CN1369498A - Medical compound containing radioactive tin element and preparation method thereof - Google Patents
Medical compound containing radioactive tin element and preparation method thereof Download PDFInfo
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- CN1369498A CN1369498A CN 02113298 CN02113298A CN1369498A CN 1369498 A CN1369498 A CN 1369498A CN 02113298 CN02113298 CN 02113298 CN 02113298 A CN02113298 A CN 02113298A CN 1369498 A CN1369498 A CN 1369498A
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- Prior art keywords
- solution
- salt
- reaction
- tin element
- acid
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- ATJFFYVFTNAWJD-UHFFFAOYSA-N Tin Chemical compound [Sn] ATJFFYVFTNAWJD-UHFFFAOYSA-N 0.000 title claims abstract description 19
- 150000001875 compounds Chemical class 0.000 title claims abstract description 17
- 230000002285 radioactive effect Effects 0.000 title claims abstract description 17
- 238000002360 preparation method Methods 0.000 title claims abstract description 14
- 238000006243 chemical reaction Methods 0.000 claims abstract description 33
- 239000003446 ligand Substances 0.000 claims abstract description 9
- 239000003513 alkali Substances 0.000 claims abstract description 5
- 239000007795 chemical reaction product Substances 0.000 claims abstract description 5
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims description 51
- 239000000243 solution Substances 0.000 claims description 42
- 150000003839 salts Chemical class 0.000 claims description 19
- QPCDCPDFJACHGM-UHFFFAOYSA-N N,N-bis{2-[bis(carboxymethyl)amino]ethyl}glycine Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(=O)O)CCN(CC(O)=O)CC(O)=O QPCDCPDFJACHGM-UHFFFAOYSA-N 0.000 claims description 10
- 229940120146 EDTMP Drugs 0.000 claims description 9
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 claims description 8
- 239000002585 base Substances 0.000 claims description 7
- DUYCTCQXNHFCSJ-UHFFFAOYSA-N dtpmp Chemical compound OP(=O)(O)CN(CP(O)(O)=O)CCN(CP(O)(=O)O)CCN(CP(O)(O)=O)CP(O)(O)=O DUYCTCQXNHFCSJ-UHFFFAOYSA-N 0.000 claims description 7
- NFDRPXJGHKJRLJ-UHFFFAOYSA-N edtmp Chemical compound OP(O)(=O)CN(CP(O)(O)=O)CCN(CP(O)(O)=O)CP(O)(O)=O NFDRPXJGHKJRLJ-UHFFFAOYSA-N 0.000 claims description 7
- YDONNITUKPKTIG-UHFFFAOYSA-N [Nitrilotris(methylene)]trisphosphonic acid Chemical compound OP(O)(=O)CN(CP(O)(O)=O)CP(O)(O)=O YDONNITUKPKTIG-UHFFFAOYSA-N 0.000 claims description 6
- 230000002535 lyotropic effect Effects 0.000 claims description 5
- -1 pentamethylene phosphonic acids Chemical class 0.000 claims description 5
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 4
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims description 4
- 229910052757 nitrogen Inorganic materials 0.000 claims description 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 4
- RGSFGYAAUTVSQA-UHFFFAOYSA-N pentamethylene Natural products C1CCCC1 RGSFGYAAUTVSQA-UHFFFAOYSA-N 0.000 claims description 4
- 229960003330 pentetic acid Drugs 0.000 claims description 4
- GFMYEVPBEJFZHH-UHFFFAOYSA-N CP(O)(O)O Chemical compound CP(O)(O)O GFMYEVPBEJFZHH-UHFFFAOYSA-N 0.000 claims description 3
- PIICEJLVQHRZGT-UHFFFAOYSA-N Ethylenediamine Chemical compound NCCN PIICEJLVQHRZGT-UHFFFAOYSA-N 0.000 claims description 3
- 239000012670 alkaline solution Substances 0.000 claims description 3
- 230000001143 conditioned effect Effects 0.000 claims description 3
- 125000004177 diethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 3
- 239000002253 acid Substances 0.000 claims description 2
- 239000012266 salt solution Substances 0.000 claims description 2
- 230000003381 solubilizing effect Effects 0.000 claims description 2
- 230000035484 reaction time Effects 0.000 claims 1
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 18
- 238000004458 analytical method Methods 0.000 description 9
- 238000005303 weighing Methods 0.000 description 8
- 210000000988 bone and bone Anatomy 0.000 description 5
- 208000018084 Bone neoplasm Diseases 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 208000011645 metastatic carcinoma Diseases 0.000 description 2
- 206010061289 metastatic neoplasm Diseases 0.000 description 2
- 206010005949 Bone cancer Diseases 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000006227 byproduct Substances 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 238000002512 chemotherapy Methods 0.000 description 1
- 230000002607 hemopoietic effect Effects 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 230000002688 persistence Effects 0.000 description 1
- 230000005855 radiation Effects 0.000 description 1
- 238000001959 radiotherapy Methods 0.000 description 1
- 238000002603 single-photon emission computed tomography Methods 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 230000009466 transformation Effects 0.000 description 1
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- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Abstract
The invention discloses a medical compound containing radioactive tin element and a preparation method thereof117mDissolving the reaction ligand with alkali solution, adjusting the pH value of the reaction ligand solution system to 3-9.5, adding the reaction ligand solution into a container containing the solution containing radioactivity117mAnd in the reaction container of the Sn solution, the required reaction product is generated by reaction. The preparation method is easy to operate and high in yield.
