Impact of pharmaceutical dosage forms on the pharmacokinetics of roxithromycin in healthy human volunteers.
OBJECTIVE
The impact of two different pharmaceutical preparations on the pharmacokinetics of roxithromycin was investigated in healthy human volunteers.


METHODS
The degradation kinetics and products of roxithromycin were investigated in simulated gastric fluid and simulated intestinal fluid. Two oral dosage forms of roxithromycin were employed: enteric-coated pellets and dispersible tablets.


RESULTS
The degradation half-time of roxithromycin in simulated gastric fluid was 0.23 h, and three main degradation products were characterized. In contrast, roxithromycin was stable in simulated intestinal fluid and remained unchanged after a 1.00 h incubation. The roxithromycin enteric-coated pellets exhibited higher bioavailability and a more potent serum antibacterial activity than the dispersible tablets.


CONCLUSIONS
The type of oral dosage forms of roxithromycin altered its pharmacokinetics. Whether or not this affects the in vivo antibacterial efficacy requires further study.
Sun
Jin
J
Department of Biopharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, 110016, Liaoning Province, China.
Zhang
Tianhong
T
Qiu
Feng
F
Liu
Yu
Y
Tang
Jingling
J
Huang
Haihua
H
He
Zhonggui
Z
D000328:Adult; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D005750:Gastric Juice / Q000378:metabolism; D006801:Humans; D007408:Intestinal Absorption; D007700:Kinetics; D008297:Male; D015575:Roxithromycin / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D013607:Tablets / Q000008:administration & dosage; D013608:Tablets, Enteric-Coated / Q000008:administration & dosage
D000900:Anti-Bacterial Agents; D013607:Tablets; D013608:Tablets, Enteric-Coated; D015575:Roxithromycin