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Total bufogenin PLGA nanoparticle freeze-drying preparation and preparation method thereof

A technology of nano-microspheres and PLGA, applied to PLGA nano-microsphere freeze-dried preparation and its preparation, total bufolide PLGA nano-microsphere freeze-dried preparation, said total bufolide PLGA nano-microsphere freeze-dried preparation In the field of preparation, it can solve the problems of high impurities, low content of active ingredients, and large toxic and side effects, and achieve the effects of good process reproducibility, less sample requirement, and low preparation cost

Inactive Publication Date: 2015-12-16
HEFEI HUAFANG PHARMA SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it has been found through research that the content of total bufolides (bufagenins, bufatoxins) with anti-tumor activity in cinobufacin injection is extremely low, mainly water-soluble indole alkaloids (such as 5 -Serotonin, bufatryptamine, bufoteni, bufa sulfur, etc.), amino acids and other components, while a large number of effective components of lactones are completely lost. At present, there is no research report on the anti-tumor activity of alkaloid components, and clinical research It is believed that the adverse reactions of cinobufacin, arrhythmia, local venous irritation, skin reactions, asthma, and hypersensitivity reactions are all caused by the pharmacological effects of water-soluble indole alkaloids.
In summary, cinobufacin has serious defects such as low content of active ingredients, many impurities, unstable quality and clinical curative effect, and large toxic and side effects. focus of our research

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] The preparation of embodiment 1 total bufolide PLGA nano microspheres

[0030] Dissolve 2 mg of total bufolide and 20 mg of PLGA (polymer PLGA molecular weight 40,000, the molar ratio of lactic acid: glycolic acid monomer is 75:25) in 2 mL of dichloromethane and ethyl acetate (volume ratio 1:1) and mix In the solution, as the dispersed phase (oil phase), the F68 aqueous solution is the continuous phase (water phase). Slowly inject the dispersed phase into 10ml of the continuous phase under stirring at room temperature at 800rpm to form an O / W emulsion, which is then transferred to a magnetic stirrer at 1000rpm Stir and continue to stir for 4 hours to fully volatilize the organic solvent, stir in an ice bath to obtain a nanosphere solution, and centrifuge at 10,000 rpm to obtain total bufolide PLGA nanospheres.

[0031] The total bufolide PLGA nano-microspheres prepared by this method were observed under an electron microscope to be uniform in size, round in shape and sm...

Embodiment 2

[0032] The preparation of embodiment 2 total bufolide PLGA nano-microspheres

[0033] Dissolve 2mg of total bufolide and 20mg of PLGA (the molecular weight of polymer PLGA is 40000, the molar ratio of lactic acid: glycolic acid monomer is 75:25) in 2mL of dichloromethane and ethyl acetate (volume ratio 1:2) and mix In the solution, as the dispersed phase (oil phase), the F68 aqueous solution is the continuous phase (water phase). Slowly inject the dispersed phase into 10ml of the continuous phase under stirring at room temperature at 800rpm to form an O / W emulsion, which is then transferred to a magnetic stirrer at 1000rpm Stir and continue to stir for 4 hours to fully volatilize the organic solvent, stir in an ice bath to obtain a nanosphere solution, and centrifuge at 10,000 rpm to obtain total bufolide PLGA nanospheres.

[0034] The total bufolide PLGA nano-microspheres prepared by this method were observed under an electron microscope to be uniform in size, round in shape ...

Embodiment 3

[0035] The preparation of embodiment 3 total bufolide PLGA nano-microspheres

[0036]Dissolve 2 mg of total bufolide and 20 mg of PLGA (polymer PLGA molecular weight 40,000, the molar ratio of lactic acid:glycolic acid monomer is 75:25) in 2 mL of dichloromethane and ethyl acetate (volume ratio 2:1) and mix In the solution, as the dispersed phase (oil phase), the F68 aqueous solution is the continuous phase (water phase). Slowly inject the dispersed phase into 10ml of the continuous phase under stirring at room temperature at 800rpm to form an O / W emulsion, which is then transferred to a magnetic stirrer at 1000rpm Stir and continue to stir for 4 hours to fully volatilize the organic solvent, stir in an ice bath to obtain a nanosphere solution, and centrifuge at 10,000 rpm to obtain total bufolide PLGA nanospheres.

[0037] The total bufolide PLGA nano-microspheres prepared by this method were observed under an electron microscope to be uniform in size, round in shape and smoo...

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Abstract

The invention discloses a total bufogenin PLGA (poly-(lactic-co-glycolic acid)) nanoparticle freeze-drying preparation and a preparation method thereof and belongs to the field of PLGA nanoparticle freeze-drying preparations and preparation thereof. At first, the invention discloses total bufogenin PLGA nanoparticles which comprise the components of total bufogenin, PLGA and a freeze-drying protective agent. The preparation method comprises the following steps: total bufogenins and PLGA are dissolved in an organic solvent to serve as a dispersion phase; an F68 water solution serves as a continuous phase; the dispersion phase is slowly injected into the continuous phase in an ultrasonic environment to form an O / W emulsion; then the O / W emulsion is transferred onto a magnetic stirrer to be stirred; after the organic solvent is fully volatilized, stirring is performed under the ice-bath condition to obtain a nanoparticle solution; and centrifugal treatment is conducted to obtain the total bufogenin PLGA nanoparticles. According to the total bufogenin PLGA nanoparticle freeze-drying preparation, the measured particle diameter of the particles is 150-210 nm, and the encapsulation efficiency is 50-90 percent. The total bufogenin PLGA nanoparticle freeze-drying preparation can effectively improve the tumor cell target ability of the total bufogenins, improves the medical bioavailability, achieves the slow-release curative effect and reduces toxic and side effects.

Description

technical field [0001] The present invention relates to freeze-dried preparations, in particular to total bufolide PLGA nano-microsphere freeze-dried preparations, and the present invention also relates to a preparation method of said total bufolide PLGA nano-microsphere freeze-dried preparations, belonging to PLGA nano-microsphere freeze-dried preparations. Field of dry formulations and their preparation. Background technique [0002] Cinobufacin, which is obtained from the skin of the traditional Chinese medicine Bufo bufo, can detoxify, reduce swelling and relieve pain. It is suitable for the treatment of middle and advanced tumors, chronic hepatitis B, etc. However, it has been found through research that the content of total bufolides (bufagenins, bufatoxins) with anti-tumor activity in cinobufacin injection is extremely low, mainly water-soluble indole alkaloids (such as 5 -Serotonin, bufatryptamine, bufoteni, bufa sulfur, etc.), amino acids and other components, whi...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K35/65A61K47/34A61P35/00
Inventor 杨贤龙吴宗好何勇
Owner HEFEI HUAFANG PHARMA SCI & TECH