comprised of 0.01M HCl + 0.15M NaCl, pH = 2.0, followed by an approximate, 10-fold dilution in simulated intestinal fluid (SIF), comprised of 0.05 M phosphate buffer, pH = 6.8, resulted in coarse emulsion formation (10-100 ^m droplet size) with no evidence of drug precipitation suggesting that these formulations should prevent PNU-74006 precipitation upon dilution in the GI tract in-vivo. In comparison, the SEDDS-c formulation, which contained Maisine (a mixture of 55% GDO, 50% GMO, and 5% GTO (18) yielded a microemulsion upon dilution with water as evidenced by instantaneous formation of a transparent solution with a faint opalescence.

Table 2 Composition of the PNU-74006 SEDDS Formulations, Behavior in the In Vitro Dilution Test and Oral Bioavailability Data


Aqueous solution (mg/mL)

PNU-74006 EtOH 95% PG

Polysorbate 80 Cremophor EL Capmul MCM Captex 300 Capmul GMO-K Maisine Citric acid NaOH


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