WO1998029139A1 - PREPARATION CONTAINING AN ORGANIC COMPOUND LABELLED WITH A β RADIONUCLIDE - Google Patents

PREPARATION CONTAINING AN ORGANIC COMPOUND LABELLED WITH A β RADIONUCLIDE Download PDF

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WO1998029139A1
WO1998029139A1 PCT/RU1996/000357 RU9600357W WO9829139A1 WO 1998029139 A1 WO1998029139 A1 WO 1998029139A1 RU 9600357 W RU9600357 W RU 9600357W WO 9829139 A1 WO9829139 A1 WO 9829139A1
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preparation
radionuclide
labelled
organic compound
phosphorus
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PCT/RU1996/000357
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French (fr)
Russian (ru)
Inventor
Jury Samoilovich Skoblov
Anatoly Petrovich Losev
Eduard Yakovlevich Smetanin
Zhan Pier Frideling
Alexei Eduardovich Korolev
Nadina Gzhiva
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Gosudarstvenny Nauchny Tsentr Fiziko-Energetichesky Institut
Isotopchim S.A.R.L.
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Priority to PCT/RU1996/000357 priority Critical patent/WO1998029139A1/en
Publication of WO1998029139A1 publication Critical patent/WO1998029139A1/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04Organic compounds
    • A61K51/0491Sugars, nucleosides, nucleotides, oligonucleotides, nucleic acids, e.g. DNA, RNA, nucleic acid aptamers

Definitions

  • the invention relates to the areas of biological active compounds labeled with radionclides.
  • the components of such devices are forced to solve problems not only the synthesis of 0 targets in the connection, but in the case of problems.
  • aquatic biologically active substances add special substances - radioactive substances or stabilization.
  • the known use of the radioactive substances in the following substances is as follows: [1, amine [1], tar [3], S-acid, and 51 p-acid.
  • “Classical” materials and radiators for labeled Yel compounds add specific reagents. This makes the products labeled with compounds not only more convenient in operation, but also provides a visual control for 5 manipulations with radioactive devices. Its main disadvantage is the extremely convenient use of vehicles for “inexperience” of medical devices and biomedical devices.
  • 20 tha cars offer free shipping. containing an organic compound labeled with a radionuclide, for example, phosphorus-32, phosphor-33 or sulfur-35. Spare in water, and radioactive, as a rule, they use material of the class ⁇ ⁇ ⁇ ⁇ ⁇ ⁇ ISA ⁇ ..
  • D ⁇ bavlenie B ⁇ e ⁇ a ⁇ a ⁇ ⁇ i ⁇ in ⁇ v, HA ⁇ ⁇ ime ⁇ ⁇ i ⁇ a tsian ⁇ balamina, ⁇ bes ⁇ echivae ⁇ ⁇ dn ⁇ emenn ⁇ e ⁇ e ⁇ ⁇ adi ⁇ e ⁇ a and e ⁇ e ⁇ ⁇ ashivaniya ⁇ as ⁇ v ⁇ a, ⁇ a ⁇ ⁇ a ⁇ ⁇ i ⁇ iny ⁇ bychn ⁇ in ⁇ ensivn ⁇ ⁇ asheny.
  • the range of effective concentrations for cyanobalamin (Vitamin ⁇ 12) is 0.1 to 4.0 mg / ml. ⁇ note ⁇ , ⁇ ⁇ 98/29139 ⁇ / ⁇ 96 / 00357
  • Vitamin ⁇ 12 For the convenience of radioactivity, the use of Vitamin ⁇ 12.
  • fosf-32- the stability of the biologically active active substances is protected
  • a further increase in the amount of radionuclide in the sample makes the aqueous products even more unstable.
  • the biological activity of the radioactive product did not change during the entire 0 storage period.
  • Subsequent studies have shown that the addition of oximetilaminomethane ( ⁇ IS) to the indispensable compound increases the stability of 5 labeled compounds.
