Slow-released 5-fluorouracil system in vitreous chamber

A vitreous cavity, fluorouracil technology, applied in the field of 5-fluorouracil vitreous cavity sustained-release system, can solve the problems of ocular tissue toxicity, unacceptable for patients, retinal detachment, etc., and achieve the effects of reducing toxic side effects, inhibiting proliferation, and preventing danger

Inactive Publication Date: 2006-10-18
毕宏生 +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In order to maintain the effective therapeutic concentration of drugs in the tissues of the posterior segment of the eye, multiple injections into the vitreous cavity were generally used in the past. This method is not only unacceptable to patients, but also easily causes

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0010] Accurately weigh 160.0 mg of PLA, dissolve in 2 ml of dichloromethane by ultrasonication for 30 seconds, accurately weigh 26.7 mg of 5-fluorouracil, add it to polylactic acid in dichloromethane solution, and continue ultrasonication for 30 seconds. Slowly add the suspension dropwise into the 20 g / L polyvinyl alcohol aqueous solution saturated with 5-fluorouracil in advance and stir for 3 hours until the dichloromethane is completely volatilized. The balls were washed 4 to 5 times with distilled water, and dried in a vacuum desiccator at room temperature for 48 hours. Select the absorbed dose of 6KGy to carry out 60 Co radiation sterilization. Implanted subcutaneously in the back of the mouse, sacrificed one mouse every other day, peeled off the back skin, cut off the skin where the drug was applied, and observed the skin and microspheres.

[0011] After subcutaneous implantation of microspheres in mice, no mental and behavioral adverse reactions were observed. After ...

Embodiment 2

[0013] The 5-fluorouracil sustained-release system in the vitreous cavity of Example 1 was implanted into the vitreous cavity of the left eyes of 6 healthy rabbits.

[0014] The elimination half-life of 5-fluorouracil sustained-release system in the vitreous cavity was significantly prolonged, and the T1 / 2 was 379.05h.

[0015] Periodic slit-lamp and ophthalmoscopy examinations revealed mild localized foreign body reactions. The choroid and retina were normal, and the vitreous was well tolerated by the 5-fluorouracil sustained-release intravitreal system. The latent time and amplitude of electroretinogram (ERG) did not change significantly before and after drug injection.

[0016] When the animals were sacrificed on the 28th day, the 5-fluorouracil vitreous cavity sustained-release system in the vitreous cavity was significantly reduced compared with when it was implanted, and there were adhesions and broken phenomena. Histopathology showed that there was no difference betwe...

Embodiment 3

[0019] The same 5-fluorouracil vitreous cavity sustained-release system as in Example 1 was injected into the vitreous cavity of an animal model of proliferative vitreoretinopathy induced by macrophages.

[0020] The occurrence of proliferative vitreoretinopathy was regularly observed after the operation. The implantation of the 5-fluorouracil vitreous cavity sustained-release system significantly reduced the incidence of proliferative vitreoretinopathy compared with the control group, and the drug release system did not need to be removed.

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Abstract

The present invention provides one kind of slow released 5-fluorouracil system in vitreous chamber. The slow released 5-fluorouracil system has medicine carrying amount of 10.44%, medicine carrier of synthesized biodegradable polymer polylactic acid, and emulsifier of water soluble polymer PVA. The slow released 5-fluorouracil system is suitable for use after the surgical operation on vitreoretinopathy, and after being injected into vitreous chamber, it may maintain smooth medicine release for 28 days to inhibit the proliferation of active cell inducing proliferative vitreoretinopathy, block the acting path of the cell factors and prevent proliferative vitreoretinopathy effectively.

Description

technical field [0001] The invention relates to a drug preparation for vitreous cavity implantation, in particular to a 5-fluorouracil vitreous cavity slow-release system using a biodegradable polymer material as a drug carrier. Background technique [0002] Proliferative vitreoretinopathy (PVR) is the main reason for the failure of rhegmatogenous retinal detachment reduction surgery, and it is also one of the most important blinding eye diseases in humans. At present, there is no effective method to prevent PVR at home and abroad. Fluorouracil (5-Fluorouracil, 5-FU) has an inhibitory effect on the cell proliferation cycle, which can prevent PVR. Some people have tried to treat the above diseases with continuous injection of 5-FU into the vitreous cavity. This method is not only difficult for patients to accept, but also easily causes various complications such as vitreous hemorrhage and retinal detachment; Fluctuations in amplitude may even cause toxic effects on eye tiss...

Claims

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Application Information

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IPC IPC(8): A61K31/513A61K9/16A61K47/34A61P27/02
Inventor 毕宏生崔彦田景振邱海霞
Owner 毕宏生
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