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Long-ncting heparin intraocular slow-released system

A heparin, long-acting technology, applied in the field of long-acting heparin intraocular sustained release system, can solve the problems of increased drug release and failure to come out, and achieve the effects of reducing fibrous exudation, preventing posterior capsule turbidity, and less drug dosage

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, heparin implant preparations with long-term drug release function have 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

[0015] Copolymer (lactic acid / glycolic acid) (PLGA) (molecular weight: 110,000) 5 parts, dissolve with 20 parts of dichloromethane, add 15 parts of heparin powder, stir evenly, pour into polytetrafluoroethylene mold, control the airflow speed, make dichloromethane Volatile. After being completely dried, the copoly(lactic acid / glycolic acid) drug sustained-release system containing heparin was taken off from the polytetrafluoroethylene mold, and kept in a vacuum oven at room temperature for 48 hours to completely remove the solvent to obtain a thickness of 2 mm. 1. A sheet-shaped medicament with a pore structure of 10 nanometers, and then punched into a heparin sustained-release system preparation with a thickness of 2 mm and a diameter of 2 mm with a die with an aperture of 2 mm. The heparin sustained-release system preparation was sterilized by fumigation with ethylene oxide for 24 hours, and then placed in the rabbit eye for 1 week, and implanted into the posterior chamber o...

Embodiment 2

[0019] The same as the heparin copolymer (lactic acid / glycolic acid) drug sustained release system in Example 1, but implanted under the conjunctiva of the rabbit eye. As a result, the heparin sustained release system disappeared completely after 8 weeks, and no adverse biological reactions were observed. .

Embodiment 3

[0021] According to the method and steps of Example 1, but using 7 parts of poly DL-lactic acid (PDLLA) (molecular weight: 60,000), 20 parts of methylene chloride and 7 parts of heparin, a medicine stick with a diameter of 2 mm is obtained, and a diameter of 2 mm is obtained. The drug stick with a pore structure of 10 nanometers and a pore structure of 10 nanometers was kept in a vacuum oven at room temperature for 48 hours to completely remove the solvent and then cut into a heparin sustained-release system with a length of 2 millimeters. Fumigate with ethylene oxide for 24 hours to sterilize, place for another week, and then implant in the anterior chamber of the rabbit eye in the same way as in Example 1. The results of postoperative macroscopic observation and local histopathological examination showed that the heparin sustained-release system has good intraocular biocompatibility. Heparin can maintain a certain concentration in the aqueous humor within 10 weeks after impla...

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Abstract

The present invention provides a long-acting heparin intraocular slow-releasing system, including heparin and medicinal carrier; their weight ratio is 0.1:0.9-0.9:0.1. Said medicinal carrier can be synthetic biodegradable high-molecular material, natural biodegradable high-molecular material or their mixture. The medicine-releasing period of said invented long-acting heparin slow-releasing systemis one week to one year. It can be used for inhibiting formation of antithrombase, resisting conversion of fibrinogen into insoluble fibrin, inhibiting proliferation and chemotaxis of fibrolast, reducing postoperative fibrinous exudation and preventing postcapsule opacity so as to inhibit the production of after-cataract.

Description

technical field [0001] The invention relates to a drug preparation for implantation in the body, in particular to a long-acting heparin intraocular sustained-release system using a biodegradable polymer material as a drug carrier. Background technique [0002] With the development of microsurgical techniques, the clinical application of modern extracapsular cataract extraction and phacoemulsification combined with intraocular lens implantation has enabled a large number of blind patients due to cataract to see again. However, late postoperative postoperative cataract (referred to as postoperative cataract) still seriously affects the vision of patients and becomes the most important postoperative complication. The incidence of after-development disorder varies with age, type of disease, and operation method of the patient. Generally, the incidence rate of adults is 50% within 2-5 years after operation, and the incidence rate of young children can be as high as 100%. Therefo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/727A61K47/30A61P27/02
Inventor 王身国谢立信贝建中孙洁陈文娜
Owner INST OF CHEM CHINESE ACAD OF SCI
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