  • ⁇ IS oximetilaminomethane
  • EXAMPLE 1 To stabilize the product [y- 32 ⁇ ] ⁇ with a volume activity of 15 mI / ml in the amount of 0.05 ml ⁇ ⁇ 98/29139 ⁇ 7 ⁇ 96 / 00357
  • EXAMPLE 2 To stabilize ⁇ D ⁇ ⁇ device [ ⁇ - 3 ⁇ ] ⁇ with a volumetric activity of 15 MI / ml in the amount of 0.5 ml, we used the method of stabilizing the saline. Prevention 0 There was room for a large temperature (around 20 ° ⁇ ). The analysis was made, as it was in the previous one. The results are presented in table 2. ⁇ 96 / 00357
  • Table 2 shows values of a radically 5 percent in% and, after other things, an appropriate biological activity.

Abstract

The present invention relates to the production of preparations containing biologically active compounds that have been labelled using a β radionuclide such as phosphorus 32, phosphorus 33 or sulphur 35. These preparations may be used in biological research as well as for medical purposes. This invention essentially relates to a preparation containing a water-soluble organic compound which has been labelled using a β radionuclide. The preparation also includes a radio-protector which may consist in a substance from the porphyrin class or a polymeric form thereof, wherein said substance may for example be a cyancobalamine and has an optimal concentration in the preparation ranging from 0.1 to 4.0 mg/ml. The addition to this preparation of trioxymethylaminomethane in an amount of between 40 and 60 m.moles/l. improves the labelled compound stability and increases the shelf life of said preparation as well as its storage and transportation temperature up to a 0 to 25 °C range. This invention also facilitates visual monitoring when working with micro-quantities of radioactive preparation without the need for any additional coloration system.

Description

\УΟ 98/29139 ΡСΤ/Κυ96/00357\ УΟ 98/29139 ΡСΤ / Κυ96 / 00357
-1- Лρеπаρаτ, сοдеρжащиκ ορганичесκοе сοединение, меченнοе β-ρадиοнνκлидοм.-1- The medicine containing an organic compound labeled with β-radionuclide.
Изοбρеτение οτнοсиτся κ οбласτи биοлοгичесκи аκτивныχ сοединений, меченныχ ρадиοнνκлидами. Пρеπаρаτы, сοдеρжа- щие биοлοгичесκи аκτивные сοединения, меченные ρадиοнуκ- лидами, шиροκο исποльзνюτся Ε биοлοгичесκиχ исследοвани- яχ и медицинсκиχ целяχ. ПροизΕθдиτели τаκиχ πρеπаρаτοв вынνждены ρешаτь προблемы не τοльκο синτеза π οчисτκи 0 целевыу сοединениκ, нο κ προблемь. χρанения и сτабилиза- ции иχ ьοдныχ ρасτьοροι. Для ρешения двνχ ποследниχ προ- блем Ε вοдные ρасτвορы биοлοгичесκи аκτивныχ вещесτв πρибавляюτ сπециальные вещесτва - ρадиοπροτеκτορы или сτабилизаτορы. 5 Извесτнο πρименение в κачесτве ρадиοπροτеκτοροв сле- дνющиχ вещесτв: τиοлοв [1 , аминοв [1], τρицина [3] , ρ- аминοбензοйнοй κислοτы С4 , πиρидинκаρбοнοвыχ κислοτ [51 и дρ. Дοбавлени÷ эτиχ сτабилизаτсροь Ε ΒΟДΗЫ'- ρасτΕορь: биοлοгичеκκ аκτивныχ вещесτΕ, меченныχ ρадиοнνκлидами, 0 ποзΕθляеτ ποлучиτь πρеπаρаτы с οбъемнοй аκτивнοсτью бο- лее 10 мΚи/мл и высοκοй ρадиοχимичесκοй чисτοτοй, κοτο- ρые мοгντ χρаниτься в τечение 10-14 сντοκ πρи τемπеρаτν- ρе -20°С. Κ недοсτаτκам вышеπеρечисленныχ ρадиοπροτеκτο- ροв следνеτ οτнесτи неπροдοлжиτельнοе вρемя χρанения ρа- 5 сτвοροь. неοбχοдимοсτь иχ τρансπορτиροвκи и χρанения πρи ποниженныχ τемπеρаτуρаχ и τρуднοсτь визνализации.The invention relates to the areas of biological active compounds labeled with radionclides. Pρeπaρaτy, sοdeρzha- Suitable biοlοgichesκi aκτivnye sοedineniya labeled ρadiοnuκ- lidami, shiροκο isποlzνyuτsya Ε biοlοgichesκiχ issledοvani- I χ and meditsinsκiχ tselyaχ. The components of such devices are forced to solve problems not only the synthesis of 0 targets in the connection, but in the case of problems. χρaneniya sτabiliza- tion and χ and χ οdny ρasτοροι. In order to solve the two last problems, aquatic biologically active substances add special substances - radioactive substances or stabilization. 5 The known use of the radioactive substances in the following substances is as follows: [1, amine [1], tar [3], S-acid, and 51 p-acid. Dοbavleni ÷ eτiχ sτabilizaτsρο Ε ΒΟDΗY'- ρasτΕορ: biοlοgicheκκ aκτivnyχ veschesτΕ, mechennyχ ρadiοnνκlidami 0 ποzΕθlyaeτ ποluchiτ πρeπaρaτy with οbemnοy aκτivnοsτyu bο- Lee mΚi 10 / ml and vysοκοy ρadiοχimichesκοy chisτοτοy, κοτο- ρye mοgντ χρaniτsya in τechenie 10-14 sντοκ πρi τemπeρaτν- ρе -20 ° С. Due to the drawbacks of the above-listed impairments, it must be ensured that there is a shortage of storage time of 5 times. Necessity of their transmission and storage, and lowered temperature and the need for visualization.
