Polymeric micelle freeze-drying preparation of taxane antitumor drugs for injection

An anti-tumor drug and polymer glue technology, which is applied in the field of taxane polymer micelle freeze-dried preparations, can solve the problems of unsatisfactory applicability universality, unsatisfactory stabilization time, unobvious improvement of micelle stability, and the like, To achieve the effect of improving stability and improving stability

Pending Publication Date: 2022-03-29
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the prior art attempts to change the stability of taxane micelles. On the one hand, it is not ideal to maintain the stability time; The technical solution of beam stability can improve the stability of micelles of paclitaxel, but the stability of micelles of other taxane drugs is not obvious

Method used

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  • Polymeric micelle freeze-drying preparation of taxane antitumor drugs for injection

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Experimental program
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Embodiment 1

[0034] The preparation of embodiment 1 polyethylene glycol-polyorthoester block copolymer

[0035] Under the protection of nitrogen, add polyethylene glycol to the glass polymerization bottle 200070g, keep stirring at 125~130°C and vacuumize to remove water for 4h; add stannous isooctanoate (0.5g) / toluene solution, stir and disperse for 30min, keep stirring at 125~130°C and vacuumize toluene for 1.5h; add polyorthoester 30g , 125 ~ 130 ℃ heat preservation and stirring reaction for 3 ~ 4h; after the reaction is completed, cool down, add dichloromethane and stir to dissolve, add metal scavenger for three times. Suction filtration, filter out the metal scavenger, add the filtrate to anhydrous ether, dissolve and crystallize twice; dissolve with dichloromethane, filter through a PTFE membrane (3 μm), add the filtrate to anhydrous ether to crystallize; the obtained product First vacuum dry at -0.08~-0.1MPa below 20°C for 6 hours, turn over the material, and then control the temper...

Embodiment 2

[0036] The preparation of embodiment 2 polyethylene glycol monomethyl ether-poly (D, L) lactide block copolymer

[0037] Under the protection of nitrogen, add polyethylene glycol monomethyl ether to the glass polymerization bottle 2000 50g, keep stirring at 125~130°C and vacuumize to remove water for 4h; add stannous isooctanoate (0.128g) / toluene solution, stir and disperse for 30min, keep stirring at 125~130°C and vacuumize toluene for 1.5h; add DL-lactide 50g, keep stirring at 125-130°C for 3-4 hours; after the reaction, cool down, add dichloromethane and stir to dissolve, add metal scavenger for three times. Suction filtration, filter out the metal scavenger, add the filtrate to anhydrous ether, dissolve and crystallize twice; dissolve with dichloromethane, filter through a PTFE membrane (3 μm), add the filtrate to anhydrous ether to crystallize; the obtained product First vacuum dry at -0.08~-0.1MPa below 20°C for 6 hours, turn over the material, and then control the tem...

Embodiment 3

[0038] The preparation of embodiment 3 polypropylene glycol-polyglycolide-lactide block copolymer

[0039] Under the protection of nitrogen, add polypropylene glycol to the glass polymerization bottle 1000 30g, keep stirring at 125~130℃ and vacuumize for 4h to remove water; add stannous octanoate (0.05g) / toluene solution, stir and disperse for 30min, keep stirring at 125~130℃ and vacuumize to remove toluene for 1.5h; add polyglycolide 70g lactide, heat-retain and stir at 125-130°C for 3-4 hours; cool down after the reaction, add dichloromethane and stir to dissolve, add metal scavenger for three times. Suction filtration, filter out the metal scavenger, add the filtrate to anhydrous ether, dissolve and crystallize twice; dissolve with dichloromethane, filter through a PTFE membrane (3 μm), add the filtrate to anhydrous ether to crystallize; the obtained product First vacuum dry at -0.08~-0.1MPa below 20°C for 6 hours, turn over the material, and then control the temperature ...

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Abstract

The invention provides a taxane polymer micelle freeze-drying preparation. The taxane polymer micelle freeze-drying preparation is prepared from taxane medicines, povidone and a polyether / polyester block copolymer, the invention also provides a related preparation method. According to the taxane polymer micelle freeze-dried preparation disclosed by the invention, the stability of liquid medicine is greatly improved while the medication safety is improved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a freeze-dried preparation of taxane polymer micelles for injection. Background technique [0002] In clinical oncology, chemotherapy is the main therapeutic approach. However, traditional chemotherapeutic agents, such as small molecule antitumor drugs, have not achieved good curative effect due to low solubility, poor stability, fast degradation rate and non-targeted tissue distribution, and also have serious adverse reactions. At present, most of the antineoplastic drugs in clinical use are hydrophobic drugs, such as paclitaxel, docetaxel, and hydroxycamptothecin, which are taxanes; although the above drugs have been widely used clinically, there are still commercially available preparations There are many problems as follows, such as the commercially available formulation Taxol is a colorless viscous solution made of polyoxyethylene castor oil / ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K9/107A61K47/32A61K47/34A61K31/337A61P35/00
CPCA61K9/0019A61K9/19A61K9/1075A61K47/32A61K47/34A61K31/337A61P35/00
Inventor 张贵民尚萍萍支运宝
Owner LUNAN PHARMA GROUP CORPORATION
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