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Abbreviations: EtOH, ethanol; GDO, glycerol di-oleate; GMO, glycerol mono-oleate; PG, propylene glycol; SEDDS, self-emulsifying drug delivery system.

Abbreviations: EtOH, ethanol; GDO, glycerol di-oleate; GMO, glycerol mono-oleate; PG, propylene glycol; SEDDS, self-emulsifying drug delivery system.

di-glycerides) or Miglyol 812 (a mixture of medium chain tri-glyerides) and each animal received a total dose of 6mg Drug X from formulations containing 300mg/g of the drug.

The Miglyol 812-containing formulation produced less than half the bioavailability of the Capmul MCM-containing formulation (p < 0.05, paired t-test). In conclusion, the absorption of Drug X was improved with the SEDDS formulation containing medium chain mono-/di- glycerides (Capmul MCM) as compared to that of the SEDDS containing the medium chain tri-glycerides (Miglyol).

Example 4

To evaluate the effect of the administered lipid volume on Drug X absorption, three SEDDS formulations containing 300mg/g Drug X were prepared which were identical in composition (see inset in Fig. 7) with the exception of the quantity of the lipid excipient (an 8:2 mixture of GDO:GMO), which ranged from 50 to 180mg/g; a fourth SEDDS, from which GDO/GMO had been omitted, was prepared and administered as a control. Addition of 45 mg/g DEA to the formulations resulted in a mean lipid droplet size of ~120-150nm, which was independent of the lipid content. This observation suggests that (i) the dispersion performance of these SEDDS formulations is dictated by the presence of a small amount of an organic amine (vide supra) and (ii) the presence of a substantial amount of lipid in the formulation does not alter the droplet size significantly. The Drug X exposure was determined in fasted rats administered a 20mg/kg dose of the drug as the predispersed microemulsion of each SEDDS formulation (prepared by 50-fold dilution in water followed by manual agitation). The mean, dose-normalized (AUC/dose) Drug X exposures were positively correlated with the amount of GDO/GMO in the formulation between 50 and

Drug X

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