Abstract
Solid dispersions containing furosemide and various amounts of hydroxypropyl methylcellulose (HPMC) were prepared by spray drying to investigate if the physical stability of amorphous furosemide during storage and dissolution could be improved by formulating the drug as a solid dispersion. All solid dispersions, containing 20, 50, or 80 w/w % HPMC, were stable for 730 days when stored at 22 °C and 33 % relative humidity (RH), whereas under accelerated storage conditions of 40 °C and 75 % RH the amorphous furosemide in the solid dispersions with 20 and 50 % HPMC converted to a crystalline form within 30 days of storage. In contrast, furosemide in solid dispersions containing 80 % HPMC stayed amorphous for 30 days. Dissolution experiments in conjunction with XRPD and in-line Raman spectroscopy showed that the addition of 80 % HPMC was necessary for complete avoidance of solid state conversion of amorphous fiirosemide to a crystalline form during dissolution.
| Original language | English |
|---|---|
| Journal | Journal of Drug Delivery Science and Technology |
| Volume | 23 |
| Issue number | 4 |
| Pages (from-to) | 409-415 |
| Number of pages | 7 |
| ISSN | 1773-2247 |
| Publication status | Published - 1 Jul 2013 |
Keywords
- Amorphous fiirosemide
- Biorelevant dissolution
- Hydroxypropyl methylcellulose
- Physical stability
- Solid dispersions
- Solid state characterisation