J Chromatogr A. 2000 Feb 18;870(1-2):121-34.
Determination of albendazole and its main metabolites in ovine plasma by liquid chromatography with dialysis as an integrated sample preparation technique.

Chiap P, Evrard B, Bimazubute MA, de Tullio P, Hubert P, Delattre L, Crommen J.

Department of Analytical Pharmaceutical Chemistry, Institute of Pharmacy, University of Liege, Belgium.

Albendazole is a benzimidazole derivative with a broad-spectrum activity against human and animal helminth parasites. In order to determine the main pharmacokinetic parameters in sheep after oral and intravenous administration of a new formulation of albendazole (an aqueous solution), a fully automated method was developed for the determination of this drug and its main metabolites, albendazole sulfoxide (active metabolite) and sulfone in ovine plasma. This method involves dialysis as purification step, followed by enrichment of the dialysate on a precolumn and liquid chromatography (LC). All sample handling operations were executed automatically by means of an ASTED XL system. After conditioning of the trace enrichment column (TEC) packed with octadecyl silica with pH 6.0 phosphate buffer containing sodium azide, the plasma sample, in which a protein releasing reagent (1 M HCl) containing Triton X-100 was automatically added, was loaded in the donor channel and dialysed on a cellulose acetate membrane in the static-pulsed mode. The dialysis liquid consisted of pH 2.5 phosphate buffer. By rotation of a switching valve, the analytes were eluted from the TEC in the back-flush mode by the LC mobile phase and transferred to the analytical column, packed with octyl silica. The chromatographic separation was performed at 35 degrees C and the analytes were monitored photometrically at 295 nm. Due to the differences in hydrophobic character between albendazole and its metabolites, a gradient elution was applied. The mobile phase consisted of a mixture of acetonitrile and pH 6.0 phosphate buffer. The proportion of organic modi




Electrophoresis. 2000 Mar;21(4):729-36.
Therapeutic drug monitoring of albendazole: determination of albendazole, albendazole sulfoxide, and albendazole sulfone in human plasma using nonaqueous capillary electrophoresis.

Prochazkova A, Chouki M, Theurillat R, Thormann W.

Department of Clinical Pharmacology, University of Bern, Switzerland.

A nonaqueous capillary electrophoretic method (NACE) for the fast determination of plasma levels of albendazole (ABZ), albendazole sulfoxide (ABZSO), and albendazole sulfone (ABZSO2) is described. The assay is based upon liquid/liquid extraction of these compounds using dichloromethane at pH 10.2 (recovery between 63 and 98%), followed by a NACE separation performed within 8 min employing a 0.036 M borate buffer (apparent pH 9.9) in a mixture of methanol and N-methylformamide (1:3) and on-column absorbance detection at 280 nm. Using 0.5 mL of plasma and extract reconstitution in 200 microL N-methylformamide, drug levels between 1.0-10 microM were found to provide linear calibration graphs. Intraday and interday imprecisions evaluated from peak area ratios (n = 5) were <10% and <12%, respectively. Corresponding imprecisions of detection times (n = 5) were <1% and <6%, respectively. The limit of detection (LOD) for ABZ, ABZSO and ABZSO2 was 8 x 10(-7) M. The reliability of the method developed was verified via analysis of 45 plasma samples obtained from patients treated with ABZ. Good agreement was obtained between the levels of ABZSO and those determined by routine HPLC. ABZ was found to be undetectable in all patient samples, whereas the levels of ABZSO2 were below or close to LOD.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10733213&dopt=Abstract albendazole Albenza




Southeast Asian J Trop Med Public Health. 1999 Jun;30(2):379-81.
Movability of advanced third-stage larva of Gnathostoma spinigerum exposed to albendazole sulphoxide in vitro.

Sukontason K, Klaolaor P, Sukontason K, Morakote N, Muangyimpong Y, Chaithong U.

Department of Parasitology, Faculty of Medicine, Chiang Mai University, Thailand. ksukontd01.med.cmu.ac.th

Movability of advanced third-stage larvae of Gnathostoma spinigerum exposed to albendazole sulphoxide (AlbSO), the active metabolite of albendazole, was determined in vitro. Larvae in control groups moved actively with the whole body for all 21 days of the study period. In larvae treated with AlbSO 1 microg/ml, the movement was significantly reduced after 11 days exposed to the drug and to be only a part of body on the 15th-21st days. In larvae treated with AlbSO 2 microg/ml, the movement was initiated in decreasing after 9th days and to be only a part of body on the 12th-17th days. Finally, worms were immobile but not dead on the 20th-21st days. Although there was no larvae died at 21st days exposed to AlbSO in both concentrations; but all worms were sluggish and may die later. These lethargic worms may not be able to migrate in patients and leading to cure. Albendazole may not be benefit for acute symptom clearance; however, it can prevent the recurrent migratory swelling after the treatment of 21 day-course.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10774713&dopt=Abstract albendazole Albenza




J Med Assoc Thai. 2000 Apr;83(4):426-32.
Scanning electron microscopic observations on advanced third-stage larva of Gnathostoma spinigerum after in vitro exposure to albendazole sulphoxide.

Sukontason K, Klaolaor P, Sukontason K, Kuntalue B, Vanittanakom P, Chaithong U.

