PL125770B1 - Method of preparation of the complex of 99-m technetium - Google Patents
Method of preparation of the complex of 99-m technetium Download PDFInfo
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- PL125770B1 PL125770B1 PL21655879A PL21655879A PL125770B1 PL 125770 B1 PL125770 B1 PL 125770B1 PL 21655879 A PL21655879 A PL 21655879A PL 21655879 A PL21655879 A PL 21655879A PL 125770 B1 PL125770 B1 PL 125770B1
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- Poland
- Prior art keywords
- preparation
- technetium
- complex
- acid
- milligrams
- Prior art date
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- 238000000034 method Methods 0.000 title claims description 7
- 229910052713 technetium Inorganic materials 0.000 title description 2
- GKLVYJBZJHMRIY-UHFFFAOYSA-N technetium atom Chemical compound [Tc] GKLVYJBZJHMRIY-UHFFFAOYSA-N 0.000 title description 2
- GKLVYJBZJHMRIY-OUBTZVSYSA-N Technetium-99 Chemical compound [99Tc] GKLVYJBZJHMRIY-OUBTZVSYSA-N 0.000 claims description 8
- 229940056501 technetium 99m Drugs 0.000 claims description 7
- 230000000694 effects Effects 0.000 claims description 6
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 5
- 239000002253 acid Substances 0.000 claims description 5
- 229910052708 sodium Inorganic materials 0.000 claims description 5
- 239000011734 sodium Substances 0.000 claims description 5
- AXZWODMDQAVCJE-UHFFFAOYSA-L tin(II) chloride (anhydrous) Chemical compound [Cl-].[Cl-].[Sn+2] AXZWODMDQAVCJE-UHFFFAOYSA-L 0.000 claims description 5
- 239000002738 chelating agent Substances 0.000 claims description 2
- 239000012299 nitrogen atmosphere Substances 0.000 claims description 2
- HPGGPRDJHPYFRM-UHFFFAOYSA-J tin(iv) chloride Chemical compound Cl[Sn](Cl)(Cl)Cl HPGGPRDJHPYFRM-UHFFFAOYSA-J 0.000 claims description 2
- 239000000243 solution Substances 0.000 claims 1
- 239000008174 sterile solution Substances 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 4
- 210000003734 kidney Anatomy 0.000 description 4
- CWERGRDVMFNCDR-UHFFFAOYSA-N thioglycolic acid Chemical compound OC(=O)CS CWERGRDVMFNCDR-UHFFFAOYSA-N 0.000 description 4
- TXUICONDJPYNPY-UHFFFAOYSA-N (1,10,13-trimethyl-3-oxo-4,5,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-17-yl) heptanoate Chemical compound C1CC2CC(=O)C=C(C)C2(C)C2C1C1CCC(OC(=O)CCCCCC)C1(C)CC2 TXUICONDJPYNPY-UHFFFAOYSA-N 0.000 description 3
- SASYRHXVHLPMQD-UHFFFAOYSA-N 2-(1,2-dicarboxyethylsulfanyl)butanedioic acid Chemical compound OC(=O)CC(C(O)=O)SC(C(O)=O)CC(O)=O SASYRHXVHLPMQD-UHFFFAOYSA-N 0.000 description 3
- 229910021626 Tin(II) chloride Inorganic materials 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 239000001119 stannous chloride Substances 0.000 description 3
- 235000011150 stannous chloride Nutrition 0.000 description 3
- PMNLUUOXGOOLSP-UHFFFAOYSA-N 2-mercaptopropanoic acid Chemical compound CC(S)C(O)=O PMNLUUOXGOOLSP-UHFFFAOYSA-N 0.000 description 2
- 229910052757 nitrogen Inorganic materials 0.000 description 2
- 239000012217 radiopharmaceutical Substances 0.000 description 2
- 229940121896 radiopharmaceutical Drugs 0.000 description 2
- 230000002799 radiopharmaceutical effect Effects 0.000 description 2
- 159000000000 sodium salts Chemical class 0.000 description 2
- 230000003068 static effect Effects 0.000 description 2
- ABXYOVCSAGTJAC-JGWLITMVSA-N (2r,3s,4r,5r)-2,3,4,5,6-pentahydroxyhexanethial Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C=S ABXYOVCSAGTJAC-JGWLITMVSA-N 0.000 description 1
- CLHYKAZPWIRRRD-UHFFFAOYSA-N 1-hydroxypropane-1-sulfonic acid Chemical compound CCC(O)S(O)(=O)=O CLHYKAZPWIRRRD-UHFFFAOYSA-N 0.000 description 1
- BMYNFMYTOJXKLE-UHFFFAOYSA-N 3-azaniumyl-2-hydroxypropanoate Chemical compound NCC(O)C(O)=O BMYNFMYTOJXKLE-UHFFFAOYSA-N 0.000 description 1
- OBDVFOBWBHMJDG-UHFFFAOYSA-N 3-mercapto-1-propanesulfonic acid Chemical compound OS(=O)(=O)CCCS OBDVFOBWBHMJDG-UHFFFAOYSA-N 0.000 description 1
- 108010006654 Bleomycin Proteins 0.000 description 1
- OCUCCJIRFHNWBP-IYEMJOQQSA-L Copper gluconate Chemical class [Cu+2].OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O.OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O OCUCCJIRFHNWBP-IYEMJOQQSA-L 0.000 description 1
