Preparation method of long-circulating nanoparticles

A nanoparticle, long-circulation technology, applied in medical preparations containing active ingredients, pharmaceutical formulations, organic active ingredients, etc., can solve problems such as low fat solubility, incomplete oral absorption, and unfavorable continuous chemotherapy.

Inactive Publication Date: 2013-04-03
魏奇
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AI Technical Summary

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 conducive to continuous chemotherapy, and has dose-dependent toxicity such as local irritation, gastrointestinal reactions, and bone marrow suppression; the antitumor activity of synthetic fluorouracil derivatives is not high, and these shortcomings limit the clinical application of 5-Fu to a certain extent. application on

Method used

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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, then evaporate the organic solvent under reduced pressure to obtain a blue-opalescent nanoparticle colloidal suspension, and the nanoparticle is subjected to ultra-speed 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 t...

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Abstract

The invention relates to a preparation method of long-circulating nanoparticles and belongs to the field of drug processing. The preparation method can be operated simply and can produce the long-circulating nanoparticles having good targeting performances and external release properties. The preparation method comprises the following steps of dissolving 5-Fu, PEG-PHDCA and phospholipid in a mixed organic solvent of tetrahydrofuran and ethanol to obtain an organic phase, slowly and dropwisely adding the organic phase into a water phase of a surfactant with magnetic stirring, then persistently stirring for 1 hour so that the organic phase is dispersed fully, carrying out reduced pressure evaporation to remove the mixed organic solvent and to obtain a nanoparticle colloidal suspension liquid having blue opalescence, carrying out overspeed centrifugal separation precipitation and washing of nanoparticles, carrying out ultrasonic dispersion by a mannitol solution having the content of 4%, and carrying out 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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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/513A61P35/00
Inventor 魏奇
Owner 魏奇
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