Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Patent
1986-05-14
1989-09-05
Lee, Mary C.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
514578, 514556, 514553, 562887, A61K 3119, C07C 5734
Patent
active
048639656
ABSTRACT:
Pharmaceutical compositions of the prodrug type, a process for the preparation thereof, a process for the preparation of the as prodrug functioning compounds and compounds obtained herein.
The pharmaceutical compositions of the invention contain organic acid anhydrides with formula 1 through 5, as well as the pharmacological acceptable salts thereof as prodrug functioning compounds, together with a suitable pharmaceutically acceptable gaseous, liquid or solid carrier.
The prodrug systems of the invention possess as favorable property that they amend the residence time of the pharmaceutical composition in the body by influencing the transport system.
Furthermore they increase the biological availability because of the more lipophilic properties of the anhydride compared with the acid, so that this improved administration performance may contribute to lower dosages.
Further the prodrug systems according to the invention contribute to the reduction of the complaints of patients, because the systems usually remove the unpleasant bitter taste and the flavor, whereas the gastro intestinal irritation of the organic acids is removed or reduced.
REFERENCES:
patent: 2577699 (1951-12-01), Cooper
patent: 4206220 (1980-06-01), Sloan
March, Advanced Organic Chemistry: Reactions, Mechanisms, and Structure, McGraw Hill, 1968, p. 325.
De Cock Etienne J.
Jansen Frans H. J.
B.V.B.A. Inpharm
Howard Mary Sue
Lee Mary C.
Lewen Bert J.
Sternberg Henry
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