Slow-releasing medicine inplanted in eye and use thereof

A slow-release drug and drug technology, applied in drug combination, drug delivery, pharmaceutical formulation, etc., can solve the problems of poor drug efficacy, unstable drug concentration in the eye, and short sustained drug release time, and achieve good tissue compatibility , Avoid causing high blood pressure, avoiding the effect of toxic damage

Inactive Publication Date: 2005-02-16
SHANDONG EYE INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The purpose of the present invention is to overcome the shortcomings of the above-mentioned existing intraocular drug release preparations, such as short sustained drug release time, unstable intraocular drug concentration, or poor drug efficacy, and provide a FK-506 macrocyclic intraocular Ester antibiotics and self-biodegradable drugs are used together in the preparation of sustained-release drugs for intraocular implantation. The FK-506 release system for intraocular implantation of long-term drug release can avoid the current intraocular drug release Formulations cannot penetrate the eye barrier and achieve effective intraocular drug concentrations

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Take 5 parts of lactic acid / glycolic acid copolymer (PLGA, molecular weight 6-110,000), dissolve it with 40 parts of chloroform, add 20 parts of FK-506 powder, stir well, inject it into a polytetrafluoroethylene mold, and wait for the chloroform to volatilize , and after complete drying, the film containing the lactic acid / glycolic acid copolymer of FK-506 is taken off from the polytetrafluoroethylene mold, and the solvent is further removed under vacuum at room temperature for 72 hours to obtain a thickness of 1.5-2.0 mm. A flaky film with a nanoscale pore structure containing FK-506 lactic acid / glycolic acid copolymer, and then punched with a die with a pore diameter of 1.5-2.0 mm to a thickness of 1.5-2.0 mm and a diameter of 1.5-2.0 mm formulation of FK-506. The FK-506 preparation was sterilized by fumigation with ethylene oxide for 24 hours, and then placed in the anterior chamber of the rabbit for another week.

[0021] The results of postoperative macroscopic ob...

Embodiment 2

[0024] Take 3 parts of poly DL-lactic acid (PDLLA, molecular weight 30,000-60,000), 20 parts of dioxane and 2 parts of FK-506 drug, dissolve and mix evenly, pour into a polytetrafluoroethylene mold, put it into a freeze dryer, and Frozen state and desolvation under vacuum for 72 hours, to obtain a sheet-shaped drug film with a thickness of 1.5-2.0 mm and a pore diameter of about 50 microns, and then use a die with a pore diameter of 1.5-2.0 mm to punch it into a film with a thickness of 1.5-2.0 mm and a diameter of 1.5-2.0 mm of FK-506 formulation. The FK-506 preparation was sterilized by fumigation with ethylene oxide for 24 hours, and then placed for another week, and implanted into the anterior chamber of the rabbit eye in the same way as in method 1.

[0025] The results of postoperative macroscopic observation and local histopathological examination showed that the FK-506 release system has good intraocular biocompatibility. Within 14 weeks after implantation, FK-506 can ...

Embodiment 3

[0027]According to the method and steps of Example 1, but using 3 parts of (glycolic acid / lactic acid / caprolactone terpolymer (PGLC, molecular weight 80,000), 18 parts of dichloromethane and FK prepared by the method of Chinese invention patent ZL 99105984.0 9 parts of -506 medicines are made the block thing that is the nanopore structure, and the punching die that is 2.0 millimeters is punched into the medicine stick that diameter is 2 millimeters with aperture again.This medicine stick is cut into the sheet preparation that requires thickness and then further in Keep in a vacuum oven at room temperature for 48 hours to completely remove the solvent, and then carry out ethylene oxide fumigation and sterilization for 24 hours. Place it for 1 week and then implant it into the anterior chamber of the rabbit eye in the same way as in Example 1.

[0028] Postoperative macroscopic observation and local histopathological examination showed that the FK-506 release system has good intr...

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PUM

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Abstract

The invention is an application of FK-506 macrolide antibiotic and medicine which can be decomposed biologically automatically which are used as planted slow release medicines in eyes. The medicine can maintain a fixed intensity and shape after release, and it can be decomposed naturally in vivo, thus it can be absorbed and discharged out of body, it will not become abnormal and generates stimulation to body, thus it need not to be taken out in the secondary operation. The period of the medicine is from two weeks to half year, the dose needed is little, it will not be affected by tears and dilution, it can release medicine slowly in a long period; it can be applied to prevent the eye diseases and cure repulsion reaction after cornea transplantation, at the same time, it can cure chronic uveitis, behcets disease, stevene-Johnson syndrome, and other diseases.

Description

technical field [0001] The present invention relates to an ophthalmic drug preparation, especially a slow-release drug for intraocular implantation and its application, specifically a FK-506 macrolide antibiotic and a self-biodegradable drug used together as a preparation for intraocular implantation. into the application of sustained-release drugs. It is a long-acting FK-506 sustained-release drug for intraocular implantation, which exerts unique curative effects in some chronic eye diseases. Background technique [0002] It is well known that keratoplasty is the only way for blind people with corneal disease to regain sight. However, postoperative immune rejection is the main reason for the failure of surgery. At present, glucocorticoids are the main means of clinical application to prevent and treat tissue rejection after corneal transplantation, etc., but long-term use of glucocorticoids will not only lead to various complications, such as hypertension, diabetes, etc., ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/4353A61K47/34A61P27/02
Inventor 谢立信王身国史伟云贝建中董晓光
Owner SHANDONG EYE INST
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