A novel formulation of albendazole solution: oral bioavailability and efficacy evaluation

Lopez, Mario; Pena-Fernandez, A.; Bolás, F; Torrado, Susana; Cadórniga, R

doi:10.1016/s0378-5173(97)00204-4

Cited by 41 publications

(23 citation statements)

References 16 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Moreover, increased systemic bioavailability of albendazole was reported when the drug co-administered with a fatty meal [11], fruit juice [12], cosolvent [13], or with surfactants [14].…”

Section: Albendazole (Abz) Methyl[ 5-(propylthio)-1-h-benzimidazol-2mentioning

confidence: 99%

Improvement of Albendazole Dissolution by Preparing Microparticles Using Spray-Drying Technique

Alanazi

2007

Sci Pharm

View full text Add to dashboard Cite

The aim of this work was to improve the dissolution rate of albendazole (ABZ) by preparing its microparticles with certain hydrophilic polymers such as hydroxypropyl methylcellulose (HPMC), polyvinyl alcohol (PVA), and polyvinyl pyrrolidone (PVP) using spray drying technique. Microparticles of ABZ with these polymers were prepared in different ratios of 1:1, 1:2, and 1:4 by spray drying technique. Morphology and characterization of the prepared ABZ microparticles was studied and photographed using a biological microscope and examined by scanning electron microscope. Smooth surface and spherical microparticles of ABZ were detected by these methods which indicating the coating of drug crystals by the studied polymers. Physicochemical properties of drug alone and its spray dried microparticles were investigated using differential scanning calorimetry (DSC) and powder X-ray diffractometry (PXRD). DSC and PXRD analysis showed that ABZ transformed from the crystalline state to amorphous state by spray drying with these polymers as confirmed by disappearance of its melting peak and characteristic crystalline peaks. Dissolution rate of ABZ from the prepared microparticles was determined and compared to its corresponding physical

show abstract

“…Moreover, increased systemic bioavailability of albendazole was reported when the drug co-administered with a fatty meal [11], fruit juice [12], cosolvent [13], or with surfactants [14].…”

Section: Albendazole (Abz) Methyl[ 5-(propylthio)-1-h-benzimidazol-2mentioning

confidence: 99%

Improvement of Albendazole Dissolution by Preparing Microparticles Using Spray-Drying Technique

Alanazi

2007

Sci Pharm

View full text Add to dashboard Cite

show abstract

“…For instance, since ABZ is basic in nature, its solubility can be increased by ionization in an acid medium, although this increase in solubility is not sufficient for the preparation of high-ABZ concentration formulations (17). Another approach involved addition of surfactants such as Tween 80 and bile salts, or co-solvent agents such as Transcu-tol (18)(19)(20). Use of liposomes (21) and a solid dispersion approach with polyvinylpyrrolidone (22)(23)(24) showed less promise.…”

mentioning

confidence: 99%

Formulation development of an albendazole self-emulsifying drug delivery system (SEDDS) with enhanced systemic exposure / Razvoj samoemulzifirajućeg sustava za isporuku albendazola (SEDDS) s pojačanom sistemskom apsorpcijom

Meena¹,

Sharma

Kandaswamy

et al. 2012

Acta Pharmaceutica

View full text Add to dashboard Cite

Most of the new chemical entities (NCEs) are poorly water-soluble and pose a challenge to developing an optimum solid oral dosage form. Oral route has been the major route of drug delivery for the treatment of various diseases. Delivery of poorly water--soluble molecules by oral route is difficult because approximately 40 % of drug compounds are limited to low aqueous solubility, which leads to restricted oral bioavailability, high intra-and inter-subject variability and lack of dose proportionality (1).To increase the oral bioavailability of poorly water-soluble compounds and eliminate the discussed drawbacks, various other formulation strategies have been adopted, including the use of cyclodextrins, nanoparticles, solid dispersions and permeation en- The aim of the study was to develop and evaluate a self--emulsifying drug delivery system (SEDDS) formulation to improve solubility and dissolution and to enhance systemic exposure of a BCS class II anthelmetic drug, albendazole (ABZ). In the present study, solubility of ABZ was determined in various oils, surfactants and co-surfactants to identify the microemulsion components. Pseudoternary phase diagrams were plotted to identify the microemulsification existence area. SEDDS formulation of ABZ was prepared using oil (Labrafac Lipopfile WL1349) and a surfactant/co-surfactant (Tween 80/PEG 400) mixture and was characterized by appropriate studies, viz., microemulsifying properties, droplet size measurement, in vitro dissolution, etc. Finally, PK of the ABZ SEDDS formulation was performed on rats in parallel with suspension formulation. It was concluded that the SEDDS formulation approach can be used to improve the dissolution and systemic exposure of poorly water-soluble drugs such as ABZ.