- 102000008100 Human Serum Albumin Human genes 0.000 description 1
- 108091006905 Human Serum Albumin Proteins 0.000 description 1
- 229920005654 Sephadex Polymers 0.000 description 1
- 239000012507 Sephadex™ Substances 0.000 description 1
- FKNQFGJONOIPTF-UHFFFAOYSA-N Sodium cation Chemical compound [Na+] FKNQFGJONOIPTF-UHFFFAOYSA-N 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 description 1
- 239000004098 Tetracycline Substances 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 239000012298 atmosphere Substances 0.000 description 1
- 229960001561 bleomycin Drugs 0.000 description 1
- OYVAGSVQBOHSSS-UAPAGMARSA-O bleomycin A2 Chemical compound N([C@H](C(=O)N[C@H](C)[C@@H](O)[C@H](C)C(=O)N[C@@H]([C@H](O)C)C(=O)NCCC=1SC=C(N=1)C=1SC=C(N=1)C(=O)NCCC[S+](C)C)[C@@H](O[C@H]1[C@H]([C@@H](O)[C@H](O)[C@H](CO)O1)O[C@@H]1[C@H]([C@@H](OC(N)=O)[C@H](O)[C@@H](CO)O1)O)C=1N=CNC=1)C(=O)C1=NC([C@H](CC(N)=O)NC[C@H](N)C(N)=O)=NC(N)=C1C OYVAGSVQBOHSSS-UAPAGMARSA-O 0.000 description 1
- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 description 1
- 238000004587 chromatography analysis Methods 0.000 description 1
- 238000004440 column chromatography Methods 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 235000011180 diphosphates Nutrition 0.000 description 1
- 210000003743 erythrocyte Anatomy 0.000 description 1
- 208000017169 kidney disease Diseases 0.000 description 1
- 239000003446 ligand Substances 0.000 description 1
- 231100000243 mutagenic effect Toxicity 0.000 description 1
- 230000003505 mutagenic effect Effects 0.000 description 1
- 238000005121 nitriding Methods 0.000 description 1
- 230000005855 radiation Effects 0.000 description 1
- 238000005514 radiochemical analysis Methods 0.000 description 1
- 231100000336 radiotoxic Toxicity 0.000 description 1
- 230000001690 radiotoxic effect Effects 0.000 description 1
- 229910001415 sodium ion Inorganic materials 0.000 description 1
- 150000003495 technetium Chemical class 0.000 description 1
- 229960002180 tetracycline Drugs 0.000 description 1
- 229930101283 tetracycline Natural products 0.000 description 1
- 235000019364 tetracycline Nutrition 0.000 description 1
- 150000003522 tetracyclines Chemical class 0.000 description 1
- 231100000820 toxicity test Toxicity 0.000 description 1
- 238000013022 venting Methods 0.000 description 1
Landscapes
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Description
Przedmiotem wynalazku jest sposób otrzymywania kompleksu technetu 99—m w postaci preparatu prze¬ znaczonego do badan statycznych i dynamicznych nerek.Znane jest stosowanie w diagnostyce kompleksów technetowo-organicznych znakowanych technetem 99—m, które nie zagrazaja napromieniowaniem pacjenta, a umozliwiaja uzycie wiekszych aktywnosci w porówna¬ niu z O-J-l 31hipuranem dla uzyskania lepszych efektów detekcji.Z opisu patentowego RFN nr 2419310 znany jest sposób otrzymywania kompleksu technetu 99-m na drodze redukcji nadtechnecjanu chlorkiem cynawym i laczenia z kwasem dwumerkaptobursztynowym lub na drodze redukcji Tc+7 do Tc+4 przy uzyciu kwasu bromowodorowego, a nastepnie laczenie z kwasem dwumerkap¬ tobursztynowym, tioglukoza, kwasem merkaptooctowym, kwasem merkaptopropionowym, kwasem merkapto- propylosulfonowym, kwasem tiomlekowym.Natomiast opis patentowy brytyjski nr 1469075 przedstawia metode otrzymywania radiofarmaceutyków znakowanych technetem 99-m na drodze redukcji nadtechnecjanu sodu chlorkiem cynawym w atmosferze azotu w obecnosci Uganda, którym moga byc: pyrofosforany, bleomycyna, albumina surowicy ludzkiej, erytrocyty, tetracyklina, sól sodowa kwasu cytrynowego, zwiazki polifosforowe, glukonaty oraz kwas dwumerkaptoburszty- nowy.Wedlug opisu patentowego polskiego nr 100774 preparat do scyntygraficznego badania nerek otrzymuje sie na drodze reakcji roztworu nadtechnecjanu sodu z chlorkiem cynawym w atmosferze azotuj nastepnie lacze¬ niu z sola sodowa kwasu dwumerkaptosulfopropanolowego.Sposobem wedlug wynalazku kompleks technetu 99—m otrzymuje sie, dodajac w atmosferze azotu do jalowo przygotowanego 1,5 miligrama kwasu