Preparation method of long-circulating nanoparticle

A nanoparticle, long-circulation technology, applied in non-active ingredients medical preparations, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problems of short half-life, low lipid solubility, and unpredictability of drugs

Inactive Publication Date: 2012-05-16
夏落
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Problems solved by technology

[0005] 5-fluorouracil can be used alone or in combination to treat various types of malignant tumors, but its main disadvantages are low fat solubility, incomplete and unpredictable oral absorption; after intravenous or arterial administration, the drug has a short half-life (only 10 minutes in the body) , is not c...

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Embodiment Construction

[0008] The preparation steps of the present invention are as follows: take 5-Fu, PEG-PHDCA and phospholipids, dissolve them in a mixed organic solvent of tetrahydrofuran and ethanol to form an organic phase, and slowly add this organic phase dropwise to the surface active In the aqueous phase of the agent, after the dropwise addition, continue to stir for 1 h to fully diffuse the organic phase, and then evaporate the organic solvent under reduced pressure to obtain a blue-opalescent nanoparticle colloidal suspension. The precipitate was separated by centrifugation and washed; ultrasonically dispersed with 4% mannitol solution and freeze-dried.

[0009] The present invention selects stirring speed, preparation temperature, V 水 :V 有机 , The amount of phospholipids is used as the influencing factor of the quality of nanoparticles, as shown in Table 1, Table 2, Table 3, and Table 4.

[0010] Table 1 The influence of stirring speed on the quality of nanoparticles

[0011] ...

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Abstract

The invention which belongs to the medicine processing field concretely relates to a preparation method of a long-circulating nanoparticle. The preparation method of the long-circulating nanoparticle provided in the invention has the advantages of simple operation, and good targeting and good in vitro release of products. The method comprises the following steps: 1, dissolving 5-Fu (5-fluorouracil), PEG-PHDCA (polyethylene glycol-poly(hexadecyl cyanoacrylate)) and a phosphatide in a mixed organic solvent of tetrahydrofuran and ethanol to form an organic phase; 2, slowly adding the organic phase to a water phase of a surfactant in a dropwise manner under magnetic stirring, and fully diffusing the organic phase by continuously stirring for 1h after finishing the dropwise addition; 3, carrying out reduced pressure evaporation to remove the organic solvent to obtain a nanoparticle colloidal suspension with a blue opalescence; 4, carrying out ultracentrifugation separation deposition on the nanoparticle, and washing; and 5, carrying out ultrasonic dispersion with a 4% mannitol solution, and freeze-drying.

Description

Technical field: [0001] The invention belongs to the field of pharmaceutical processing, and more specifically relates to a preparation method of long-circulation nanoparticles. Background technique: [0002] As we all know, the human body has a strong defense function, and its powerful reticuloendothelial phagocytic system has a strong ability to recognize foreign bodies. Many studies have found that after intravenous administration of nanoparticles, they are mainly concentrated in monocyte-macrophage (MPS)-rich organs, especially the liver, spleen, and bone marrow, which is certainly desirable for drugs targeting these organs Yes, but for other drugs, nanoparticles are concentrated in these organs, so that the circulation time of the drug in the blood is very short, and it cannot reach the target organs, and cannot produce long-term sustained release. To address the above issues, long-circulating nanoparticles have been developed. [0003] Long-cycle nanoparticles mainly...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/513A61K47/34A61J3/02A61P35/00
Inventor 夏落
Owner 夏落
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