Porous embolization microspheres comprising drugs

A technology of microspheres and drugs, applied in drug delivery, medical preparations containing active ingredients, medical science, etc., can solve problems such as insoluble, achieve high absolute load, large correlation, and improve the effect of drug holding capacity

Pending Publication Date: 2020-10-02
范里恩贝希尔有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, most cytostatics are poorly soluble in water

Method used

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  • Porous embolization microspheres comprising drugs
  • Porous embolization microspheres comprising drugs
  • Porous embolization microspheres comprising drugs

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Embodiment Construction

[0032] The full advantages of the invention are achieved when the organic solvent is at least partially miscible with water at 20°C. Preferably, the organic solvent is completely miscible with water at 20°C. This results in a rapid diffusion of the solvent molecules out of the microspheres in step c of the method according to the invention and an optimal retention of the therapeutic agent(s) in the microspheres during washing, and thus a higher microsphere load capacity.

[0033] The concentration of therapeutic agent in the organic solvent is preferably at least 20 mg / mL. Such concentrations result in injectable polymeric microspheres comprising a high amount of therapeutic agent, for example at least 10% by weight of therapeutic agent relative to the weight of the loaded microsphere.

[0034] More preferably, the concentration of the therapeutic agent in the organic solvent is at least 100 mg / mL at 20°C. Such concentrations result in injectable polymeric microspheres comp...

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Abstract

The current invention provides a method of forming polymeric microspheres loaded with a therapeutic agent, comprising: a. exposing porous polymeric microspheres to an organic solvent comprising a dissolved therapeutic agent thereby creating microspheres loaded with therapeutic agent, b. separating the microspheres loaded with therapeutic agent from the organic solvent, c. washing the microspheresloaded with therapeutic agent with water, and d. drying the washed microspheres. The microspheres are particularly useful in embolization therapy.

Description

technical field [0001] The present invention relates to a method of forming therapeutic agent-loaded polymer microspheres, therapeutic agent-loaded polymer microspheres, a kit comprising a container containing therapeutic agent-loaded polymer microspheres, for active use in mammals Embolization method, use of polymer microspheres in the treatment of malignant or benign cancers, pharmaceutical compositions of polymer microspheres loaded with therapeutic agents, and drugs comprising polymer microspheres for embolization of tumors. Background technique [0002] Embolization therapy is a well-established and reliable minimally invasive, image-guided technique for treating tumors. During embolization, physicians (interventional radiologists) use embolic particles to stop blood flow to the tumor vascular bed. A catheter is inserted percutaneously and directed towards the tumor. Navigate under serial X-ray fluoroscopy and use a contrast agent. There are a variety of embolization...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/4412A61K31/519
CPCA61K9/0019A61K9/1635A61K9/1694A61K31/44A61B2090/3966A61B17/12186A61B2017/00526A61B2017/00893A61K9/0024A61K49/0438
Inventor 列维努斯·亨德里克·库勒
Owner 范里恩贝希尔有限公司
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