Pharmacol Res. 2003 Oct;48(4):389-95.
Influence of albendazole on the disposition kinetics and milk antimicrobial equivalent activity of enrofloxacin in lactating goats.

El-Sooud KA.

Pharmacology Department, Faculty of Veterinary Medicine, Cairo University, P.O. Box 12211, Giza, Egypt. kasoouotmail.com

The pharmacokinetics of single intravenous and intramuscular administrations and milk antimicrobial equivalent activity of enrofloxacin at a dose of 5 mg per kilogram body weight were studied in clinically healthy lactating goats which were either not treated or had received 7.5 mg per kilogram body weight of albendazole orally. The concentrations of enrofloxacin in serum and milk were determined using microbiological assay. Following intravenous injection, enrofloxacin antimicrobial equivalent activity versus time data in serum was described by a two-compartmental open model. Albendazole treatment significantly decreased the elimination half-life (t(1/2beta)) (P>or=0.05) and the mean residence time (MRT) (P>or=0.05), whereas, the rate of enrofloxacin return to central compartment from peripheral tissue (K(21)) was significantly increased (P>or=0.01). In contrast, the volumes of distribution V(d(area)) and V(d(SS)) were significantly decreased (P>or=0.01 and P>or=0.05, respectively) in albendazole-treated goats. After intramuscular injection, enrofloxacin was rapidly absorbed in control and albendazole-treated lactating goats with absorption half-lives (t(1/2ab)) 0.43 and 0.39 h, respectively. The mean peaks of serum concentration (C(max)) were 0.68 and 0.65 mcg ml(-1) attained at (t(max)) 1.08 and 1.12 h, before and after albendazole dosing, respectively. The elimination half-life (t(1/2el)) and (MRT) following intramuscular injections were also shorter in the albendazole-treated lactating goats. The systemic bioavailability of enrofloxacin was significantly decreased from 110.16 to 84.38% in albendazole-treated lactating goats. Concomitant administration of albendazole w




Drug Dev Ind Pharm. 2003 Aug;29(7):777-84.
Comparison of dissolution profiles for albendazole tablets using USP apparatus 2 and 4.

Hurtado y de la Pena M, Vargas Alvarado Y, Dominguez-Ramirez AM, Cortes Arroyo AR.

Departamento Sistemas Biologicos, Universidad Autonoma Metropolitana Unidad Xochimilco, Colonia Villa Quietud, Mexico D.F., Mexico. mhurtadueyatl.uam.mx

The in vitro dissolution of albendazole from three different commercially available products (200 mg tablets) was studied using U.S. Pharmacopeia (USP) Apparatus 2 and USP Apparatus 4 in order to compare the release performance of the drug in two essentially different dissolution systems. For both cases, 0.1 N HCl was used as dissolution medium. Only the reference product and one of the generic products studied met the 80% USP 24 specification for albendazole dissolved at 30 min, using USP Apparatus 2. Although the reference product reached 80% of albendazole dissolved at 30 min when Apparatus 4 was used, the generic products' dissolution performance was markedly reduced in this system. Though dissolution rate was slower using Apparatus 4, the total quantity of albendazole dissolved from the reference product, represented by area under the dissolution profile, was practically the same regardless of the system used. Dissolution kinetics of albendazole was adequately described by Weibull's function for all the products. The dissolution time (t(d)) derived from data fitting to this function showed significant differences among the products studied. Data analysis based on analysis of variance (ANOVA) showed nonequivalence among the dissolution profiles of generic products compared with the reference product either with the dissolution vessel system or the flow-through cell, as well as nonequivalence among the dissolution profiles using both apparatuses with the same product. Though differences in the dissolution profiles for generic products against the reference product in both systems were found, USP Apparatus 4 showed higher discri




Boll Chim Farm. 2003 May;142(4):180-6.
Preparation, physicochemical characterization and drug release studies of albendazole solid dispersions.

Mallick S, Sahoo A, Mitra SS.

