Drug – bio-affecting and body treating compositions – Radionuclide or intended radionuclide containing; adjuvant...
Patent
1997-10-22
2000-09-12
Dees, Jose' G.
Drug, bio-affecting and body treating compositions
Radionuclide or intended radionuclide containing; adjuvant...
424 165, 424 91, 424 93, 424 94, 556 30, A61K 5100, A61M 3614
Patent
active
061174122
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to the use in diagnostic imaging, in particular X-ray, MRI, ultrasound and scintigraphy, of contrast agents comprising bismuth clusters and/or organic bismuth compounds, and to contrast media containing such bismuth compounds. Another aspect of the present invention is the use of the bismuth compounds in therapy, in particular as antiulcer agents.
All diagnostic imaging is based on the achievement of different signal levels from different structures within the body. Thus in X-ray imaging, for example, for a given body structure to be visible in the image the X-ray attenuation by that structure must differ from that of the surrounding tissues. The difference in signal between the body structure and its surroundings is frequently termed contrast and much effort has been devoted to means of enhancing contrast in diagnostic imaging since the greater the contrast between a body structure and its surroundings the higher the quality of the images and the greater their value to the physician performing the diagnosis. Moreover, the greater the contrast the smaller the body structures that may be visualized in the imaging procedure, i.e. increased contrast can lead to increased spatial resolution.
The diagnostic quality of images is strongly dependent on the inherent noise level in the imaging procedure--the ratio of the contrast level to the noise level can thus be seen to represent an effective diagnostic quality factor for diagnostic images.
Achieving improvement in such a diagnostic quality factor has long been and still remains an important goal. In techniques such as X-ray and ultrasound, one approach to improve the diagnostic quality factor has been to introduce contrast enhancing materials, contrast agents, into the body region being imaged.
Thus in X-ray, for instance, early examples of contrast agents were insoluble inorganic barium salts which enhanced X-ray attenuation in the body zones into which they distributed. More recently the field of X-ray contrast agents has been dominated by soluble iodine containing compounds such as those markedet by Nycomed AS under the trade names Omnipaque.RTM. and Visipaque.RTM..
Much recent work on X-ray contrast agents has concentrated on aminopolycarboxylic acid (APCA) chelates of heavy metal ions and, recognising that effective imaging of many body sites requires localization at the body sites in question of relatively high concentrations of the metal ions, there have been suggestions that polychelants, that is substances possessing more than one separate chelant moiety, might be used to achieve this.
Various bismuth compounds have been suggested in the prior art as X-ray absorbing agents. Other prior art documents focus on the use of metal chelates in diagnostic imaging, mainly in MRI. In addition, bismuth compounds have a long history in therapeutic medicine specially in treatment of gastrointestinal diseases such as ulcers. Although antiulcer agents such as the H.sub.2 -antagonists cimetidine and ranitidine, and more recently proton pump inhibitors such as omeprazole, have been developed, there is still medical use of bismuth compounds in ulcer treatment.
The most frequently used bismuth compounds as gastrointestinal drugs today are bismuth subnitrate and bismuth subsalicylate. Bismuth subnitrate or bismuth hydroxide nitrate oxide (Bi.sub.5 O(OH).sub.9 (NO.sub.3).sub.4 is prepared by hydrolysis of bismuth nitrate and is practically insoluble in water. It is usually used as a suspension (milk of bismuth). Bismuth subnitrate is also used topically in lotions and ointments. Bismuth subsalicylate or basic bismuth salicylate (C.sub.7 H.sub.5 BiO.sub.4) is also practically insoluble in water and is administered as a suspension or in the form of tablets. Products containing bismuth subsalicylate are used against indigestion, nausea and diarrhea. As an antidiarrheal agent it shows good activity against Salmonella with less activity versus E. coli.
Several bismuth compounds are known to be biologically active and have been suggested as active i
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Almen Torsten
Berg Ame
Droege Michael
Golman Klaes
Klaveness Jo
Dees Jos,e G.
Jones Dameron
Nycomed Imaging AS
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