Comparative study on gastric absorption of albendazole and mebendazole in rats

Prieto, J. E.; Justel, Antonio León; Estal, J.L. del; Barrio, J.P.; Alvarez, Ana I.

doi:10.1016/0742-8413(91)90014-k

Cited by 11 publications

(6 citation statements)

References 19 publications

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“…As ABZSO has also anthelmintic properties, [33] the bioavailability characteristics of ABZ were assessed from the plasma concentrations of ABZSO obtained after administration of the two dosage forms. The kinetics of ABZ absorption in the GI tract follows a passive diffusion process [34] and is independent of the administered dose. Mean concentration-time profiles of ABZSO obtained after a single dose (10 mg/kg) of ABZ SMEDDS and the ABZ commercial suspension are reported in Figure 5.…”

Section: Oral Bioavailability Studymentioning

confidence: 99%

Development and oral bioavailability assessment of a supersaturated self-microemulsifying drug delivery system (SMEDDS) of albendazole

Mukherjee

Plakogiannis

2010

Journal of Pharmacy and Pharmacology

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Section: Oral Bioavailability Studymentioning

confidence: 99%

Development and oral bioavailability assessment of a supersaturated self-microemulsifying drug delivery system (SMEDDS) of albendazole

Mukherjee

Plakogiannis

2010

Journal of Pharmacy and Pharmacology

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“…Although a first consideration of the con tents of the figure la may suggest the exis tence of a saturable uptake mechanism, the results obtained in previous experiments [4,5] suggested that the gastrointestinal absorp tion of ABZ and MBZ follows a passive diffu sion process which was evident with isolated enterocytes down to concentrations of 100 pM. The nonlinear uptake at higher concen trations would be due to the precipitation of In contrast to the studies concerning the disappearance of xenobiotics from the intesti nal lumen, normally conducted using in vivo techniques, the use of isolated cell techniques reduce the number and facilitate handling of experimental animals.…”

Section: Resultsmentioning

confidence: 56%

“…intestinal perfusion techniques showed that the absorption kinetics of both drugs follows a diffusion-passive process [4,5]. It is known that a single layer of epithelial cells in the intestine is responsible for most of the intestinal functions: absorption and me tabolism of nutrients and xenobiotics.…”

Section: Introductionmentioning

confidence: 99%

Albendazole and Mebendazole Uptake by Isolated Enterocytes

Villaverde

Álvarez²,

Estal³

et al. 1992

Dev Pharmacol Ther

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Uptake of albendazole (ABZ) and mebendazole (MBZ) by isolated rat enterocytes was carried out. These drugs, widely used oral anthelmintics, exhibit a scarce water solubility which reduce its absorption by the oral tract. The present study was designed to assess the captation for ABZ and MBZ in different enterocyte populations isolated from upper to crypt villus. The concentration range used for the absorption experiments was within 10-500 μM for both drugs, using DMSO as solvent. The results obtained show the existence of a passive mechanism for the uptake of ABZ and MBZ at concentrations between 10 and 100 μM, with a maximum intake value around 20 μM/mg protein. No differences were found with respect to the cell populations analyzed. The drug uptake levels seem to be higher for MBZ than for ABZ prior to reaching the maximum plateau.

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“…Reduction of the carbonyl group is generally considered a deactivation pathway protecting organisms against the toxic effect of re-active aldehydes and ketones. Because reduced mebendazole lacks any anthelmintic activity [17,18], FLU reduction probably also represents deactivation. However, no exact information about the anthelmintic activity of reduced flubendazole is available.…”

Section: Introductionmentioning

confidence: 99%

Dicrocoeliosis of Old Mouflon Ewes - Effect on Biotransformation Enzymes and Metabolism of Anthelmintics In Vitro

Křížová¹,

Lamka²,

Szotáková³

et al. 2008

TOVSJ

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Parasitic infections can modify the host's ability to metabolize drugs by altering the biotransformation enzymes. Mouflon (Ovis musimon), the wild sheep, is very sensitive to parasitic diseases. In the present study, in vitro activities of thirteen hepatic biotransformation enzymes and the in vitro metabolism of albendazole and flubendazole were compared in old mouflon ewes, either non-infected or infected with lancet flukes (Dicrocoelium dendriticum). The most pronounced decline in 6 testosteron hydroxylase, glutathione-S-transferase and UDP-glucuronosyl transferase activities was observed in Dicrocoelium-infected animals. In addition, dicrocoeliosis caused a decrease in both albendazole and flubendazole phase I hepatic metabolism. However, the changes were very slight therefore any undesirable alterations in albendazole and flubendazole pharmacokinetics are not expected. Decreased activities of 6 testosterone hydroxylase, glutathione-S-transferase and UDP-glucuronosyl transferase can impair drug elimination from the infected animals. This should be taken into consideration in pharmacotherapy or pharmacoprophylaxis of mouflons and sheep.

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Comparative study on gastric absorption of albendazole and mebendazole in rats

Cited by 11 publications

References 19 publications

Development and oral bioavailability assessment of a supersaturated self-microemulsifying drug delivery system (SMEDDS) of albendazole

Development and oral bioavailability assessment of a supersaturated self-microemulsifying drug delivery system (SMEDDS) of albendazole

Albendazole and Mebendazole Uptake by Isolated Enterocytes

Dicrocoeliosis of Old Mouflon Ewes - Effect on Biotransformation Enzymes and Metabolism of Anthelmintics In Vitro

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