Drug – bio-affecting and body treating compositions – Radionuclide or intended radionuclide containing; adjuvant... – In aerosol – fine spray – effervescent – pressurized fluid,...
Patent
1991-12-18
1994-11-08
Stoll, Robert L.
Drug, bio-affecting and body treating compositions
Radionuclide or intended radionuclide containing; adjuvant...
In aerosol, fine spray, effervescent, pressurized fluid,...
A61K 4902
Patent
active
053624734
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to a metal-radionuclide-labelled particulate composition which may be used in the form of a dry aerosol for lung scintigraphy or for radiotherapy of diseases of the respiratory system, to a method of preparing the composition and to a kit for carrying out the method. The invention further relates to a method of performing a radiodiagnostic lung examination, in particular of the mucociliary transport systems.
Radiolabelled aerosols have been used for lung scintigraphy for some 15 years already, usually for lung ventilation studies and to detect and localize lung abnormalities. It is desirable for this purpose to cause deposition of aerosol particles to take place in the alveoli, hence alveolarly. A nebulizer developed for this purpose which generates aerosol particles having an average diameter of 0.8 .mu.m, is described by Kotrappa c.s. in J. Nucl. Med. 18 1977, 1082-1085. An improved aerosol generator-inhalator with which dry aerosol particles having a smaller spreading in particle size can be generated is the subject of European Patent Application 85200830.9.
The present invention relates in particular to a radiolabelled particulate composition which after nebulization may be used for the examination of the mucociliary transport system and hence of bronchial diseases which are related to an unsatisfactory functioning of the mucociliary transport system. In the non-respiratory part of the bronchial tubes there exists a very effective barrier against inhaled particles which may comprise toxic or infectious agents and may have allergenic or carcinogenic effects. This barrier is formed by a mucus layer which is transported in the direction of the mouth in a constant stream by microscopically small cilia. This transport is termed the mucociliary transport. Conditions for an undisturbed mucociliary transport are a normal coordinated cilia movement and a normal mucus production. An unsatisfactory functioning of the mucociliary transport may play a part in chronic bronchial diseases. A simple and reliable method of measuring the mucociliary transport is therefore of extremely great importance. In fact, a considerable part of the world population suffers from bronchial diseases and for these CARA-patients a good method of diagnosis is indispensable before medical treatment can proceed. However, good quantitative methods to measure the mucociliary transport have failed so far. In the past a number of invasive or semi-invasive methods were used which, in addition to the disadvantage of the medical surgery as such, also influence the mucociliary transport itself unfavorably, so that the results obtained are not reliable.
It is the object of the present invention to provide a radiolabelled particulate composition which after nebulization may be used for lung scintigraphy and which is intended in particular for the examination of the mucociliary transport. The particles of the composition, to be suitable for the examination of the mucociliary transport, must satisfy various requirements: should not vary; this means that the particles should not become smaller due to evaporation, but also that they should not grow, for example, as a result of active absorption of water by the particles. particle size to enable a selective examination. "label" should be sufficiently stable, i.e. should not be released from the particles during the nebulization, breathing and the subsequent lung examination. spherical, to be able to reach the lung tissue to be examined. enable the desired lung examination and should be completely inert with respect to the lung tissue, i.e. it should be so tolerable for the lungs that even the mucociliary transport is not influenced by it.
This object can be achieved by means of a particulate composition which is labelled with a metal-radionuclide and which according to the present invention is characterized in that it comprises radiolabelled particles having a base of silica gel, another siliceous material or a non-swelling polymer, at the surface of which organic ligands ar
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Chapman Lara E.
Mallinckrodt Medical Inc.
Stoll Robert L.
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