Storage-stable porphin compositions and a method for their manuf

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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540145, A61K 3140, C07D43722

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active

048822345

ABSTRACT:
Carboxyhydroxyporphin compounds such as hematoporphyrin exhibit instability upon warming. However, if this warming is extended and carried out in solution in the presence of a buffer so as to constitute a moderate temperature heat-treatment, a new composition of matter results which contains as much at 95% or more of an ester-linked oligomeric porphin-based material which is exceedingly storage-stable. This composition has superior activity as a photoimaging and photodynamic therapy agent. This process and the products it produces are disclosed. The oligomer products so formed can be formulated into pharmaceutical compositions for use in neoplastic tissue photoimaging and in photodynamic therapy of neoplastic tissues.

REFERENCES:
patent: 4649151 (1987-03-01), Dougherty et al.
J. Natl. Cancer Inst., vol. 26, 1961, The Use and Derivative of Hematoporphyrin in Tumor Detection.
J. Natl. Cancer Inst., vol. 52, 1974, Activated Dyes as Antitumor Agents.
Chemistry in Britain, May 1986, Light and Porphyrins in Cancer Therapy.
Porphyrin Photosensitization Workshop, (PPW).
Porphyrins in Tumor Therapy, Dougherty et al., Plenum Press, N.Y. and London, 1984.
Photochemistry and Photobiophysics, Moan et al., vol. 9, (1985), pp. 253-261.
Progress in Clinical and Biological Research, pp. 301-314, (1984), The Structure of the Active Component of Hematoporphyrin Derivative.

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