Effect of Roux-en-Y gastric bypass on the bioavailability of metoprolol from immediate and controlled release tablets: a single oral dose study before and after surgery

Oral doses of mimosine (ranging from 400 to 800 mg/kg body weight) were given to 71 sheep, either as two successive daily doses (10 sheep) or as a single dose (61 sheep). The effectiveness of these treatments for defleecing was assessed and in some sheep measurements were made of the concentration of mimosine in plasma after dosing, and of the rate of wool growth before and after dosing. In addition, the effectiveness as defleecing agents of two related compounds (an analogue of mimosine, 'isomimosine', and a metabolite, 3,4-dihydroxypyridine (DHP)) was assessed. Two successive daily doses of mimosine (300 mg/kg/day) allowed all sheep to be defleeced. With sheep consuming a daily ration of 600 g, a single oral dose of mimosine (400 mg/kg) was sufficient to allow defleecing of most sheep; when the daily ration was 1200 g, a dose of 600 mg/kg was required to allow defleecing of most sheep. The effectiveness of oral doses for defleecing could be explained by the absorption of mimosine over a period in excess of 24 hr. Concentrations of mimosine in plasma were usually above 100 µmoles/l 24 hr after an effective dose. Failure to achieve complete cessation of fibre growth occurred occasionally, irrespective of dose level, and two sheep died after dosing. Fasting prior to dosing appeared to obviate the effects of previous high nutrition, but increased the risk of toxic effects. Fasting resulted in exceptionally high concentrations of mimosine in plasma (200–300 µmoles/l) 1 and 2 days after dosing. Both fibre diameter and mass of wool grown were increased in the early regrowth after dosing with mimosine. 'Isomimosine' had a similar potency to mimosine for stopping fibre growth in sheep, whether given as an intravenous infusion or as a single oral dose. DHP, given as an intravenous infusion, was ineffective as a defleecing agent.

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Pharmacokinetic characteristics of cilostazol 200 mg controlled-release tablet compared with two cilostazol 100 mg immediate-release tablets (Pletal) after single oral dose in healthy Korean male volunteers

Translational and Clinical Pharmacology ◽

10.12793/tcp.2016.24.4.183 ◽

2016 ◽

Vol 24 (4) ◽

pp. 183 ◽

Cited By ~ 1

Author(s):

Jin Dong Son ◽

Sang Min Cho ◽

Youn Woong Choi ◽

Soo-Hwan Kim ◽

In Sun Kwon ◽

...

Keyword(s):

Controlled Release ◽

Oral Dose ◽

Single Oral Dose ◽

Immediate Release ◽

Male Volunteers ◽

Release Tablet

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Safety, Tolerability, Pharmacokinetics, and Pharmacodynamic Properties of Taranabant, a Novel Selective Cannabinoid-1 Receptor Inverse Agonist, for the Treatment of Obesity: Results From a Double-Blind, Placebo-Controlled, Single Oral Dose Study in Health

The Journal of Clinical Pharmacology ◽

10.1177/0091270008314467 ◽

2008 ◽

Vol 48 (4) ◽

pp. 418-427 ◽

Cited By ~ 37

Author(s):

Carol Addy ◽

Susie Li ◽

Nancy Agrawal ◽

Julie Stone ◽

Anup Majumdar ◽

...

Keyword(s):

Oral Dose ◽

Single Oral Dose ◽

Inverse Agonist ◽

Double Blind ◽

Double Blind Placebo ◽

Cannabinoid 1 Receptor ◽

Dose Study ◽

Treatment Of Obesity ◽

Receptor Inverse Agonist

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Structural identification of bitespiramycin metabolites in rat: A single oral dose study

Xenobiotica ◽

10.1080/00498250500087580 ◽

2005 ◽

Vol 35 (4) ◽

pp. 343-358 ◽

Cited By ~ 7

Author(s):

X. G. Shi ◽

J. P. Fawcett ◽

X. Y. Chen ◽

D. F. Zhong

Keyword(s):

Oral Dose ◽

Single Oral Dose ◽

Structural Identification ◽

Dose Study

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Mass balance, pharmacokinetics, and metabolism of [14C] brivanib (BMS-582664), prodrug of BMS-540215, in subjects with advanced or metastatic solid tumors

Journal of Clinical Oncology ◽

10.1200/jco.2009.27.15_suppl.3566 ◽

2009 ◽

Vol 27 (15_suppl) ◽

pp. 3566-3566

Author(s):

R. Ganapathi ◽

T. Mekhail ◽

C. Wu ◽

B. Fischer ◽

J. Gong ◽

...

