Intestinal Absorption, Pharmacokinetics and Tissue Distribution of Gossypol Nanosuspensions

2014 ◽  
Vol 1015 ◽  
pp. 708-712
Author(s):  
Si Tao Yang ◽  
Xue Ying ◽  
Hui Tang ◽  
Jian Chen Wang ◽  
Bing Bing Wu
Keyword(s):  
Plasma Concentration ◽  
Tissue Distribution ◽  
Intestinal Absorption ◽  
Reticuloendothelial System ◽  
Polyphenolic Compounds ◽  
Water Soluble ◽  
High Uptake ◽  
Distribution Study ◽  
Poorly Water Soluble ◽  
Tissue Distribution Study

Gossypol (GP) is a kind of poorly water-soluble polyphenolic compounds. In this study, gossypol nanosuspensions (GP-NS) were prepared. The ability of intestinal absorption was evaluated. The result indicated that GP-NS could be absorbed in whole intestinal sections and permeated across the intestine, the process of gossypol nanosuspensions were not affected by P-gp efflux.The pharmacokinetics and tissue distribution of GP-NS after intravenous administration to mice was studied. GP-NS resulted in a higher plasma concentration and lower clearance.The tissue distribution study indicated that GP-NS showed a high uptake in reticuloendothelial system organs. In conclusion, the nanosuspensions system is a promising approach for gossypol.

Pharmacokinetics and Tissue Distribution Study of Ferruginol in Wistar Rat by High-performance Liquid Chromatography

2018 ◽  
Vol 15 (1) ◽  
pp. 67-73 ◽  
Author(s):  
Guiyun Cao ◽  
Suqiao Han ◽  
Keke Li ◽  
Li Shen ◽  
Xiaohong Wang ◽  
...  
Keyword(s):  
Tissue Distribution ◽  
Mobile Phase ◽  
High Performance ◽  
Wistar Rat ◽  
Freezing And Thawing ◽  
Promising Candidate ◽  
Distribution Study ◽  
Substance Loss ◽  
Tissue Distribution Study ◽  
The Brain

Background: Ferruginol (FRGN) exhibits a broad range of pharmacological properties which make it a promising candidate for chemoprevention. However, little is known about its absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties. Methods: A rapid, sensitive and specific HPLC-DAD method was established to quantify FRGN in the plasma and tissues of Wistar rats. After extraction of FRGN with ethyl acetate (EtOAc), chromatographic separation was performed on a YMC ODS C18 column (250 × 4.6 mm I.D., 5 µm) with a mobile phase consisting of methanol-water (92:8, v/v) at a flow rate of 0.9 mL/min. Detection was conducted with a wavelength of 273 nm at 25 °C. Results: The calibration curves for FRGN were linear in the concentration range of 0.5-20 µg/mL for plasma, 0.5-10 µg/mL for heart, liver, spleen, lung, kidney, stomach, intestine, brain and muscle. After three cycles of freezing and thawing, the concentration variations were within ± 7% of nominal concentrations, indicating no significant substance loss during repeated thawing and freezing. The assay was applied to pharmacokinetic and tissue distribution study in rats. Results suggested that lung, heart, liver, spleen and kidney were the major distribution tissues of FRGN in rats, and FRGN could permeate the blood-brain barrier to distribute in the brain of rats. Conclusion: The information provided by this research is very useful for gaining knowledge of the pharmacokinetic process and tissue distribution of FRGN.

scholarly journals Quantitative method for whole body autoradiography and application to tissue distribution study of FO-1561 in rats.

1988 ◽  
Vol 3 (6) ◽  
pp. 747-760
Author(s):  
Eiichi NAKAJIMA ◽  
Yoshie YASUKAWA ◽  
Hayao SHINOZAKI ◽  
Yukio MATSUBARA ◽  
Shigeto FUJISHITA ◽  
...  
Keyword(s):  
Tissue Distribution ◽  
Quantitative Method ◽  
Whole Body ◽  
Distribution Study ◽  
Whole Body Autoradiography ◽  
Tissue Distribution Study

Studies of the Toxicological Potential of Capsinoids, XI: Pharmacokinetic and Tissue Distribution Study of 14C-Dihydrocapsiate and Metabolites in Rats

2010 ◽  
Vol 29 (2_suppl) ◽  
pp. 3S-14S ◽  
Author(s):  
Bruce K. Bernard ◽  
Kazuyuki Ubukata ◽  
Ryuichi Mihara ◽  
Yoshiaki Sato ◽  
Hiroyuki Nemoto
Keyword(s):  
Body Weight ◽  
Plasma Concentration ◽  
Vanillic Acid ◽  
Male Rats ◽  
Vanillyl Alcohol ◽  
Tissue Concentrations ◽  
Distribution Study ◽  
Maximal Plasma ◽  
Tissue Distribution Study ◽  
Kidney Liver

Pharmacokinetics of a single gavage dose of 14C-labeled dihydrocapsiate (10 mg/kg) were investigated in male rats. Maximal plasma concentration was achieved in 40 minutes and exhibited an apparent half-life of 2.4 hours. Excretion of radioactivity in the urine, feces, and expired air was 78.2%, 19.4%, and 0.5% of the dose, respectively. Highest tissue concentrations were achieved in the kidney, liver, and blood; the data indicate that radioactivity accumulation following daily exposure at a dose of 10 mg/kg body weight is unlikely. Radioactivity in the plasma was associated with metabolites and their conjugates, probably vanillyl alcohol, vanillic acid, glucuronide of vanillyl alcohol, sulphate of vanillyl alcohol, and sulphate of vanillic acid. These results suggest dihydrocapsiate is metabolized by hydrolysis in the gut, or esterase or other enzymes in the blood, and the metabolites were rapidly absorbed and converted to their conjugates in the liver and eliminated by the kidneys into the urine.

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