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Long-acting tretnoin intraocular slow-releasing system

A retinoic acid, long-acting technology, applied in non-active ingredients medical preparations, anhydride/acid/halide active ingredients, sensory diseases, etc., can solve the problems of inability to come out, increased drug release, etc., and achieve high drug effect. Effect

Inactive Publication Date: 2003-08-06
INST OF CHEM CHINESE ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because the problem of the drug carrier has not been solved, so far, the retinoic acid implantation preparation with long-term drug release function has not yet come out.
In addition, as the material degrades, the structure becomes looser and the drug is released from it more easily, thus tending to increase the amount of drug released

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Copolymer (lactic acid / glycolic acid) (PLGA) (molecular weight: 110,000) 15 parts, dissolve with 20 parts of dichloromethane, add 10 parts of retinoic acid powder, stir evenly, pour into polytetrafluoroethylene mold, control the airflow speed, make dichloromethane Methane evaporates. After being completely dried, this copolymer (lactic acid / glycolic acid) drug slow-release system containing retinoic acid was taken off from the polytetrafluoroethylene mold, kept in a vacuum oven at room temperature for 48 hours to completely remove the solvent, and obtained a thickness of 2 mm and a sheet-like medicament with a pore structure of 10 nanometers, and then use a die with an aperture of 2 mm to punch a retinoic acid sustained-release system with a thickness of 2 mm and a diameter of 2 mm. The retinoic acid slow-release system was sterilized by fumigation with ethylene oxide for 24 hours, and placed in the vitreous cavity of the rabbit eye after being left for 1 week.

[0019...

Embodiment 2

[0022] According to the method and steps of Example 1, but adopting 10 parts of poly DL-lactic acid (PDLLA) (molecular weight 60,000), 20 parts of methylene chloride and 4 parts of retinoic acid, a medicine rod with a diameter of 2 mm is obtained, and a diameter of 2 mm is obtained. 2 mm, pore structure of 10 nanometers of drug rods, kept in a vacuum oven at room temperature for 48 hours to completely remove the solvent and then cut into 2 mm long retinoic acid sustained-release system. The retinoic acid slow-release system was sterilized by fumigation with ethylene oxide for 24 hours, placed for another week, and then implanted into the vitreous cavity of the rabbit eye in the same manner as in Example 1. The results of postoperative macroscopic observation and local histopathological examination showed that the retinoic acid sustained-release system has good intraocular biocompatibility, and retinoic acid can maintain a certain concentration in the aqueous humor within 10 wee...

Embodiment 3

[0024] According to the method and steps of Example 1, but using (prepared by the method of Chinese invention patent application number 99105984.0) (glycolic acid / lactic acid / caprolactone) terpolymer (PGLC) (molecular weight 80,000) 10 parts, dichloro 18 parts of methane and 9 parts of retinoic acid were used to obtain a block with a length of 10 mm on each side, which was kept in a vacuum oven at room temperature for 48 hours to completely remove the solvent and then cut into a 2 mm square retinoic acid sustained-release system. The retinoic acid slow-release system was sterilized by fumigation with ethylene oxide for 24 hours, placed for another week, and then implanted into the vitreous cavity of the rabbit eye in the same manner as in Example 1.

[0025] The results of postoperative macroscopic observation and local histopathological examination showed that the retinoic acid sustained-release system has good intraocular biocompatibility. The retinoic acid can maintain a cer...

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PUM

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Abstract

The present invention relates to a long-acting tretinoin intraocular slow-releasing system, including tretinoin and medicinal carrier, their weight ratio is 0.1:0.9-0.9:0.1, the medicinal carrier canbe synthetic biodegradable high-molecular material, natural biodegradable high-molecular material or their mixture. The medicine-releasing period of said invented long-acting tretinoin slow-releasingsystem is one week to one year. It has the important regulation action for proliferation and differentiation of cell, can influence differentiation and proliferation of tissue cell so as to can inhibit the growth of retinal pigment epithelial cell and fibroblast and production of PVR.

Description

technical field [0001] The invention relates to a drug preparation for implantation in the body, in particular to a long-acting retinoic acid intraocular slow-release system using a biodegradable polymer material as a drug carrier. Background technique [0002] PVR (Proliferative Vitreoretinopathy, PVR) is a pathological process that occurs in rhegmatogenous retinal detachment, or after penetrating eyeball injury, intraocular cell proliferation, fibrous membrane shrinkage, and eventually retinal detachment. PVR is the leading cause of failure in retinal detachment surgery and the final adverse outcome of many repairs of severe ocular trauma. Although vitrectomy can greatly improve the success rate of PVR, 7-10% of patients still have PVR after operation. Multiple surgical treatments will not only reduce the success rate of retinal reattachment, but also increase the possibility of PVR recurrence. Therefore, the prevention of PVR is more important than the treatment of PVR....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/19A61K47/30A61P27/02
Inventor 王身国董晓光贝建中陈楠陈文娜
Owner INST OF CHEM CHINESE ACAD OF SCI
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