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Effect of pharmaceutical excipients (PEs) on the rate-liming factors of model drugs for bioavailability was screened and designed.The desired bioavailability of acetaminophen (BCS Ⅰ) could be controlled by modifying release rate with an aid of PEs.Contrarily, the PEs could change aqueous and solid state stability of rabeprazole (BCS Ⅰ with low stability).The solubility and dissolution rate of poorly soluble itraconazole or cisapride (BCS Ⅱ) were also highly modified by PEs as well as delivery systems such as self-emulsifying system (SES) or dual-layered beads containing solubilizers and polymers, which could readily maximize in vivo drug bioavailability in rats and dogs.