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Biomedical subjects

J Barth

Publications and source records attributed to J Barth.

At least 289 records · Page 16Linked to original sources
PubMedDate not supplied

Pharmacokinetics of prednisolone after high doses of prednisolone hemisuccinate.

Prednisolone in the form of its hemisuccinate was given intravenously in two different doses (1200 mg and 75 mg). Plasma levels of the ester and prednisolone were measured and pharmacokinetic parameters were calculated. The results indicate a dose-dependency in the pharmacokinetics of both hemisuccinate and the free alcohol. For the high dose 8 per cent of the administered ester was found unchanged in the urine indicating incomplete conversion of the pro-drug. Comparison with previous studies leads to the conclusion that prednisolone shows doubled non-linear pharmacokinetics with higher total body clearance in the medium dose range than in the low and high dose range. Volume of distribution changes accordingly, but overall elimination rate remains remarkably constant. Saliva levels of prednisolone were low and agree reasonably well with calculated plasma concentrations of free, non-protein-bound prednisolone. No prednisolone hemisuccinate was found in saliva.

Adult↗
PubMedDate not supplied

Pharmacokinetics of dexamethasone and its phosphate ester.

Dexamethasone in form of its phosphate was given intravenously in two different doses (1.5 mg kg-1 and 15 mg). Plasma levels of the ester and dexamethasone were measured and pharmacokinetic parameters were calculated. The results indicate no dose-dependency of the pharmacokinetic parameters in the investigated range for dexamethasone. Conversion from the prodrug to the active form was rapid; maximum dexamethasone plasma concentrations were reached after 10 min. The results were verified by dexamethasone level monitoring in patients after chronic dosing. Predicted and achieved steady state levels agreed well.

Adult↗
PubMedDate not supplied

Pharmacokinetics and dose linearity testing of methylprednisolone phosphate.

The pharmacokinetics of methylprednisolone and methylprednisolone phosphate were investigated after intravenous administration of methylprednisolone phosphate to six healthy subjects at seven different doses between 16 and 1000 mg. Plasma, urine, and saliva were analyzed for methylprednisolone and methylprednisolone phosphate. Furthermore, endogenous hydrocortisone was measured in plasma. No non-linearity in the total body clearance of methylprednisolone phosphate or methylprednisolone could be detected. The average elimination half-life for the prodrug was 3.7 min indicating rapid hydrolysis. After 15 min more than 90 per cent of the phosphate has been hydrolyzed. No prodrug could be detected in saliva; very little of the ester (average 0.9 per cent of the dose) was excreted unchanged into the urine. Methylprednisolone is formed rapidly. The total body clearance was 21 1h-1, the terminal half-life 2.8 h. In the post-distribution phase methylprednisolone levels in saliva went parallel to plasma levels. The mean saliva/plasma ratio was 0.22. An average of 5.2 per cent of the dose was eliminated into the urine in the form of methylprednisolone. Hydrocortisone suppression was dose-dependent. For doses above 125 mg hydrocortisone levels were significantly lowered after 24 h. For doses above 500 mg the suppression was still significant after 48 h. The results indicate a rapid and predictable in vivo conversion of methylprednisolone phosphate to its active form methylprednisolone.

Adolescent↗