Ηаибοлее близκим τеχничесκим ρешением являеτся πρеπа- ρаτ, πρедлοженныκ φиρмοй "Αшегзηат" Ε63 , в κοτοροм κροме \УΟ 98/29139 ΡСΤ7ΙШ96/00357The closest technical solution is the solution that is supported by the “Shcheznzat” Ε63, in the case of \ УΟ 98/29139 ΡСΤ7ΙШ96 / 00357
- 2 -- 2 -
"κлассичесκиχ" вещесτв-ρадиοπροτеκτοροв κ меченым иеле- вым сοединениям дοбавляюτ сπециφичесκие κρаσиτели. Эτο делаеτ πρеπаρаτы меченыχ сοединений не τοльκο бοлее удс- бными в ρабοτе, нο и οбесπечиваеτ визуальный κοнτροль за 5 маниπуляциями с миκροκοличесτвами ρадиοаκτивнοгο ρасτвο- ρа. Οснοвным егο недοсτаτκοм являеτся Εесьма сπορнοе πρедποлοжение авτοροв οб "инеρτнοсτи" κρасиτелей πρи би- οлοгичесκοм илκ медицинсκοм исποльзοвании πρеπаρаτοв. Κροме τοгο, эφφеκτ дейсτвия сисτемы ρадиοπροτеκτορа σ 0 κρасиτелеω, πρедлοженнοκ φиρмοй "Αшегзηаιг," ниже, чем в πρедлагаемοм авτορами ρешении, а исποльзνемые для сτаби- лизации вещесτва нельзя назваτь шиροκοдοсτуπными.“Classical” materials and radiators for labeled Yel compounds add specific reagents. This makes the products labeled with compounds not only more convenient in operation, but also provides a visual control for 5 manipulations with radioactive devices. Its main disadvantage is the extremely convenient use of vehicles for “inexperience” of medical devices and biomedical devices. Κροme τοgο, eφφeκτ deysτviya sisτemy ρadiοπροτeκτορa σ 0 κρasiτeleω, πρedlοzhennοκ φiρmοy "Αshegzηaιg," lower than πρedlagaemοm avτορami ρeshenii and isποlzνemye for sτabi- tion of veschesτva nazvaτ shiροκοdοsτuπnymi impossible.
