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Method for controlling dichloromethane residue in polymer microsphere preparation

A dichloromethane and polymer technology, which is applied in the field of controlling dichloromethane residues in polymer microsphere preparations, can solve problems such as increasing the dosage of administration, increase in particle size, and release effects, and achieves control of residual problems and high levels of production. The effect of drug loading and encapsulation efficiency, process stability

Active Publication Date: 2013-12-25
ZHEJIANG HISUN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Such as Chu Dafeng et al (for the treatment of senile dementia Huperzine A long-acting slow-release microsphere preparation research, Jilin University doctoral dissertation, 2007) using mannitol as a protective agent, then programmed to 60 ℃ vacuum drying, can Reduce the residue of methylene chloride to less than 600ppm, but it needs to add about 50% of mannitol as a protective agent, which will increase the dosage, and will cause the microspheres to expand at the same time, and the particle size will increase by more than 20%. influential

Method used

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  • Method for controlling dichloromethane residue in polymer microsphere preparation
  • Method for controlling dichloromethane residue in polymer microsphere preparation
  • Method for controlling dichloromethane residue in polymer microsphere preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] prescription:

[0025] Risperidone 3g

[0026] PLGA 75255A 3g

[0027] Dichloromethane 15ml

[0028] Preparation process: add 3g of PLGA 75255A and 3g of risperidone into 15ml of dichloromethane at room temperature, after being completely dissolved, add into 3L of water phase containing 1% PVA and emulsify and stir for 4min with a high-shear emulsifying disperser (rotating speed 900rpm), then stirred slowly at 100rpm for 4h, evaporated dichloromethane, filtered, collected and washed the microspheres with 10% ethanol, and freeze-dried at 45°C. After lyophilization, the appearance, content, encapsulation efficiency, release, etc. were determined according to the quality evaluation of the microsphere preparation.

Embodiment 2

[0030] prescription:

[0031]

[0032] Preparation process: Dissolve 3g of PLGA 75255A and 3g of risperidone in 15ml of dichloromethane at room temperature, add 3ml of benzyl alcohol, mix well and add to 3L of water phase containing 1% PVA with a high-shear emulsifying disperser Emulsify and stir for 4 minutes (rotating speed 900 rpm), then slowly stir at 100 rpm for 4 hours, evaporate dichloromethane, filter, collect and wash the microspheres with 10% ethanol, and freeze-dry at 45°C (lyophilization conditions are the same as Example 1). After lyophilization, the appearance, content, encapsulation efficiency, release, etc. were determined according to the quality evaluation of the microsphere preparation.

Embodiment 3

[0034] prescription:

[0035]

[0036]

[0037] Preparation process: Dissolve 3g PLGA 75255A in 15ml dichloromethane at room temperature, dissolve 2g risperidone in 9ml benzyl alcohol, mix well after completely dissolving, add to 3L water phase containing 1% PVA and 5% benzyl alcohol for use A high-shear emulsifying disperser was used to emulsify and stir for 4 minutes (rotating speed 900 rpm), followed by slow stirring at 100 rpm for 4 hours, dichloromethane was evaporated, filtered, collected and washed with 5% benzyl alcohol, and freeze-dried at 30°C. After lyophilization, the appearance, content, encapsulation efficiency, release, etc. were determined according to the quality evaluation of the microsphere preparation.

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Abstract

The present invention relates to a method for controlling dichloromethane residue in a polymer microsphere preparation. According to the present invention, during a polymer microsphere preparation process, an external leakage bridge solvent is added to a dichloromethane oil phase and / or a water phase, dichloromethane is carried to the water phase during a microsphere curing process through the external leakage bridge solvent, and finally drying is performed, such that dichloromethane residue in the polymer microsphere preparation can be controlled to less than 600 ppm; the method has characteristics of high efficiency, controllability, stable process, safety, and reasonability; and with the method, the problem of dichloromethane residue in the polymer microsphere preparation can be effectively controlled, and complete form, high drug loading, high encapsulation efficiency and good release effect of microspheres can be maintained.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a method for controlling the residue of dichloromethane in polymer microsphere preparations. Background technique [0002] Microspheres refer to tiny spherical entities prepared by dissolving or dispersing drugs in suitable polymer excipients and by microencapsulation technology. Various preparations are made according to different clinical routes of administration and uses. Generally, those with a particle size between 1 and 250 um are called microspheres, those with a particle size between 0.1 and 1 um are called submicrospheres, and those with a particle size between 10 and 100 nm are called nanospheres. It can be used as a drug carrier to become a new type of drug delivery system. Because of its targeting to specific organs and tissues, slow release of drug release, long-acting, high efficiency, and low toxicity, it is biodegradable and long-acting. Sustained-...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K47/34
Inventor 苏正兴王端统曹金全詹新安
Owner ZHEJIANG HISUN PHARMA CO LTD
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