Excretion of pantoprazole in human breast.

OBJECTIVE: To measure the amount of pantoprazole in human milk following its oral administration to a breast-feeding mother and to estimate human exposure. STUDY DESIGN: One woman was studied over a 24-hour interval after oral administration of 40-mg pantoprazole. Serial plasma and milk samples were collected over 24 hours, and pantoprazole concentrations were measured by high-performance liquid chromatography. A milk/plasma ratio of 0.022 was observed at tmax, 2 hours after dose administration. Infant exposure was measured as maximum concentration in milk multiplied by an estimated maximum consumption of 200 mL at this time. RESULTS: The relative infant dose was estimated to be 7.3 microg of pantoprazole, which is equivalent to 0.14% of the weight-normalized dose received by the mother. Because pantoprazole is unstable in acidic pH, the systemic dose received by the infant is expected to be lower if the ingested pantoprazole is exposed to acid in the infant's stomach. The mother detected no adverse events in the infant. CONCLUSION: These limited data show that pantoprazole is minimally excreted into breast milk. While it is not known if pantoprazole affects breast milk production, women who are breast-feeding do not have to stop breastfeeding when taking pantoprazole chronically.

Oral bioavailability of pantoprazole suspended in sodium bicarbonate solution.

The bioavailability of pantoprazole when administered as a suspension in sodium bicarbonate solution and as the oral tablet was studied. In an open-label, randomized, two-period crossover study, healthy fasting subjects received either one enteric-coated 40-mg pantoprazole tablet by mouth with 240 mL of water or 20 mL of a suspension prepared from one crushed pantoprazole tablet and 840 mg of sodium bicarbonate solution and administered via a nasogastric tube. Treatments were separated by a 48-hour washout period. Blood samples were collected at intervals up to 24 hours after drug administration for measurement of pantoprazole concentration by high-performance liquid chromatography (HPLC) and estimation of pharmacokinetic values. A separate study was conducted to determine pantoprazole's stability in the suspension for up to three months at 25, 5, and -20 degrees C; concentrations were measured by HPLC. Twelve subjects completed the study. The suspension yielded pantoprazole Cmax values similar to those of the tablet formulation, but the drug was 25% less bioavailable. There was no lag time for the suspension. The suspension was stable for up to two weeks at 5 degrees C and up to three months at -20 degrees C. A suspension of pantoprazole in sodium bicarbonate solution yielded a Cmax similar to that of the tablet formulation, and the drug was quickly absorbed. However, bio-availability was slightly lower with the suspension than with the tablet.