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Radioactive sustained-release particle and preparation and use thereof

A technology of radioactivity and radioactivity, applied in the field of radiology medicine, achieves huge application advantages and prospects, increases local drug concentration, and prolongs the effect of action time

Inactive Publication Date: 2008-12-17
王自正 +7
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is currently no use of PLLA with 32 Radioactive antitumor drug combined with P-CP colloid

Method used

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  • Radioactive sustained-release particle and preparation and use thereof
  • Radioactive sustained-release particle and preparation and use thereof
  • Radioactive sustained-release particle and preparation and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1: 32 Preparation of P-CP-PLLA sustained-release particles and investigation of their general shape and particle size.

[0025]Put 0.75~1.25g PLLA and 10~20mg magnesium stearate into the grinder, add 4.5~7.5ml 32 P-CP colloidal solution (radioactive concentration is 1875 ~ 5625MBq / ml), with 2ml of absolute ethanol as a dispersant, stirred at a low speed (150r / min) at a constant temperature (50°C) for 30min, placed in a vacuum oven to dry for 5h, Grind it to a powder in a grinder and press to make radioactive 32 P-CP-PLLA sustained-release particles. income 32 The specifications of P-CP-PLLA particles are as follows: the particles are light green cylindrical, with a diameter of 0.85mm-0.9mm, a length of 2.2mm-2.5mm, a round shape, tiny pores on the surface, a hard texture, and a mass of 0.9-1.1mg / granule. The radioactivity is 11.25~37.5MBq / capsule, and the single particle is packaged and sealed for storage.

Embodiment 2

[0026] Example 2: Radioactivity 32 Study on the radioactive release rate of P-CP-PLLA sustained-release particles in vitro.

[0027] Select 90 grains with uniform mass and radioactivity 32 P-CP-PLLA slow-release particles (mass 1 ± 0.05mg, radioactivity 33.75 ± 1.6875MBq), were randomly divided into 9 groups, 10 particles in each group, and the total radioactivity of each group of particles was measured, recorded as A (n·0) (n is the group, recorded as 1-9 groups), placed in 9 petri dishes, each 3 petri dishes as a group, add release medium saline, 1640 culture solution, human serum 5.0ml each. Put it in a water bath shaker, the temperature is 37°C, and the shaking frequency is 100 times / min. On days 1, 3, 7, 15, 21, and 30 (represented by t, the time point is recorded as 1-6), 1.0ml of the release medium was taken from the culture dish, and the radioactive count was measured by an enhanced activity meter, which was recorded as B (n·t) , the radioactivity after attenuation ...

Embodiment 3

[0031] Example 3: 32 P-CP-PLLA slow-release particles implanted in mice biodegradation and 32 P Biodistribution.

[0032] Select 35 BALB / c mice, weighing 20±2g, randomly divide them into 7 groups, 5 mice in each group, measure and select the ones with more uniform mass and radioactivity 32 35 P-CP-PLLA sustained-release particles (mass 1 ± 0.05mg, radioactivity 33.75 ± 1.6875MBq), radioactive counts were measured and implanted into the left hind leg muscle of mice by percutaneous puncture, one for each mouse Dynamically observe the local and general conditions of the mice implanted with particles, and take 1ml of blood from the orbital vein of a group of mice at 0.5, 1, 3, 7, 14, 21, and 30 days after implantation, and then remove The cervical spine was sacrificed, and major organs and tissues such as the heart, liver, spleen, lung, kidney, pancreas, stomach, intestine, brain, right hind leg muscle, muscle around the particle, and femur were harvested, the wet weight was mea...

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Abstract

The invention discloses a radioactive slow-release particle and a preparation method and the application thereof, pertaining to the field of radiation medicine. The particle mainly consists of <32> P-chromium phosphate and poly-L-lactic acid and can better solve the problem of targeted delivery of drugs in the treatment of tumors. The transplant of the particles in a tumor body or around a tumor can increase the local concentration of the drug, prolong the time of drug action and reduce systemic toxic and side effects.

Description

Technical field: [0001] The invention belongs to the field of radiation medicine, and relates to a radioactive slow-release particle and its preparation method and application. Background technique: [0002] radiopharmaceutical 32 P-chromium phosphate ( 32 P-chromic phosphate, 32 P-CP) colloid was used in the treatment of malignant effusion in the cavity, interstitial tissue and lymphatic treatment in the early years [1-4] . 32 P is pure beta - The emitter has an average energy of 0.695 MeV (the maximum energy is 1.71 Mev), a half-life of 14.28 days, and an average range of 3 to 4 mm in the tissue (the maximum range is 7.6 mm). The radioactive distribution of the whole body can be roughly observed through bremsstrahlung imaging. It is easy to protect against radiation in clinical application, and the source is easy and the price is moderate, so it is an ideal nuclide for treatment. 32 The size of P-CP colloidal particles is about 20-50nm (accounting for 60%), its physi...

Claims

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Application Information

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IPC IPC(8): A61K51/12A61K51/06A61P35/00
Inventor 王自正刘璐黄培林祁本忠王峰李少华杜同信邵国强
Owner 王自正
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