Self-assembling diketopiperazine drug delivery system

Details Self-assembling diketopiperazine drug delivery system Self-assembling diketopiperazine drug delivery system

A - Human Necessities

61

K

A61K 47/22 (2006.01) A61K 9/16 (2006.01) A61K 38/28 (2006.01) A61K 31/725 (1990.01)

Patent

CA 2131366

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 the most preferred embodiment the microparticle are formed in the presence of the drug to be delivered, for example; insulin or heparin. The diketopiperazine synthetic intermediates are preferably formed by cyclodimerization to form diketopiperazine derivatives at elevated conditions under dehydrating conditions, then precipitated with drug to be incorporated into microparticles.

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