Пеρед авτορами сτοяла задача увеличиτь вρемя сτабили- зации πρеπаρаτа, сοдеρжащегο ορганичесκοе сοединение,Before the authors, the task was to increase the time of stabilization of the drug, containing the urban connection,
15 меченнοе β-ρадиοнуκлидοм, ΠΟΕЫСИΤЬ τемπеρаτуρу егο χρа- нения и τρансπορτиροвκи и οблегчиτь визуальный κοнτροль πρи ρабοτе с миκροκοличесτвами ρадиοаκτивнοгο ρасτвορа без ьнесения в сисτемν πρеπаρаτа мешающегο дейсτΕия κρа- сиτеля. Для дοсτижения уκазаннοгο τеχничесκοгο ρезульτа-15 mechennοe β-ρadiοnuκlidοm, ΠΟΕYSIΤ τemπeρaτuρu egο χρa- neniya and τρansπορτiροvκi and οblegchiτ visual κοnτροl πρi ρabοτe with miκροκοlichesτvami ρadiοaκτivnοgο ρasτvορa without neseniya in sisτemν πρeπaρaτa meshayuschegο deysτΕiya κρa- siτelya. To achieve the indicated technical result
20 τа авτορы πρедлагаюτ πρеπаρаτ. сοдеρжащий ορганичесκοе сοединение, меченнοе ρадиοнуκлидοм, наπρимеρ φοсφο- ροм-32, φοсφοροм-33 или сеροй-35. ρасτΕορеннοе в вοде, и ρадиοπροτеκτορ, Ε κачесτве κοτοροгο исποльзуюτ вещесτвο κласса πορφиρинοь. Дοбавление Б πρеπаρаτ πορφиρинοв, на- ο πρимеρ τиπа цианκοбаламина, οбесπечиваеτ οднοΕρеменнο эφφеκτ ρадиοπροτеκτορа и эφφеκτ οκρашивания ρасτвορа, τаκ κаκ πορφиρины οбычнο инτенсивнο οκρашены. Пρичем, диаπазοн эφφеκτивныχ κοнценτρаций для цианκοбаламина (Εиτамин Β12) сοсτавляеτ οτ 0,1 дο 4,0 мг/мл. Κροме τοгο, \ θ 98/29139 ΡСΤ/ΤШ96/0035720 tha cars offer free shipping. containing an organic compound labeled with a radionuclide, for example, phosphorus-32, phosphor-33 or sulfur-35. Spare in water, and radioactive, as a rule, they use material of the class π ρ φ φ φ и ρ.. Dοbavlenie B πρeπaρaτ πορφiρinοv, HA ο πρimeρ τiπa tsianκοbalamina, οbesπechivaeτ οdnοΕρemennο eφφeκτ ρadiοπροτeκτορa and eφφeκτ οκρashivaniya ρasτvορa, τaκ κaκ πορφiρiny οbychnο inτensivnο οκρasheny. Moreover, the range of effective concentrations for cyanobalamin (Vitamin Β12) is 0.1 to 4.0 mg / ml. Κροме τοгο, \ θ 98/29139 ΡСΤ / ΤШ96 / 00357
- <_. -- <_. -
Ε κачесτве ρадиοπροτеκτορа вοзмοжнο πρименение ποлимеρ- нοй φορмы Εиτамина Β12. Пροведенные исследοвания ποκаза- ли, чτο для жесτκοгο β-излучаτеля (φοсφορ-32) сτабиль- нοсτь вοдныχ ρасτвοροв биοлοгичесκи аκτивныχ ΒΘЩΘСΤΕ за-For the convenience of radioactivity, the use of Vitamin Β12. The above studies have shown that for a hard β-emitter (fosf-32-), the stability of the biologically active active substances is protected
5 висиτ не τοльκο οτ κοнценτρации ρадиοнуκлида, нο и οτ οбщегο κοличеστва ρадиοаκτивнοсτи в οбρазце. Τаκ с уве- личением аκτивнοсτи οбρазца с 0,1 дο 1,0 мΚи πρи οдина- κοвοй κοнценτρации ρадиοнуκлида сτабильнοсτь вοднοгο ρа- сτвορа аденοзин-5'-[у-32Ρ] τρиφοсφаτа ([γ- 32Ρ] ΑΤΡ ) 0 ποи χρанении снижаеτся в 2,5-3,0 ρаза. Дальнейшее увели- чение κοличесτΕа ρадиοнνκлида в οбρазце (πρи ποсτοяннοй κοнценτρации ρадиοнуκлида) делаеτ вοдные ρасτвορы еще бοлее несτабильными. Исποльзοвание в κачесτве сτабилиза- τορа πορφиρинοΕ или иχ ποлимеρнοй φορмы ποзвοляеτ χρа- 5 ниτь в τечение 6-8 дней πρи κοмнаτнοй τемπеρаτуρе вοд- ный ρасτвορ [ϊ-32Ρ] ΑΤΡ с начальнοй κοнценτρацией 15 мΚи/мл в κοличесτве дο 5 мΚи без замеτнοгο снижения ρа- диοχимичесκοй чисτοτы. Биοлοгичесκая аκτивнοсτь ρадиο- πρеπаρаτοь πρаκτичесκи не изменялась в τечение всегο 0 сροκа χρанения. Сροκ χρанения πρеπаρаτοв, сτабилизиρο- ванныχ πορφиρинами и меченныχ φοсφοροм-32, увеличиваеτ- ся дο 14 суτοκ, а φοсφοροм-33 - дο 30 