Bioavailability of clarithromycin cyclodextrin ternary complexes upon oral administration to healthy beagle dogs.
The dissolution profiles of clarithromycin (CLM) and its beta-cyclodextrin-citric acid ternary complexes (CTC) were examined. CTC showed an enhanced dissolution rate in pH 6.8 phosphate buffers. The relative bioavailability was evaluated by comparing area under the plasma concentration-time curve (AUC) of the pure CLM with that of its cyclodextrin-citric acid ternary complexes those were filled into hard gelatin capsules. To compare the pharmacokinetic behavior, both plasma levels of parent compound and the active metabolite 14-OH-CLM concentrations were estimated. The relative bioavailability value as the ratios of CLM of mean total AUC for CTC relative to CLM was 120.3%. The relative bioavailability value as the ratios of 14-OH CLM of mean total AUC for CTC relative to CLM was 95.3%. The results suggest that the absorption of CTC in beagle dogs was slightly improved because of the enhanced dissolution rate of CTC at pH 6.8.
Zhang
Xiangrong
X
College of Pharmacy, Shenyang Pharmaceutical University, Shenyang, People's Republic of China.
Zou
Meijuan
M
Li
Sanming
S
Chen
Xiaoyan
X
Zhong
Dafang
D
D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D019343:Citric Acid / Q000737:chemistry*; D017291:Clarithromycin / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D004285:Dogs; D005260:Female; D006863:Hydrogen-Ion Concentration; D008297:Male; D013058:Mass Spectrometry; D012995:Solubility; D047392:beta-Cyclodextrins / Q000737:chemistry*
D047392:beta-Cyclodextrins; C056228:14-hydroxyclarithromycin; D019343:Citric Acid; D017291:Clarithromycin; C031215:betadex