CN1732962A - Process for preparing nanometer particle of adriacin-PACA-PBCA - Google Patents

Process for preparing nanometer particle of adriacin-PACA-PBCA Download PDF

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Publication number
CN1732962A
CN1732962A CNA2004100466489A CN200410046648A CN1732962A CN 1732962 A CN1732962 A CN 1732962A CN A2004100466489 A CNA2004100466489 A CN A2004100466489A CN 200410046648 A CN200410046648 A CN 200410046648A CN 1732962 A CN1732962 A CN 1732962A
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CN
China
Prior art keywords
add
stir
pbca
alpha
dextran70
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CNA2004100466489A
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Chinese (zh)
Inventor
张阳德
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Individual
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Individual
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Individual filed Critical Individual
Priority to CNA2004100466489A priority Critical patent/CN1732962A/en
Priority to PCT/CN2005/001056 priority patent/WO2006015534A1/en
Publication of CN1732962A publication Critical patent/CN1732962A/en
Pending legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/51Nanocapsules; Nanoparticles
    • A61K9/5107Excipients; Inactive ingredients
    • A61K9/513Organic macromolecular compounds; Dendrimers
    • A61K9/5138Organic macromolecular compounds; Dendrimers obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/58Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. poly[meth]acrylate, polyacrylamide, polystyrene, polyvinylpyrrolidone, polyvinylalcohol or polystyrene sulfonic acid resin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/61Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule the organic macromolecular compound being a polysaccharide or a derivative thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Physics & Mathematics (AREA)
  • Biomedical Technology (AREA)
  • Nanotechnology (AREA)
  • Optics & Photonics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The invention provides a process for preparing nanometer particle of adriacin-PACA-PBCA, which comprises, reacting HCl solution with doxorubicin hydrochloride powder, stirring to dissolve, charging Dextran70 and charging alpha-butylcyanoacrylate, stirring and adjusting pH to be 7, passing through 0.45um filtration film and drying.

Description

The preparation method of amycin-paracyanogen base NBCA nanoparticle
Technical field
The present invention relates to a kind of preparation method to the cancer treatment drug nano-particle.
Technical background
Hepatocarcinoma is one of modal malignant tumor in the world, and at present, it is main comprehensive therapeutic plan that treatment hepatocarcinoma is still taked excision clinically, and many cases still need be accepted chemotherapy.But the toxicity of chemotherapy makes liver function and the out of condition person of whole body lose smelting and treats chance.In recent years, produce and developed the gene smelting and treat, but the prerequisite that the effective gene smelting is treated is nucleic acid molecules effectively must be delivered in the target cell.
Summary of the invention
Purpose of the present invention is that a kind of preparation method with amycin-paracyanogen base NBCA nanoparticle (DOX-PBCA-NP) of stronger targeting will be provided.
The preparation method of DOX-PBCA-NP of the present invention is: with HCl solution and the effect of doxorubicin hydrochloride powder, stir and make its dissolving, add Dextran again 70, add the positive fourth fat of alpha-cyanoacrylate, stir and wait to occur orange-yellow opalescence, regulate PH=7, cross 0.45 μ m filter membrane, drying promptly makes the present invention.
DOX-PBCA-NP with the present invention's acquisition, can deliver the multiple medicine that comprises chemotherapeutics, genomic medicine, its Targeting Performance significantly reduces the toxicity of chemotherapeutics, improve curative effect, can reduce drug dose and medication number of times, improve patient's compliance, improve the stability of genomic medicine ribozyme, prolong biological half-life, improve drug level and action time in the born of the same parents.
The specific embodiment
Specifically introduce the present invention below in conjunction with embodiment.
Get 0.1N HCl solution 50ml with pipet and place conical flask, add the doxorubicin hydrochloride powder 10mg that is dried to constant weight, stir and make its dissolving, the reuse micropipettor adds 1.5%Dextran 700.3ml, under the magnetic stirring apparatus effect, slowly add the positive fourth fat of alpha-cyanoacrylate 0.2ml, stir while dripping, be controlled at and added in 10 minutes.Seal a bottle, continue to stir 1000rpm 3h, wait to occur orange-yellow opalescence, regulate PH=7, cross 0.45 μ m filter membrane with 0.2NNaOH solution.Filtrate in vacuum drying oven 25 ℃ ,-dry under the 0.1kPa condition, promptly make the present invention.

Claims (2)

1, the preparation method of a kind of amycin-paracyanogen base NBCA nanoparticle, the steps include: with HCl solution and the effect of doxorubicin hydrochloride powder, stirring makes its dissolving, add Dextran70 again, add the positive fourth fat of alpha-cyanoacrylate, stir and wait to occur orange-yellow opalescence, regulate PH=7, cross 0.45 μ m filter membrane, drying promptly makes the present invention.
2, press the preparation method of the described amycin of claim 1-paracyanogen base NBCA nanoparticle, a DOX-PBCA-NP is got in making and settlement, the steps include: that getting 0.1N HCl solution 50ml with pipet places conical flask, add the doxorubicin hydrochloride powder 10mg that is dried to constant weight, stirring makes its dissolving, the reuse micropipettor adds 1.5%Dextran70 0.3ml, under the magnetic stirring apparatus effect, slowly add the positive fourth fat of alpha-cyanoacrylate 0.2ml, stir while dripping, be controlled at and added in 10 minutes; Seal a bottle, continue to stir 1000rpm3h, wait to occur orange-yellow opalescence, regulate PH=7, cross 0.45 μ m filter membrane with 0.2N NaOH solution, filtrate in vacuum drying oven 25 ℃ ,-dry under the 0.1kPa condition, promptly make the present invention.
CNA2004100466489A 2004-08-11 2004-08-11 Process for preparing nanometer particle of adriacin-PACA-PBCA Pending CN1732962A (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
CNA2004100466489A CN1732962A (en) 2004-08-11 2004-08-11 Process for preparing nanometer particle of adriacin-PACA-PBCA
PCT/CN2005/001056 WO2006015534A1 (en) 2004-08-11 2005-07-18 The preparation method of doxorubicin-polybutylcyanoacrylate nanoparticles

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CNA2004100466489A CN1732962A (en) 2004-08-11 2004-08-11 Process for preparing nanometer particle of adriacin-PACA-PBCA

Publications (1)

Publication Number Publication Date
CN1732962A true CN1732962A (en) 2006-02-15

Family

ID=35839132

Family Applications (1)

Application Number Title Priority Date Filing Date
CNA2004100466489A Pending CN1732962A (en) 2004-08-11 2004-08-11 Process for preparing nanometer particle of adriacin-PACA-PBCA

Country Status (2)

Country Link
CN (1) CN1732962A (en)
WO (1) WO2006015534A1 (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115444810B (en) * 2022-04-27 2023-10-13 贵州医科大学 Preparation method of doxorubicin-loaded nanoparticle composite temperature-sensitive gel

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IE80468B1 (en) * 1995-04-04 1998-07-29 Elan Corp Plc Controlled release biodegradable nanoparticles containing insulin

Also Published As

Publication number Publication date
WO2006015534A1 (en) 2006-02-16

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