Bioavailability of seocalcitol II: development and characterisation of self-microemulsifying drug delivery systems (SMEDDS) for oral administration containing medium and long chain triglycerides.

摘要: Abstract By constructing ternary phase diagrams it was possible to identify two self-microemulsifying drug delivery systems (SMEDDS) containing either medium chain triglycerides (MC-SMEDDS) or long (LC-SMEDDS), with the same ratio between lipid, surfactant and co-surfactant. The SMEDDS ended up having a composition of 25% 48% 27% co-surfactant, MC-SMEDDS: viscoleo, cremophor RH40, akoline MCM LC-SMEDDS: sesame oil, peceol. Upon dilution water both resulted in clear bluish transparent microemulsions narrow droplet size 30 nm. industrial usefulness developed evaluated regard bioavailability chemical stability using vitamin D analogue, seocalcitol, as model compound. absorption seocalcitol rats were approximately 45% 18%, respectively, from MC-SMEDDS LC-SMEDDS indicating similar vivo behavior formulations, despite difference nature lipid component. There no improvement by use SMEDDS, compared achieved simple MCT LCT solutions (22–24%) (Grove, M., Pedersen, G.P., Nielsen, J.L., Mullertz, A., 2005. Bioavailability seocalcitol. I. Relating solubility biorelevant media oral rats-effect triglycerides. J. Pharm. Sci. 94, 1830–1838.). After 3 months’ storage at accelerated conditions (40 °C/75% RH), decrease concentration 10–11% found degradation less than 3% for LCT. In this study seem be better choice due slightly higher