Prednisolone concentrations in cerebrospinal fluid after oral prednisone. Preliminary data

Penetration of prednisolone across the blood-brain barrier was studied in 17 patients (ten women and seven men) with a mean age of 64 +/- 17 years admitted for nerve root pain warranting a lumbar puncture. One blood sample and one cerebrospinal fluid sample were obtained concomitantly from each patient, two hours (n = 7), four hours (n = 5) or six hours (n = 5) after an oral dose of 40 mg of prednisone. Prednisolone was assayed in all samples using high performance liquid chromatography and its binding to plasma proteins was determined using ultrafiltration. Total plasma prednisolone levels declined over time from 597 +/- 174 ng/ml two hours post-dose to 422 +/- 106 ng/ml four hours post-dose and 250 +/- 85 ng/ml six hours post-dose. Plasma levels of free prednisolone were 95 +/- 21 ng/ml, 59 +/- 17 ng/ml, and 18 +/- 14 ng/ml, respectively, at the same time points. Prednisolone was detectable in all cerebrospinal fluid samples, in levels of 14 +/- 2 ng/ml after two hours, 29 +/- 9 ng/ml after four hours and 17 +/- 7 ng/ml after six hours. These data demonstrate that equilibration of plasma and cerebrospinal fluid levels is achieved after six hours.