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A kind of lyophilization method of risperidone microspheres with low ethanol residue

A technology of risperidone and microspheres, which is applied in the field of medicine, can solve the problems of high ethanol content in products, lower ethanol content of risperidone microspheres, and high ethanol residual content of risperidone microspheres, so as to reduce the residual amount and improve the flow rate. sexual effect

Active Publication Date: 2021-03-05
ZHEJIANG SUNDOC PHARMA SCI & TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But on the whole, the product ethanol content that this process obtains is still higher
[0007] The study found that the fluidity of the microspheres obtained by using the freeze-drying technique is very good, and the next sub-packaging process can be carried out immediately after the drying is completed. It is necessary to develop a method that can further reduce the ethanol content in risperidone microspheres

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053]For 100 g batch production of microspheres, 60 g of 7525 polylactide glycolide copolymer and 40 g of risperidone were dissolved into 720.2 g of ethyl acetate and 220 g of benzyl alcohol as the organic phase, and the aqueous phase contained 72 g of polyvinyl alcohol, 7128 g of water , 517g ethyl acetate and 238.6g benzyl alcohol, the organic phase and the aqueous phase were passed through a static mixer to form an emulsion. The formed emulsion was transferred to 13.6kg of water and 3590.2g of ethyl acetate to quench the night, and the microspheres washed for 4 hours below 10°C were collected by filtration and dried. The dried microspheres were dispersed with a solution containing 2250 g of water and 750 g of ethanol at 10 °C, transferred to a solution of 27 kg of water and 9 kg of ethanol at 25 °C for washing for 4 hours, then heated to 35 °C for 2 hours, and then the microspheres were collected by filtration and Freeze-drying, pre-lyophilization treatment: the microspher...

Embodiment 2

[0067] For 100 g batch production of microspheres, 60 g of 7525 polylactide glycolide and 40 g of risperidone were dissolved in 720.2 g of ethyl acetate and 220 g of benzyl alcohol as the organic phase, and the aqueous phase contained 72 g of polyvinyl alcohol, 7128 g of water , 517g ethyl acetate and 238.6g benzyl alcohol, the organic phase and the aqueous phase were passed through a static mixer to form an emulsion. The formed emulsion was transferred to 13.6kg of water and 3590.2g of ethyl acetate to quench the night, and the microspheres washed for 4 hours below 10°C were collected by filtration and dried. The dried microspheres were dispersed with a solution containing 2250g water and 750g ethanol at 10°C, transferred to a solution of 27kg water and 9kg ethanol at 25°C for washing for 4 hours, then heated to 35°C for 2 hours, and then the microspheres were collected by filtration and frozen. Drying, pre-lyophilization treatment: the microspheres washed with 25% ethanol so...

Embodiment 3

[0081] For 100 g batch production of microspheres, 60 g of 7525 polylactide glycolide and 40 g of risperidone were dissolved in 720.2 g of ethyl acetate and 220 g of benzyl alcohol as the organic phase, and the aqueous phase contained 72 g of polyvinyl alcohol, 7128 g of water , 517g ethyl acetate and 238.6g benzyl alcohol, the organic phase and the aqueous phase were passed through a static mixer to form an emulsion. The formed emulsion was transferred to 13.6kg of water and 3590.2g of ethyl acetate to quench the night, and the microspheres washed for 4 hours below 10°C were collected by filtration and dried. The dried microspheres were dispersed with a solution containing 2250g water and 750g ethanol at 10°C, transferred to a solution of 27kg water and 9kg ethanol at 25°C for washing for 4 hours, then heated to 35°C for 2 hours, and then the microspheres were collected by filtration and frozen. Drying, pre-lyophilization treatment: the microspheres washed with 25% ethanol so...

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PUM

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Abstract

The invention relates to the field of medicines, and discloses a freeze-drying method of risperidone microspheres low in ethanol residues. The freeze-drying method comprises the following steps of (1)performing freeze-drying pretreatment; (2) performing pre-freezing: setting the temperature of a partition board to be minus 40-minus 10 DEG C, performing heat preservation for 1-4h, raising the temperature of the partition board to minus 2-0 DEG C within 0.5-3h, performing heat preservation for 0.5-3h, reducing the temperature of the partition board to minus 40-minus 10 DEG C within 0.5-3h, andat least repeating the pre-freezing step once; (3) performing a main drying stage; (4) performing a parsing and drying stage: raising the temperature of the partition board to be 10-40 DEG C within 2-30h, maintaining the temperature to be 10-40 DEG C for 1-5h, maintaining ultimate vacuum in the respect of vacuum degree, maintaining the temperature of the partition board unchanged, increasing the vacuum degree to 10-200mbar, and maintaining the vacuum degree for 0.1-5h. According to the method disclosed by the invention, the residual quantity of the ethanol in the freeze-dried risperidone microspheres can be effectively reduced, and the residual quantity of the ethanol can be controlled to be 0.2% or below.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a method for lyophilizing risperidone microspheres with low ethanol residue. Background technique [0002] In the preparation process of pharmaceutical microspheres, highly volatile organic solvents are usually difficult to remove during lyophilization, and the residual amount is relatively large, so it is usually not recommended to use them, but such solvents are inevitably used in some processes. The current common method is to use a liquid nitrogen freeze dryer. The temperature of the cold trap of the liquid nitrogen freeze dryer can be lowered below the freezing point of this type of organic solvent, so the residual amount can be effectively reduced, but the equipment is difficult to manufacture and expensive. [0003] U.S. Patent No. 7,247,319 discloses a method for improving the fluidity of microspheres. The fluidity of the microspheres dried by the drying sieve P12Y6 is relatively ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/519A61K9/19
Inventor 杜保国蒋朝军丁多浩张鸿
Owner ZHEJIANG SUNDOC PHARMA SCI & TECH CO LTD