Division of Pharmaceutics, Seemanta Institute of Pharmaceutical Sciences, Jharpokharia, Mayurbhanj, Orissa, India.

Albendazole (ALB) solid dispersions were prepared by codissolvation and solvent evaporation technique using water soluble carrier such as polyethylene glycol (PEG) and polyvinylpyrrolidone (PVP) to improve the aqueous solubility of the drug and thus enhancing its bioavailability. The physicochemical characteristics of these solid dispersions were performed by scanning electron microscopy (SEM), X-ray diffraction (XRD), fourier-transform infrared (FT-IR) spectroscopy and dissolution rate analyses. SEM was used to clarify the surface and shape characteristics of the different samples. All characteristic bands of albendazole are seen in the FT-IR spectra of solid dispersions. Basically no significant changes in the frequency and shape of albendazole were noticed which leads to the conclusion that no strong interaction between the drug and the polymer exists in the solid dispersion (SD) particles. The degree of crystallinity of ALB decreased and also differed with the SD of different polymers. Dissolution rate and percent dissolution efficiency were significantly increased in the solid dispersions in comparison with drug alone. The drug release kinetics was ascertained by using F-test statistics using kinetic models of zero order, first order, Higuchi and Hixson-Crowell. Albendazole formed solid dispersions with water soluble polymers like PVP and PEG and the dissolution rate of the drug in the SD system was faster when the ratio of polymer to drug was greater. First order model may be used for explaining the kinetics of drug release from all the SD formulations as suggested by F-test.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12918228&dopt=Abstract albendazole Albenza




J Med Assoc Thai. 2003 Jun;86 Suppl 2:S257-62.
Efficacy of albendazole against early and late stage of Trichinella spiralis infection in mice.

Siriyasatien P, Yingyourd P, Nuchprayoon S.

Department of Parasitology, Faculty of Medicine, Chulalongkorn University, Bangkok 10330, Thailand.

Efficacy of albendazole against early and late stage of Trichinella spiralis infection in mice was determined. To determine the efficacy of albendazole against the early stage (enteral phase) of trichinosis, mice experimentally infected with T. spiralis were treated with albendazole 20 mg/kg at 7 days post infection for 15 days. Larvae were recovered from the infected mice 7 days after the treatment. The reduction rate of the larvae was 100 per cent. Efficacy of albendazole against the late stage (parenteral phase) of infection was determined at 30 days post infection. Mice were treated with albendazole at 20 mg/kg for 30 days. Larvae were recovered from the infected mice 7 days after the treatment. The reduction rate of the larvae was 71 per cent compared to the control group. In conclusion, albendazole was more effective in the early stage of infection than the late stage, the reduction was 100 per cent and 71 per cent with respect to the control group respectively.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12929998&dopt=Abstract albendazole Albenza




J Am Vet Med Assoc. 2003 Aug 15;223(4):495-500.
Evaluation of prevalence and clinical implications of anthelmintic resistance in gastrointestinal nematodes in goats.

Mortensen LL, Williamson LH, Terrill TH, Kircher RA, Larsen M, Kaplan RM.

Danish Center for Experimental Parasitology, Department of Veterinary Microbiology, Section for Parasitology, Royal Veterinary and Agricultural University, DK-1870 Frederiksberg C, Denmark.

