Biomedical subjects

Sandeep Dutta

Publications and source records attributed to Sandeep Dutta.

21 records · Page 2Linked to original sources

PubMed2002

Single- and multiple-dose pharmacokinetics of fiduxosin under nonfasting conditions in healthy male subjects.

Selective alpha1a-adrenoreceptor antagonists are effective agents for treatment of benign prostatic hyperplasia, a disorder occurring in middle-aged and elderly males. The objective of this study was to determine the single- and multiple-dose pharmacokinetics of fiduxosin, a novel, selective alpha1a-adrenoreceptor antagonist. This was a Phase I, randomized, double-blind, placebo-controlled, parallel-group, single and multiple oral dose study of fiduxosin. Single daily oral doses of 30, 60, or 90 mg of fiduxosin or placebo were administered to healthy adult male subjects (N = 36; 8 active and 4 placebo per dosing group) on Day 1 and Days 5 to 11 (7 consecutive days) after a high-fat breakfast. Fiduxosin plasma concentration-time profiles for Days 1 and 11 were used to assess fiduxosin pharmacokinetics. Fiduxosin single-dose and steady-state pharmacokinetics were dose independent after oral administration under nonfasting conditions. Steady state was achieved after 4 days of qd dosing. Approximately 28% of the oral dose was eliminated by the fecal route as unchanged drug. Less than 1% of the unchanged drug was recovered in the urine after oral administration.

Administration, Oral↗

PubMed2002

Multiple dose pharmacokinetics of fiduxosin under fasting conditions in healthy elderly male subjects.

Selective alpha1a-adrenoceptor antagonists are effective agents for treatment of benign prostatic hyperplasia, a disorder occurring in middle-aged and elderly males. The objective of this study was to determine the pharmacokinetics of fiduxosin, a novel alpha1a-adrenoceptor antagonist, following multiple dose administration. This was carried out in a Phase I, randomized, double-blind, placebo-controlled, parallel group, multiple oral dose study of fiduxosin. Single once-daily oral doses of 30, 60, 90 or 120 mg of fiduxosin or placebo were administered to healthy elderly male subjects (n = 48; 8 active and 4 placebo per dosing group) for 14 consecutive days. Fiduxosin plasma concentration-versus-time profiles for days 1, 7 and 14 were used to assess fiduxosin pharmacokinetics. Steady state was achieved by day 7. At steady-state mean Tmax (time to maximum plasma concentration), CL/F (apparent oral clearance) and Vbeta/F (apparent volume of distribution) ranges were 1.8-7.8 h, 27.3-47.2 L h(-1) and 846-1399 L, respectively. Tmax and VbetaF were independent of dose. Cmax (maximum plasma concentration), Cmin (minimum plasma concentration) and AUC24 (area under plasma concentration vs time curve from 0 to 24 h) for days 7 and 14 were linearly proportional with dose overthe 30-120 mg/day dose range and were unchanged from day 7 to day 14. It was concluded that fiduxosin multiple-dose pharmacokinetics were dose-independent and time-invariant over the 30-120 mg/day dose range under fasting conditions.

Administration, Oral↗

PubMedDate not supplied

Effect of food on the pharmacokinetics of fiduxosin in healthy male subjects.

The effect of food on the pharmacokinetics of fiduxosin, a novel selective alpha1a-receptor antagonist, was determined in healthy male subjects. This was a Phase I, open-label, single-center, randomized, two-period, crossover, single oral dose study of fiduxosin. Healthy male subjects (N= 14) were administered single oral doses of 30 mg of fiduxosin under fasting or nonfasting (1026 Kcal, 54 g fat, 46% calories from fat) conditions in each period. Fiduxosin plasma concentration profiles were used to assess fiduxosin pharmacokinetics. The mean Cmax, Tmax, AUC(infinity), CL/F and Vbeta/F values under fasting and nonfasting conditions were 34.3 and 150 ng/mL, 5.4 and 5.4 h, 822 and 1940 ng x h/mL, 42.5 and 17.2 L/h, and 924 and 235 L, respectively. The harmonic mean t 1/2 under fasting and nonfasting conditions were 13.9 and 9.28 h, respectively. Food significantly increased the bioavailability of fiduxosin. Under the nonfasting regimen, the Cmax central value was more than 4-fold and the AUC(infinity) central value more than 2-fold the central value of the fasting regimen. Tmax was not significantly different between fasting and nonfasting regimens. Food also decreased fiduxosin oral clearance (CL/F) by 60% and volume of distribution (Vbeta/F) by 75%.

Adolescent↗