Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Particulate form
Patent
1994-09-01
1996-04-02
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Particulate form
424489, 424490, A61K 916, A61K 950
Patent
active
055038522
ABSTRACT:
Drug delivery systems have been developed based on the formation of diketopiperazine (or analogs) microparticles. In the preferred embodiment the microparticle is stable at low pH and disintegrates at physiological pH, and is particularly useful for oral drug delivery. In other embodiments, the microparticles are stable at high pH and disintegrate at neutral or basic pH, or are stable at neutral pH and disintegrate at high or low pH. In the most preferred embodiment the microparticles are formed in the presence of the drug to be delivered, for example, insulin, felbamate, calcitonin or heparin. The diketopiperazine synthetic intermediates are preferably formed by cyclodimerization to form diketopiperazine derivatives at elevated temperatures under dehydrating conditions, functionalized on the side chains, and then precipitated with drug to be incorporated into microparticles.
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McCabe R. Tyler
Rhodes Christopher A.
Shen Gregory S.
Steiner Solomon S.
Benston, Jr. William E.
Page Thurman K.
Pharmaceutical Discovery Corporation
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