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Oil in water-oil in oil-water in oil method for preparing microballoons

An oil-in-oil and water-in-oil technology is applied in the field of oil-in-water-oil-in-oil-water-in-oil preparation of microspheres, which can solve the problems of incomplete release, easy sudden release of drugs, and low encapsulation rate, etc. Good dispersion effect

Inactive Publication Date: 2009-06-24
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these two methods have the disadvantages that the encapsulated drug is easy to release suddenly, the encapsulation rate is not high, and there is incomplete release. The W / O / O method reported in the literature also has disadvantages such as environmental pollution.

Method used

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  • Oil in water-oil in oil-water in oil method for preparing microballoons
  • Oil in water-oil in oil-water in oil method for preparing microballoons

Examples

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Comparison scheme
Effect test

Embodiment 1

[0030] Example 1: Preparation of PLGA Microspheres Loaded with Small Molecule Drugs

[0031] (1) Prepare a drug solution, and dissolve the small molecule drug in water directly or by adding excipients;

[0032] In this embodiment, the small molecule drugs used are tumor chemotherapy drugs (tumor chemotherapy drugs are selected from: doxorubicin, cyclophosphamide, dactinomycin, bleomycin, daunorubicin, doxorubicin, epirubicin Mitomycin, Mitomycin, Methotrexate, Fluorouracil, Carboplatin, Carmustine (BCNU), Semustine, Cisplatin, Etoposide, Camptothecin and its derivatives, Cholesterol , paclitaxel and its derivatives, docetaxel and its derivatives, vinblastine, vincristine, tamoxifen, etoposide, piposulfan, cyclophosphamide, or flutamide and its derivatives; sustained release Microspheres can be loaded with one or more of the above drugs;) or antibiotics (antibiotics are selected from cyclosporine, levofloxacin, ofloxacin, or epinastine hydrochloride; slow-release microspheres ...

Embodiment 2

[0045] Example 2: Preparation of PLGA microspheres loaded with biomacromolecular drugs

[0046] (1) Prepare a biomacromolecular drug solution, and dissolve the biomacromolecular drug in water by adding auxiliary materials;

[0047] In this example, the biomacromolecular drugs used are erythropoietin (EPO), recombinant human granulocyte colony-stimulating factor (G-CSF), granulocyte-macrophage colony-stimulating factor (GM-CSF), vaccines, Interferon (INF), growth hormone (GH), insulin (Insulin), epidermal growth factor (EGF), fibroblast growth factor (FGF), transforming growth factor (TGF-β), insulin-like growth factor (IGF), Vascular endothelial growth factor (VEGF), platelet growth factor (PDGF), endothelial growth factor (ECGF), nerve growth factor (NGF), bone-derived growth factor (BDGF), bone morphogenic protein (BMP), tissue polypeptide antigen ( TPA), antibody (antibody), coagulation factor VIII (VIII), genetic factor IX, antisense nucleotide (anti-RNA), small molecule ...

Embodiment 3

[0059] Example 3: Preparation of PLA Microspheres Loaded with Small Molecule Drugs

[0060] Step (1) is the same as in Embodiment 1.

[0061] (2) According to the dichloromethane, acetonitrile or ethyl acetate solution of the drug solution and PLA: 1:1, 1:2, 1:3, 1:4, 1:5, 1:6, 1:7, 1: 8. 1:9, 1:10 equal ratio stirring, vortex or ultrasonic for 1-5 minutes to form a uniform suspension that is water in oil (W / O 1 ) lotion;

[0062] Steps (3), (4), (5) are the same as in Embodiment 1.

[0063] The microsphere that present embodiment obtains, its specific component ratio is as follows:

[0064] drug solution

[0065] Epirubicin 1

[0066] The microspheres prepared by this method can be used for diseases requiring long-term treatment, especially for diseases requiring local treatment such as tumor vascular embolization microspheres. The encapsulation rate of the microspheres prepared by this method can reach at least 70%, and the burst release is small and ...

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Abstract

The invention relates to a method for preparing microspheres by water-in-oil-in-oil-in-water in the technical field of pharmacy, which comprises the following steps: a medicine solution is prepared first, and is dispersed into an organic solution with a slow release or controlled release functional material, and the stirring or swirling and so on is preformed to make the medicine solution dispersed evenly to form a suspension; then the suspension is added into an external oil phase to be stirred or swirled to form microspheres, and finally the microspheres are transferred into a large water phase for solidification; and then the microspheres are centrifugally collected, freeze-dried and preserved, wherein in the obtained microspheres, the medicine accounts for 0.01 to 50 percent of the weight of the entire microshperes, the slow release or controlled release material accounts for 20 to 99.99 percent of the weight of the entire microshperes, and an auxiliary material accounts for 0 to 30 percent of the weight of the entire microshperes. The microspheres prepared by the method have smooth and round surfaces and good uniformity, are regular, have no adhesion, and have adjustable grain diameters; the used organic solvent is environment-friendly, is easy to remove by water, and does not affect the treatment effect of the medicine; and the microspheres have high envelope rate, and small burst release and incomplete release.

Description

technical field [0001] The invention relates to a method for preparing pharmaceutical microspheres in the technical field of pharmacy, in particular to a method for preparing microspheres by oil-in-water-oil-in-oil-water-in-oil (W / O / O / W). 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; others 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 dosage forms; for the treatment of some tumors, some drugs need to be targeted to the disease, such as embolization microsphere preparations that target tumor blood vessels; Since recombinant technology has been used in the expression and production of therapeutic pro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16
Inventor 金拓袁伟恩吴飞郭梅燕窦学文
Owner SHANGHAI JIAO TONG UNIV
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