Tissue Distribution

Publication Title: 
Annual Review of Nutrition
Emken, E. A.
Publication Title: 
Mechanisms of Ageing and Development

Total boron concentrations in Drosophila changed during development and ageing. The highest concentration of boron was found during the egg stage followed by a decline during the larval stages. Newly emerged flies contained 35.5 ppm boron. During the adult stage the boron concentration increased by 52% by 9 weeks of age. Adding excess dietary boron during the adult stage decreased the median life span by 69% at 0.01 M sodium borate and by 21% at 0.001 M sodium borate. Lower concentrations gave small but significant increases in life span.

Massie, H. R.
Whitney, S. J.
Aiello, V. R.
Sternick, S. M.
Publication Title: 
The Journal of Pharmacy and Pharmacology

The displacement of midazolam, a new water-soluble, short acting benzodiazepine, from its plasma binding sites by sodium valproate, has been studied in man. An increase of its free fraction (ranging from 2.71 to 5.35%) in plasma from epileptic patients receiving sodium valproate was observed. A similar situation was created in rabbits by pretreatment with sodium valproate (600 mg kg-1 day-1) and posterior hypnosis with midazolam.

Calvo, R.
Suárez, E.
Rodríguez-Sasiain, J. M.
Aguilera, L.
Publication Title: 
Yakugaku Zasshi: Journal of the Pharmaceutical Society of Japan

Spinosin is the major effective single constituent in the traditional Chinese herb Semen Ziziphi Spinosae, which is used for sedation and hypnosis. For the further use of spinosin in treating insomnia, the pharmacokinetics and tissue distribution of spinosin after intravenous administration to rats was investigated. An HPLC method with an ODS column (250 mm x 4.6 mm, i.d.) and a mobile phase of acetonitrile-water-acetic acid (23:77:1) was used for the determination of spinosin in the plasma and tissues of rats. Vanillin was used as an internal standard, and spinosin was detected at 334 nm.

Li, Yu-Juan
Dai, Yue-Han
Yu, Ye-Ling
Li, Yan
Deng, Yu-Lin
Publication Title: 
Zhongguo Yao Li Xue Bao = Acta Pharmacologica Sinica

TLC scanning technique was found to have good specificity for studying the absorption and distribution of artemether in rats. Plasma or tissue homogenates 0.2-1.0 ml were placed in glass extraction tubes and water was added to make 1.0 ml. Each sample was extracted 3 times with 4 ml mixed organic solvent (n-pentane: dichloromethane = 1:1, vol:vol). The organic layers of 3 extractions were combined and evaporated. The residue was dissolved in 100-300 microliters of ethylacetate and spotted on TLC plates.

Jiang, J. R.
Zou, C. D.
Shu, H. L.
Zeng, Y. L.
Publication Title: 
Drug Metabolism and Disposition: The Biological Fate of Chemicals

beta-Artemether (AM), the O-methyl ether prodrug of dihydroartemisinin (DHA), is an endoperoxide antimalarial. The biliary metabolites of AM in adult male Wistar rats were characterized with particular reference to potential antimalarial compounds and stable derivatives of free radical intermediates. [13-(14)C]-AM (35 micromol kg(-1), i.v.) was administered to anesthetized rats. Within 0 to 3 h, 38.6 +/- 4.8% (mean +/- S.D., n = 6) of the radiolabel was recovered in bile; the 0- to 5-h recovery was 42.3 +/- 4.3%.

Maggs, J. L.
Bishop, L. P.
Edwards, G.
O'Neill, P. M.
Ward, S. A.
Winstanley, P. A.
Park, B. K.
Publication Title: 
The American Journal of Tropical Medicine and Hygiene

The neurotoxicity of beta-arteether (AE) is related to drug accumulation in blood due to slow and prolonged absorption from the intramuscular injection sites. In this efficacy and toxicity study of AE, the traditional sesame oil vehicle was replaced with cremophore to decrease the accumulation and toxicity of AE. Dihydroartemisinin (DQHS), a more toxic and active metabolite of AE, was also analyzed.

Li, Q. G.
Mog, S. R.
Si, Y. Z.
Kyle, D. E.
Gettayacamin, M.
Milhous, W. K.
Publication Title: 
Antimicrobial Agents and Chemotherapy

A detailed pharmacokinetic analysis was performed with 47 children from Papua New Guinea with uncomplicated falciparum or vivax malaria treated with artesunate (ARTS) suppositories (Rectocaps) given in two doses of approximately 13 mg/kg of body weight 12 h apart. Following an intensive sampling protocol, samples were assayed for ARTS and its primary active metabolite, dihydroartemisinin (DHA), by liquid chromatography-mass spectrometry. A population pharmacokinetic model was developed to describe the data.

Karunajeewa, Harin A.
Ilett, Kenneth F.
Dufall, Kitiya
Kemiki, Adedayo
Bockarie, Moses
Alpers, Michael P.
Barrett, P. Hugh
Vicini, Paolo
Davis, Timothy M. E.
Publication Title: 

The discovery of artemisinin more than 30 years ago provided a completely new antimalarial structural prototype; that is, a molecule with a pharmacophoric peroxide bond in a unique 1,2,4-trioxane heterocycle. Available evidence suggests that artemisinin and related peroxidic antimalarial drugs exert their parasiticidal activity subsequent to reductive activation by haem, released as a result of haemoglobin digestion by the malaria-causing parasite.

Vennerstrom, Jonathan L.
Arbe-Barnes, Sarah
Brun, Reto
Charman, Susan A.
Chiu, Francis C. K.
Chollet, Jacques
Dong, Yuxiang
Dorn, Arnulf
Hunziker, Daniel
Matile, Hugues
McIntosh, Kylie
Padmanilayam, Maniyan
Santo Tomas, Josefina
Scheurer, Christian
Scorneaux, Bernard
Tang, Yuanqing
Urwyler, Heinrich
Wittlin, Sergio
Charman, William N.
Publication Title: 
The American Journal of Tropical Medicine and Hygiene

The present study reports the tissue distribution, pharmacokinetics, mass balance, and elimination of [(14)C] artesunate (AS) following single intravenous administration in rats. Protein binding was performed with rat and human plasma. Radioactivity and drug levels in blood, plasma, tissues, urine, and feces up to 192 hours were collected and measured. The mean terminal half-life of plasma (76 h) and blood (105 h) radioactivity was prolonged compared with that of unchanged AS (0.43 h) and dihydroartemisinin (0.75 h), an active metabolite of AS.

Li, Qigui
Xie, Lisa H.
Haeberle, Adam
Zhang, Jing
Weina, Peter


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