Medical iodine-131 carbon microspheres and preparation method thereof

A technology of carbon microspheres and preparations, which is applied in the field of medical iodine-131 carbon microspheres and its preparation technology, can solve the problems of limited cation resin exchange capacity, low specific activity of resin microspheres, and influence on popularization and application, etc. Environmental protection, easy promotion and application, good safety effect

Active Publication Date: 2016-12-07
CHENGDU NEW RADIOMEDICINE TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But Yttrium-90 ( 90 Y) Glass microspheres and phosphorus-32 ( 32 P) Glass microspheres must be obtained by placing non-radioactive yttrium glass microspheres or phosphorus glass microspheres in a high-flux nuclear reactor and irradiating them with neutrons. Because the number of high-flux nuclear reactors in the world is limited, timely production of yttrium- 90 ( 90 Y) Glass microspheres and phosphorus-32 ( 32 P) Glass microspheres are restricted, which affects the promotion and application
Yttrium-90 ( 90 Y) Resin microspheres are prepared by cation resin microspheres adsorbing yttrium-90 separated by strontium-90 / yttrium-90 separation device, and then curing. Due to the limited exchange capacity of cation resin, yttrium-90 ( 90 Y) The specific activity of resin microspheres is relatively low, and the popularization and application are also limited

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] (1) Purification of carbon microspheres: Soak in organic solvents such as ethyl acetate, acetone or ethanol to remove fat; soak in dilute sodium hydroxide solution (0.1-0.5mol / L) to remove alkali-soluble impurities, and then repeatedly wash to weak alkali (PH value of 8-10); then soak in dilute nitric acid (0.1mol / L-0.5mol / L) to remove acid-soluble impurities, and wash until the pH value is 1-2.

[0054] (2) Use 5 mL of HNO with a pH value of 1 3 1-3 grams of purified carbon microspheres are soaked in the solution, and after solid-liquid separation (centrifugation or filtration), the pH value of the soaked carbon microspheres is 1-2.

[0055] (3) Add Na containing the required radioactivity (such as 0.185-11.1GBq (5-300mCi) 131 I solution (contains I - Ionophore 10-20mg ) 1-2mL, add HNO with a pH value of 1 3 Soak 1-3 grams of carbon microspheres in 8 mL of the solution.

[0056] (4) Add 2mL (concentration is 30% (mL / mL)) H 2 o 2 solution, shaken at 45°C for 50 mi...

Embodiment 2

[0062] (1) Treat 1-3 grams of carbon microspheres according to the method of steps (1) and (2) in Example 1, so that the pH value of the carbon microspheres is 1-2.

[0063] (2) Add the required radioactivity (such as 0.185-11.1GBq (5-300mCi) of Na 131 I solution (contains I - Ionophore 10-20mg ) 1-2mL.

[0064] (3) Add 0.10mol / L KIO 3 Solution 2mL, shaking at 45°C for 50 minutes, negative iodide ions (including 131 I - Ionic and non-radioactive I - ions) are oxidized to iodine molecules (IO 3 - +6H + +5I - =3 I 2 +3H 2 0) while being adsorbed by medical carbon microspheres ( 131 The adsorption efficiency of I is higher than 99%), after solid-liquid separation (centrifugation or filtration), the medical iodine-131 carbon microspheres after the oxidative adsorption of iodine is processed by the solidification treatment method in the step (4) in the embodiment 1, The release rate of iodine-131 is lower than 0.01%, Ag + The ion concentration is lower than 20ng / L, so ...

Embodiment 3

[0066] (1) Treat 1-3 grams of carbon microspheres according to the method of steps (1) and (2) in Example 1, so that the pH value of the carbon microspheres is 1-2.

[0067] (2) Add the required radioactivity (such as 0.185-11.1GBq (5mCi-300mCi) of Na 131 I solution (contains I - Ionophore 10-20mg ) 1-2mL.

[0068] (3) Add 0.10mol / L KMnO 4 The best solution is 2mL, then add 25% H 2 SO 4 2.0mL to control the acidity of the reaction solution. Shake at 45°C for 50 minutes, and negative iodide ions (including 131 I - Ionic and non-radioactive I - ions) oxidized to iodine molecules (2MnO 4 - +10I - +16 H + =2Mn 2+ +5I 2 +8 H 2 O) and was adsorbed by medical carbon microspheres ( 131The adsorption efficiency of I is higher than 99%), after solid-liquid separation (centrifugation or filtration), the medical iodine-131 carbon microspheres after the oxidative adsorption of iodine is processed by the solidification treatment method in the step (4) in the embodiment 1, T...

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Abstract

The invention discloses medical iodine-131 carbon microspheres for tumor radiotherapy or tumor early-stage imaging diagnosis and a preparation method thereof. The medical iodine-131 carbon microspheres are prepared in the manner that molecular iodine (I2) generated by a reaction of a medical Na131I solution and an oxidizing agent like hydrogen peroxide is adsorbed with carbon microspheres, and then curing treatment is carried out; or, the medical iodine-131 carbon microspheres are prepared in the manner that carbon microspheres are treated with an Ag(NO3) solution and then react with a medical Na131I solution to generate Ag131I, and Ag131I is deposited in the carbon microspheres and cured. The adsorption or curing efficiency of the medical iodine-131 carbon microspheres on iodine-131 nuclides is higher than 99%, the 131I release rate of the medical iodine-131 carbon microspheres subjected to further curing treatment is lower than 0.01%, and the medical iodine-131 carbon microspheres are good in biocompatibility and applicable to in-vivo tumor radiotherapy or tumor early-stage imaging diagnosis.

Description

technical field [0001] The invention relates to a medicine for tumor radiotherapy and tumor radiation imaging diagnosis and a preparation process thereof, in particular to a medical iodine-131 carbon microsphere and a preparation process thereof. Background technique [0002] Radioactive microspheres have a certain history as human arterial embolization radiotherapy for tumors. Yttrium-90 (90Y) glass microspheres have been approved by the US FDA for many years and are widely used in the United States, Canada, Europe and many Asian countries. Yttrium-90 (90Y) Resin microspheres have been approved for marketing in Australia【Bruno Sangro, Mercedes Inarrairaegui, JoseI.Bilbao.Radioembolization for hepatocellular carcinoma.Journal of Hepatology2012;56:464-473】Phosphorus-32 (32P) glass microspheres have been developed in China for many years. There have been many reports on clinical research [Zheng Guangyong, Wang Dazhang. A new anticancer therapy-radioactive glass microspheres in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/12A61P35/00A61P35/04C01B7/14A61K101/02
CPCA61K51/1251A61K51/1268C01B7/14C01P2004/61C01P2004/62C01P2004/64C01P2004/80C01P2006/80A61K51/12A61P35/00A61P35/04
Inventor 李茂良蔡继鸣
Owner CHENGDU NEW RADIOMEDICINE TECH CO LTD
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