Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
  • A61K51/02—Preparations 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
  • A61K51/04—Organic compounds
  • A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K2123/00—Preparations for testing in vivo

Definitions

• radio isotopes which fulfill the criteria set forth above are I and '"Tc. Without question “Tc is the most desirable of these radio isotopes. Because of its short physical half life, larger quantities of radioactivity (ie mCi against 300 u Ci for 1) thereby in creasing the photon flux while maintaining a level of radiation which can safely be absorbed by the patient.
• Eckelman confirms the findings of Richards, Jap. Nucl. Med., 7, 165 (1968) that the removal of stannous hydroxide formed in the course of the reaction is highly advantageous since apparently some radioisotope is occluded upon 'or in the colloidal stannous hydroxide. Eckelman suggests that the optimum conditions of labeling human serum albumin comprise treating the serum albumin with stannous chloride, adjusting the pH to between pH 2 and pH 6, removing any un-bound stannous chloride or stannous hydroxide, and then adding the pertechnetate.
• Streptokinase and Urokinase covalently labeled with "'Tc covalently labeled with "'Tc.
• a solution of "'Tc pertechnetate is added to the appropriate enzyme and treated with freshly prepared stannous chloride in dilute hydrochloric acid.
• the reaction mixture is buffered to a pH greater than 7 allowed to react for a few minutes and the unreacted anions removed, suitably by passage through an anion exchange column.
• stannous chloride in dilute aqueous hydrochloric acid.
• stannous chloride in dilute aqueous hydrochloric acid.
• an alkalizing buffer Any of the commonly used alkaline buffers yielding a pH greater than 7 may be utilized. It is especially preferred however-to utilize buffers having a pH between about 8 and about 12, resulting in a final solution pH between 78.
• phosphate buffers There may be mentioned phosphate buffers, barbital buffers, and glycine buffers. (Teorell and Steinhagen J. Biol. Chem. 49, 1 83 (1921); Michaelis J. Biol. Chem., 8 7 33 (1930) and idem., Bio chem Z. 234 139 1931; and Sorensen, Biochem Z. 21, 131 (1909) respectively)
• the mixture is allowed to stand for about 5 minutes and passed through an anion exchange column which will permit the radiolabeled enzyme solution to pass therethrough.
• Thromboembolists are indicated due to increased radioactivity at the site of the embolists.
• a radio labeled thrombolytic enzyme selected from the group consisting of "Tc-Streptokinase and '"Tc-Urokinase.
• Tc-Streptokinase being a compound of claim 1.
• Tc-Streptokinase being a compound-of claim 2 having an activity of between 0.8 and 2.5 mCi per 10 Kiuof Streptokinase.
• Tc-Urokinase being a compound of claim 1.
• a covalent compound of '"Te and Urokinase having an activity of between 0.8 to 2.5 mCi per 10 Kiu of Urokinase.
• a method of preparing a radio labeled thrombolytic enzyme selected from the group consisting of Streptokinase and Urokinase labeled with *"Tc which comprises the steps of:
• Step (a) treating from about 5 to about 250 Kiu of said enzyme with from about 15 to about 20 mCi of 99m b. adding to the mixture of Step (a) from about 0.01 to about 4 mg. of freshly prepared stannous chloride and hydrochloric acid,
• a method according to claim 8 which comprises the sequential steps of:
• Step (a) treating from about 50 to about 100 Kiu of Streptokinase with from about 15 to about 20 mCi of "'TcO b. adding to the mixture of Step (a) from about 0.1 to about 1 mg. of freshly prepared stannous chloride i fi L LQ-MQQPQH! N YSlI Q acid,
• Step (b) adding to the acidic solution of Step (b) an alkaline buffer in an amount sufficient to raise the pH to between about 7 and about 8, and
• a method of detecting thromboembolisms in a vascular system which comprises introducing into said vascular system under examination between about 8 and 350 Kiu of a physiologically acceptable solution of "Tc labeled Streptokinase or Urokinase having a strength of between about 1 and about 20 mCi/Kiu and scanning said vascular system to determine the point of increased gamma radiation.

Landscapes

• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Proteomics, Peptides & Aminoacids (AREA)
• Epidemiology (AREA)
• General Health & Medical Sciences (AREA)
• Medicinal Chemistry (AREA)
• Optics & Photonics (AREA)
• Pharmacology & Pharmacy (AREA)
• Physics & Mathematics (AREA)
• Animal Behavior & Ethology (AREA)
• Chemical & Material Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
• Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
• Investigating Or Analysing Biological Materials (AREA)
• Enzymes And Modification Thereof (AREA)

Priority Applications (7)

Applications Claiming Priority (1)

Publications (1)

Family

ID=23080113

Family Applications (1)

Country Status (7)

Cited By (9)

Families Citing this family (5)

• 1972
  • 1972-08-21 US US00282100A patent/US3812245A/en not_active Expired - Lifetime
• 1973
  • 1973-06-06 FR FR7320558A patent/FR2196788B1/fr not_active Expired
  • 1973-07-06 BE BE6044231A patent/BE802052A/xx unknown
  • 1973-07-12 GB GB3338073A patent/GB1432878A/en not_active Expired
  • 1973-07-17 NL NL7309907A patent/NL7309907A/xx unknown
  • 1973-07-19 DE DE19732336751 patent/DE2336751A1/de active Pending
  • 1973-08-15 JP JP9164173A patent/JPS5346915B2/ja not_active Expired

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