Method for making self-assembling diketopiperazine drug delivery system
US5503852A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Sep 1, 1994 |
| Grant date | Apr 2, 1996 |
| Priority date | — |
| Expiry date | Sep 1, 2014 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61K9/1617
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.