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Biomedical subjects

E Mroszczak

Publications and source records attributed to E Mroszczak.

10 recordsLinked to original sources
PubMed1994

Tolerability, central effects and pharmacokinetics of intravenous ketorolac tromethamine in volunteers.

The central effects, tolerability and pharmacokinetics of multiple intravenous doses of the analgesic ketorolac tromethamine (30 mg 4 times daily for 5 days) were studied in male volunteers. In this double-blind, randomized, parallel group study, 13 subjects received ketorolac tromethamine and 7 subjects received placebo (vehicle). To determine the effects of withdrawal all subjects were then given further dosing with placebo (4 times daily) for 2 days while maintaining the double-blind nature of the previous drug assignment. Physical examinations and laboratory tests were obtained prior to the drug administration and after completion of the study. Scales for assessment of anxiety, depression, sleep and opiate withdrawal were presented to the subjects on day 2, 5, 6, 7 and 8 of the study. After 5 days of multiple intravenous doses ketorolac showed overall good systemic tolerance and safety in comparison with placebo. Myalgia and taste perversion were more frequently reported in the ketorolac group. The frequency of injection site complaints, mostly transient pain, was about 80% for both ketorolac and placebo, indicating these were likely caused by the vehicle. There were no significant changes in the scales assessing anxiety, depression, sleep and opiate withdrawal during treatment with ketorolac and after its withdrawal, suggesting that the drug has neither any major central effects nor any clear addiction potential in this dose schedule. Pharmacokinetic parameters were derived from plasma samples collected after the first and last active doses.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1989

Bioequivalence of two oral contraceptive drugs containing norethindrone and ethinyl estradiol.

Two oral contraceptive drugs, Formulation A and Formulation B, both of similar hormonal content, were compared with each other to determine if they were bioequivalent. Both drugs contain 1 mg of norethindrone (NET) and 0.035 mg of ethinyl estradiol (EE). Application of an interval test for the ratio of the computed parameter means demonstrated equivalence for the two formulations with respect to the 0-24 hour area under the plasma level versus time curve (AUC24), the total area under the curve (AUCtot) and for the maximum plasma concentration (Cmax) for both ethinyl estradiol and norethindrone. The data support the hypothesis for bioequivalence of the two formulations with respect to total absorption.

Adult↗
PubMed1988

Absorption of naproxen controlled-release tablets in fasting and postprandial volunteers.

The absorption of naproxen in a new controlled-release (CR) formulation (1000 mg tablet) was studied in fasting and postprandial volunteers. The total area under the plasma concentration-time curve averaged 2221 micrograms.hr/mL in fasting participants and 2111 micrograms.hr/mL in postprandial participants; whereas the difference was statistically significant (P = .025), the 95% confidence intervals indicated equivalent values. The peak plasma concentration was lower in the fasting state (63.1 micrograms/mL) than in the fed state (86.1 micrograms/mL) (P = .0001). There were no statistically significant differences between fasting versus postprandial values for the mean absorption time (9.7 hr vs. 7.7 hr) or plasma half-life (17.3 hr vs. 17.6 hr). Hence, the rate and extent of absorption of CR naproxen was not substantially altered by the ingestion of food.

Adult↗
PubMed1988

Pharmacokinetics of ketorolac tromethamine in humans after intravenous, intramuscular and oral administration.

The pharmacokinetics of ketorolac tromethamine, a potent non-narcotic analgesic agent used for relief of moderate to severe pain, has been studied in 15 healthy volunteers who received single 10 mg doses intravenously (i.v.), intramuscularly (i.m.) and orally (p.o.) in a three-way cross-over design. The kinetics of i.v. ketorolac were characterized by a terminal half-life of 5.09 h, a small plasma clearance (CL = 0.35 ml.min-1.kg-1) and a small tissue distribution (Vss = 0.11 l.kg-1, V beta = 0.17 l.kg-1; mean (SD). Following i.m. and p.o. administration, peak levels of approximately 0.8 microgram/ml were rapidly attained (tmax = 0.8 and 0.9 h, respectively) and the systemic bioavailability was essentially complete.

Administration, Oral↗
PubMed1986

Bioequivalence of norethindrone and ethinyl estradiol for two different weight tablets with the same hormonal content.

