title: [Pharmacokinetics and relative bioavailability of probucol inclusion complex capsule in healthy dogs].
abstract: OBJECTIVE
  To study the pharmacokinetics and relative bioavailability of probucol inclusion complex capsule.
  
  
  METHODS
  Following oral administration of a single dose of 250 mg of conventional tablet (formulation A, purchased from the market) and probucol inclusion complex capsule (formulation B, a new formulation for preclinical trial) to each of 6 healthy dogs in a randomized crossover design, the plasma levels of the active drug at different time points were determined by HPLC and the plasma concentration-time profiles of formulation A and B were obtained. The pharmacokinetic parameters as well as relative bioavailability were analyzed.
  
  
  RESULTS
  The concentration-time curves of formulation A and formulation B were found to fit a two-compartment open model. The Tmax values of formulation A and formulation B were (9.3 +/- 2.1) h and (9.3 +/- 2.1) h, the Cmax values were (1.5 +/- 1.0) microgram.mL-1 and (2.3 +/- 0.9) microgram.mL-1 and the AUC0-240 values were (85 +/- 56) microgram.h.mL-1 and (134 +/- 55) microgram.h.mL-1, respectively. The relative bioavailability of formulation B was found to be (198 +/- 90)% compared with formulation A. The results of variance analysis and two one-side t-test showed that there was significant difference between the two formulations in the AUC0-240.
  
  
  CONCLUSIONS
  The high bioavailability by the inclusion of formulation B is attributed to the improvement of its water-solubility by the inclusion process and this is supposed to be a key factor for improving drug bioavailability.
authors.affiliation: Department of Pharmacy, Cardiovascular Institute and Fu Wai Hospital, Beijing 100037, China.
authors.forename: Zheng
authors.initials: Z
authors.lastname: Zhang
authors.forename: Bao-ling
authors.initials: BL
authors.lastname: Chen
authors.forename: Ke
authors.initials: K
authors.lastname: Wang
authors.forename: Yi-ling
authors.initials: YL
authors.lastname: Huang
authors.forename: Shu-qing
authors.initials: SQ
authors.lastname: Fang
authors.forename: De-liang
authors.initials: DL
authors.lastname: Gu
authors.forename: Li
authors.initials: L
authors.lastname: Fang
authors.forename: Shao-jun
authors.initials: SJ
authors.lastname: Han
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000924:Anticholesteremic Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001682:Biological Availability; D002214:Capsules; D004285:Dogs; D005260:Female; D011341:Probucol / Q000008:administration & dosage / Q000493:pharmacokinetics*; D011897:Random Allocation; D013607:Tablets
chemical_list: D000924:Anticholesteremic Agents; D002214:Capsules; D013607:Tablets; D011341:Probucol