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Pharmacotherapy. 2001 Aug;21(8):891-7.

Pharmacokinetics of cycloserine under fasting conditions and with high-fat meal, orange juice, and antacids.

Author information

1
Department of Medicine, National Jewish Medical and Research Center, Denver, Colorado 80206, USA.

Abstract

STUDY OBJECTIVES:

To determine the effect of a high-fat meal, orange juice, and antacids on absorption of a single oral dose of cycloserine and to estimate its population pharmacokinetic parameters.

DESIGN:

Randomized, four-period, crossover study.

SETTING:

Clinical research center.

PATIENTS:

Twelve healthy volunteers.

INTERVENTIONS:

Subjects received single doses of cycloserine 500 mg after a 12-hour fast (reference), with a high-fat meal, with orange juice, and with antacids. They also received clofazimine 200 mg, ethionamide 500 mg, and p-aminosalicylic acid granules 6000 mg.

MEASUREMENTS AND MAIN RESULTS:

Plasma samples were collected for 48 hours and assayed by validated high-performance capillary electrophoresis assay. Concentration-time data were analyzed with noncompartmental, one-compartment, and population methods. The maximum concentration (Cmax) of cycloserine was decreased (p=0.02) by the high-fat meal. No other statistically significant differences were observed for Cmax and area under the curve from time zero to infinity across the four treatments. The high-fat meal significantly (p<0.0001) delayed time to maximum concentration by 4.7 times compared with that of the reference (1.1 hr).

CONCLUSION:

The pharmacokinetics of cycloserine were minimally affected by orange juice and antacids, whereas the high-fat meal delayed absorption. Administering cycloserine without a high-fat meal avoids potential alterations in the pattern of absorption.

PMID:
11718495
DOI:
10.1592/phco.21.11.891.34524
[Indexed for MEDLINE]

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