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Magnetic pirarubicin nano-drug composite

A magnetic pirarubicin and pirarubicin technology, which can be used in drug combinations, antitumor drugs, pharmaceutical formulations, etc., can solve the problems of inability to withstand perfusion chemotherapy, lack of targeting of chemotherapy drugs, and bladder epithelial cell killing, etc. To achieve the effect of good dispersion and reduce toxic and side effects

Inactive Publication Date: 2014-01-29
代宏 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, unfortunately, there are still many patients who cannot withstand infusion chemotherapy due to the lack of targeting of chemotherapy drugs infused into the bladder, resulting in the killing of normal bladder epithelial cells.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1 Preparation of Magnetic THP Nano-Preparation

[0031] 1) Magnetic Fe 3 o 4 Preparation of nanoparticles:

[0032] With reference to the method of J MagnMagn Mater, 2006, 302 (2): 397-404, which is incorporated by reference in its entirety, the preparation of magnetic Fe 3 o 4 Nanoparticles, the specific preparation process is as follows:

[0033] Under nitrogen protection, 8.14 g of ferric chloride hexahydrate and 3.00 g of ferrous chloride tetrahydrate were dissolved in 30 mL of deionized water, and 0.85 mL of 12 mol / L hydrochloric acid solution was added. Add the above solution dropwise to 250 mL of 1.5 mol / L sodium hydroxide solution, stir for 30 min, collect the precipitate, wash with deionized water three times, and dry in vacuum to obtain Fe with an average particle size of about 40 nm. 3 o 4 nanoparticles.

[0034] 2) Aminated Fe 3 o 4 preparation:

[0035] Under the protection of nitrogen, the 0.1g Fe obtained in step 1) 3 o 4 Nanoparticles...

Embodiment 2

[0038] Example 2 Characterization of Magnetic THP Nano-Preparations

[0039] Observation by scanning electron microscopy (Inspect F50, FEI, USA) of magnetic Fe 3 o 4 The shape of nanoparticles, the nanoparticles with a particle size of about 40nm, the particle size distribution is relatively uniform, see Figure 1a .

[0040] Aminated Fe was scanned using a Fourier transform infrared spectrometer (Spectrum GX, Perkin Elmer, USA) 3 o 4 ,See Figure 1b 1 ,exist Figure 1b 1 Medium, 3431cm -1 and 1630cm -1 It is the characteristic absorption peak of N-H, which proves that the magnetic nano-Fe 3 o 4 The surface is modified by 3-aminopropyltriethoxysilane, and the surface is rich in active amino groups; determine the infrared spectrum of the magnetic THP nano drug composition, see Figure 1b 2 ,exist Figure 1b 2 Medium, 3000cm -1 Three weaker absorption peaks appear nearby, which are the absorption peaks of C-H on the benzene ring. 1620cm -1 The left and right pea...

Embodiment 3

[0046] Example 3 Determination of Stability of Magnetic THP Nano-Preparations

[0047] Weigh 0.0039g of magnetic THP nano-preparations, ultrasonically disperse them in PBS buffers with pH 7.4, 6.0, and 5.7, place them in dialysis bags, seal them, and immerse the whole in 50mL of PBS buffers with the same pH, at 37°C After standing still at 0.5 h, 1.0 h, 1.5 h, and 2 h, 2 mL of the solution was taken to measure the concentration of THP in it with a UV-Vis spectrophotometer (Lambda900, Perkin Elmer, USA). In addition, under the stirring condition of 700rpm, the THP concentration at the same time point was measured. The drug residue rate was calculated separately.

[0048] Figure 3 shows the THP drug residual rate of magnetic THP nanocomposites in PBS buffer with different pH values ​​under static state and stirred state. The results show that the magnetic THP nano-preparation or composition is pH=7.4 under normal physiological conditions ( Figure 3a ) in the buffer solution,...

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Abstract

The invention belongs to the field of pharmaceutical preparations, and particularly relates to a magnetic pirarubicin nano-drug composite. The magnetic pirarubicin nano-drug composite comprises pirarubicin, an Fe3O4 nanoparticle and 3-aminopropyl triethoxysilane, wherein the particle diameter of the Fe3O4 nanoparticle is 10-100 nanometers. The magnetic pirarubicin nano-drug composite disclosed by the invention has good stability and dispersity and property of being positioned to a tumour part in a targeted way through an external magnetic field and reduces the toxic side effect on a normal structure by restricting the dual inhibiting effect of THP and Fe3O4 on a cell on a specific tumour part.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a magnetic pirarubicin nanometer pharmaceutical composition and its application for treating bladder cancer. Background technique [0002] Bladder cancer is the malignant overgrowth of cells in the bladder that develops into a malignant tumor. Worldwide, bladder cancer is the seventh most common cancer in men, causing 112,300 deaths per year. In contrast, female patients are slightly less than male patients. Bladder cancer is the most common malignant tumor of the urinary system, 90% of which are transitional cell carcinomas, about 5% are phosphorous cell carcinomas, and 2% are adenocarcinomas. [0003] Currently, the most common treatments for bladder cancer are radical cystectomy and radiotherapy. But this treatment can cause irreversible damage to the patient, resulting in loss of organs, loss of sexual function, damage to normal tissues, etc. Therefo...

Claims

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Application Information

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IPC IPC(8): A61K33/26A61K47/48A61P35/00A61P13/10A61K31/7048A61K47/52A61K47/69
Inventor 代宏黄啸王春梅郑曦杨忠新潘君李风贾尚琼刘银
Owner 代宏
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