Porous microspheres for medicine carriers, preparation method and medicine loading method

A technology of porous microspheres and drugs, applied in the field of drug loading, can solve the problems of uneven particle size and pore size distribution of porous microspheres, uncontrollable release, low drug activity, etc., achieve the same bumping speed, increase loading rate, and maintain The effect of biological activity

Active Publication Date: 2011-11-30
INST OF PROCESS ENG CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Aiming at the problems of uneven particle size and pore size distribution of porous microspheres, low drug loading rate, uncontrollable release and low drug

Method used

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  • Porous microspheres for medicine carriers, preparation method and medicine loading method
  • Porous microspheres for medicine carriers, preparation method and medicine loading method
  • Porous microspheres for medicine carriers, preparation method and medicine loading method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] The hydrophilic microporous membrane with a pore size of 2.8 μm is soaked in water to fully wet the porous membrane. The molecular weight of 0.4g is 10,000 polylactic acid-polyethylene glycol copolymer (PELA) (the proportion of hydrophilic block is 4%) is dissolved in 8ml methylene chloride, as oil phase, this oil phase Join in the polyethylene glycol (PVA) aqueous solution of 1%wt of 80ml, the ratio of oil phase and water phase is 1: 10, magnetic stirring 300rpm stirs 1min and prepares pre-emulsion, then this pre-emulsion is under the operating pressure of 400kPa Pressed through a microporous membrane device (such as figure 1 ) to obtain an emulsion, and the membrane passing time of the emulsion is less than 10s, then the emulsion is stirred at room temperature for 24h to remove the organic solvent methylene chloride, and then centrifuged to obtain the drug-loaded microspheres. The obtained microspheres were vacuum-dried for 48 h to obtain finished microspheres. The ...

Embodiment 2

[0061] The hydrophilic membrane with a pore size of 7.2 μm is soaked in water to fully wet the porous membrane. 0.7g of molecular weight is 50,000 polylactic acid-polyglycolic acid and polyethylene glycol copolymer (the proportion of hydrophilic block is 10%) dissolved in 10ml of chloroform, as the oil phase, the oil Phase is added in the PVA aqueous solution of 50ml 1.2%wt, and the ratio of oil phase and water phase is 1: 5, and magnetic stirring 300rpm stirs 1min to prepare pre-emulsion, and then this pre-emulsion is pressed through the microporous membrane under the operating pressure of 200kPa device to obtain an emulsion, and the membrane-passing time of the emulsion is less than 10s, and then the emulsion is stirred at room temperature for 24 hours to remove the organic solvent chloroform, and then centrifuged to obtain the drug-loaded microspheres. The obtained microspheres were vacuum-dried for 48 h to obtain finished microspheres. The dried microspheres were redisper...

Embodiment 3

[0063] The hydrophilic membrane with a pore size of 9 μm is soaked in water to fully wet the porous membrane. The molecular weight of 0.8g is 20,000 polylactic acid-polyethylene glycol copolymer (the proportion of hydrophilic block is 20%) is dissolved in 15ml carbon disulfide, as oil phase, this oil phase is added to 300ml of 1.4 In the PVA aqueous solution of %wt, the ratio of oil phase and water phase is 1: 20, magnetic stirring 300rpm stirs 1min to prepare pre-emulsion, then this pre-emulsion is pressed through the microporous membrane device under the operating pressure of 150kPa, obtains emulsion, emulsion The membrane passing time is less than 10s, and then the emulsion is stirred at room temperature for 24 hours to remove the organic solvent chloroform, and then centrifuged and washed to obtain the drug-loaded microspheres. The obtained microspheres were vacuum-dried for 48 h to obtain finished microspheres. The dried microspheres were redispersed in water, and the su...

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Abstract

The invention relates to the field of preparation of porous microspheres, in particular to porous microspheres for medicine carriers, a preparation method and a medicine loading method. The method comprises the following steps of: 1) dissolving a degradable di-block amphiphilic polymer material in an organic solvent to form an oil phase O; 2) adding the oil phase O into a water phase W which contains a stabilizing agent to form O/W pre-emulsion; 3) allowing the O/W pre-emulsion obtained in the step 2 to pass through a microporous membrane to obtain O/W emulsion; and 4) removing the organic solvent from the emulsion obtained in the step 3, and curing, performing centrifugal washing and freeze drying to obtain porous medicine carrying microspheres. The organic solvent in the step 1) at least comprises a solvent of which the solubility in water is less than 2 percent; and the volume ratio of the oil phase O to the water phase W is 1:5-20. The porous microspheres overcome the problem thatthe conventional sustained release microspheres cannot be completely released at a later stage, and can effectively keep the medicine activity in the processes of carrying, storing and releasing the medicines.

Description

technical field [0001] The invention relates to the field of preparation of porous microspheres, in particular, the invention relates to a porous microsphere used as a drug carrier, a preparation method and a drug loading method. Background technique [0002] With the development of emerging biotechnology and genetic engineering, protein and polypeptide macromolecular biochemical medicines (such as growth hormone, insulin, heparin, interferon, interleukin, etc.) During the course of treatment, it shows the characteristics of strong pharmacological effects, few side effects and rarely causing allergic reactions, so it has attracted much attention. Due to the poor stability of peptide and protein drugs, they are easily degraded in the stomach and have low bioavailability, so injections are often used. However, due to the short half-life of such drugs in vivo, multiple injections are often required for clinical application. In response to these problems, researchers basically...

Claims

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Application Information

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IPC IPC(8): A61K47/34
Inventor 马光辉韦祎王玉霞苏志国周炜清
Owner INST OF PROCESS ENG CHINESE ACAD OF SCI
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