tiodwubursztynowego (TDSA) oraz 0,2 miligramów bezwodnego chlorku cynawego jalowego roztworu nadtechnecjanu sodowego w objetosci odpowiadajacej aktywnosci 74 MBq, po czym roztwór mieszasie. " % Zaleta otrzymanego kompleksu technetu 99—m otrzymanego sposobem wedlug wynalazkujestjego forma, gdyz preparat ten moze byc sporzadzony w postaci trwalych suchych zestawów (kitów), które latwo moga byc przechowywane i w kazdej chwili w zaleznosci od potrzeby moga byc znakowane technetem i podane pacjen¬ towi.1 125770 Otrzymany sposobem wedlug wynalazku radiofarmaceutyk nie stanowi zagrozenia radiotoksycznego dla badanych. Zastosowany w preparacie kwas tiodwubursztynowy nie wykazuje wlasciwosci mutagennych, a prze¬ prowadzone badania toksycznosci wykazaly DL50 powyzej 1400 mg/kg.Ponizej podano przyklad wykonania wynalazku.Przyklad. W zakapslowanej fiolce objetosci 10 mililitrów w atmosferze azotu umieszcza sie 1,5 mili¬ grama kwasu tiodwubursztynowego i 0,2 miligrama bezwodnego chlorku cynawego. Nastepnie do fiolki wprowa¬ dza sie bez igly odpowietrzajacej roztwór nadtechnecjanu sodu o aktywnosci okolo 74 MBq i calosc miesza sie.Po uplywie 10 minut preparat podaje sie dozylnie pacjentowi. Rejestracje zapisu aktywnosci nad nerkami prowadzi sie bezposrednio po podaniu preparatu, renografem w sposób ciagly lub gamma kamera polaczona z komputerem w odstepach 20 sekundowych w czasie do 20 minut.Analize radiochemiczna preparatu wykonuje sie metoda chromatografii kolumnowej przy uzyciu zelu sefadeksu G-25 F oraz chromatografii bibulowej, które to metody analiz dla kompleksów technetowych 99-m opisano w Nucl.Med. XV, 282-286, 1976 i Nucl.Med. XVIII, 26-35, 1979.Na podstawie analiz stwierdzono, ze postepujac sposobem wedlug wynalazku otrzymuje sie okolo 90% kompleksu technetowego 99-m (TDSA).W wyniku przeprowadzonych badan stwierdzono przydatnosc radiofarmaceutyku otrzymanego sposobem wedlug wynalazku do renoscyntygrafii (badan statycznych i dynamicznych) w przypadku chorób nerek.Zalaczony rysunek przedstawia porównanie dwóch krzywych renograficznych z tego samego obszaru znad nerek po podaniu preparatu otrzymanego sposobem wedlug wynalazku - kompleksu Tc—TDSA i O-J—131-hi- puranu (OJH).Zastrzezenie patentowe Sposób otrzymywania kompleksu technetu 99-m polegajacy na reakcji nadtechnecjanu z chlorkiem cyna- wym i zwiazkiem chelatujacym, znamienny tym, ze do jalowo przygotowanego 1,5 miligrama kwasu tiodwubursztynowego oraz 0,2 miligramów bezwodnego chlorku cynawego, w atmosferze azotu dodaje sie jalo¬ wego roztworu nadtechnecjanu sodowego w objetosci odpowiadajacej aktywnosci 74 MBq, po czym roztwór miesza sie.X3 IROUK r 1 + ?+ L* ?• r ° 1 0 1 * * 4* r i 69 NO 1 |VI2/7 ^TDSfl ;x v +.Y I 89B9( B RE . o i \,2}H ^¦J 136 9908 1 NO RIJJHT KII "V* **cy n ***** ^^ooJ JsEY *+Hl. 4* oomoooooI Pracownia PongraficznaUPPRL. Naklad 100 egz.Cena 100 zl PLThe subject of the invention is a method of obtaining technetium 99-m complex in the form of a preparation intended for static and dynamic kidney examinations. It is known to use technetium-99-m-labeled technetium complexes in diagnostics, which do not pose a threat to the patient's radiation and allow the use of greater activities compared to ¬ with OJl 31hipuran for better detection results. The German patent specification No. 2419310 describes a method of obtaining technetium 99-m complex by reducing pertechnetate with stannous chloride and combining with dicapentosuccinic acid or by reducing Tc + 7 to Tc + 4 using hydrobromic acid, followed by a combination with dimacapto succinic acid, thioglucose, mercaptoacetic acid, mercapto-acetic acid, mercapto-propylsulfonic acid, thiolactic acid. sodium ion with stannous chloride under nitrogen atmosphere in the presence of ligand, which may be: pyrophosphates, bleomycin, human serum albumin, erythrocytes, tetracycline, sodium salt of citric acid, polyphosphorus compounds, gluconates and dimacaptosuccinate acid. According to Polish patent description 100774 The scintigraphic examination of the kidneys is obtained by reacting a solution of sodium pertechnetate with stannous chloride in an atmosphere of