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Preparation method of high-gloss high-stability Elsinochrome silicon oxide nano granule and application thereof in preparing intravenous injection agent

A technology of coelomycin and silicon dioxide, which is applied in the field of photosensitizers, can solve the problems of poor photostability, poor water solubility, and inconvenient preparation of pharmaceuticals, and achieve high stability, easy operation, and favorable preparation and preservation. Effect

Active Publication Date: 2012-05-30
常熟紫金知识产权服务有限公司
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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 overcome the shortcoming that coelomectin is inconvenient to be made into medicament due to poor photostability and poor water solubility, and at the same time, according to the requirements of phototherapy drugs in the clinical treatment process of photodynamic therapy, the nanometer bismuth with core-shell structure Silica was introduced into the application research of estrocystin, and the echinoclavin silica nanoparticles with high photostability and good water solubility were prepared with clinical application prospects, and the nanoparticles were applied to the preparation of Intravenous injection of photodynamic drugs, that is, the application will provide a preparation method of escarcin dioxide nanoparticles with high photostability and good water solubility and its application in the preparation of intravenous injections

Method used

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  • Preparation method of high-gloss high-stability Elsinochrome silicon oxide nano granule and application thereof in preparing intravenous injection agent
  • Preparation method of high-gloss high-stability Elsinochrome silicon oxide nano granule and application thereof in preparing intravenous injection agent
  • Preparation method of high-gloss high-stability Elsinochrome silicon oxide nano granule and application thereof in preparing intravenous injection agent

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] A single silane was used to prepare high photostability coelomycin A silica nanoparticles, and the reaction system and conditions were as follows:

[0030] After adding 24 mL of methanol, 50 μL of echinocin A in DMSO (8 mmol / L), 200 μL of N-(β-aminoethyl)-γ-aminopropyl-triethoxysilane, and 200 μL of ammonia water to the experimental system, , magnetic stirrer for 20 hours, after the reaction, use hydrochloric acid to adjust the pH value of the solution to 7.0, dialyze to remove methanol and DMSO, freeze-dry to obtain high photostability estrocysin A silica nanoparticles.

Embodiment 2

[0032] Composite silanes were used to prepare highly photostable coelomycin A silica nanoparticles. The reaction system and conditions were as follows:

[0033]Add 24 mL of methanol, 50 μL of echinocin A in DMSO (8 mmol / L), 200 μL of N-(β-aminoethyl)-γ-aminopropyl-triethoxysilane, tetramethoxy After 200 μL of base silane and 200 μL of ammonia water, 20 hours on a magnetic stirrer, vacuum drying at 50°C, 50 mL of double distilled water and 80 μL of hydrochloric acid were added to adjust the pH to 7.0. The experimental temperature was kept at room temperature (20±2)°C.

Embodiment 3

[0035] Composite silane was introduced into surfactant CTAB to prepare coelomycin A silica nanoparticles. The reaction system and conditions were as follows:

[0036] Dissolve 0.36g CTAB and 800μL n-butanol in 20mL double-distilled water, stir with a magnetic stirrer until clarification, then add 50μL DMSO solution (8mmol / L) of estrocystin A to the solution, do not add to the empty nanoparticles Stir the solution with a magnetic stirrer until it becomes clear, add 200 μL TEVS and stir for one hour, then add 10 μL APTES and stir for 20 hours. The solution was then dialyzed against water for 48 hours using a 12-14 KD cellulose dialysis bag to remove the surfactants CTAB and n-butanol. Finally, the solution is freeze-dried to obtain escarcin A silica nanoparticles.

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Abstract

The invention relates to a method for preparing elsinochrome silicon dioxide nanoparticle with high photostability and fine water-solubility and application thereof in preparing vein injection, comprising the following preparation steps: (1) hydrolyzing a single silane terpenoid or multiple silane terpenoids under alkaline conditions to generate nanometer silicon dioxide with a nuclear shell structure; (2) encapsulating elsinochrome in absence or in presence of surface active agents to prepare the elsinochrome silicon dioxide nanoparticle which suits vein injection, features relatively high photostability and fine water-solubility and has a particle diameter less than 200 nm; and mole ratio relation between the reagents elsinochrome and silane ranging from 1:1 to 1: 10000. The photostability of the silicon dioxide nanoparticle is improved, photodegradation loss, preservation difficulty and preservation cost caused in the process of R&D, production and transportation and in use links are effectively reduced; moreover, the preparation method is simple, the operation is easy; furthermore, the capacity of active oxygen such as <1>O2 is strengthened, the invisible toxicity is low and the optical toxicity is high.

Description

technical field [0001] The invention belongs to the technical field of photosensitizers with photodynamic activity, and relates to a preparation method of estrocytin silica nanoparticles with high photostability and the high photostability echinoclavin silica nanoparticles Application in preparation of photodynamic drug intravenous injection. Background technique [0002] Compared with traditional tumor treatment techniques, photodynamic therapy (PDT) is a new type of tumor clinical therapy, which has the ability to specifically kill tumor cells, cause less damage to healthy tissues, have low toxic and side effects, and have fewer complications after treatment. And unique advantages such as economy and convenience, especially for those patients who are old or have contraindications to surgery, radiotherapy, and chemotherapy, as well as patients who relapse after surgery or radiotherapy, so this treatment method is currently recognized as a very promising Tumor treatment tec...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/04
Inventor 周家宏周林魏少华冯玉英董超沈健
Owner 常熟紫金知识产权服务有限公司
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