Department of Parasitology, Faculty of Medicine, Chiang Mai University, Thailand.

Gnathostomiasis is the parasitic disease caused by the migration of an advanced third-stage larva of Gnathostoma spinigerum. To date, albendazole is claimed to be the effective drug in preventing the reoccurrence of migratory swelling in patients. After being exposed to 1 and 2 micrograms/ml albendazole sulphoxide (AlbSO) in vitro, the parasites moved deteriorately, however, no dead larva was found even exposed to these concentrations for 21 consecutive days. The topographical alterations after 21 days of albendazole sulphoxide exposure are described using a scanning electron microscope. The marked changes in surface morphology were observed in both neck and body regions. The tegumental surface on the neck region was swollen and covered with fuzzy materials, whereas, the spines on the posterior region of the body were dislodged. These changes would probably lead to reduction of intermittent cutaneous migratory swelling in human gnathostomiasis patients.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10808703&dopt=Abstract albendazole Albenza




Eur J Clin Pharmacol. 2002 Sep;58(6):403-8. Epub 2002 Aug 06.
Effect of gender in the disposition of albendazole metabolites in humans.

Mirfazaelian A, Dadashzadeh S, Rouini MR.

Biopharmaceutics Lab, Division of Pharmacokinetics, Department of Pharmaceutics, Faculty of Pharmacy, Tehran University of Medical Sciences, P.O.Box 14155/6451, Tehran, Iran.

The pharmacokinetics of albendazole in different single oral doses (400 mg, 800 mg & 1200 mg) was studied and compared in healthy male and female human volunteers using a double-blind design. The serum levels of albendazole main metabolites (albendazole sulphoxide and albendazole sulphone) were analysed using a modified high-pressure liquid chromatography method. For both metabolites, there was no significant difference in the biological half-life ( t(1/2)), time to reach peak concentration (t(max)) and mean residence time (MRT) between men and women, whereas apparent oral clearance (Cl(p)/F) and apparent distribution volume (V(d)/F) were less and serum peak concentration (C(max)), area under the serum concentration-time curve (AUC) and area under the first moment curve (AUMC) were more in women than in men. These observations indicate sex dimorphism in pharmacokinetics of albendazole (observed for albendazole sulphoxide and albendazole sulphone) which were explained on the basis of a change in fraction of the main drug turned to metabolite as a result of more extensive first-pass metabolism of the main drug in the liver of adult female subjects.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12242599&dopt=Abstract albendazole Albenza




Popul Sci. 1991 Jan;10:89-99.
A new method of management of hypertensive pregnant patients and its effect on foeto maternal health.

El-sadek S, Kandil O, Badraoui MH.

PIP: Mass treatment of schoolchildren with anthelmintics has been recommended to improve the growth and educational performance of children infected with intestinal worms. The present study evaluated whether symptomless trichuriasis is associated with growth impairment and, thus, whether a multiple-dose regimen of drugs can be justified. 622 children 2-10 years of age from Coatzacoalcos, Mexico, were randomly assigned to one of three treatment regimens: 3 days of 400 mg/day of albendazole (high efficacy), 1 dose of 400 mg of albendazole (moderate efficacy), and 1 dose of 11 mg/kg of pyrantel embonate (low efficacy). After three rounds of treatment over a 12-month period, the geometric mean level of trichuriasis infection was reduced by 99%, 87%, and 67%, respectively. Among the 127 children with heavy but asymptomatic pretreatment infections, 1200 mg of albendazole was significantly superior to pyrantel in terms of an increase in arm circumference. Among children with low pretreatment levels of infection, the growth estimates were in the opposite direction. Changes in weight, arm circumference, and thickness of triceps skinfold were significantly less over the 12-month period in children receiving 1200 mg of albendazole compared with those in the pyrantel group. These findings suggest that the estimated one-third of children in the community who are not infected may have reduced growth if treated repeatedly with albendazole.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12284663&dopt=Abstract albendazole Albenza




J Med Assoc Thai. 2000 Sep;83(9):1095-100.
Successful eradication of Ascaris lumbricoides and hookworm infection after three repeated doses of albendazole.

Sukontason K, Sukontason K, Piangjai S, Na-Bangchang K, Karbwang J.

Department of Parasitology, Chiang Mai University, Thailand.

Three repeated orally doses of albendazole 400 mg in 6 weekly intervals were evaluated in Thai hill-tribe students who had at least one kind of soil-transmitted helminths (i.e. Ascaris lumbricoides, hookworm and Trichuris trichiura). Stool examination and parasite egg count were performed using Beaver's standard direct smear method and Kato-Katz's cellophane thick smear method prior to treatment and then 1 month after the first, second and third dose of drug administrations. A single dose of albendazole was very effective against A. lumbricoides and hookworm infections, with cure rates of 98.68 per cent and 92.16 per cent, respectively. The second and third dosages eradicated A. lumbricoides and hookworm infections, respectively. Conversely, the first to third cure rates for T. trichiura infection were relatively low, being 37.76-58.16 per cent. Three repeated doses of albendazole proved to be beneficial in eradication of A. lumbricoides and hookworm infections, and decreased the prevalence of T. trichiura infected cases. For eradication of T. trichiura infection, further regimen and period of drug administration is required.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=11075978&dopt=Abstract albendazole Albenza