Pharmacokinetic evaluation of pamidronate after oral administration: A study on dose proportionality, absolute bioavailability, and effect of repeated administration

1993 ◽  
Vol 53 (5) ◽  
pp. 297-300 ◽  
Author(s):  
L. Hyldstrup ◽  
G. Flesch ◽  
S. A. Hauffe
Keyword(s):  
Oral Administration ◽  
Repeated Administration ◽  
Dose Proportionality ◽  
Absolute Bioavailability ◽  
Pharmacokinetic Evaluation

Dose Proportionality of Bisoprolol Enantiomers in Humans After Oral Administration of the Racemate

1994 ◽  
Vol 34 (8) ◽  
pp. 829-836 ◽  
Author(s):  
Atanu Dutta ◽  
Robert Lanc ◽  
Evan Begg ◽  
Richard Robson ◽  
Luisa Sia ◽  
...  
Keyword(s):  
Oral Administration ◽  
Dose Proportionality

scholarly journals Mouse, rat, and dog bioavailability and mouse oral antidepressant efficacy of (2R,6R)-hydroxynorketamine

2018 ◽  
Vol 33 (1) ◽  
pp. 12-24 ◽  
Author(s):  
Jaclyn N Highland ◽  
Patrick J Morris ◽  
Panos Zanos ◽  
Jacqueline Lovett ◽  
Soumita Ghosh ◽  
...  
Keyword(s):  
Oral Administration ◽  
Learned Helplessness ◽  
Oral Bioavailability ◽  
Forced Swim Test ◽  
Abuse Potential ◽  
Absolute Bioavailability ◽  
Forced Swim ◽  
Antidepressant Effects ◽  
Immobility Time ◽  
Antidepressant Efficacy

Background: ( R,S)-ketamine has gained attention for its rapid-acting antidepressant actions in patients with treatment-resistant depression. However, widespread use of ketamine is limited by its side effects, abuse potential, and poor oral bioavailability. The ketamine metabolite, ( 2R,6R)-hydroxynorketamine, exerts rapid antidepressant effects, without ketamine’s adverse effects and abuse potential, in rodents. Methods: We evaluated the oral bioavailability of ( 2R,6R)-hydroxynorketamine in three species (mice, rats, and dogs) and also evaluated five candidate prodrug modifications for their capacity to enhance the oral bioavailability of ( 2R,6R)-hydroxynorketamine in mice. Oral administration of ( 2R,6R)-hydroxynorketamine was assessed for adverse behavioral effects and for antidepressant efficacy in the mouse forced-swim and learned helplessness tests. Results: ( 2R,6R)-hydroxynorketamine had absolute bioavailability between 46–52% in mice, 42% in rats, and 58% in dogs. Compared to intraperitoneal injection in mice, the relative oral bioavailability of ( 2R,6R)-hydroxynorketamine was 62%, which was not improved by any of the candidate prodrugs tested. Following oral administration, ( 2R,6R)-hydroxynorketamine readily penetrated the brain, with brain to plasma ratios between 0.67–1.2 in mice and rats. Oral administration of ( 2R,6R)-hydroxynorketamine to mice did not alter locomotor activity or precipitate behaviors associated with discomfort, sickness, or stereotypy up to a dose of 450 mg/kg. Oral ( 2R,6R)-hydroxynorketamine reduced forced-swim test immobility time (15–150 mg/kg) and reversed learned helplessness (50–150 mg/kg) in mice. Conclusions: These results demonstrate that ( 2R,6R)-hydroxynorketamine has favorable oral bioavailability in three species and exhibits antidepressant efficacy following oral administration in mice.

scholarly journals Pharmacokinetics of rosmarinic acid in rats by LC-MS/MS: absolute bioavailability and dose proportionality

RSC Advances ◽  
2017 ◽  
Vol 7 (15) ◽  
pp. 9057-9063 ◽  
Author(s):  
Jingxian Wang ◽  
Guoyuan Li ◽  
Tianqi Rui ◽  
An Kang ◽  
Guochun Li ◽  
...  
Keyword(s):  
Rosmarinic Acid ◽  
Dose Proportionality ◽  
Absolute Bioavailability ◽  
Rapid Absorption ◽  
Pharmacokinetic Properties