Description
1, technical field
The invention belongs to medical nuclear pharmaceuticals field, be specifically related to a kind of medical compound that contains radioactive tin element and preparation method thereof.
2, background technology
According to medical statistics, after malignant tumour generation bone shifted, the ostalgia of violent persistence can appear in the patient of most (greater than 70%).How to control ostalgia, be the thorny problem that the doctor faces always.Radiotherapy, chemotherapy and operative treatment commonly used are relatively poor to the curative effect of multiple bone metastatic carcinoma.Seek the medicine of effectively alleviating ostalgia, improving patient's life quality is the emphasis that people study.
For bone tumor, nucleic when the first-selected bone that becomes strong
89Sr,
153Sm,
32P etc., still
89Sr and
153The ray mean range that Sm sends is respectively 0.5mm and 8mm, so they may produce certain influence to tissues such as red corpuscle in the blood and marrow when acting on focus.A large amount of experimental results show that
32P has the obvious suppression effect to hemopoietic function, and reason is that the energetic ray of its 1.7MeV has very high radiation dose damage to whole human body and marrow.
3, summary of the invention
The object of the present invention is to provide a kind of medical compound that contains radioactive tin element and preparation method thereof.This compound is expected to be used for the treatment of bone tumor.
A kind of medical compound that contains radioactive tin element of the present invention is made up of radioactive tin element and reaction part.
Radioactive tin element is
117mSn,
117mSn adopts and contains radioactivity
117mSn
4+Lyotropic salt obtain.
The reaction part is any among alpha-amino phosphonate compounds 2-N-hydroxyethylethylene diamine trimethylene phosphonic or its salt HEDTMP, diethyl triamine base pentamethylene phosphonic acids or its salt DTPMP, ethylenediamine tetraacetic methyl-phosphorous acid or its salt EDTMP, inferior nitrogen trimethylene phosphonic or its salt NTMP; The reaction part also can be diethylenetriamine pentaacetic acid or its salt DTPA.
A kind of medical preparation method who contains the compound of radioactive tin element of the present invention comprises following reactions steps:
1. will contain radioactivity
117mSn
4+The lyotropic salt wiring solution-forming;
2. in container, add an amount of reaction part, with the alkaline solution dissolving, the pH value of using acid-base solution conditioned reaction ligand solution system commonly used is made required reaction ligand solution between 3～9.5 more then;
3. required reaction ligand solution is joined and to contain radioactive tin element
117mSn
4+The reaction vessel of lyotropic salt solution in, normal temperature reaction 5-30 minute down generates required reaction product.
With the mark rate of ply of paper analysis method assaying reaction product, expanding body is an acetone.
The reaction part adopts any among HEDTMP, DTPMP, EDTMP, NTMP, the DTPA.The reaction product that generates is respectively
117mSn-HEDTMP tin-117-2-N-hydroxyethylethylene diamine trimethylene phosphonic compound,
117mSn-DTPMP tin-117-diethyl triamine base pentamethylene phosphinic acid compounds,
117mSn-EDTMP tin-117-ethylenediamine tetraacetic methyl-phosphorous acid compound,
117mSn-NTMP tin-117-time nitrogen trimethylene phosphonic compound,
117mSn-DTPA tin-117-diethylenetriamine pentaacetic acid compound perhaps is respectively the salt of above compound correspondence.
