Drug – bio-affecting and body treating compositions – Radionuclide or intended radionuclide containing; adjuvant...
Patent
1989-11-21
1992-12-01
Stoll, Robert L.
Drug, bio-affecting and body treating compositions
Radionuclide or intended radionuclide containing; adjuvant...
534 10, 534 14, A61K 4902
Patent
active
051679485
DESCRIPTION:
BRIEF SUMMARY
The invention relates to a diagnostic or radiotherapeutic composition comprising a hydrogen containing compound. The invention further relates to a compound to be used for said composition and to a kit for preparing a radiodiagnostic composition.
Frequently used diagnostic compositions comprise radionuclide-labelled compounds. Such compounds are used for diagnostic examination e.g. into deviations in shape and function of internal organs and into the presence and location of pathological processes in the body. For this purpose, a composition in which the radioactive compound is present is administered to the patient, for example, in the form of an injectable liquid. By means of a suitable detector, e.g. a gamma camera, images can be obtained by recording the emitted radiation of, for example, the organ or the pathological process in which the radioactive compound has been incorporated.
Another important tool in medical diagnostics is NMR imaging. In this technic generally diagnostic compositions are used comprising NMR contrast agents. These contrast agents cause an image producing or contrast intensifying effect in the organ or tissue wherein they are incorporated, thus allowing the obtainment of images by using suitable detection apparatus.
Radiotherapeutic compositions are injectable compositions comprising a radioactive compound for radiotherapeutic application. It is in the purpose of this radioactive compound to emit a suitable radiation, preferably beta-rays after incorporation in the target organ or tissue, generally a malignant tumour. By this irradiation the tumour can be eliminated or its growth can be prevented.
The above radioactive compounds or agents have one characteristic in common in that they are administered in very low dosages to achieve the desired purpose, viz. to enable a diagnostic examination or to irradiate the target organ or tissue without causing adverse side-effects. Administration of radiodiagnostic agents in larger quantities than the minimal dosages needed for imaging enhances the risk of accumulation of these agents in other places of the body than in the target organ or tissue, as a consequence of which the concentration of the agent in the environment of said target organ or tissue is increased. These background disturbances may have a serious impact on the examination of the target organ or tissue due to a decreased contrast between target organ and environmental tissue. In addition, when using radionuclide-labelled compounds, accumulation of radioactivity in other organs and tissues than the organ or tissue to be examined constitutes an extra radiation burden for these other organs and tissues which may adversely influence their health and proper functioning. This last-mentioned problem applies even more strongly to radiotherapeutic compounds, which compounds are only intended to be vehicles for carrying the radiation dose to the target organ or tissue, in particular a malignant tumour. In addition, diagnostic agents which are in particular intended to give information on the functioning of body organs should be administered in dosages which are as small as possible to not disturb endogenic biochemical processes or equilibriums in the body.
It will be evident from the above explanation that in particular the "target organ specificity" is of utmost importance for the above compounds or agents to be used in diagnostic or radiotherapeutic compositions. By the term "target organ specificity" is to be understood the presence of the compound in question in the target organ or tissue selectively (i.e. compared to other organs or tissues, like blood and muscles) during a predetermined well-defined period of time. This latter requirement means that the compound is carried along to and accumulated in the target organ or tissue sufficiently fast and that its residence time in said organ or tissue is sufficiently long to allow a diagnostic examination or, for a radiotherapeutic compound, to make an optimum use of its radiation potential.
The "target organ specificity" of many kno
REFERENCES:
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Wenzel et al. "Verbesserte Diagnostik durch deuterierte Radiopharmaka?", Appl. Radiat. Isot. 39, 10, 1988 (Wenzel I).
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Mallinckrodt Medical Inc.
Sayala C.
Stoll Robert L.
Witt Evan R.
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