OBJECTIVE: To determine prevalence of resistance to all anthelmintics that are commonly used to treat gastrointestinal nematodes (GINs) in goats. DESIGN: Prospective study. ANIMALS: 777 goats. PROCEDURE: On each farm, goats were assigned to 1 of 5 treatment groups: untreated controls, albendazole (20 mg/kg [9.0 mg/lb], p.o., once), ivermectin (0.4 mg/kg [0.18 mg/lb], p.o., once), levamisole (12 mg/kg [5.4 mg/lb], p.o., once), or moxidectin (0.4 mg/kg, p.o., once), except on 3 farms where albendazole was omitted. Fecal samples were collected 2 weeks after treatment for determination of fecal egg counts (FECs), and percentage reductions were calculated by comparing data from anthelmintic-treated and control groups. Nematode populations were categorized as susceptible, suspected resistant, or resistant by use of guidelines published by the World Association for the Advancement of Veterinary Parasitology. RESULTS: Resistance to albendazole was found on 14 of 15 farms, and resistance to ivermectin, levamisole, and moxidectin was found on 17, 6, and 1 of 18 farms, respectively. Suspected resistance to levamisole and moxidectin was found on 4 and 3 farms, respectively. Resistance to multiple anthelmintics (albendazole and ivermectin) was found on 14 of 15 farms and to albendazole, ivermectin, and levamisole on 5 of 15 farms. Mean overall FEC reduction percentages for albendazole, ivermectin, levamisole, and moxidectin were 67, 54, 94, and 99%, respectively. CONCLUSIONS AND CLINICAL RELEVANCE: Anthelmintic resistance in GINs of goats is highly prevalent in the southern United States.




Res Vet Sci. 2003 Dec;75(3):231-9.
The effects of albendazole and its metabolites on hepatic cytochromes P450 activities in mouflon and rat.

Baliharova V, Velik J, Lamka J, Balarinova R, Skalova L.

Department of Biochemical Sciences, Faculty of Pharmacy, Charles University, Heyrovskeho 1203, CZ-50005 Hradec Kralove, Czech Republic. 95bav336af.cuni.cz

Albendazole (ABZ) is a benzimidazole anthelmintic widely used in veterinary medicine. The effects of ABZ on cytochromes P450 were investigated in primary cultures of mouflon (Ovis musimon) and rat (Rattus norvegicus) hepatocytes. Besides ABZ, its two main metabolites (albendazole-sulphoxide, ABZSO and albendazole-sulphone, ABZSOO) were tested to clarify which compound is responsible for the induction potency of this benzimidazole drug. After 48 h incubation of hepatocytes with benzimidazoles (0.2-25 microM), ethoxyresorufin O-deethylation (EROD) and benzoxyresorufin O-dearylation (BROD) were measured and the P4501A and 3A protein levels were determined by Western blotting. All benzimidazoles provoked a significant increase of EROD and BROD activities in rat hepatocytes. ABZSO and ABZSOO seemed to be responsible for the induction effect of ABZ on P450s in rat. In mouflon, no pharmacologically significant induction of EROD and BROD activities by benzimidazoles tested was observed. From this point of view, anthelmintic therapy of mouflons with ABZ seems to be safe.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=13129672&dopt=Abstract albendazole Albenza

163.com

AIM: To prepare the target drug delivery systems(TDDS), albendazole polybutycyanocrylate nanoparticles (ABZ-PBCA-NP), its pharmaceutical characters and tissue distributions were simultaneously investigated. METHODS: Albendazole nanoparticles were prepared with the emulsification-polymerization method and the drug-load mechanism of polybutycyanocrylate nanoparticles was studied with the equal-tempaerature adsorption principle. The dialyse dynamic of albendazole from ABZ-PBCA-NP was investigated in four formulations in vitro. The tissue distribution of albendazole in different drug vehicles was studied with isotope labelling experiment. RESULTS: ABZ-PBCA-NP and ABZ-PVP-PBCA-NP fit to the Higuchi and bi-exponent function in vitro respectively. The drug loaded in nanoparticles was abide by the Langmuir adsorption equation. Targeting index of albendazole in liver and spleen in mice are 11.4 and 3.9 after ig 3H-ABZ-PBCA-NP. The bioavailability of albendazole nanoparticle and suspension are 76.0% and 36.9% respectively. CONCLUSION: The absorptive capability of drug was enhance when 4% PVP was added into the nanoparticle, and its release time was lengthen. At the same time, the nanoparticles vehicles increase the albendazole bioavailability.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=14513810&dopt=Abstract albendazole Albenza