Source: https://patents.google.com/patent/US4923969A/en
Timestamp: 2018-09-21 01:13:29
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US4923969A - Preparation of 99m Tc radiopharmaceuticals - Google Patents
Preparation of 99m Tc radiopharmaceuticals Download PDF
US4923969A
US4923969A US07241471 US24147188A US4923969A US 4923969 A US4923969 A US 4923969A US 07241471 US07241471 US 07241471 US 24147188 A US24147188 A US 24147188A US 4923969 A US4923969 A US 4923969A
US07241471
R.sup.+ [.sup.99m TcNX.sub.4 ].sup.-                       I
TABLE 1______________________________________Biological Distribution of .sup.99 m TcN-MDP inmice*______________________________________     % Injected Dose/OrganTime after Injection       30 min         60 min     120 min______________________________________Heart       0.6    (0)     0.4  (0)   0.3  (1)Lung        2.9    (5)     3.0  (14)  1.9  (15)Liver       10.4   (4)     9.4  (8)   6.2  (13)Spleen      0.4    (1)     0.3  (1)   0.4  (1)Stomach     1.1    (1)     0.8  (2)   1.2  (11)Kidneys     6.9    (27)    3.3  (5)   2.6  (7)Intestines  4.3    (4)     4.1  (6)   6.1  (13)Femurs      0.3    (0)     0.3  (0)   0.3  (0)Blood       26.5   (46)    18.8 (18)  13.5 (40)______________________________________     % Injected Dose/Gram OrganHeart       4.2    (2)     2.4  (4)   2.0  (4)Liver       5.7    (3)     4.7  (5)   3.8  (1)Kidneys     13.0   (54)+   5.6  (11)  5.8  (18)Femurs      1.7    (2)     1.4  (2)   1.5  (1)Blood       13.0   (22)    8.1  (3)   6.7  (19)+______________________________________ Standard deviation of last significant digit(s) in brackets. *n = 3 unless otherwise stated + 2 mice
TABLE 2______________________________________Biological Distribution of .sup.99 m TcN-DTPA inmice*.______________________________________       % Injected Dose/OrganTime After Injection         30 min     60 min   120 min______________________________________Heart         0.1(0)     0.1(0)   0.1(0)Lung          0.7(1)     0.7(2)   0.4(1)Liver         1.7(2)     1.5(3)   1.1(2)Spleen        0.1(0)     0.1(0)   0.1(0)Stomach       1.1(2)     1.3(4)   0.9(0)Kidneys       1.5(1)     1.3(2)   0.8(0)Intestines    2.1(4)     2.0(3)   2.1(2)Femurs        0.1(0)     0.1(0)   0.1(0)Blood         6.2(8)     4.0(5)   2.4(1)______________________________________       % Injected Dose/Gram OrganHeart         0.6(0)     0.5(1)   0.4(1)Liver         0.8(1)     0.7(1)   0.6(1)Kidneys       2.5(1)     2.2(4)   1.5(2)Femurs        0.5(1)     0.4(1)   0.4(1)Blood         2.8(5)     1.8(2)   1.2(0)______________________________________ Standard deviation of last significant digit(s) in brackets. *n = 3
TABLE 4______________________________________Urinary Clearance of .sup.99 m TcN-MDP, .sup.99 m TcN-DPTAand .sup.99 m TcN-CYS*% Retained Activity.sup.99 m TcN-MDP           .sup.99 m TcN-DTPA                       .sup.99 m TcN-CYS______________________________________30 min 71.9(43)     24.8(42)    35.8(43)60 min 51.4(14)     21.4(31)    18.7(28)120 min  44.7(57)     14.6(6)     15.7(15)______________________________________ Standard deviation of last significant digit(s) in brackets. *n = 3
TABLE 5______________________________________Biological Distribution of .sup.99 m TcN-GLUC in mice.______________________________________Time After     % Injected Dose/OrganInjection 30 min       60 min   120 min______________________________________Heart     0.7(0.1)     0.7(0.1) 0.4(0.1)Lung      2.2(0.6)     3.0(0.5) 1.4(0.2)Liver     6.4(1.6)     6.2(1.7) 7.1(2.1)Spleen    0.3(0.1)     0.3(0.1) 0.2(0.1)Stomach   1.4(0.4)     1.5(0.4) 1.6(0.7)Kidneys   4.7(0.6)     3.9(0.3) 3.4(0.1)Intestines     5.4(0.7)     4.1(0.8) 7.0(1.4)Femurs    0.3(0.0)     0.3(0.0) 0.2(0.1)Blood     25.7(2.3)    21.7(3.6)                           12.7(1.9)______________________________________Time After     % Injected Dose/Gram OrganInjection 30 min       60 min   120 min______________________________________Heart     4.5(0.7)     4.6(1.0) 2.6(0.6)Liver     3.3(0.8)     3.1(0.9) 3.3(0.8)Kidneys   8.4(1.0)     6.6(0.7) 5.6(0.6)Femurs    1.7(0.1)     1.3(0.1) 0.8(0.2)Blood     12.0(1.0)    9.5(1.8) 5.2(0.3)______________________________________ Standard deviation in brackets. n = 3.
