Microspheres comprising therapeutic and diagnostic radioactive isotopes

A radioisotope, radioactivity technology, applied in the directions of radioactive carrier, radioactive physical shape, radioactive preparations in vivo, etc., can solve the problems of measuring the biodistribution of microspheres, unable to directly measure the biodistribution, complicated development of microspheres, etc.

Inactive Publication Date: 2006-07-05
BIOSPHERE MEDICAL INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

2. Loading cannot be directly measured in clinical trials 90 The biodistribution of Y microspheres, because 90 Y is a pure beta emitter, producing no imageable gamma rays
[0010] As mentioned above 90 Development of microspheres for radionuclide therapy appears complicated by difficulties in measuring microsphere biodistribution in vivo

Method used

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  • Microspheres comprising therapeutic and diagnostic radioactive isotopes
  • Microspheres comprising therapeutic and diagnostic radioactive isotopes
  • Microspheres comprising therapeutic and diagnostic radioactive isotopes

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0139] Calculation contains 89 Y The glass microspheres required for optimal 197 Au quantity

[0140] experimental design

[0141] In this example, we want to use a sufficient amount of 198 Au labeled radioactive 90 Y glass microspheres so that the microspheres can be detected by a gamma camera. In this example, in addition to containing gold compounds, the microspheres have the same composition as commercially available Theraspheres (40% Y 2 o 3 (weight) or 31% Y) the same composition. Activation by neutrons containing stable isotope Y 89 and Au 197 The glass microspheres were used for this method. In this example, if the sample is removed from the neutron flux, the radioactivity required per 50 mg of glass microspheres is 100 mCi Y 90 and 1 μCi Au 198 , we wish to calculate the required initial Au 197 quantity. Y 89 and Au 197 The neutron capture cross-sections are 1.3 target and 98.8 target respectively, and Y 90 and Au 198 The decay constants are 3.0...

Embodiment 2

[0152] In this example, we assume that the glass composition contains 13% Y 2 o 3 (weight) (or 10% Y), and the radioactive Y required per 50 mg of glass microspheres 90 100mCi, Au 198 10μCi. Other amounts are with embodiment 1. Similar calculations show that the glass should contain 291ppb gold and require a neutron activation time of 6.10×10 5 s. Similar calculations can be made for other proportions of these elements, or other elements combined in any proportion.

Embodiment 3

[0154] Preparation of glass beads

[0155] There have been previous reports on the preparation of glass microspheres. See US Patent 5,302,369. In these preparations, Si, Al, K, Mg, Al, Pb, and P 2 o 5 of different compositions of glass. 50 g of glass obtained in batches was melted in a platinum crucible using an electric furnace at close temperature. A typical melt cycle requires 3 hours per charge at 1000°C and 3 to 4 hours to purify the melt at the approximate melting temperature.

[0156] The crucible containing the melt was quenched with 25°C water, and then the glass feedstock obtained in the crucible was crushed and ground to -100 mesh. The -100 mesh glass powder was then slowly fed with a vibrating doctor blade to an oxygen / propane flame where surface tension pulled the molten particles into balls. The flow rates of oxygen and propane for each glass composition were adjusted to produce spherical particles of the highest particle size fraction. After spheroidizati...

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Abstract

One aspect of the present invention relates to a microsphere impregnated with a radioisotope that emits therapeutic ß-particles and a radioisotope that emits diagnostic gamma radiation; wherein the atomic number of the first radioisotope is not the same as the atomic number of the second radioisotope. In one preferred embodiment, the microsphere is composed of glass impregnated with 90 Y as the source of the therapeutic ß-emissions and 98 Au as the source of the diagnostic gamma emissions. Another aspect of the present invention relates to the preparation of a microsphere impregnated with a radioisotope that emits therapeutic ß-particles and a radioisotope that emits diagnostic gamma radiation; wherein the atomic number of the first radioisotope is not the same as the atomic number of the second radioisotope. In one preferred embodiment, a glass microsphere containing 90 Y and 198 Au is prepared by neutron activation of a glass microsphere comprising glass, 89 Y and 197 Au. Another aspect of the present invention relates to administration to a mammal of a therapeutically effective amount of microspheres impregnated with a ß-emitting radioisotope and a gamma emitting radioisotope; wherein the atomic number of the first radioisotope is not the same as the atomic number of the second radioisotope. In one preferred embodiment, said microspheres are administered to the patient through a catheter.

Description

[0001] related application [0002] This application claims the benefit of priority to US Patent Application Serial No. 10 / 407,144, filed April 4,2003. Background of the invention [0003] The development of new and more effective treatments for cancer is of great interest. This need is especially acute for the treatment of malignancies arising in the liver, as current treatment options are unsatisfactory. Currently, the preferred method of treatment for patients with liver metastases is surgical resection. Unfortunately, the 5-year survival rate for patients undergoing this form of treatment is only about 35%. Scheele J and Altendorf-Hofmann A. Resection of colorectal liver metastases. Langenbeck's Arch. Surg. 1999; 313-327. This disappointingly low survival rate is exacerbated by the fact that most tumors are inoperable at diagnosis. Other options for treating these tumors include conventional chemotherapy and external beam rad...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/00A61M36/14A61K51/02A61K51/12
CPCA61K51/1251A61K51/02A61P35/00A61K51/12
Inventor A·施瓦茨J·A·克洛姆
Owner BIOSPHERE MEDICAL INC
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