Improving the oral bioavailability of albendazole in rabbits by the solid dispersion technique.
We have investigated the oral bioavailability of granules of albendazole, a drug used for treating echinococcosis in man, prepared by the solid dispersion technique. Rapid dissolution and supersaturation were observed when hydroxypropylmethylcellulose and hydroxypropylmethylcellulose phthalate were used as carriers in the solid dispersion. They inhibited the crystallization of albendazole from the supersaturated solution and maintained an amorphous state for 8 h. Gastric acidity-controlled rabbits were used to evaluate the variation in absorption after oral administration of the albendazole solid dispersion. For rabbits with low gastric acidity the bioavailability of orally administered albendazole in the granular form prepared by solid dispersion was more than three times that of albendazole in physical mixtures. These results suggest that the bioavailability of albendazole in solid dispersions might be high even if there is a great variation in the gastric pH of patients.
Kohri
N
N
Department of Pharmacy, Hokkaido College of Pharmacy, Hokkaido University, Sapporo, Japan.
Yamayoshi
Y
Y
Xin
H
H
Iseki
K
K
Sato
N
N
Todo
S
S
Miyazaki
K
K
D000284:Administration, Oral; D015766:Albendazole / Q000097:blood / Q000493:pharmacokinetics*; D000818:Animals; D000923:Anticestodal Agents / Q000097:blood / Q000493:pharmacokinetics*; D001682:Biological Availability; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry; D006863:Hydrogen-Ion Concentration; D065347:Hypromellose Derivatives; D007408:Intestinal Absorption; D008297:Male; D008747:Methylcellulose / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000737:chemistry; D011817:Rabbits; D013997:Time Factors; D014961:X-Ray Diffraction
D000923:Anticestodal Agents; D004337:Drug Carriers; D065347:Hypromellose Derivatives; D008747:Methylcellulose; C053309:hydroxypropyl methylcellulose phthalate; D015766:Albendazole