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Thermo-sensitive hydrogel for inhibiting corneal stromal fibrosis and preparation method of thermo-sensitive hydrogel

A technology of temperature-sensitive hydrogel and corneal stroma, which is applied in the direction of medical formulations, organic active ingredients, and medical preparations of non-effective ingredients, etc., can solve the problems of poor drug treatment effect and undiscovered corneal stroma fibrosis, etc. To achieve the effect of enhancing the apparent solubility

Pending Publication Date: 2022-04-26
河南省立眼科医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] There are three unique barriers in ocular drug delivery: tear film, cornea and blood-aqueous humor barrier, making the bioavailability of topical drug delivery less than 5%, resulting in poor therapeutic effect
So far, no reports have been found on the application of its pharmaceutical preparations to inhibit corneal stromal fibrosis

Method used

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  • Thermo-sensitive hydrogel for inhibiting corneal stromal fibrosis and preparation method of thermo-sensitive hydrogel

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] This embodiment provides a tripterine thermosensitive hydrogel, the preparation method of which comprises:

[0028] (1) Weigh 10g polyethylene glycol 15-hydroxystearate and 0.8g tripterine, and dissolve them in 10mL absolute ethanol;

[0029] (2) Under ultrasonic stirring, add the mixed solution obtained in step (1) dropwise into 100 mL of water for injection, and remove absolute ethanol by rotary evaporation to obtain drug-loaded polymer micelles;

[0030] (3) 1 g of drug-loaded polymer micelles obtained in step (2) and 1.8 g of chitosan-based polymer hydrogel (TSG) are mixed, and after mixing, add water for injection to make the volume to 100 mL.

[0031] Tripteryglide thermosensitive hydrogel prepared in this example is in a liquid state in a low temperature environment (20°C) in vitro, and becomes solid when the temperature rises to body temperature (32°C) (see figure 1 A).

Embodiment 2

[0033] The difference from Example 1 is that the consumption of tripterine is 1.5g, and the others are the same as in Example 1.

[0034] The appearance properties of tripterine thermosensitive hydrogel prepared in this example are not significantly different from those in Example 1 at different temperatures.

Embodiment 3

[0036] The difference from Example 1 is that the consumption of tripterine is 0.1 g, and the others are the same as in Example 1.

[0037] The appearance properties of tripterine thermosensitive hydrogel prepared in this example are not significantly different from those in Example 1 at different temperatures.

[0038] animal testing

[0039] The temperature-sensitive tripterine hydrogel prepared in Example 1 was used to evaluate the anti-corneal stromal fibrosis effect of the tripterycin thermo-sensitive hydrogel using New Zealand white rabbit lamellar keratoplasty as an animal model. The specific method refers to the published article (ACS Applied Bio Materials 2021 4(4), 3579-3586), and the detailed steps are as follows:

[0040] 3% pentobarbital sodium saline solution was injected into ear vein to induce general anesthesia in New Zealand white rabbits, and the dose was calculated according to 3ml / kg. Povidone-iodine disinfected the eye area, rinsed the conjunctival sac w...

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Abstract

The embodiment of the invention discloses thermo-sensitive hydrogel for inhibiting corneal stromal fibrosis and a preparation method of the thermo-sensitive hydrogel. The preparation method comprises the following steps: dissolving polyethylene glycol-15 hydroxy stearate and tripterine in an organic solvent to obtain a mixed solution; under ultrasonic stirring, dropwise adding the obtained mixed solution into water for injection, and carrying out rotary evaporation to remove the organic solvent, so as to obtain a drug-loaded polymer micelle; and preparing and uniformly mixing the drug-loaded polymer micelle and the temperature-sensitive polymer hydrogel, and supplementing water for injection, so as to obtain the tripterine temperature-sensitive hydrogel. The tripterine thermo-sensitive hydrogel provided by the invention can improve the water solubility of the medicine and prolong the action time of the medicine, and can be injected in the operation process and effectively inhibit corneal stromal fibrosis.

Description

technical field [0001] The embodiments of the present invention relate to the technical field of pharmaceutical preparations, in particular to a thermosensitive hydrogel for inhibiting corneal stroma fibrosis and a preparation method thereof. Background technique [0002] There are about 5 million patients with corneal blindness in my country, which is the second most common blindness eye disease in my country. It brings heavy economic and spiritual burdens to patients and their families, and a huge social burden to the country. Corneal trauma, surgery, infection, etc. can lead to corneal stroma fibrosis. Corneal stromal fibrosis is the most common manifestation of corneal blindness, which can lead to vision loss and is also one of the important reasons for affecting vision after lamellar keratoplasty. There is no clinically approved drug that can reverse fibrosis. To alleviate corneal scarring, the main topical drugs currently include glucocorticoids and mitomycin C. Howe...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K47/14A61K47/36A61K31/56A61P27/02
CPCA61K9/06A61K9/0048A61K47/14A61K47/36A61K31/56A61P27/02
Inventor 栗占荣李景果刘瑞星祝磊张颖张俊杰
Owner 河南省立眼科医院
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