 37°C water bath, add 20 μL of artificial tears in sequence, vortex quickly, and tilt the sample at 90° to observe whether the sample is gelling. Complete gelation of the sample was demonstrated when no flow was observed. When the preparation is completely gelled, record the total amount of artificial tears added at the end of the experiment as V m , record the gel formation time as T g .

[0038] When the precursors are exposed to artific...

Embodiment 3

[0040] Polarizing microscope observation of dexamethasone in situ liquid crystal gel

[0041] The dexamethasone in situ liquid crystal gel prepared in Example 1 was taken for polarizing microscope observation. In order to investigate the internal morphology of the gel, a small amount of sample was placed on a glass slide and covered with a cover glass, and then observed under a polarizing microscope at room temperature. The results are as follows: figure 1 As shown, both before and after in situ (phase transition) of dexamethasone liquid crystal gel are in dark field.

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Abstract

The invention discloses a dexamethasone in-situ liquid crystal gel preparation for treating diabetic retinopathy, and a preparation method and application thereof, and belongs to the technical field of diabetic retinopathy treatment drugs. The dexamethasone lipid injection is prepared from 60-70 mg of a lipid material, 0.01-3 mg of dexamethasone, 25-35 mg of a cosolvent and 0-5 [mu]L of water for injection. the lipid material is heated in a water bath at a corresponding melting temperature to serve as an oil phase, and dexamethasone, a cosolvent and water for injection are heated under a water bath condition until the medicine dexamethasone is dissolved to serve as a water phase; and the water phase is added into the oil phase, and quick whirling is performed until the mixture is colorless and transparent. According to the dexamethasone in-situ liquid crystal gel preparation, efficient eye application of dexamethasone is achieved, the dexamethasone in-situ liquid crystal gel preparation has the advantages of being convenient to administrate and capable of rapidly gelling after being dripped into eyes, and meanwhile the dexamethasone in-situ liquid crystal gel preparation is safe, free of stimulation, good in biological adhesion and long in eye residence time, so that the administration frequency is reduced, the bioavailability of drugs is improved, and the curative effect of dexamethasone on treating diabetic retinopathy can be enhanced.

Description

technical field [0001] The invention belongs to the technical field of drugs for treating diabetic retinopathy, and in particular relates to a dexamethasone in-situ liquid crystal gel preparation, preparation method and application for treating diabetic retinopathy. Background technique [0002] As the global prevalence of diabetes continues to increase, diabetic retinopathy remains the leading cause of vision loss in many developed countries. Diabetic retinopathy is the most common and serious eye disease caused by diabetes. According to the literature, about one-third of diabetic patients have signs of diabetic retinopathy, and one-third of them may have vision-threatening retinopathy, defined as severe retinopathy or macular edema. Diabetic retinopathy not only affects vision but also increases the risk of vascular complications. [0003] Diabetic retinopathy is divided into two stages, the early non-proliferative diabetic retinopathy stage and the late proliferative di...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K9/06A61K47/14A61K47/10A61K47/26A61K31/573A61P3/10A61P9/10A61P27/02
CPCA61K9/08A61K9/06A61K9/0048A61K47/14A61K47/10A61K47/26A61K31/573A61P3/10A61P9/10A61P27/02
Inventor 储晓琴吴文青陈晶宝曹文轩
Owner ANHUI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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