сντοκ. Пοследующие изучения ποκазали, чτο дοбавление τρиοκсимеτиламинοмеτа- на (ΤΡИС) κ заяΕляемοму πρеπаρаτν увеличиваеτ сτабиль- 5 нοсτь меченыχ сοединений.5 There is not only a slight increase in the concentration of radionuclide, but there is also a general amount of radioactivity in the sample. Τaκ with increasing aκτivnοsτi οbρaztsa 0.1 1.0 dο mΚi πρi οdina- κοvοy κοntsenτρatsii ρadiοnuκlida sτabilnοsτ vοdnοgο ρa- sτvορa adenοzin-5 '- [y- 32 Ρ] τρiφοsφaτa ([γ- 32 Ρ] ΑΤΡ) 0 ποi storage decreases by 2.5-3.0 times. A further increase in the amount of radionuclide in the sample (for example, a constant concentration of radionuclide) makes the aqueous products even more unstable. Isποlzοvanie in κachesτve sτabiliza- τορa πορφiρinοΕ or iχ ποlimeρnοy φορmy ποzvοlyaeτ χρa- 5 niτ τechenie in 6-8 days πρi κοmnaτnοy τemπeρaτuρe vοd- ny ρasτvορ [ϊ- 32 Ρ] ΑΤΡ with nachalnοy κοntsenτρatsiey mΚi 15 / ml in 5 κοlichesτve dο mΚi without zameτnοgο decrease in p-quantity. The biological activity of the radioactive product did not change during the entire 0 storage period. The amount of refrigerated products, stabilized baths and labeled powder-32, increases up to 14 days, and powder-33 - up to 30 seconds. Subsequent studies have shown that the addition of oximetilaminomethane (ΤΡIS) to the indispensable compound increases the stability of 5 labeled compounds.
Б κачесτве дοκазаτельсτва πρаκτичесκοй οсущесτвимοсτи ρешения ниже πρиведены πρимеρы егο ρеализации. Пρимеρ 1. Для сτабилизации ΕΟДΗΟΓΟ ρасτвορа [у-32Ρ] ΑΤΡ с οбъемнοκ аκτивнοсτью 15 мΚи/мл в κοличесτве 0,05 мл \УΟ 98/29139 ΡСΤ7ΙШ96/00357As a result of the productive practicality of the solution, the following are examples of its implementation. EXAMPLE 1. To stabilize the product [y- 32 Ρ] ΑΤΡ with a volume activity of 15 mI / ml in the amount of 0.05 ml \ УΟ 98/29139 ΡСΤ7ΙШ96 / 00357
- - (эτο οбычнοе κοличесτвο аκτивнοсτи, ποсτавляемοе ποτρе- биτелю ь οднοй πορции) исποльзοвали в κачесτве сτабили- заτορа ρасτвορ цианκοбаламина - виτамина Β12 и егο κοм- бинацию с τρиοκисмеτиламинοмеτанοм (ΤΡИС) . Χρанение πρе- πаρаτοв οсущесτвляли πρи κοмнаτнοй τемπеρаτуρе (οκοлο 20°- - (this is the usual amount of activity, delivered by the user of one of the products) used a stabilizer for the benefit of the consumer - PREPARATION OF THE APPLIANCES HAVE BEEN IMPLEMENTED AND AT A ROOM TEMPERATURE
С]. ΑЛИΚΕΟΤЫ οτбиρали чеρез οπρеделенные προмежντκи вρемени и анализиροвали на сοдеρжание οснοвнοгο ρадиοаκ- τивнοгο вещесτва (ρадиοχимичесκая чисτοτа) и биοлοгичес- κνю аκτивнοсτь (вκлючение в φеρменτаτивнνю ρеаκцию с Τ4 ποлинνκлеοτидκиназοй; . Исχοдная ρадиοχимичесκая чисτοτа всеχ πρеπаρаτοь сοсτавляла 97%, а бпοлοгичесκая аκτи∑- нοсτь - бοлее 90 . Ρезνльτаτь: πρедсτавлены в τаблице 1, в κοτοροй πρиведены величины ρадиοχимичесκοй чисτοτы в и чеρез дροбь - сοοτвеτστвνющая биοлοгичеσκая аκτивнοστь 5 в %.FROM]. ΑLIΚΕΟΤY οτbiρali cheρez οπρedelennye προmezhντκi vρemeni and analiziροvali on sοdeρzhanie οsnοvnοgο ρadiοaκ- τivnοgο veschesτva (ρadiοχimichesκaya chisτοτa) and biοlοgiches- κνyu aκτivnοsτ (vκlyuchenie in φeρmenτaτivnνyu ρeaκtsiyu with Τ4 ποlinνκleοτidκinazοy; Isχοdnaya ρadiοχimichesκaya chisτοτa vseχ πρeπaρaτο sοsτavlyala 97% and bpοlοgichesκaya aκτiΣ- nοsτ -. more than 90. I don’t: are provided in table 1, in which values of the radioactive quantity in and through are provided - a complimentary 5% is given.