TABLE 6______________________________________Biological Distribution of .sup.99 m TcN-HEDP in mice.______________________________________Time After     % Injected Dose/OrganInjection 30 min      60 min   120 min______________________________________Heart     0.5(0.0)    0.3(0.0) 0.3(0.0)Lung      2.5(0.6)    1.8(0.3) 1.5(0.4)Liver     12.1(0.3)   9.0(1.0) 7.7(0.5)Spleen    0.6(0.1)    0.3(0.0) 0.3(0.1)Stomach   0.6(0.1)    0.7(0.1) 0.6(0.1)Kidneys   4.1(0.2)    3.2(0.2) 3.0(0.2)Intestines     6.9(0.5)    7.0(0.2) 6.8(0.6)Femurs    0.5(0.0)    0.5(0.1) 0.4(0.1)Blood      28.0(5.0)≠                 16.2(2.0)                           13.2(1.0)≠______________________________________Time After     % Injected Dose/Gram OrganInjection 30 min      60 min   120 min______________________________________Heart     4.3(0.5)    2.4(0.3) 2.3(0.2)Liver     8.1(0.8)    5.5(0.7) 4.8(0.4)Kidneys   9.1(0.4)    6.5(0.4) 6.1(0.3)Femurs    3.4(0.5)    3.1(0.8) 2.7(0.6)Blood      16.2(1.0)≠                 7.3(1.1)  7.7(0.5)≠______________________________________ Standard deviation in brackets. n = 3 unless otherwise stated. ≠ n = 2
TABLE 7______________________________________Biological Distribution of .sup.99 m TcN-HIDA in mice.______________________________________Time After     % Injected Dose/OrganInjection 30 min       60 min   120 min______________________________________Heart     0.4(0.1)     0.4(0.0) 0.2(0.0)Lung      2.3(0.3)     2.0(0.3) 1.2(0.3)Liver     7.2(1.4)     6.7(1.2) 3.6(0.2)Spleen    0.4(0.1)     0.3(0.0) 0.1(0.0)Stomach   1.1(0.2)     2.0(0.4) 1.0(0.0)Kidneys   3.5(0.2)     3.4(0.2) 2.1(0.0)Intestines     . 6.8(1.0)   9.2(0.4) 6.9(0.2)Femurs    0.3(0.1)     0.4(0.0) 0.2(0.0)Blood     25.8(1.6)    20.6(1.3)                           16.3(2.2)______________________________________Time After     % Injected Dose/Gram OrganInjection 30 min       60 min   120 min______________________________________Heart     2.9(0.5)     2.7(0.4) 1.6(0.1)Liver     4.2(0.8)     3.9(0.6) 2.1(0.1)Kidneys   6.9(0.5)     6.7(0.4) 4.2(0.1)Femurs    2.0(0.4)     2.3(0.1) 1.0(0.1)Blood     13.6(0.6)    10.8(0.6)                           8.7(1.1)______________________________________ Standard deviation in brackets. n = 3.
