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Oil-soluble medicine degradable polymer microcapsule injecta and preparing method

A technology for degrading polymers and injection preparations, which is applied in the field of degradable polymer microcapsule injection preparations of oil-soluble drugs and their preparation, can solve the problem that the research reports and applications of drug release carriers are few, it is difficult to obtain long-acting sustained release, and it is difficult to Microcapsules and other problems, to achieve the effects of good physiological compatibility and biodegradability, good biocompatibility and biodegradability, and good stability

Inactive Publication Date: 2006-03-08
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For polyester synthetic polymers, the main chain of the molecule is composed of hydrophobic C-C bonds and ester bonds, and its relative chemical inertness makes it difficult to directly obtain microcapsules through chemical reactions. Therefore, the hollow microcapsule drug release carrier There are few research reports and applications
However, due to the good water solubility and permeability of the capsule material, the microencapsulated drug carrier of natural polymer is difficult to obtain long-term sustained release performance.

Method used

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  • Oil-soluble medicine degradable polymer microcapsule injecta and preparing method
  • Oil-soluble medicine degradable polymer microcapsule injecta and preparing method
  • Oil-soluble medicine degradable polymer microcapsule injecta and preparing method

Examples

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Effect test

example 1

[0030] (1) Grind lactide and stannous chloride crystals into powder, add a certain amount of allyloxyethylene glycol, place it in a reaction container, remove oxygen and nitrogen, and close the container. The amount of stannous chloride It is 0.8‰ of lactide weight, and the molar ratio of lactide / allyloxyethylene glycol is 55;

[0031] (2) The above reaction device is placed in an oil bath at 140°C, and the temperature is lowered after 8 hours at a constant temperature. Using acetone as a solvent and deionized water as a precipitating agent, it is purified by dissolution-precipitation to remove impurities, and vacuum-dried at 40°C to constant weight or freeze-drying to obtain double bond-containing polylactic acid;

[0032] (3) At 25° C. and a pH value of 7.0, methacrylic acid with a concentration of 1 g / ml is dissolved in an aqueous solution containing water-soluble carbodiimide, and the weight ratio of methacrylic acid and carbodiimide is 1:2, After stirring for 2 hours, ad...

example 2

[0038] (1) Grind lactide and stannous chloride crystals into powder, add a certain amount of allyloxyethylene glycol, place it in a reaction container, remove oxygen and nitrogen, and close the container. The amount of stannous chloride It is 2‰ of the weight of lactide, and the molar ratio of lactide / allyloxyethylene glycol is 200;

[0039] (2) The above-mentioned reaction device was placed in an oil bath at 200°C, and the temperature was lowered after 24 hours at a constant temperature. Using acetone as a solvent and deionized water as a precipitant, it was purified by dissolution-precipitation to remove impurities, and vacuum-dried at 40°C to constant weight. Obtain double bond-containing polylactic acid;

[0040] (3) At room temperature, after dissolving ciprofloxacin, medical grade polylactic acid (molecular weight 10,000), polylactic acid containing double bonds and polyethylene glycol diacrylate in chloroform, add 0.2% polyvinyl alcohol ( PVA) aqueous solution, an O / W ...

example 3

[0044] (1) step (1) and (2) in the synthetic repetition example 1 containing double bond polylactic acid, difference is that the consumption of stannous chloride is 10‰ of lactide weight;

[0045] (2) At room temperature, after dissolving ciprofloxacin, medical grade polylactic acid (molecular weight 8,000), polylactic acid containing double bonds and divinylbenzene (DVB) in chloroform, add 0.2% polyvinyl alcohol (PVA ) in an aqueous solution to obtain an O / W emulsion. The concentration of polylactic acid in chloroform is respectively 8.5, 17, 25.5 and 42.5mg / ml, and the DVB weight accounts for 1% of the polylactic acid weight containing double bonds, and the consumption of ciprofloxacin is 0.1% of the polylactic acid gross weight, O / W volume ratio is 1:5;

[0046] (3) Pass nitrogen and maintain the nitrogen atmosphere in the above container, after mechanical stirring for 0.5 hours (600rmp), keep the temperature at 40°C, K 2 S 2 o 8 with NaHSO 3 (1:1 weight ratio, concen...

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Abstract

The present invention discloses a degradable polymer microcapsule injection preparation of oil-soluble medicine and its preparation method. It uses polysaccharide containing double-bond and polylactic acid which have good biological compatibity and biological degradability as capsule shell material, adopts O / W emulsion polymerization technique and controls the ratio of mixing polysaccharide and polylactic acid to obtain the invented medicine microcapsule injection preparation whose grain size is 100-3000 nm.

Description

technical field [0001] The invention relates to a degradable polymer microcapsule injection reagent for oil-soluble drugs and a preparation method thereof, in particular to a biodegradable polymer composed of medical-grade polylactic acid, polysaccharides containing double bonds, polylactic acid, and polylactic acid. Nano-microcapsule injection preparation and its preparation technology in which drug is coating material and oil-soluble drug is capsule core material. technical background [0002] Biodegradable polymer carriers play an extremely important role in the field of drug controlled release systems because of their unique excellent characteristics (good degradation characteristics and low biotoxicity). Many researchers have reported the preparation, release behavior and functionalization of surface groups of microspheres or microparticle carriers of biodegradable polymers (such as polyester polymers and their copolymers and natural macromolecules of proteins and polys...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K47/32
Inventor 高长有江兵兵沈家骢
Owner ZHEJIANG UNIV
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