Method for making rhenium-186/188 labeled human serum albumin microspheres and kit for making the same and method for using the kit

Patent metadata

Field	Value
Publication number	US-9295740-B2
Application number	US-201213538105-A
Country	US
Kind code	B2
Filing date	Jun 29, 2012
Priority date	Dec 30, 2011
Publication date	Mar 29, 2016
Grant date	Mar 29, 2016

Abstract

The present invention relates to a method for preparing 186/188 Re-labeled human serum albumin (HSA) microspheres by 186/188 Re(I)-tricarbonyl ion. This radioactive particle can be subjected to radioembolization for liver tumor. In this method, 186/188 Re(I)-tricarbonyl ion ( 186/188 Re(OH 2 ) 3 (CO) 3 ) + ) are employed as a precursor for directly labeling HSA microspheres with 186/188 Re at appropriate temperature.

First claim

What is claimed is:

1. A method for preparing 186/188Re labeled HSA microspheres, the method comprising:
reacting 186/188Re(I)-tricarbonyl ions with Human Serum Albumin (HSA) microspheres to produce 186/188Re-HSA microspheres.

2. The method according to claim 1 , wherein the HSA microspheres are dried particles with a diameter of 0.1 μm to 10000 μm.

3. The method according to claim 1 , wherein said reaction step is performed at a temperature of 25-150° C.

4. The method according to claim 1 , further comprising using said 186/188Re-HSA microspheres as a radiotherapeutic and diagnostic agent for cancer.

5. The method according to claim 2 , the method further comprising the steps of:
keep flushing vial (A) with CO gas;
adding 186/188Re solution withdrawn from vial (C) into vial (A);
incubating the mixture solution in vial (A) at an appropriate temperature;
suspending HSA microspheres in vial (B) with polysorbate 80; and
injecting 186/188Re(I)-tricarbonyl ion synthesized from vial (A) into vial (B) to produce and purify 186/188Re-HSA microspheres at appropriate temperature.

6. The performing method according to claim 5 , wherein the appropriate temperature is 25-150° C.

7. The performing method according to claim 5 , wherein 186/188Re-HSA microspheres can be radiotherapeutic and diagnostic agent for cancer disease.

8. The method of claim 1 , further comprising:
providing a first vial with borane ammonia (NH3BH3);
providing a second vial with dried HSA microspheres;
flushing said first vial with CO gas;
adding a solution of 186/188Re in saline to said first vial to create an 186/188Re(I)-tricarbonyl ion solution;
adding polysorbate 80 to said second vial to create a suspension of said HSA microspheres;
injecting said 186/188Re(I)-tricarbonyl ion solution from said first vial into said second vial create 186/188Re-HSA microspheres; and
purifying said 186/188Re-HSA microspheres.

9. The method according to claim 8 , wherein said injecting step is performed at a temperature of 25-150° C.

10. The method according to claim 8 , further comprising using said 186/188Re-HSA microspheres as a radiotherapeutic and diagnostic agent for cancer.

Assignees

• Yu Chia-Yu
• Lee Te-Wei
• Chen Su-Jung
• Chen Liang-Cheng
• Lin Chien-Hong
• Iner Aec Executive Yuan

Inventors

• Yu Chia-Yu
• Lee Te-Wei
• Chen Su-Jung
• Chen Liang-Cheng
• Lin Chien-Hong

Classifications

• A61P35/00

  Antineoplastic agents · CPC title

• A61K51/081 Primary

  the protein being an albumin, e.g. human serum albumin [HSA], bovine serum albumin [BSA], ovalbumin · CPC title

• A61K51/1251

  micro- or nanospheres, micro- or nanobeads, micro- or nanocapsules · CPC title