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.

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

The Absolute Bioavailability and Dose Proportionality of Intravenous and Oral Dosage Regimens of Recainam

1991 ◽  
Vol 31 (5) ◽  
pp. 433-439 ◽  
Author(s):  
Steven M. Troy ◽  
William H. Cevallos ◽  
Kenneth A. Conrad ◽  
Soong T. Chiang ◽  
Jeffrey R. Latts
Keyword(s):  
Dose Proportionality ◽  
Oral Dosage ◽  
Absolute Bioavailability ◽  
Dosage Regimens ◽  
The Absolute

Pharmacokinetics of isochlorgenic acid C in rats by HPLC-MS: Absolute bioavailability and dose proportionality

2016 ◽  
Vol 185 ◽  
pp. 105-109 ◽  
Author(s):  
Li Hua Huang ◽  
Xiao Hong Xiong ◽  
Yun Ming Zhong ◽  
Mei Feng Cen ◽  
Xuan Ge Cheng ◽  
...  
Keyword(s):  
Dose Proportionality ◽  
Absolute Bioavailability

scholarly journals PHARMACOKINETIC PROPERTIES OF A NEW KAPPA-OPIOID ANALGESIC RU-1205 COMPOUND AT A SINGLE PERORAL ADMINISTRATION

2021 ◽  
Vol 9 (2) ◽  
pp. 149-160
Author(s):  
A. A. Spasov ◽  
L. A. Smirnova ◽  
O. Yu. Grechko ◽  
N. V. Eliseeva ◽  
Yu. V. Lifanova ◽  
...  
Keyword(s):  
Oral Administration ◽  
Analgesic Activity ◽  
Half Life ◽  
The Body ◽  
Absolute Bioavailability ◽  
Peroral Administration ◽  
Pharmacokinetic Parameters ◽  
Tail Flick ◽  
Test Substance ◽  
Pharmacokinetic Properties

The aim of the study is the investigation of the pharmacokinetic properties of the RU-1205 compound, with previously identified kappa-agonistic and analgesic effects, at a single oral administration, as well as comparison of the relationship between its pharmacokinetic and analgesic properties.Materials and methods. Pharmacokinetic parameters of RU-1205 after the oral administration at the dose of 50 mg / kg were investigated using the method of High Performance Liquid Chromatography  with determination of the concentration of the compound according to the previously constructed calibration schedule. The indices of the area under the pharmacokinetic curve, clearance, half-life, residence time of the drug molecule in the body, a total (apparent) volume of distribution, as well as the indicator of absolute bioavailability, were calculated. The tissue distribution and excretion of RU-1205 were studied.Potential metabolites of RU-1205 were predicted using the PALLAS 3.00 program. The study of the analgesic activity was carried out on a model of central somatogenic pain with electricalstimulation, with the dynamics assessment of the voltage amplitude of the corresponding reaction of the "tail-flick" reflex.Results. The compound under study is rapidly adsorbed from the gastrointestinal tract, reaching a maximum concentration by the end of the first hour of the study, and is determined in plasma within 12 hours. Its half-life is 17.7 hours. The absolute oral bioavailability is 37.3%. It was found out that the compound is withdrawn within 3-4 days. The main route of excretion is extrarenal. Biotransformation of a substance probably proceeds mainly with the formation of oxidized forms of the initial molecule by reactions of the first phase of metabolic transformation. The analgesic effect is long-lasting: it starts after 15 minutes and lasts for 12 hours with flattening of the curve by the 8th hour.Conclusion. When administered orally, the test substance undergoes a long process of elimination, has the greatest tropism for the elimination organs and undergoes active biotransformation processes in the body of animals. As a result of it, active metabolic products with an analgesic activity are, possibly, formed.

Development and validation of UPLC-MS/MS assay for quantification of cladrin: Absolute bioavailability and dose proportionality study in rats

2018 ◽  
Vol 152 ◽  
pp. 289-297 ◽  
Author(s):  
Mamunur Rashid ◽  
Sandeep K. Singh ◽  
Mohd Yaseen Malik ◽  
Sadaf Jahan ◽  
Swati Chaturvedi ◽  
...  
Keyword(s):  
Dose Proportionality ◽  
Absolute Bioavailability ◽  
Development And Validation
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