Mycophenolate mofetil intraocular medicament releasing system

A mycophenolate mofetil, drug release technology, applied in the field of long-acting mycophenolate mofetil intraocular sustained release system, can solve the difficulty of penetrating the intraocular drug concentration of mycophenolate mofetil, limit the application of mycophenolate mofetil, and cause serious adverse reactions and other problems, to achieve the effect of reducing the dosage, high drug utilization and long-lasting drug effect

Inactive Publication Date: 2009-12-02
SHANDONG EYE INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Adverse reactions are serious after oral systemic administration. It has been reported in the literature that 18% of patients receiving mycophenolate mofetil were forced to discontinue medication due to drug side effects; in addition, due to the influence of the blood-ocular barrier, it is difficult for the drug to enter the eye after oral administration effective drug concentration
For topical application of the eye, because mycophenolate mofetil is a fat-soluble drug, it is difficult to penetrate the eyeball wall to achieve an effective intraocular drug concentration, which limits its clinical application to a large extent.
These all limit the further application of mycophenolate mofetil in ophthalmology

Method used

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  • Mycophenolate mofetil intraocular medicament releasing system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] Get polylactide-glycolide 250mg of molecular weight 10000 Daltons, add mycophenolate mofetil powder 250mg after dissolving with dichloromethane 5ml (the weight ratio of biodegradable pharmaceutical macromolecule auxiliary material and mycophenolate mofetil 0.5:0.5), stirred and dissolved evenly, poured into a polytetrafluoroethylene mold, placed in a vacuum oven to volatilize dichloromethane. After being completely dried, the polylactide-glycolide drug delivery system containing mycophenolate mofetil 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 1.5-2 mm sheet-like drug with a pore structure, and then use a die with a 1.5-2 mm aperture to form a mycophenolate mofetil preparation with a thickness of 1.5-2 mm and a diameter of 1.5-2 mm.

Embodiment 2

[0013] According to the method and steps of Example 1, but adopting 400 mg of polylactide-glycolide with a molecular weight of 100,000 Daltons and 10 ml of dichloromethane to dissolve, add 600 mg of mycophenolate mofetil (biodegradable pharmaceutical polymer adjuvant and The weight ratio of mycophenolate mofetil is 0.4:0.6), and a medicine stick with a diameter of 2 mm is prepared, kept in a vacuum oven at room temperature for 48 hours to completely remove the solvent and then cut into 2 mm long mycophenolate mofetil release formulation. The mycophenolate mofetil preparation was sterilized by fumigation with ethylene oxide for 24 hours, and then placed for another week before use.

Embodiment 3

[0015] Get polylactide-glycolide 0.5g of molecular weight 35000 Daltons, add mycophenolate mofetil powder 0.5g after dissolving with dichloromethane 5ml The weight ratio is 0.5:0.5), stirred and dissolved evenly, poured into a polytetrafluoroethylene mold, and placed in a vacuum drying oven to volatilize dichloromethane. After being completely dried, the polylactide-glycolide drug delivery system containing mycophenolate mofetil 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 1.5-2 mm sheet-like drug with a pore structure, and then use a die with a 1.5-2 mm aperture to form a mycophenolate mofetil preparation with a thickness of 1.5-2 mm and a diameter of 1.5-2 mm.

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Abstract

The invention relates to a mycophenolate mofetil intraocular medicament releasing system, which comprises mycophenolate mofetil. The system is characterized by also comprising a biodegradable macromolecule auxiliary material, wherein the mycophenolate mofetil and biodegradable medicinal macromolecule auxiliary material form a homogeneous mixture together; the weight ratio of the biodegradable macromolecule auxiliary material to the mycophenolate mofetil is 0.4:0.6-0.6:0.4; and the molecular weight of the biodegradable medicinal macromolecule auxiliary material is between 10,000 and 100,000 daltons. The biodegradable medicinal macromolecule auxiliary material is made of one of lactide-glycolide, polylactic acid, and polylactic acid-glycollic acid. The medicament releasing cycle of the system is a week or half a year, and the system has the advantages of little dosage, low drug administration frequency, high medicament utilization degree, high local concentration and lasting medicine effect, and reduction of the dosage of the whole body and the complications.

Description

technical field [0001] The invention relates to a drug preparation for intraocular implantation, in particular to a long-acting mycophenolate mofetil intraocular slow-release system using a biodegradable polymer material as a drug carrier. Background technique [0002] Among the blinding eye diseases in our country, corneal disease ranks second only to cataract. Currently, corneal transplant rejection is the leading cause of transplant failure. In avascular implant beds, the incidence of rejection is 5-10%, while in high-risk corneal transplants, the incidence of rejection can be as high as 65%. How to effectively prevent and treat immune rejection after penetrating keratoplasty and improve the survival rate of grafts has become one of the focuses of research by ophthalmologists. [0003] Mycophenolate mofetil (MMF) is an effective anti-immune rejection drug, but currently only oral preparations are available. Adverse reactions are serious after oral systemic administrati...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/20A61K31/5377A61K47/34A61P37/06
Inventor 史伟云辛萌吴祥根
Owner SHANDONG EYE INST
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