show abstract

“…In animal studies, the main strategy to enhance albendazole bioavailability was by that of increasing water and lipid solubility by the use of cosolvents or surfactants or of incorporating albendazole into particles. The relative bioavailability of albendazole in mice increased 1.8-fold by combining it with the cosolvent Transcutol (diethylene glycol monoethylether) (18). A formulation of a solid dispersion enhanced the relative bioavailability in rabbits threefold (11).…”

mentioning

confidence: 99%

Relative Bioavailability of Three Newly Developed Albendazole Formulations: a Randomized Crossover Study with Healthy Volunteers

Rigter¹,

Schipper

Koopmans³

et al. 2004

Antimicrob Agents Chemother

View full text Add to dashboard Cite

This study of healthy volunteers shows that the relative bioavailability of albendazole formulations that use arachis oil-polysorbate 80 or hydroxypropyl-␤-cyclodextrin as an excipient was enhanced 4.3-and 9.7-fold compared to the results seen with commercial tablets. Administration of macrogol suppositories did not result in measurable plasma concentrations of albendazole sulfoxide.The therapeutic response of albendazole (20 to 50%) in cases of echinococcosis is variable and difficult to predict (2, 8). Albendazole's poor intestinal absorption (Ͻ5%) (due to its low aqueous solubility) is probably a major determinant of the variable response rate (9). In animal studies, the main strategy to enhance albendazole bioavailability was by that of increasing water and lipid solubility by the use of cosolvents or surfactants or of incorporating albendazole into particles. The relative bioavailability of albendazole in mice increased 1.8-fold by combining it with the cosolvent Transcutol (diethylene glycol monoethylether) (18). A formulation of a solid dispersion enhanced the relative bioavailability in rabbits threefold (11). Albendazole coadministered with the surfactant sodium taurocholate or polysorbate enhanced the area under the concentration curve (AUC) value for rats by 55 or 88%, respectively (3, 4, 5), whereas incorporation into liposomes increased the uptake in rats by more than twofold (19) and incorporation into a cyclodextrin increased the AUC for sheep by 37% (6, 16).For humans, several strategies were studied to enhance albendazole bioavailability. When combined with a fatty meal, administration of albendazole sulfoxide (ABZSX) increased the maximum concentration of drug in serum (C max ) 4.5-to 9-fold (1,7,12,15). To inhibit CYP3A4 isozyme-related ABZSX degradation, albendazole was coadministered with cimetidine. However, this caused a 52% decrease in ABZSX C max values (probably due to inhibition of gastric acid secretion) (15,17), suggesting that absorption is pH dependent. When coadministered with grapefruit juice, the ABZSX C max was enhanced 3.2-fold, probably due to inhibition of the intraluminal degradation of albendazole by CYP3A4 enzymes (15). In one human study, a soybean oil emulsion was used to enhance albendazole solubility and showed a 1.6-fold enhancement of relative bioavailability compared with tablets (14).The present report presents findings for a human study comparing the relative levels of bioavailability of three new pharmaceutical albendazole formulations with that of the commercially available tablet. These three new formulations include an oral suspension with arachis oil and the surfactant polysorbate 80 (aimed at increasing lipid solubility), an oral solution of albendazole incorporated into hydroxypropyl-␤-cyclodextrin (aimed at increasing water solubility), and a macrogol suppository (aimed at avoiding the intestinal degradation of albendazole).The suspension was prepared by mixing 9.0 g of albendazole (Duchefa, Haarlem, The Netherlands) with 36.0 g of arachis oil, 2.0 g of a...

show abstract

A novel formulation of albendazole solution: oral bioavailability and efficacy evaluation

Cited by 41 publications

References 16 publications

Improvement of Albendazole Dissolution by Preparing Microparticles Using Spray-Drying Technique

Improvement of Albendazole Dissolution by Preparing Microparticles Using Spray-Drying Technique

Formulation development of an albendazole self-emulsifying drug delivery system (SEDDS) with enhanced systemic exposure / Razvoj samoemulzifirajućeg sustava za isporuku albendazola (SEDDS) s pojačanom sistemskom apsorpcijom

Relative Bioavailability of Three Newly Developed Albendazole Formulations: a Randomized Crossover Study with Healthy Volunteers

Contact Info

Product

Resources

About