The alkali of solubilizing reaction part is dilute sodium hydroxide, potassium hydroxide solution; Common alkali is sodium hydroxide, potassium hydroxide.Common acid is hydrochloric acid, sulfuric acid.
The reaction part between 3～9.5, can reduce the generation of by product with acid-base solution conditioned reaction system pH commonly used after dissolving with alkaline solution, obtains higher productive rate.
117mSn has good nulcear properties.Its transformation period is 13.6 days, the IT decay, and emitted energy is that the 158.6KeV gamma-rays does not have particle ray, is well suited for doing the SPECT video picture.Close bone will itself just be had
117mSn forms stable complex with reaction part alpha-amino phosphonate compounds, is expected to become the new medicinal compound that is used for bone tumour therapy, and the ostalgia effect is effectively alleviated in performance in the treatment of osteocarcinoma and metastatic carcinoma of bone.
Adopt a kind of medical compound that contains radioactive tin element of the present invention's preparation, preparation method's easy handling, productive rate height.
4, preferred forms
Embodiment 1
Take by weighing HEDTMP in beaker, with the dissolving of the NaOH solution of 2mol/l, with the NaOH of 0.5mol/L or HCL the pH of solution is transferred in 7.0～7.5 the scope, making concentration is the HEDTMP solution of 0.05mol/L.The HEDTMP that gets 2ml 0.05mol/L adds
117mSn
4+The solution of (stanniferous 2.5mg) reacts 5min at normal temperatures, measures mark rate with the ply of paper analysis method, and expanding body is an acetone.Generate the Sn-HEDTMP of mark rate 99%.
Embodiment 2
Take by weighing HEDTMP in beaker, with the dissolving of the NaOH solution of 2mol/l, with the NaOH of 0.5mol/L or HCL the pH of solution is transferred in 3.0～3.5 the scope, making concentration is the HEDTMP solution of 0.05mol/L.The HEDTMP that gets 2ml0.05mol/L adds
117mSn
4+The solution of (stanniferous 3.5mg) reacts 5min at normal temperatures, measures mark rate with the ply of paper analysis method, and expanding body is an acetone.Generate the Sn-HEDTMP of mark rate 96%.
Embodiment 3
Take by weighing HEDTMP in beaker, with the dissolving of the NaOH solution of 2mol/l, with the NaOH of 0.5mol/L or HCL the pH of solution is transferred in 9.0～9.5 the scope, making concentration is the HEDTMP solution of 0.05mol/L.The HEDTMP that gets 2ml 0.05mol/L adds
117mSn
4+(stanniferous 1.5mg) solution reacts 15min at normal temperatures, measures mark rate with the ply of paper analysis method, and expanding body is an acetone.Generate the Sn-HEDTMP of mark rate 97%.
Embodiment 4
Take by weighing HEDTMP in beaker, with the dissolving of the NaOH solution of 2mol/l, with the NaOH of 0.5mol/L or HCL the pH of solution is transferred in 7.0～7.5 the scope, making concentration is the HEDTMP solution of 0.05mol/L.The HEDTMP that gets 2ml 0.05mol/L adds
117mSn
4+(stanniferous 2.0mg) solution reacts 30min at normal temperatures, measures mark rate with the ply of paper analysis method, and expanding body is an acetone.Generate the Sn-HEDTMP of mark rate 98%.
Embodiment 5
Take by weighing DTPMP in beaker, with the dissolving of the NaOH solution of 2mol/l, with the NaOH of 0.5mol/L or HCL the pH of solution is transferred in 7.0～7.5 the scope, making concentration is the DTPMP solution of 0.05mol/L.The DTPMP that gets 2ml 0.05mol/L adds
117mSn
4+(stanniferous 1.6mg) solution reacts 5min at normal temperatures, measures mark rate with the ply of paper analysis method, and expanding body is an acetone.Generate the Sn-DTPMP of mark rate 98%.
Embodiment 6
Take by weighing EDTMP in beaker, with the dissolving of the NaOH solution of 2mol/l, with 0.5mol/LNaOH or HCL the pH of solution is transferred in 8.0～8.5 the scope, making concentration is the EDTMP solution of 0.05mol/L.The EDTMP that gets 1ml 0.05mol/L adds
117mSn
4+(stanniferous 3.2mg) solution reacts 10min at normal temperatures, measures mark rate with the ply of paper analysis method, and expanding body is an acetone.Generate the Sn-EDTMP of mark rate 98%.
