Rapamycin eye-in implantation type medicine release system with bletilla striata glue as carrier

A technology of rapamycin and bletilla jelly, which is applied in the field of intraocular implant drug delivery system, to achieve the effect of inhibiting new blood vessels, improving the effect of prevention and treatment, and reducing the dosage

Inactive Publication Date: 2008-09-24
SHANDONG EYE INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, the formation of corneal neovascularization is an extremely complicated pathological process, and its occurrence is related to multiple factors such as the increase of pro-angiogenic factors, the decrease of anti-angiogenic factors, and inflammatory reactions. These factors are compensatory, and one factor acts If inhibited, the effects of other factors can be enhanced compensatoryly. For example, the expression of pro-angiogenic factor VEGF is inhibited, and the expression of pro-angiogenic factors such as fibroblast growth factor (bFGF) and interleukin 6 (IL-6) will be correspondingly increased. increase, resulting in "tolerance"

Method used

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  • Rapamycin eye-in implantation type medicine release system with bletilla striata glue as carrier
  • Rapamycin eye-in implantation type medicine release system with bletilla striata glue as carrier
  • Rapamycin eye-in implantation type medicine release system with bletilla striata glue as carrier

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Experimental program
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Effect test

Embodiment 1

[0025] The extraction of the bletilla striata gum of the present invention: extract and purify the bletilla striata gum required by the present invention with the following process.

[0026] 1. Crude polysaccharide extraction

[0027] The dried tuber products of Bletilla striata were crushed, sieved, dried, added 20 times the volume of distilled water, and extracted under reflux at 60°C for 4 hours. Repeat the extraction once. Combine the two extracts. Centrifuge (5000×g, 10min), take the supernatant, concentrate under reduced pressure at 70°C, add three volumes of 95% ethanol to precipitate. The precipitate was collected by centrifugation and freeze-dried to obtain crude bletilla striata gum (abbreviated as BRO).

[0028] 2. Separation and purification

[0029] Dissolve BRO in the minimum volume of water, deproteinize by Sevag method until almost no protein is detected by Coomassie Brilliant Blue G-250 method, then dialyze with convective water for three days, and vacuum ...

Embodiment 2

[0034] Select the Bletilla striata glue prepared in Example 1, prepare 12% bletilla striata glue aqueous solution, take 20.0ml of bletilla striata glue aqueous solution, add it into a sterile glass bottle, add rapamycin micronized powder 600mg under aseptic conditions, stir and disperse evenly, Then add 20 mg of ethylene glycol diglycidyl ether, stir evenly, and place in a water bath at 55°C for 3-5 hours. Take it out and wash it sufficiently to remove the residual cross-linking agent, pour the cross-linked glue solution into a polytetrafluoroethylene mold, and place it in an oven at 40°C to dry to form a film. After the diaphragm is fully dried, take it out and put it in normal saline for injection to fully soak and wash it, take out the diaphragm, and after it is completely dry, obtain a sheet medicine with a thickness of 1.5-2 mm, and then stamp it with a die with an aperture of 1.5-2.0 mm Formulations with a thickness of 1.0-2.0 mm and a diameter of 1.5-2.0 mm. The prepar...

Embodiment 3

[0036] In Example 1, ethylene glycol diglycidyl ether is replaced with propylene glycol diglycidyl ether, and the rest of the conditions are unchanged, and the same crosslinking effect can also be obtained.

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Abstract

The invention provides a Rapamycin intraocular implantable drug releasing system taking bletilla striata gum as the carrier, which includes the medicine Rapamycin served as medicine and the carrier. The Rapamycin intraocular implantable drug releasing system is characterized in that the carrier is bletilla striata gum, the main component of the bletilla striata gum is glucomannan which is polymerized by mannose and glucose at the ratio of 1 to 4; the average molecular weight is from 65000 to 150000, the bletilla striata gum is accounted as glucomannan with a content being more than 85 percent, and the amount of the added medicine is accounted as the dry weight of the bletilla striata gum, being 0.05-50 percent. Cross-linking agent is also added in the bletilla striata gum. The cross-linking agent is formaldehyde, glutaraldehyde, glycol diglycidyl ether, and propanediol diglycidyl ether. Albumin, gelatin, etc. are also added in the bletilla striata gum. The bletilla striata gum can inhibit neovascularization and can resist tumor, the joint usage can take the effect of synergetic treatment. The system of the invention takes the full advantages that the bletilla striata gum are biodegraded inside the body; active medicine is slowly released; the dosage, the taking times, and the harmful side effect of the medicine are reduced; better curative effect can also be realized on the site at which the medicine is difficult to be absorbed.

Description

technical field [0001] The present invention relates to an intraocular implantable drug release system, in particular to a long-acting intraocular sustained release system for rapamycin using bletilla jelly as a drug carrier—a rapamycin intraocular drug carrier using bletilla jelly Implantable drug delivery system. Background technique [0002] Corneal transplantation is an important sight restoration operation for corneal blindness, and it is also the main measure for treating some stubborn corneal lesions. Immune rejection after keratoplasty is still the leading cause of keratoplasty failure. Especially for patients with high-risk corneal transplants such as vascularized corneas and multiple corneal transplants, the incidence of postoperative immune rejection is as high as 60%, which greatly reduces the survival rate of corneal grafts. Among them, corneal neovascularization is the most important and common factor of high-risk corneal transplantation. Therefore, if the f...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/36A61K31/436A61P27/02A61P37/06C08B37/00
Inventor 吴祥根史伟云谢立信
Owner SHANDONG EYE INST
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