Enhancing Posaconazole Absorption

Posaconazole is useful in the prophylaxis and treatment of fungal infections, particularly in neutropenic patients and bone marrow transplant recipients. However, it is administered orally, and in seriously ill patients, absorption is often suboptimal. Now, in an industry-sponsored study, researchers have examined the effects of various gastric conditions on posaconazole absorption. The four-part, open-label, randomized, crossover trial involved 49 healthy adult volunteers (12 or 13 in each group).

Administration of 400 mg of posaconazole with a carbonated acidic beverage, compared with administration under fasting conditions, increased mean area under the curve (AUC) by 70%, whereas administration with a proton-pump inhibitor (PPI) decreased mean AUC by 32%. Administration with a nutritional supplement increased mean AUC by 66%, and administration during — or 20 minutes after — a high-fat meal increased mean AUC by about 385%. Under fasting conditions, giving posaconazole in split doses (i.e., 200 mg 4 times daily, rather than 400 mg twice daily) increased mean AUC by 161%.