Evaluation of in-vitro dissolution and in-vivo absorption for two different film-coated pellets of clarithromycin.
The aim of this study was to compare two formulations of film-coated pellets containing clarithromycin after single oral dose study in healthy male volunteers. Two formulations with different coating polymers were prepared: formulation-1 (F-1) was prepared by incorporating three kinds of pH-dependent gradient-release coated pellets into capsules and formulation-2 (F-2) was prepared by coated with an insoluble semiosmotic film. Release profiles of film-coated pellets were evaluated using paddle method under different conditions. Pharmacokinetic profiles of these formulations were obtained in three healthy male volunteers and compared to commercially available immediate release (IR) tablets. The relative bioavailability based on the AUC0-24h was found to be 96.2% and 58.7% for F-1 and F-2 compared with IR, and the Tmax was delayed.
Zhang
Xiang-Rong
XR
Department of Pharmacy, Laboratory of Drug Metabolism and Pharmacokinetics, Shenyang 110016, PR. China.
Chen
Xiao-Yan
XY
Hu
Lian-Dong
LD
Tang
Xing
X
Li
San-Ming
SM
Zhong
Da-Fang
DF
D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D017291:Clarithromycin / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D018592:Cross-Over Studies; D003692:Delayed-Action Preparations; D006801:Humans; D006863:Hydrogen-Ion Concentration; D065347:Hypromellose Derivatives; D007408:Intestinal Absorption; D008297:Male; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D011108:Polymers / Q000737:chemistry; D011109:Polymethacrylic Acids / Q000737:chemistry; D012995:Solubility; D013608:Tablets, Enteric-Coated
D000900:Anti-Bacterial Agents; D003692:Delayed-Action Preparations; D011108:Polymers; D011109:Polymethacrylic Acids; D013608:Tablets, Enteric-Coated; C038300:methylmethacrylate-methacrylic acid copolymer; D065347:Hypromellose Derivatives; D008747:Methylcellulose; D017291:Clarithromycin