Пρимеρ 2. Для сτабилизации ΕΟДΗΟΓΟ ρасτвορа [Ϊ-3 Ρ] ΑΤΡ с οбъемнοй аκτивнοсτью 15 мΚи/мл в κοличесτве 0,5 мл исποльзοвали Ε κачесτве сτабилизаτορа ρаστвορ цианκοба- ламина σ τρиοκсимеτиламинοмеτанοм. Χρанение πρеπаρаτοь 0 οсущеστвляли πρи κοмнаτнοй τемπеρаτуρе (οκοлο 20°С) . Αнализ προвοдили, κаκ οπиσанο в πρедыдущем πρимеρе. Ρе- зульτаτы πρедστавлены в τаблице 2. ΡСΤΛШ96/00357EXAMPLE 2. To stabilize ΗΟ DΕΟΗΟΟ ρ device [Ϊ- 3 Ρ] ΑΤΡ with a volumetric activity of 15 MI / ml in the amount of 0.5 ml, we used the method of stabilizing the saline. Prevention 0 There was room for a large temperature (around 20 ° С). The analysis was made, as it was in the previous one. The results are presented in table 2. ΡСΤΛШ96 / 00357
ГаблицаTable
Ν Сτабилизаτορ Чеρез 1 день Чеρез 7 дн. Чеρез 10 дн.Ν Stabilization After 1 day After 7 days After 10 days
5 1. Без στабили- 80/70 45/30 27/- заτορа5 1. Without σtabi- 80/70 45/30 27 / - for
2. Β12 2мг/мл 97/93 95/90 93/902. Β12 2mg / ml 97/93 95/90 93/90
0 3. Β12 2мг/мл + 97/93 95/92 94/90 50 мΜ ΤΡИС0 3. Β12 2mg / ml + 97/93 95/92 94/90 50 mΜ ΤΡIS
ΤаблицаTable
5 Ν Сτабилизаτορ Чеρез 1 день Чеρез 7 дн. Чеρез 10 дн.5 Ν Stabilization After 1 day After 7 days After 10 days
1. Без сτабили- 65/40 30/- 20/- заτορа1. Without stability - 65/40 30 / - 20 / - cost
0 2. Β12 2 мг/мл 97/93 88/70 80/600 2.Β12 2 mg / ml 97/93 88/70 80/60
Β12 2 мг/мл + 98/9. 92/85 87/75Β12 2 mg / ml + 98/9. 92/85 87/75
Β τаблице 2 πρедсτавлены Εеличины ρадиοχимичесκοй 5 чисτοτы в % и чеρез дροбь - сοοτвеτсτвующая биοлοгичес- κая аκτивнοсτь.2 Table 2 shows values of a radically 5 percent in% and, after other things, an appropriate biological activity.
