Self assembling diketopiperazine drug delivery system
US5352461A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Mar 11, 1992 |
| Grant date | Oct 4, 1994 |
| Priority date | — |
| Expiry date | Mar 11, 2012 |
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 the most preferred embodiment the microparticles 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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.