Cladded nuclide labeled protein microsphere, preparation method and applications thereof

A technology for labeling proteins and microspheres, which is applied in the field of encapsulated nuclide-labeled protein microspheres, can solve the problems of radionuclide off-labeling, no chitosan/sodium alginate wrapping, etc., to reduce off-labeling and clinical use Safe, prolonging the effect of degradation time

Inactive Publication Date: 2011-01-12
WEST CHINA HOSPITAL SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Generally speaking, raw materials and radionuclides that can be used as sustained-release preparations are two types of substances with different properties. At present, there is no relevant literature report on the use of chitosan / sodium alginate for encapsulating radionuclides to prevent radionuclides from coming off the label.

Method used

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  • Cladded nuclide labeled protein microsphere, preparation method and applications thereof
  • Cladded nuclide labeled protein microsphere, preparation method and applications thereof
  • Cladded nuclide labeled protein microsphere, preparation method and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] The preparation method of embodiment 1 microsphere of the present invention

[0049] 1. Raw materials:

[0050] Na 131 I, Na 125 I (sodium iodide)

[0051] Medical type B gelatin: Sigma type A gelatin 50g microspheres are prepared by the modified emulsification condensation method. Bottled after chloramine-T labeling

[0052] Marked with Na 131 I is 2mCi, that is 2ul; use Na 125 I is 4mCi, that is, 4ul; use gelatin microspheres 0.8g; use sodium alginate is 0.3g; use chitosan is 0.3g. Therefore, the ratio of the components of the encapsulating nuclide microspheres in this test is: 0.002:0.004:0.8:0.3:0.3.

[0053] where Na 131 I, Na 125 The specific radioactive concentration of I is: 37GBq / ml.

[0054] The specific preparation method is:

[0055] 1. Microsphere Fabrication

[0056] Prepared by improved emulsification condensation method. Take 80ml of liquid paraffin, add 0.8ml of Span-80, put it into a round bottom flask, and place it in a water bath at 55°C...

Embodiment 2

[0076] Embodiment 2 Energy peak determination of double-labeled microspheres of the present invention

[0077] The non-coated microspheres prepared in step 2 of Example 1 were labeled with energy peaks, and the specific results were as follows, wherein the labeled microspheres were washed 4 times with normal saline, and after each cleaning, the 131 I and 125 I activity is measured, and concrete assay method and result are as follows:

[0078] Radiation dosimetry:

[0079] When using the CRC-15R medical activity meter of American CAPINTEC.INC company to measure mixed markers, select 131 I channel measurement 131 When the radioactivity of I 125 I would interfere, too, by choosing 125 I channel measurement 125 When the radioactivity of I 131 I will also cause interference. Therefore, the measured value of the CRC-15R medical activity meter of the American CAPINTEC. 131 I and 125 I activities, and restore the measured values ​​to their actual activities.

[0080] method:...

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Abstract

The invention provides a cladded nuclide labeled protein microsphere, comprising the following bulk pharmaceutical chemicals and auxiliary materials in parts by weight: 1-5 parts of Na131I, 1-5 parts of Na125I, 300-1000 parts of chitosan, 100-500 parts of sodium alginate and 300-800 parts of gelatin, wherein, the specific radioactivity concentrations of the Na131I and the Na125I are both 37GBq / ml. The invention also provides a preparation method and applications of the cladded nuclide labeled protein microsphere; the cladded nuclide labeled protein microsphere adopts the inclusion of the chitosan and the sodium alginate; the actual half-life period of the cladded nuclide microsphere in the bodies of animals is longer, and is close to the half-life period of the nuclide; and the blood gamma counts and urine gamma counts of two microspheres are compared to discover that the nuclide released by the cladded nuclide microsphere is more stable than the nuclide released by the uncladded nuclide microsphere, thereby reliving the effect of the explosive release, thus the cladding can protect the nuclide microsphere, reduce the label peeling, and prolong the degrading time of the microsphere in the bodies.

Description

technical field [0001] The invention relates to a shelled nuclide-labeled protein microsphere. It belongs to the field of medicine. Background technique [0002] According to the World Health Organization (WHO), about 10 million new cancer patients and 6 million people die of malignant tumors in the world every year, and the incidence of malignant tumors is still increasing at an annual rate of 1.8-4%. Malignant tumors have become the third leading cause of death after cardiovascular and cerebrovascular diseases and infectious diseases. Even after years of hard work, the prognosis of many malignant tumors has not been significantly improved. Malignant tumors are still a worldwide medical problem for a long time now and in the future. In my country, due to the prevalence of hepatitis B in the past, the incidence of primary liver cancer, which is directly related to the etiology and pathology of hepatitis B, is extremely high. The incidence of malignant tumors of the liver a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/12A61K51/06A61P35/00A61K101/02
Inventor 陈晓理李林夏传琴马宇
Owner WEST CHINA HOSPITAL SICHUAN UNIV
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