Absolute bioavailability, dose proportionality, and tissue distribution of rotundic acid in rats based on validated LC-QqQ-MS/MS method

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

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

Clinical Neuropharmacology ◽

10.1097/00002826-199202001-00835 ◽

1992 ◽

Vol 15 ◽

pp. 430B ◽

Cited By ~ 1

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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Absolute bioavailability, tissue distribution, and excretion of 2,4,5-trimethoxybenzaldehyde in rats

Journal of Functional Foods ◽

10.1016/j.jff.2017.05.035 ◽

2017 ◽

Vol 35 ◽

pp. 90-96 ◽

Cited By ~ 1

Author(s):

Yi-Kai Wu ◽

Chin-Chu Chen ◽

Ting-Wei Lin ◽

Pei-Ching Tsai ◽

Chia-Feng Kuo

Keyword(s):

Tissue Distribution ◽

Absolute Bioavailability

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HPLC-MS/MS-Mediated Analysis of the Pharmacokinetics, Bioavailability, and Tissue Distribution of Schisandrol B in Rats

International Journal of Analytical Chemistry ◽

10.1155/2021/8862291 ◽

2021 ◽

Vol 2021 ◽

pp. 1-12 ◽

Cited By ~ 1

Author(s):

Dahu Liang ◽

Zijing Wu ◽

Yanhao Liu ◽

Chao Li ◽

Xianghong Li ◽

...

Keyword(s):

Tissue Distribution ◽

Oral Bioavailability ◽

Internal Standard ◽

Rat Plasma ◽

Absolute Bioavailability ◽

Sprague Dawley ◽

Linear Calibration ◽

Tissue Homogenates ◽

Distribution Studies

Schisandrol B, a lignan isolated from dried Schisandra chinensis fruits, has been shown to exhibit hepatoprotective, cardioprotective, renoprotective, and memory-enhancing properties. This study sought to design a sensitive and efficient HPLC-MS/MS approach to measuring Schisandrol B levels in rat plasma and tissues in order to assess the pharmacokinetics, oral bioavailability, and tissue distributions of this compound in vivo. For this analysis, bifendate was chosen as an internal standard (IS). A liquid-liquid extraction (LLE) approach was employed for the preparation of samples that were subsequently separated with an Agilent ZORBAX Eclipse XDB-C18 (4.6 × 150 mm, 5 μm) column with an isocratic mobile phase consisting of methanol and water containing 5 mM ammonium acetate and 0.1% formic acid (90 : 10, v/v). A linear calibration curve was obtained over the 5–2000 ng/mL and 1–1000 ng/mL ranges for plasma samples and tissue homogenates, respectively. This established method was then successfully applied to investigate the pharmacokinetics, oral bioavailability, and tissue distributions of Schisandrol B in Sprague-Dawley (SD) rats that were intravenously administered 2 mg/kg of Schisandrol B monomer, intragastrically administered Schisandrol B monomer (10 mg/kg), or intragastrically administered 6 mL/kg SCE (equivalent to 15 mg/kg Schisandrol B monomer). The oral absolute bioavailability of Schisandrol B following intragastric Schisandrol B monomer and SCE administration was approximately 18.73% and 68.12%, respectively. Tissue distribution studies revealed that Schisandrol B was distributed throughout several tested tissues, with particular accumulation in the liver and kidneys. Our data represent a valuable foundation for future studies of the pharmacologic and biological characteristics of Schisandrol B.

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Absolute Bioavailability and Dose Proportionality of BMS-181885, an Antimigraine Agent, Following the Administration of Single Intranasal Doses to Cynomolgus Monkeys

Journal of Pharmaceutical Sciences ◽

10.1021/js9802042 ◽

1998 ◽

Vol 87 (9) ◽

pp. 1170-1172 ◽

Cited By ~ 4

Author(s):

Nuggehally R. Srinivas ◽

Wen Chyi Shyu ◽

Chi Wen Soong ◽

Douglas Greene

Keyword(s):

Dose Proportionality ◽

Absolute Bioavailability ◽

Cynomolgus Monkeys

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Absolute Bioavailability, Tissue Distribution, and Excretion of Erinacine S in Hericium erinaceus Mycelia

Molecules ◽

10.3390/molecules24081624 ◽

2019 ◽

Vol 24 (8) ◽

pp. 1624 ◽

Cited By ~ 1

Author(s):

Jun-Hao Hu ◽

I-Chen Li ◽

Ting-Wei Lin ◽

Wan-Ping Chen ◽

Li-Ya Lee ◽

...

