Biodegradable implantation controlled-release microsphere using vibration membrane technique

A technology of biodegradation and microspheres, applied in the direction of non-active ingredient medical preparations, drug combinations, powder delivery, etc., can solve the problems of easy degradation and failure of raw materials, low drug loading, etc., to avoid the loss of raw materials, Effect of reducing residue, avoiding degradation and failure

Inactive Publication Date: 2009-04-29
王剑
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The technical problem to be solved by the present invention is to overcome the problems of low drug loading of the existing local controlled-release preparations in the target a

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Embodiment 1 Preparation of polylactic acid microparticles of the present invention

[0036] The raw material drug is 5-Fu fluorouracil. First make 5-Fu fluorouracil into 10-50nm particles for later use.

[0037] Using chloroform as a solvent, polylactic acid is dissolved to prepare a polylactic acid solution with a concentration of 30% by weight. The above-mentioned nanoscale 5-Fu fluorouracil was mixed into the polylactic acid solution, stirred evenly, and the chloroform in the solution was vacuum-sucked to let it volatilize rapidly. The drug-loaded polylactic acid solution is solidified into particles with a diameter of 2-3 mm by extrusion, mixed with liquid nitrogen as a coolant, and then added to a vibrating membrane machine, so that the temperature of the drug-loaded particles drops to -60 ° C. machine. Sieve to collect drug-loaded particles with a size of 20-200 microns for later use.

[0038] It is detected by the method on page 395 of the Pharmacopoeia of the...

Embodiment 2

[0040] Example 2 Preparation of polylactic acid-glycolic acid microparticles of the present invention

[0041] The raw material drug is carboplatin. First make carboplatin 10-50nm for use.

[0042] Polylactic acid-glycolic acid was dissolved in chloroform as a solvent to make a 20% solution. Mix the above-mentioned nanoscale carboplatin into the polylactic acid solution, stir evenly, and vacuum the chloroform in the solution to let it volatilize rapidly. The drug-loaded polylactic acid solution was solidified into particles with a diameter of 23 mm by extrusion, mixed with liquid nitrogen, and then added to a vibrating membrane machine, so that the temperature of the drug-loaded particles dropped to -50°C, and then discharged from the machine after repeated crushing. Sieve to collect drug-loaded particles with a size of 20-100 microns for later use.

[0043] It is detected by the method on page 108 of the Pharmacopoeia of the People's Republic of China 2005 edition, and its...

Embodiment 3

[0045] Embodiment 3 Preparation of polylactic acid microparticles of the present invention

[0046] Cisplatin was made into 10-50nm microparticles for use. The polylactic acid is heated slowly in the temperature control box, and the solid polylactic acid becomes viscous after melting, and the interior lacks convection and conduction similar to water heating, mainly due to the lack of convective internal heat exchange. In order to prevent uneven heating, the heating rate was controlled at 25°C / hour. At 175°C, polylactic acid is in a liquid state, add nano-sized cisplatin, and stir well. Pour into the mold, cool slowly at room temperature, and make 5mm square particles. Pulverize into a particle size of 0.1-0.5 mm in a pulverizer, mix with coolant liquid nitrogen, add to a vibrating membrane machine for fine pulverization, and keep the temperature below 0°C. Sieve, select particles with a particle size of 30-100 microns and bottle them for later use. All operations were carr...

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PUM

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Abstract

The invention relates to a biodegradable implanting controlled release microsphere prepared by adopting a vibrating diaphragm technology, and a preparation method thereof, pertaining to the filed of pharmacy. The invention aims at overcoming the technical problems that parts of the existing target area have low controlled release drug-load rate and a crude drug is easy to be degraded and become ineffective during the preparation process, and providing a new preparation method of the biodegradable implanting controlled release microspheres. The preparation method adopts the physical method of the vibrating diaphragm technology, evenly spreads the crude drug with the particle diameter of 10nm to 50nm in a carrier to prepare nano-particles with the particle diameter of 10 nanometers to 200 nanometers. The biodegradable implanting controlled release microsphere has the drug-load rate reaching about 20 percent to 40 percent; the use and residual of various toxic organic solvents are reduced during the preparation process; meanwhile, the transferring process from oil phase and aqueous phase of the crude drug does not exist, thereby avoiding crude drug loss; furthermore, low-temperature grinding is adopted during the preparation process, thereby preventing the crude drug from degrading and becoming ineffective during the preparation process and being capable of realizing the scale and target of industrialized production.

Description

technical field [0001] The invention relates to a biodegradable anti-tumor locally implanted controlled-release preparation and a preparation method thereof, belonging to the field of pharmacy. Background technique [0002] Targeted preparations can improve the specificity of anti-tumor drugs, make the drugs relatively concentrated in the tumor target tissue area, increase the drug concentration in the target tissue area, thereby improving the bioavailability of the drug and effectively reducing its side effects. Targeting preparations are divided into two types: active and passive. Active targeting preparations are represented by monoclonal antibodies as drug carriers. Due to the lack of specific antigens in tumor cells and non-homologous antibodies, strong allergic reactions can be caused, and the molecular weight is huge. Difficult to pass through the Jain's barrier and a series of reasons, it is difficult to achieve ideal clinical efficacy at this stage. Passive targeti...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K47/34A61K47/36A61P35/00
Inventor 王建
Owner 王剑
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