nitriding, followed by combining with sodium salt of dicapto sulfopropanol. According to the invention, a technetium 99-m complex is obtained by adding 1.5 milligrams of acid to sterile prepared acid under nitrogen. TDSA and 0.2 milligrams of anhydrous stannous chloride of sterile sodium pertechnetate in a volume corresponding to an activity of 74 MBq, and the solution is stirred. "% The advantage of the obtained technetium 99-m complex obtained by the method according to the invention, its form, because this preparation can be made in the form of permanent dry sets (putties), which can be easily stored and at any time, depending on the needs, can be marked with technetium and given to patients tow.1 125770 The radiopharmaceutical obtained by the method according to the invention does not pose a radiotoxic hazard to the subjects. The thiodisuccinic acid used in the preparation does not show mutagenic properties, and the toxicity tests carried out showed DL50 above 1400 mg / kg. Below is an example of an embodiment of the invention. In a 10 milliliter vial, 1.5 milliliters of thiodisuccinic acid and 0.2 milligrams of anhydrous stannous chloride are placed under nitrogen in a vial. The vial is then filled with a sodium pertechnetate solution of about 74 MBq activity without a venting needle and mixed. after 10 minutes, the preparation is administered intravenously to the patients here. Recording of activity over the kidneys is carried out immediately after administration of the preparation, with a continuous renograph or a gamma camera connected to a computer at intervals of 20 seconds for up to 20 minutes. Radiochemical analysis of the preparation is performed by column chromatography using a G-25 F sephadex gel and chromatography paper, which methods of analysis for technetium 99-m complexes are described in Nucl.Med. XV, 282-286,1976 and Nucl.Med. XVIII, 26-35, 1979. On the basis of the analyzes it was found that by following the method according to the invention, about 90% of the technetium 99-m complex (TDSA) is obtained. As a result of the conducted tests, the radiopharmaceutical obtained according to the invention was found to be suitable for renoscintigraphy (static and dynamic tests). ) in the case of kidney diseases. The enclosed figure shows a comparison of two renographic curves from the same area of the kidney after administration of the preparation obtained according to the invention - Tc-TDSA complex and OJ-131-hyprurane (OJH). - m consisting in the reaction of pertechnetate with tin chloride and a chelating compound, characterized in that 1.5 milligrams of thiodisuccinic acid and 0.2 milligrams of anhydrous stannous chloride are added to sterile-prepared sodium pertechnetate in the amount of corresponding to an activity of 74 MBq, then the solution is mixed. X3 IROUK r 1+ ? + L *? • r ° 1 0 1 * * 4 * r i 69 NO 1 | VI2 / 7 ^ TDSfl; x v + .Y I 89B9 (B RE. o i \, 2} H ^ ¦J 136 9908 1 NO RIJJHT KII "V * ** cy n ***** ^^ ooJ JsEY * + Hl. 4 * oomoooooI Pongographic Laboratory UPPRL. Mintage 100 copies Price PLN 100 PL
Claims (1)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PL21655879A PL125770B1 (en) | 1979-06-22 | 1979-06-22 | Method of preparation of the complex of 99-m technetium |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PL21655879A PL125770B1 (en) | 1979-06-22 | 1979-06-22 | Method of preparation of the complex of 99-m technetium |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| PL216558A1 PL216558A1 (en) | 1981-01-30 |
| PL125770B1 true PL125770B1 (en) | 1983-06-30 |
Family
ID=19997035
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PL21655879A PL125770B1 (en) | 1979-06-22 | 1979-06-22 | Method of preparation of the complex of 99-m technetium |
Country Status (1)
| Country | Link |
|---|---|
| PL (1) | PL125770B1 (en) |
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1979
- 1979-06-22 PL PL21655879A patent/PL125770B1/en unknown
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| Publication number | Publication date |
|---|---|
| PL216558A1 (en) | 1981-01-30 |
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