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Method for preparing microspheres by using oil-in-nanoparticle mixed suspension-nanometer medicament-in-oil

A nanoparticle and nanomedicine technology, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve local microencapsulation and inflammation, incomplete release and burst release, encapsulation Low sealing rate and other problems, to achieve the effect of regular and non-adhesive particles, smooth and round particle surface, and reduce drug burst release

Inactive Publication Date: 2014-03-19
JINSHAN HOSPITAL FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to address the deficiencies in the prior art and provide a method for preparing microspheres from nanoparticle suspension oil-in-oil nanomedicine (N / O / N) to solve the problem of microsphere preparations in the prior art. Low encapsulation efficiency, incomplete release and burst release, hydrophobic surface can cause local microencapsulation and inflammation

Method used

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  • Method for preparing microspheres by using oil-in-nanoparticle mixed suspension-nanometer medicament-in-oil
  • Method for preparing microspheres by using oil-in-nanoparticle mixed suspension-nanometer medicament-in-oil
  • Method for preparing microspheres by using oil-in-nanoparticle mixed suspension-nanometer medicament-in-oil

Examples

Experimental program
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Effect test

Embodiment 1

[0059] Example 1 Preparation of microspheres loaded with small molecule drug doxorubicin (1)

[0060] Doxorubicin has antibacterial and anticancer effects. The preparation of polylactic-glycolic acid (PLGA) microspheres loaded with doxorubicin nano-medicine includes the following steps:

[0061] (1) Dissolve 20 mg of doxorubicin in 0.5 ml of water, then stir with 20 mg of porous silica nanoparticles for 24 hours, so that the doxorubicin is fully adsorbed in the porous silica nanoparticles, and centrifuge to remove the supernatant solution, fully washed 3 times, and then freeze-dried to form adriamycin nano-medicine;

[0062] (2) Mix the above-mentioned doxorubicin nanomedicine with 20% (w / w) PLGA in dichloromethane solution at a weight ratio of 1:9 and sonicate for 5 minutes to form a uniform suspension, that is, doxorubicin in oil Suspension of element nano drug (N / O);

[0063] (3) Add the doxorubicin in oil nano drug (N / O) suspension obtained in step (2) dropwise into 50...

Embodiment 2

[0070] Example 2 Preparation of microspheres loaded with small molecule drug doxorubicin (2)

[0071] The preparation of polycaprolactone (PCL) microspheres loaded with doxorubicin nanomedicine comprises the following steps:

[0072] (1) Dissolve 20 mg of doxorubicin in 0.5 ml of water, then stir with 20 mg of porous titanium dioxide nanoparticles for 24 hours, so that the doxorubicin is fully adsorbed in the porous titanium dioxide nanoparticles, centrifuge to remove the supernatant, and then fully Washed 3 times, then freeze-dried to form doxorubicin nanomedicine;

[0073] (2) Mix the above-mentioned doxorubicin nanomedicine with the ethyl acetate solution of PCL with a concentration of 0.5% (w / w) according to the weight ratio of 1:10 and ultrasonicate for 5 minutes to form a uniform suspension, that is, doxorubicin in oil Suspension of element nano drug (N / O);

[0074] (3) Add the doxorubicin in oil nano-drug (N / O) suspension obtained in step (2) dropwise to 50 ml conta...

Embodiment 3

[0079] Example 3 Preparation of Microspheres Loaded with Macromolecular Drug Growth Hormone (1)

[0080] Growth hormone has the effect of cell adhesion and promoting growth or delaying aging. The preparation of polylactic-glycolic acid (PLGA) microspheres loaded with growth hormone nano-medicine includes the following steps:

[0081] (1) Dissolve 10 mg of growth hormone and 10 mg of dextran into 0.4 ml of water to form a drug aqueous solution, and then transfer the above solution to 3.2 ml of 5% (w / w) polyethylene glycol (PEG8000) aqueous solution Mix well, then pre-freeze in a -80°C refrigerator for 12 hours, then freeze-dry with a lyophilizer, then dissolve PEG with dichloromethane and centrifuge to remove PEG to obtain growth hormone nanomedicine;

[0082] (2) Mix the above-mentioned somatotropin nanomedicine with 30% (w / w) PLGA acetonitrile solution at a weight ratio of 1:8, and ultrasonicate for 1 minute to form a uniform suspension, that is, somatotropin in oil drug (...

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Abstract

The invention discloses a method for preparing microspheres by using oil-in-nanoparticle mixed suspension-nanometer medicament-in-oil. The method comprises the following steps of: preparing a medicament and medicinal auxiliary materials into a nanometer medicament; adding the nanometer medicament into a polymer-containing organic solvent mixed solution for emulsifying; adding a nanometer medicament-in-oil mixed suspension into a water mixed suspension containing nanoparticles or containing nanoparticles and a surfactant for emulsifying to obtain an oil-in-nanoparticle mixed suspension-nanometer medicament-in-oil compound emulsion; and curing the obtained compound emulsion, and centrifugally collecting microspheres, wherein the obtained microspheres comprise the medicament, nanoparticles, the polymer and the medicinal auxiliary materials. An appropriate polymer material and an appropriate microsphere preparation method are selected, the prepared microspheres have high envelop rate, and a layer of self-assembled nanoparticles on the surfaces of the microspheres has the effects of improving cell adhesion and reducing inflammation and microencapsulation caused by local excessive acid and hydrophobic materials. The method disclosed by the invention can be applied to preparation of other medicament slow release or controlled release microspheres.

Description

technical field [0001] The invention relates to a method for preparing drug microsphere preparations, in particular to a method for preparing microspheres from oil-in-oil-in-oil nanometer medicine (N / O / N) in nanoparticle suspension, and belongs to the technical field of pharmacy. Background technique [0002] In the pharmaceutical industry, from drug discovery to clinical application, the last link is drug preparation. Some of the drugs need long-term administration to be cured, and some of them need targeted and other local administration. To achieve these goals, raw materials must be prepared into corresponding dosage forms. For example, drugs that require long-term administration but have a short half-life in the body should be prepared as sustained-release or controlled-release dosage forms; for the treatment of some tumors, some drugs need to be targeted to the lesion, such as embolization microsphere preparations that target tumor blood vessels, etc. . [0003] Rega...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K45/00A61K47/34A61K47/38
Inventor 袁伟恩陈英辉
Owner JINSHAN HOSPITAL FUDAN UNIV
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