TABLE 8______________________________________Biological Distribution of .sup.99 m TcN-PIPIDA in mice.______________________________________Time After     % Injected Dose/OrganInjection 30 min       60 min   120 min______________________________________Heart     0.4(0.0)     0.3(0.1) 0.4(0.1)Lung      2.3(0.3)     1.8(0.6) 1.8(0.2)Liver     14.6(1.0)    16.2(6.1)                           10.1(1.0)Spleen    0.2(0.1)     0.3(0.0) 0.2(0.0)Stomach   0.7(0.1)     1.0(0.0) 0.8(0.1)Kidneys   4.6(0.5)     7.6(5.6) 3.3(0.1)Intestines     12.8(1.5)    12.0(0.8)                           14.9(2.1)Femurs    0.3(0.0)     0.2(0.0) 0.2(0.0)Blood     26.8(3.0)    23.2(0.4)                           20.0(3.7)______________________________________Time After     % Injected Dose/Gram OrganInjection 30 min       60 min   120 min______________________________________Heart     3.4(0.2)     2.1(0.8) 2.8(0.5)Liver     8.8(0.6)     8.9(3.1) 5.8(0.8)Kidneys   9.4(0.6)     14.1(7.2)                           6.3(0.2)Femurs    2.0(0.3)     1.1(0.1) 1.0(0.2)Blood     14.8(1.9)    11.5(0.7)                           10.2(1.5)______________________________________ Standard deviation in brackets. n = 3. ≠ n = 2
TABLE 9______________________________________Urinary Clearance of .sup.99 m TcN-GLUC, .sup.99 m TcN-HEDP,.sup.99 m TcN-HIDA and .sup.99 m TcN-PIPIDA% Retained Activity.sup.99 m TcN-       .sup.99 m TcN-                  .sup.99 m TcN-GLUC        HEDP       HIDA     .sup.99 m TcN-PIPIDA______________________________________30 min 72.6(4.2)           68.8(9.5)  74.9(5.8)                             79.5(1.2)60 min 59.3(6.4)           52.2(1.2)  66.3(0.9)                             73.2(2.7)120 min  45.6(5.6)           47.2(4.5)  54.7(1.1)                             62.0(2.5)______________________________________ Standard deviation in brackets. n = 3.
TABLE 10______________________________________Biological distribution of .sup.99 m TcN-DMSA______________________________________Time after     % Injected Dose/OrganInjection 30 min       60 min   120 min______________________________________Heart     0.3(0.0)     0.3(0.0) 0.2(0.0)Lung      1.6(0.1)     1.1(0.2) 1.1(0.2)Liver     4.3(0.1)     3.9(0.3) 3.4(0.2)Spleen    0.4(0.1)     0.4(0.1) 0.3(0.0)Stomach   0.6(0.1)     0.7(0.2) 0.5(0.1)Kidney    10.3(0.5)    12.3(0.8)                           17.1(0.7)Intestines     5.3(0.7)     5.1(0.4) 4.8(0.5)Femurs    0.5(0.1)     0.5(0.0) 0.4(0.1)Blood     18.0(1.7)    13.5(0.9)                           9.5(0.5)Urine     39.9(11.4)   57.8(4.4)                           65.3(4.3)______________________________________Time after     % Injected Dose/Gram OrganInjection 30 min       60 min   120 min______________________________________Heart     1.8(0.1)     1.8(0.2) 1.2(0.0)Liver     2.0(0.2)     2.1(0.3) 1.7(0.2)Kidney    16.4(0.7)    22.2(1.4)                           29.0(2.9)Femurs    2.0(0.5)     2.4(0.2) 1.9(0.4)Blood     7.1(0.8)     6.4(0.3) 4.1(0.2)______________________________________ Standard Deviation in brackets n = 3.