Two tablets of differing weights, 100 mg (A) and 50 mg (B), of an oral contraceptive drug (OC) were compared with each other and to a solution (C) of the same components. The composition of the OC consisted of 1 mg of norethindrone (NET) and 0.035 mg of ethinyl estradiol (EE2). Both tablets were shown to differ from the solution, which was more rapidly absorbed, but were not significantly different from each other. Formulation means for NET and EE2, for each of the two products, were similar. Application of an interval test for the ratio of computed parameters demonstrated equivalence of the two formulations with respect to 0-24 hr area under the curve (AUC24) and total area under the curve (AUC+o+) for both NET and EE2 and with respect to concentration maximum (Cmax) for EE2. The data support the hypothesis for bioequivalence of the two formulations with respect to total absorption.

Absorption↗
PubMed1984

Pharmacokinetics of nicardipine following oral and intravenous administration in man.

The pharmacokinetics of nicardipine have been studied following oral and intravenous administration in man and the effects of food on nicardipine kinetics investigated. Following intravenous administration of nicardipine as an infusion plasma levels declined in a biphasic manner and plasma clearance values were of the same order as hepatic plasma flow. Following oral administration in the starved state nicardipine was rapidly absorbed but subject to presystemic elimination. Maximal plasma concentrations were achieved typically between 20 minutes and 2 hours after administration. The oral bioavailability of nicardipine determined by reference to a co-administered intravenous radiolabelled dose was found to be non-linearly related to dose. Bioavailability ranged from 15-45% approximately over the dose range 10-40 mg. Administration of nicardipine following a meal reduced the bioavailability of nicardipine.

Administration, Oral↗
PubMed1981

Effect of Mylanta on naproxen bioavailability.

The effect of Mylanta on naproxen bioavailability was studied in 11 healthy volunteers. In separate experiments, single oral doses of naproxen (250 mg) and multiple oral doses (250 mg twice daily for 7 days) were administered with and without Mylanta. Coadministration of naproxen with Mylanta in the single-dose experiment did not significantly affect the area under the curve (579 vs. 580 microgram/ml X hr with and without Mylanta, respectively), time to peak serum concentration (2.5 vs. 2.6 hr), peak serum concentration (37.2 vs. 34.8 microgram/ml) or plasma half-life (16.1 vs. 16.4 hr). There was no significant difference between trough level naproxen concentrations at steady state (29.6 microgram/ml with Mylanta vs. 30.7 microgram/ml without Mylanta). The data were also used to investigate naproxen pharmacokinetics predicted by two different pharmacokinetic models, one of which allowed for protein binding. The nonlinear protein-binding model accurately predicted steady-state concentration, while the values predicted by the linear model exceeded actual values by 33-54%.

Adult↗
PubMed1980

Relationship among particle size distribution, dissolution profile, plasma values, and anthelmintic efficacy of oxfendazole.

Three mean particle sizes of oxfendazole raw material (1.65 micron, lot A; 3.2 micron, 10t B; 12.0 micron, lot C) were prepared and identically formulated as corresponding (A, B, and C) suspensions at 2.26% (W/V) concentration. Studies involving microscopic examination, scanning electron microscope analysis, particle size distribution, and surface area measurement were carried out on raw materials. In vitro dissolution profiles were obtained for the suspensions. A comparative bioavailability study of these 3 suspensions was performed in 12 sheep with each sheep given each formulation in a Latin square crossover study design; oxfendazole was dosed at rate of 5 mg/kg of body weight. Plasma-value measurements were made followed by an analysis of various bioavailability studies. Plasma area values indicated that suspension C (dw = 12.0 micron) was significantly (P less than 0.05) less bioavailable than was suspension A (dw = 1.65 micron); there was no difference between suspension A and suspension B. Significant differences were not seen in biological half-life and maximum plasma concentrations. The term dw refers to that particle diameter (determined by Coulter counting) at which 50% of the oxfendazole mass was in the form of particles having a lesser diameter and 50% was in the form of particles having a greater diameter. In a separate study involving 20 Merino weaner sheep infected with benzimidazole-resistant Haemonchus contortus larvae, oxfendazole's anthelmintic efficacy was demonstrated in the 2.26% suspension dosage form (90% particles less than 10 micron) at a dosing rate of 5 mg/kg. A correlation was found between its anthelmintic activity and plasma area values when compared in individual sheep. Data demonstrated that substantial differences in particle size distribution of oxfendazole could influence its dissolution rate, plasma concentrations, and absorption characteristics, thus indicating that oxfendazole's absorption could be dissolution-rate limited.

Administration, Oral↗