Embodiment 7
Take by weighing NTMP in beaker, with the dissolving of the NaOH solution of 2mol/l, with 0.5mol/LNaOH or HCL the pH of solution is transferred in 7.5～8.0 the scope, making concentration is the NTMP solution of 0.05mol/L.Add
117mSn
4+Solution reacts 20min at normal temperatures, measures mark rate with the ply of paper analysis method, and expanding body is an acetone.Generate the Sn-NTMP of mark rate 99%.
Embodiment 8
Take by weighing DTPA in beaker, with the dissolving of the NaOH solution of 2mol/l, with 0.5mol/LNaOH or HCL the pH of solution is transferred in 6.0～6.5 the scope, making concentration is the DTPA solution of 0.05mol/L.Add
117mSn
4+Solution reacts 15min at normal temperatures, measures mark rate with the ply of paper analysis method, and expanding body is an acetone.Generate the Sn-DTPA of mark rate 98%.
Claims (8)
1. the medical compound of radioactive tin element that contains is by radioactivity
117mSn and reaction part are formed.
2. a kind of medical compound that contains radioactive tin element according to claim 1, it is characterized in that: radioactive tin element is
117mSn
4+
3. a kind of medical compound that contains radioactive tin element according to claim 1 is characterized in that: the reaction part is any among alpha-amino phosphonate compounds 2-N-hydroxyethylethylene diamine trimethylene phosphonic or its salt HEDTMP, diethyl triamine base pentamethylene phosphonic acids or its salt DTPMP, ethylenediamine tetraacetic methyl-phosphorous acid or its salt EDTMP, inferior nitrogen trimethylene phosphonic or its salt NTMP; The reaction part also can be diethylenetriamine pentaacetic acid or its salt DTPA.
4. a kind of medical compound that contains radioactive tin element according to claim 1, its preparation method is characterised in that and comprises following reactions steps:
1) will contain radioactivity
117mSn
4+The lyotropic salt wiring solution-forming;
2) elder generation adds an amount of reaction part in container, and with the alkaline solution dissolving, the pH value of using acid-base solution conditioned reaction ligand solution system commonly used is made required reaction ligand solution between 3～9.5 more then;
3) required reaction ligand solution joined contain radioactive tin element
117mSn
4+The reaction vessel of lyotropic salt solution in, normal temperature reaction down generates required reaction product.
5. according to the described preparation method of claim 4, it is characterized in that: the reaction part is any among alpha-amino phosphonate compounds 2-N-hydroxyethylethylene diamine trimethylene phosphonic or its salt HEDTMP, diethyl triamine base pentamethylene phosphonic acids or its salt DTPMP, ethylenediamine tetraacetic methyl-phosphorous acid or its salt EDTMP, inferior nitrogen trimethylene phosphonic or its salt NTMP; The reaction part also can be diethylenetriamine pentaacetic acid or its salt DTPA.
6. according to the described preparation method of claim 4, it is characterized in that: the tin that contains in the solution of tin of radionuclide is
117mSn
4+
7. according to the described preparation method of claim 4, it is characterized in that: the following reaction times of normal temperature is 5～30 minutes.
8. according to the described preparation method of claim 4, it is characterized in that: the alkali of solubilizing reaction part is dilute sodium hydroxide or rare potassium hydroxide solution; Common alkali is sodium hydroxide, potassium hydroxide; Common acid is hydrochloric acid, sulfuric acid.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02113298 CN1369498A (en) | 2002-01-30 | 2002-01-30 | Medical compound containing radioactive tin element and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02113298 CN1369498A (en) | 2002-01-30 | 2002-01-30 | Medical compound containing radioactive tin element and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1369498A true CN1369498A (en) | 2002-09-18 |
Family
ID=4742555
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 02113298 Pending CN1369498A (en) | 2002-01-30 | 2002-01-30 | Medical compound containing radioactive tin element and preparation method thereof |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105017313A (en) * | 2015-07-06 | 2015-11-04 | 中国工程物理研究院核物理与化学研究所 | 117mSn marked polyamido hosphonic acid system for therapeutic drug for skeleton system diseases |
-
2002
- 2002-01-30 CN CN 02113298 patent/CN1369498A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105017313A (en) * | 2015-07-06 | 2015-11-04 | 中国工程物理研究院核物理与化学研究所 | 117mSn marked polyamido hosphonic acid system for therapeutic drug for skeleton system diseases |
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