Keyword(s):

Oral Dose ◽

Oral Administration ◽

Single Oral Dose ◽

Solid Tumors ◽

Kinase Inhibitor ◽

Total Radioactivity ◽

Open Label ◽

Single Dose Study ◽

Brivanib Alaninate ◽

Dose Study

3566 Background: Brivanib alaninate (BMS-582664, B) is an oral prodrug of BMS-540215, a dual tyrosine kinase inhibitor of VEGFR and FGFR signaling pathways which are important for angiogenesis and tumor growth. The recommended phase II/III dose of B is 800 mg daily. Methods: A two-part, open-label, single-dose study was conducted in subjects with advanced or metastatic solid tumors. Part A represented the period for assessment of the pharmacokinetics (PK), metabolism, and elimination of B, In part A, subjects received a single oral dose of 800 mg [14C]-labeled B containing 100 μCi of total radioactivity (0.125 μCi/mg). Blood was collected at selected time points for analyses of PK, biotransformation, and total radioactivity over a 10-day period. Complete urinary and fecal output was collected over the 10-day period or until discharge, and analyzed for total radioactivity and biotransformation. Part B began when subjects completed Part A. Part B subjects received B administered orally at a dose of 800 mg once daily starting on approximately Day 15 to 17 of study. Subjects continued in this study until disease progression or unacceptable toxicity. Results: 4 subjects (2 NSCLC, 1 ovarian, 1 renal cell carcinoma) were treated with B in both parts A & B. B was tolerable with few G3/4 AEs (increased fatigue, 1 event, cognitive disturbance, 1 event). The results revealed that B is completely converted to active moiety, BMS-540215, after oral administration. BMS-540215 is extensively metabolized in humans. Elimination is primarily via the feces. Following a single oral dose of [14C]-labeled B, approximately 12% and 82% of the administered radioactivity was recovered in the urine and feces, respectively, within 10 days. BMS-540215 accounted for 0.00% and 7.4% of the administered dose in urine and feces, respectively, with the remainder of the dose being minor metabolites. The mean terminal t1/2 of BMS-540215 was 14 hours. Conclusions: After oral administration of single 800 mg oral doses of [14C] B, BMS-540215 was found to be the major active circulating moiety in plasma (22.5%). BMS-540215 is primarily eliminated via metabolism. [14C]-labeled B formulation was well tolerated with no AEs leading to the discontinuation of any subject. [Table: see text]

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Pharmacokinetics of diltiazem hydrochloride delay-onset sustained-release pellet capsules in healthy volunteers

Brazilian Journal of Pharmaceutical Sciences ◽

10.1590/s1984-82502013000100004 ◽

2013 ◽

Vol 49 (1) ◽

pp. 29-38 ◽

Cited By ~ 2

Author(s):

Xi-Qing Yan ◽

Zhi-Gang Chen ◽

Rong-Liang Wang ◽

Jun Yang ◽

Fang Ai ◽

...

Keyword(s):

Controlled Release ◽

Oral Dose ◽

Sustained Release ◽

Healthy Volunteers ◽

Single Oral Dose ◽

High Performance ◽

Reversed Phase ◽

Pharmacokinetic Parameters ◽

Diltiazem Hydrochloride ◽

New Formulation

The pharmacokinetics (PK) of ordinary tablets and sustained release capsules of diltiazem hydrochloride in human clinical trials had been studied. The PK of diltiazem hydrochloride delay-onset sustained-release pellet capsules, a new dosage form, has not been reported, although it is very important to clinical use. In this paper, we investigated the PK of diltiazem hydrochloride delay-onset sustained-release pellet capsules and the food influence in Chinese healthy volunteers. The PK parameters indicated that the diltiazem hydrochloride delay-onset sustained-release pellet capsules appeared marked characteristics of delayed and controlled release. An opened-label, randomized and parallel clinical trial was conducted in 36 Chinese healthy volunteers with single oral dose (90 mg, 180 mg or 270 mg) and a multiple oral dose (90 mg d-1×6 d) administration. The effect of food on the PK of one single oral dose (360 mg) was investigated in 24 healthy Chinese volunteers. Plasma diltiazem concentration was determined by reversed-phase high-performance liquid chromatography (RP-HPLC) and the main pharmacokinetic parameters were analyzed by PKSolver (Ver 2.0). All clinical studies were conducted in the Clinical Pharmacological Center (No. JDX1999064) of Xiangya Hospital Affiliated Central South University, China. The PK parameters suggested that the new formulation had marked characteristics of delayed and controlled release of diltiazem, and food intake did not alter significantly diltiazem pharmacokinetic parameters.

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