R.sup.+ [.sup.99m TcNX.sub.4 ].sup.-
US07241471 1983-12-29 1988-09-07 Preparation of 99m Tc radiopharmaceuticals Expired - Fee Related US4923969A (en)
AUPG3034/83 1983-12-29
AUPG303483 1983-12-29
US06774592 Division US4851515A (en) 1983-12-29 1984-12-21 Preparation of 99m Tc radiopharmaceuticals
US07461398 Division US5011916A (en) 1983-12-29 1990-01-05 Preparation of 99m Tc radiopharmaceuticals
US4923969A true US4923969A (en) 1990-05-08
ID=3770463
US06774592 Expired - Fee Related US4851515A (en) 1983-12-29 1984-12-21 Preparation of 99m Tc radiopharmaceuticals
US07241471 Expired - Fee Related US4923969A (en) 1983-12-29 1988-09-07 Preparation of 99m Tc radiopharmaceuticals
US07461398 Expired - Fee Related US5011916A (en) 1983-12-29 1990-01-05 Preparation of 99m Tc radiopharmaceuticals
US (3) US4851515A (en)
EP (1) EP0166746B1 (en)
JP (1) JPS61501087A (en)
DE (1) DE3484511D1 (en)
WO (1) WO1985003063A1 (en)
US20060083684A1 (en) * 2002-02-12 2006-04-20 Walton Paul H Method of radio-labelling biomolecules
GB8711496D0 (en) * 1987-05-15 1987-06-17 Amersham Int Plc Tc-99m radiopharmaceuticals
WO1989008657A3 (en) * 1988-03-09 1989-10-19 Oris Sa Preparation of nitruro compounds usable as radio-pharmaceutical products
FR2639542B1 (en) * 1988-11-25 1991-03-22 Oris Ind Radiopharmaceutical has cardiac tropism nitrido comprising a complex of a transition metal, and process for its preparation
FR2639638B1 (en) * 1988-11-25 1991-07-26 Oris Ind Process for the preparation of suitable transition metal complexes as radiopharmaceuticals or for the synthesis of new radiopharmaceuticals
FR2648049B1 (en) * 1989-06-12 1994-10-21 Cis Bio Int Radiopharmaceutical has cardiac tropism comprising a nitride complex of a transition metal, and process for its preparation
US5589576A (en) * 1989-08-29 1996-12-31 Amersham International Plc Cores for technetium radiopharmaceuticals
US4851515A (en) * 1983-12-29 1989-07-25 The Commonwealth Of Australia Preparation of 99m Tc radiopharmaceuticals
"Synthetic and Structural Aspects of Technetium Chemistry as Related to Nuclear Medicine: Inorganic Chemistry in Biology and Medicine", Tc Chemistry, E. Deutsch and B. L. Barnett, 1980, pp. 103-119.
Baldas et al., CA 95:214309t (1981). *
Baldas et al., CA 95:54003h (1981). *
Baldas et al., CA 96:57736f (1982). *
Baldas et al., CA 97:60987q (1982). *
Comments. Inorg. Chem., vol. 3, Nos. 2 3, pp. 83 103 (1984). *
Comments. Inorg. Chem., vol. 3, Nos. 2-3, pp. 83-103 (1984).
Kadan et al., CA 95:17322r (1981). *
Radioimmunoimaging and Radioimmunotherapy, S. W. Burchiel and B. A. Rhodes, Eds., Elsevier, N.Y. 1983, pp. 207 222. *
Radioimmunoimaging and Radioimmunotherapy, S. W. Burchiel and B. A. Rhodes, Eds., Elsevier, N.Y. 1983, pp. 207-222.
Synthetic and Structural Aspects of Technetium Chemistry as Related to Nuclear Medicine: Inorganic Chemistry in Biology and Medicine , Tc Chemistry, E. Deutsch and B. L. Barnett, 1980, pp. 103 119. *
Williams et al., CA 98:149778r (1983). *
EP0166746A1 (en) 1986-01-08 application
US4851515A (en) 1989-07-25 grant
EP0166746B1 (en) 1991-04-24 grant
JPS61501087A (en) 1986-05-29 application
DE3484511D1 (en) 1991-05-29 grant
EP0166746A4 (en) 1988-01-20 application
WO1985003063A1 (en) 1985-07-18 application
US5011916A (en) 1991-04-30 grant
Goldenberg et al. 1989 Imaging of colorectal carcinoma with radiolabeled antibodies