Effect of Food on Nifedipine Sustained-Release Preparation

DICP ◽  
1989 ◽  
Vol 23 (9) ◽  
pp. 662-665 ◽  
Author(s):  
Kazuyuki Ueno ◽  
Syuichi Kawashima ◽  
Kiyotaka Uemoto ◽  
Tomoko Ikada ◽  
Kazuyoshi Miyai ◽  
...  

The effect of food on the bioavailability of a nifedipine sustained-release preparation was studied. Each of seven male volunteers received a single oral 20 mg dose with 100 mL of water under two conditions, fasting and after a meal, with a crossover after a seven-day wash-out period. Blood samples were drawn at time zero (just prior to dose), and 1, 2, 3, 4, 6, 8, 10, and 12 hours after dosing. Nifedipine assays were performed by gas chromatography. The area under the serum concentration-time curve (AUC) from 0 to 12 hours and maximum serum concentration (Cmax) were significantly increased by food. Blood pressure was significantly decreased by food. The mean AUC for fasting and meal conditions were 315.0 and 411.4 ng•h/mL, and the mean Cmax were 42.6 and 86.6 μg/mL, respectively. The results indicate that food may increase the bioavailability of nifedipine sustained-release preparation.

1981 ◽  
Vol 9 (3) ◽  
pp. 222-225 ◽  
Author(s):  
M Helliwell ◽  
D Berry

Plasma theophylline concentrations were measured in six volunteers given 675 mg of a sustained-release preparation (Phyllocontin®). Significant reductions in both the mean recorded peak theophylline plasma concentrations and the mean 12-hour theophylline bioavailability were observed after the administration of effervescent activated charcoal (Medicoal®) in single and multiple doses. These results indicate the potential use of activated charcoal in the management of theophylline poisoning.


1984 ◽  
Vol 140 (8) ◽  
pp. 477-479
Author(s):  
Gillian M. Shenfield ◽  
Bernard J. Hudson ◽  
John S. Boutagy ◽  
Ian A. Munro ◽  
Russel A. Vandenberg

2016 ◽  
Vol 76 (3) ◽  
pp. 566-570 ◽  
Author(s):  
Dae Hyun Yoo ◽  
Chang-Hee Suh ◽  
Seung Cheol Shim ◽  
Slawomir Jeka ◽  
Francisco Fidencio Cons-Molina ◽  
...  

ObjectiveTo demonstrate pharmacokinetic equivalence of CT-P10 and innovator rituximab (RTX) in patients with rheumatoid arthritis (RA) with inadequate responses or intolerances to antitumour necrosis factor agents.MethodsIn this randomised phase I trial, patients with active RA were randomly assigned (2:1) to receive 1000 mg CT-P10 or RTX at weeks 0 and 2 (alongside continued methotrexate therapy). Primary endpoints were area under the serum concentration–time curve from time zero to last quantifiable concentration (AUC0–last) and maximum serum concentration after second infusion (Cmax). Additional pharmacokinetic parameters, efficacy, pharmacodynamics, immunogenicity and safety were also assessed. Data are reported up to week 24.Results103 patients were assigned to CT-P10 and 51 to RTX. The 90% CIs for the ratio of geometric means (CT-P10/RTX) for both primary endpoints were within the bioequivalence range of 80%–125% (AUC0–last: 97.7% (90% CI 89.2% to 107.0%); Cmax: 97.6% (90% CI 92.0% to 103.5%)). Pharmacodynamics and efficacy were comparable between groups. Antidrug antibodies were detected in 17.6% of patients in each group at week 24. CT-P10 and RTX displayed similar safety profiles.ConclusionsCT-P10 and RTX demonstrated equivalent pharmacokinetics and comparable efficacy, pharmacodynamics, immunogenicity and safety.Trial registration numberNCT01534884.


2011 ◽  
Vol 17 (2) ◽  
pp. 297-300 ◽  
Author(s):  
Naoko Kanazawa ◽  
Kazuaki Matsumoto ◽  
Tomohide Fukamizu ◽  
Akari Shigemi ◽  
Keiko Yaji ◽  
...  

1996 ◽  
Vol 40 (11) ◽  
pp. 2577-2581 ◽  
Author(s):  
D R Luke ◽  
G Foulds ◽  
S F Cohen ◽  
B Levy

To date, the clinical pharmacology of large intravenous doses of azithromycin has not been described. In the present study, single 2-h intravenous infusions of 1, 2, and 4 g of azithromycin were administered to three parallel groups (in each group, six received active drug and two received placebo) of healthy male subjects. Toleration (assessed by scores of subject-administered visual analog scale tests spanning 0 [good] to 10 [poor]), safety, pharmacokinetics, and serum motilin levels were monitored for up to 240 h after the start of each intravenous infusion. Mean nausea scores of 0.0, 0.0, 1.0, and 0.5 and abdominal cramping scores of 0.0, 0.0, 0.4, and 0.4 for 12-h periods after doses of 0, 1, 2, and 4 g of azithromycin, respectively, suggested that azithromycin was well tolerated. Because of the standardized 1-mg/ml infusates, all subjects in the 4-g dosing group complained of an urgent need to urinate. There were no consistent trends in endogenous motilin levels throughout the study. The maximum concentration of azithromycin in serum (10 micrograms/ml after a 4-g dose) and the area under the concentration-time curve (82 micrograms.h/ml after a 4-g dose) were dose related. The mean pharmacokinetic parameters were an elimination half-life of 69 h, total systemic clearance of 10 ml/min/kg, and a volume of distribution at steady state of 33.3 liters/kg. The pharmacokinetic results suggest that the long half-life of azithromycin is due to extensive uptake and slow release of the drug from tissues rather than an inability to clear the drug. Single intravenous doses of up to 4 g of azithromycin in healthy subjects are generally well tolerated, and quantifiable concentrations may persist in serum for 10 days or more.


2019 ◽  
Vol 92 ◽  
pp. 22-32 ◽  
Author(s):  
Jian Ju ◽  
Xueqi Chen ◽  
Yunfei Xie ◽  
Hang Yu ◽  
Yahui Guo ◽  
...  

1997 ◽  
Vol 41 (5) ◽  
pp. 1143-1145 ◽  
Author(s):  
U Wintergerst ◽  
B Rolinski ◽  
J R Bogner ◽  
G Notheis ◽  
F D Goebel ◽  
...  

We evaluated the pharmacokinetics of rectally administered zidovudine (ZDV) in 10 human immunodeficiency virus-infected adults. After rectal administration of an aqueous ZDV solution (250 mg of ZDV), mean peak ZDV levels were 1.3 +/- 0.7 micromol/liter (mean +/- standard deviation) versus 5.0 +/- 2.2 micromol/liter (P < 0.0001) after oral intake of a 250-mg ZDV capsule. The half-life at beta phase was 87.8 +/- 39.6 min for rectally administered ZDV versus 55.8 +/- 20.1 min (P = 0.035) for orally administered ZDV. The mean area under the concentration-time curve from 0 min to infinity was 232 +/- 181 micromol/liter x min after rectal administration versus 362 +/- 110 micromol/liter x min after oral intake. Although the two routes were not bioequivalent, ZDV was absorbed considerably after rectal administration, with a pharmacokinetic profile resembling that of a sustained-release device.


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