Application of Tripterygium in Preparation of Anti-Keratoplasty Rejection Eye Drops

A technology of triptolide and transplant rejection, which is applied in the intersection of biomedical materials and medicine, can solve the problems of undiscovered ophthalmic diseases, limited clinical application and curative effect, poor water solubility, etc., and achieves anti-corneal transplant rejection and high encapsulation. rate, the effect of high drug loading

Active Publication Date: 2019-04-26
河南省眼科研究所
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although Celastrol has strong biological activity and is a potential drug for anti-inflammation and anti-corneal neovascularization, its poor water solubility limits its further clinical application and curative effect. Reports on Eye Diseases

Method used

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  • Application of Tripterygium in Preparation of Anti-Keratoplasty Rejection Eye Drops
  • Application of Tripterygium in Preparation of Anti-Keratoplasty Rejection Eye Drops
  • Application of Tripterygium in Preparation of Anti-Keratoplasty Rejection Eye Drops

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Weigh 10.0 g of ternary block copolymer PEG-PCL-PEI and 3.0 g of tripterine, and dissolve them together in 20 mL of a mixed solvent consisting of methanol and acetonitrile at a volume ratio of 1:1; then, under ultrasonic stirring, Add the mixture dropwise to 50mL of water for injection, vacuum distill to remove the organic solvent, and then pass through an ultrafiltration device (molecular weight cut-off: 100,000 Da) for 3 times to remove free tripterine to obtain drug-loaded polymer micelles , adding water for injection to make the volume to 100mL, to obtain tripterine eye drops.

Embodiment 2

[0016] The difference from Example 1 is: 10.0 g of PEG-PCL-PEI, 1.5 g of tripterine, and the others are the same as in Example 1.

Embodiment 3

[0018] The difference from Example 1 is: 10.0 g of PEG-PCL-PEI, 0.75 g of tripterine, and the others are the same as in Example 1.

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Abstract

The invention belongs to the crossing field of biomedical materials and medical science and particularly discloses application of celastrol in the preparation of keratoplasty rejection resistant eye drops preparations. Eye drops are prepared by: weighing 7.04-67.55 g of Three-element block copolymer PEG-PCL-PEI and 0.68-2.11 g of celastrol, and co-dissolving in a mixed solvent composed of methanol and acetonitrile at a volume ratio of 1:(1-3); dropwise adding mixed liquid into injection water of dissolution equivalent under ultrasonic stirring, removing the organic solvent by vacuum distilling, removing free celastrol by ultrafiltration to obtain drug-loading polymer micelles, and additionally adding injection water to fixed volume of 100 mL; PEG-PCL-PEI is used as a support for the first time to load celastrol to produce eye drops, ocular surface administration is implemented, and the eye drops have millstone significance.

Description

technical field [0001] The invention belongs to the interdisciplinary field of biomedical materials and medicine, and in particular relates to the application of tripterine in the preparation of anti-corneal transplantation rejection eye drop preparation. Background technique [0002] Corneal disease is one of the most common diseases in ophthalmology, and the blinding rate ranks second. Corneal transplantation is the most effective way to treat corneal blindness. Postoperative corneal graft rejection is the most important factor in surgical failure. Corneal transplant rejection is an immune inflammatory response caused by the host against the graft. At present, clinically, drugs to prevent and treat rejection after keratoplasty mainly include: glucocorticoids, cyclosporine A (CsA), tacrolimus (FK506), etc. Local and long-term use of glucocorticoids can induce glaucoma, cataract, etc., and systemic use has greater side effects; CsA has a large molecular weight, poor water...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/56A61K9/107A61K47/34A61P37/06A61P27/02
CPCA61K9/0048A61K9/1075A61K31/56A61K47/34
Inventor 栗占荣李景果祝磊张颖张俊杰王丽娅
Owner 河南省眼科研究所
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