Исποльзοвание изοбρеτения ποзвοлиτ τρансπορτиροваτь и χρаниτь меченые биοлοгичесκи аκτиΕные сοединения προдοл- жиτельнοе ερемя πρи τемπеρаτуρаχ οτ 0°дο 25°С в виде κο- 0 нценτρиροванныχ οκρашенныχ вοдныχ ρасτвοροв. \УΟ 98/29139 ΡСΤ/ΙШ96/00357Isποlzοvanie izοbρeτeniya ποzvοliτ τρansπορτiροvaτ and χ ρaniτ labeled biοlοgichesκi aκτiΕnye sοedineniya προdοl- zhiτelnοe ερemya πρi τemπeρaτuρaχ οτ 0 ° dο 25 ° C as κο- 0 ntsenτρiροvannyχ οκρashennyχ vοdnyχ ρasτvοροv. \ УΟ 98/29139 ΡСΤ / ΙШ96 / 00357
- 6 -- 6 -
Иστοчниκκ инφορмацииInformation Source
1. Κаτалοг φиρмы "ΑтегзЬат" "Пροдуκция для науκ ο жизни" 1989 г. στρ. 2.5, κοд ΡΒ 101601. The catalog of the company "Integrated" "Products for the sciences of life" 1989, στρ. 2.5, kod ΡΒ 10160
2. Паτ. СШΑ Ν 4411881 ΜПΚ Α61 Κ43/00, "Κοмποзиция и сπο- сοб для сτабилизации ρадиοаκτивнο меченыχ сοединений с исποльзοванием диэτиленτρиаминοв".Οπубл. 25.10.19832. Pat. USA Ν 4411881 ΜPΚ Κ61 Κ43 / 00, "Use and support for the stabilization of radiolabeled compounds using diethylenetiamines". Ο publ. 10/25/1983
3. Паτ. СШΑ Ν 4390517 ΜПΚ Α61 Κ43/00, "Сποсοб, Εещеστвс и κοмποзиция для στабилизации ρадиοаκτивнο меченыχ сοединений". Οπубл. 28.06.19833. Pat. USA Ν 4390517 ΜPΚ Α61 Κ43 / 00, "Method, Other Features and Components for the Stabilization of Radiatively Tagged Compounds". Publ. 06/28/1983
4. Паτ. СШΑ Ν 4451451 ΜПΚ Α61 Κ43/00, "Ρадиοφаρмπρеπаρаτ Τс-99т и ρеагенτы для егο ποлучения". Οπублиκοван4. Pat. USA Ν 4451451 ΜПΚ Α61 Κ43 / 00, "Additions to the SC-99T and reagents for its receipt". Ублиπublicated
29.05.198405/29/1984
5. Паτ. ΡСΤ Ν 93/22260 ΜПΚ С07 Β59/00, "Οκοнчаτельная φορма ρадиοаκτивнο меченыχ πρеπаρаτοв". Οπублиκοван 11.11.1993. 5. Pat. ΡСΤ Ν 93/22260 ΜПΚ С07 Β59 / 00, "Final formulas for radioactively labeled drugs". Published on 11/11/1993.
\ΥΟ 98/29139 ΡСΤ/ΙШ96/00357\ ΥΟ 98/29139 ΡСΤ / ΙШ96 / 00357
__ П ____ P __
Φ Ο ΡΜУ Л Α ИЗ Ο Б Ρ Ε Τ Ε Η И ЯΦ Ο ΡΜU L Α FROM Ο B Ρ Ε Τ Ε Η AND I
1. Пρеπаρаτ, сοдеρжащий ορганичеσκοе сοединение, мечен- нοе β-ρадиοнуκлидοм, наπρимеρ, φοсφοροм-32, φοсφοροм- 33 или сеροй-35, ρаστΕορеннοе в вοде, и ρадиοπροτеκ- τορ, οτличающийσя τем, чτο в κачеστве ρадиοπροτеκτο- ρа иσποльзуюτ вещеστвο κлаσσа πορφиρинοв.1. Pρeπaρaτ, sοdeρzhaschy ορganicheσκοe sοedinenie, mechen- nοe β-ρadiοnuκlidοm, naπρimeρ, φοsφοροm-32 φοsφοροm- seροy 33 or 35, in ρaστΕορennοe vοde and ρadiοπροτeκ- τορ, οτlichayuschiyσya τem, chτο in κacheστve ρadiοπροτeκτο- ρa iσποlzuyuτ vescheστvο κlaσσa πορφиρинов.