Keyword(s):

Body Weight ◽

Oral Administration ◽

Tissue Distribution ◽

Neurological Diseases ◽

Amyloid Plaque ◽

Oral Dosage ◽

Absolute Bioavailability ◽

Sprague Dawley ◽

Hericium Erinaceus ◽

The Absolute

Erinacine S, so far known to have been produced only in Hericium erinaceus mycelia, has just recently been discovered and is able to reduce amyloid plaque growth and improve neurogenesis in aged brain of rats. However, few investigations have been conducted on the absorption, distribution, and excretion study of Erinacine S. This study aimed to investigate the absolute bioavailability, tissue distribution, and excretion of Erinacine S in H. Erinaceus mycelia in eight-week old Sprague-Dawley rats. After oral administration and intravenous administration of 2.395 g/kg body weight of the H. erinaceus mycelia extract (equivalent to 50 mg/kg body weight Erinacine S) and 5 mg/kg of Erinacine S, respectively, the absolute bioavailability was estimated as 15.13%. In addition, Erinacine S was extensively distributed in organs such as brain, heart, lung, liver, kidney, stomach, small intestine, and large intestine. The maximum concentration of Erinacine S was observed in the stomach, 2 h after the oral administration of H. erinaceus mycelia extract, whereas the maximum amount of Erinacine S found in other tissues were seen after 8 h. Total amount of unconverted Erinacine S eliminated in feces and urine in 24 h was 0.1% of the oral dosage administrated. This study is the first to show that Erinacine S can penetrate the blood–brain barrier of rats and thus support the development of H. erinaceus mycelia, for the treatment of neurological diseases.

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Preclinical Bioavailability, Tissue Distribution, and Protein Binding Studies of Erinacine A, a Bioactive Compound from Hericium erinaceus Mycelia Using Validated LC-MS/MS Method

Molecules ◽

10.3390/molecules26154510 ◽

2021 ◽

Vol 26 (15) ◽

pp. 4510

Author(s):

Pei-Ching Tsai ◽

Yi-Kai Wu ◽

Jun-Hao Hu ◽

I-Chen Li ◽

Ting-Wei Lin ◽

...

Keyword(s):

Protein Binding ◽

Tissue Distribution ◽

Bioactive Compound ◽

Passive Diffusion ◽

Absolute Bioavailability ◽

Sprague Dawley ◽

Binding Studies ◽

Hericium Erinaceus ◽

Major Route ◽

Erinacine A

Erinacine A, derived from the mycelia of Hericium erinaceus, has attracted much attention due to its neuroprotective properties. However, very few studies have been conducted on the bioavailability, tissue distribution, and protein binding of erinacine A. This study aimed to investigate the bioavailability, tissue distribution, and protein binding of erinacine A in Sprague-Dawley rats. After oral administration (po) and intravenous administration (iv) of 2.381 g/kg BW of the H. erinaceus mycelia extract (equivalent to 50 mg/kg BW of erinacine A) and 5 mg/kg BW of erinacine A, respectively, the absolute bioavailability of erinacine A was estimated as 24.39%. Erinacine A was detected in brain at 1 h after oral dosing and reached the peak at 8 h. Protein binding assay showed unbound erinacine A fractions in brain to blood ratio is close to unity, supporting passive diffusion as the dominating transport. Feces was the major route for the elimination of erinacine A. This study is the first to show that erinacine A can penetrate the blood-brain barrier of rats by the means of passive diffusion and thus support the development of H. erinaceus mycelia for the improvement of neurohealth.

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