The pharmacokinetic properties of RA were characterized as rapid absorption, middle-speed elimination, poor absolute bioavailability, and lack of dose proportionality.

scholarly journals Physicochemical Effects of the Major Quassinoids in a Standardized Eurycoma longifolia Extract (Fr 2) on the Bioavailability and Pharmacokinetic Properties, and their Implications for Oral Antimalarial Activity

2011 ◽  
Vol 6 (3) ◽  
pp. 1934578X1100600 ◽  
Author(s):  
Bin-Seng Low ◽  
Chin-Hoe Teh ◽  
Kah-Hay Yuen ◽  
Kit-Lam Chan
Keyword(s):  
Oral Administration ◽  
Intravenous Administration ◽  
Antimalarial Activity ◽  
Elimination Rate ◽  
Rat Plasma ◽  
Chemical Degradation ◽  
Absolute Bioavailability ◽  
Phytochemical Analysis ◽  
Eurycoma Longifolia ◽  
Pharmacokinetic Properties

A simple validated LC-UV method for the phytochemical analysis of four bioactive quassinoids, 13α(21)-epoxyeurycomanone (EP), eurycomanone (EN), 13α,21-dihydroeurycomanone (ED) and eurycomanol (EL) in rat plasma following oral (200 mg/kg) and intravenous administration (10 mg/kg) of a standardized extract Fr 2 of Eurycoma longifolia Jack was developed for pharmacokinetic and bioavailability studies. The extract Fr 2 contained 4.0%, 18.5%, 0.7% and 9.5% of EP, EN, ED and EL, respectively. Following intravenous administration, EP displayed a relatively longer biological half-life (t½ = 0.75 ± 0.25 h) due primarily to its lower elimination rate constant (ke) of 0.84 ± 0.26 h−1) when compared with the t½ of 0.35 ± 0.04 h and ke of 2.14 ± 0.27 h−1, respectively of EN. Following oral administration, EP showed a higher Cmax of 1.61± 0.41 μg/mL over that of EN (Cmax = 0.53 ± 0.10 μg/mL). The absolute bioavailability of EP was 9.5-fold higher than that of EN, not because of chemical degradation since both quassinoids were stable at the simulated gastric pH of 1. Instead, the higher log Kow value of EP (-0.43) contributed to greater membrane permeability over that of EN (log Kow = −1.46) at pH 1. In contrast, EL, being in higher concentration in the extract than EP, was not detected in the plasma after oral administration because of substantial degradation by the gastric juices after 2 h. Similarly, ED, being unstable at the acidic pH and together with its low concentration in Fr 2, was not detectable in the rat plasma. In conclusion, upon oral administration of the bioactive standardized extract Fr 2, EP and EN may be the only quassinoids contributing to the overall antimalarial activity; this is worthy of further investigation.

Pharmacokinetic Evaluation of Visnagin and Ammi visnaga Aqueous Extract after Oral Administration in Rats

Planta Medica ◽  
2012 ◽  
Vol 78 (17) ◽  
pp. 1831-1836 ◽  
Author(s):  
Karin Haug ◽  
Benjamin Weber ◽  
Guenther Hochhaus ◽  
Veronika Butterweck
Keyword(s):  
Oral Administration ◽  
Aqueous Extract ◽  
Ammi Visnaga ◽  
Pharmacokinetic Evaluation

Absolute bioavailability of PF-01367338 tablets following oral administration in cancer patients.

2011 ◽  
Vol 29 (15_suppl) ◽  
pp. e13615-e13615 ◽  
Author(s):  
D. D. Wang ◽  
K. A. Kern ◽  
M. Carpentieri ◽  
S. Zhang ◽  
B. Hee ◽  
...  
Keyword(s):  
Oral Administration ◽  
Cancer Patients ◽  
Absolute Bioavailability

INVESTIGATION OF DOSE PROPORTIONALITY AND ABSOLUTE BIOAVAILABILITY OF BROFAROMINE IN HEALTHY VOLUNTEERS

1992 ◽  
Vol 15 ◽  
pp. 430B ◽  
Author(s):  
K. H. Antonin ◽  
K. Kucher ◽  
L. Fuchs ◽  
P. R. Bieck ◽  
E. Schmidt
Keyword(s):  
Healthy Volunteers ◽  
Dose Proportionality ◽  
Absolute Bioavailability
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