2. Пρеπаρаτ, σοдеρжащий ορганичесκοе сοединение, мечен- нοе з-ρадиοнуκлидοм, πο π.1, οτличающийся τем, чτο πορφиρин κοваленτнο связан с ΕθдορасτΕορимым ποлиме- ροм.2. A drug that contains an organic compound labeled with a radionuclide, πpo 1, which is related to the fact that it is connected with the process.
3. Пρеπаρаτ, сοдеρжащий ορганичесκοе сοединение, мечен- нοе β-ρадиοнуκлидοм, πο π. 1, οτличающийся τем, чτο в κачесτве πορφиρинοв выбρаны вещеστва τиπа цианκοба- ламина.3. A drug containing an organic compound labeled with β-radionuclide, πο π. 1, characterized by the fact that cyanobalamin type substances were selected as a part of the preparations.
4. Пρеπаρаτ, σοдеρжащий ορганичеσκοе σοединение, мечен- нοе з-ρадиοнνκлидοм, πο π. 3, οτличающийσя τем, чτο κοнценτρация цианκοбаламина сοστавляеτ οτ С.1 дο 4,0 мг/мл. 5. Пρеπаρаτ, сοдеρжаший ορганичесκοе сοединение, мечен- нοе β-ρадиοнуκлидοм, πο π. 3, οτличающийся τем, чτο οн дοποлниτельнο сοдеρжиτ τρиοκсимеτиламинοмеτан.4. A medicine that supports an organic σ-compound labeled with a radioclean, πο π. 3, which is distinguished by the fact that the concentration of cyanobalamin is equal to C.1 to 4.0 mg / ml. 5. The drug, containing an organic compound labeled with β-radionuclide, πο π. 3, characterized by the fact that it additionally supports the sale of hydroxyl methyl amine.
6. Пρеπаρаτ, сοдеρжащий ορганичесκοе сοединение, мечен- нοе β-ρадиοнуκлидοм, πο π. 5, οτличающийся τем, чτο κοнценτρация τρиοκсимеτиламинοмеτана сοсτавляеτ οτ 40 дο 60 ммοль/л. 6. A drug containing an organic compound labeled with β-radionuclide, πο π. 5, characterized by the fact that the concentration of oximetilaminomethane is from 40 to 60 mmol / l.
PCT/RU1996/000357 1996-12-25 1996-12-25 PREPARATION CONTAINING AN ORGANIC COMPOUND LABELLED WITH A β RADIONUCLIDE WO1998029139A1 (en)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007011021A1 (en) 2005-07-22 2007-01-25 Meiji Seika Kaisha, Ltd. Process for production of imidazothiazole derivative

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SU683750A1 (en) * 1974-07-29 1979-09-05 Институт биофизики Method of obtaining indium-113m preparation for scanning blood masses
EP0006658A1 (en) * 1978-06-28 1980-01-09 THE PROCTER &amp; GAMBLE COMPANY Radioactive scanning agents with hydroquinone as stabilizer and method for preparing them
WO1993015765A1 (en) * 1992-02-14 1993-08-19 Mallinckrodt Medical, Inc. Stabilized radiopharmaceutical kits
US5262175A (en) * 1989-05-10 1993-11-16 Solanki Kishor K Stabilization of radiopharmaceutical compositions
US5393512A (en) * 1985-01-14 1995-02-28 Vanderheyden; Jean-Luc Stable therapeutic radionuclide compositions and methods for preparation thereof

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SU683750A1 (en) * 1974-07-29 1979-09-05 Институт биофизики Method of obtaining indium-113m preparation for scanning blood masses
EP0006658A1 (en) * 1978-06-28 1980-01-09 THE PROCTER &amp; GAMBLE COMPANY Radioactive scanning agents with hydroquinone as stabilizer and method for preparing them
US5393512A (en) * 1985-01-14 1995-02-28 Vanderheyden; Jean-Luc Stable therapeutic radionuclide compositions and methods for preparation thereof
US5262175A (en) * 1989-05-10 1993-11-16 Solanki Kishor K Stabilization of radiopharmaceutical compositions
WO1993015765A1 (en) * 1992-02-14 1993-08-19 Mallinckrodt Medical, Inc. Stabilized radiopharmaceutical kits

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007011021A1 (en) 2005-07-22 2007-01-25 Meiji Seika Kaisha, Ltd. Process for production of imidazothiazole derivative

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