PMID- 19167587
OWN - NLM
STAT- MEDLINE
DCOM- 20090319
LR  - 20221207
IS  - 0149-2918 (Print)
IS  - 0149-2918 (Linking)
VI  - 30
IP  - 12
DP  - 2008 Dec
TI  - Bioequivalence and comparison of pharmacokinetic properties of 4-mg tablet 
      formulations of rosiglitazone hydrochloride and rosiglitazone maleate: a 
      single-dose, randomized, open-label, two-period crossover study in healthy adult 
      male Chinese volunteers.
PG  - 2272-9
LID - 10.1016/j.clinthera.2008.12.011 [doi]
AB  - BACKGROUND: Rosiglitazone is an insulin-sensitizing oral thiazolidinedione used 
      for treating patients with type 2 diabetes mellitus. There are 9 oral generic and 
      branded formulations of rosiglitazone available in the People's Republic of China 
      (PRC); however, a literature search did not identify any published data 
      concerning the bioavailability of these formulations in the Chinese population. 
      OBJECTIVES: The aims of this study were to compare the pharmacokinetic properties 
      and determine the bioequivalence of 2 formulations of rosiglitazone 4-mg 
      tablets-rosiglitazone hydrochloride (test) and rosiglitazone maleate 
      (reference)-in healthy adult male Chinese volunteers. METHODS: This single-dose, 
      randomized, open-label, 2-period crossover study was conducted at Zhejiang 
      Provincial People's Hospital, Hangzhou, PRC. Healthy adult male Chinese 
      volunteers were randomly assigned to receive a single 4-mg dose of the test or 
      reference formulation, followed by a 7-day washout period and administration of 
      the alternate formulation. The study drugs were administered after a >or=12-hour 
      (overnight) fast. Plasma was analyzed for rosiglitazone concentration using a 
      validated high-performance liquid chromatography method. For analysis of 
      pharmacokinetic properties, including C(max), AUC(0-t), and AUC(0-infinity), 
      blood samples were drawn before (0 hour; baseline) and at 10, 20, 30, 45, 60, 75, 
      and 90 minutes and 2, 4, 6, 8, 12, and 24 hours after administration. The 
      formulations were to be considered bioequivalent if the logarithm-normal 
      (ln)-transformed ratios of C(max) and AUC were within the predetermined range of 
      80% to 125%, as established by the US Food and Drug Administration. Tolerability 
      was assessed using physical examination, including monitoring of vital signs, 
      laboratory testing (hematology, blood biochemistry, hepatic function, renal 
      function, and urinalysis), and questioning subjects about adverse events (AEs). 
      RESULTS: Twenty subjects were enrolled and completed the study (mean [SD] age, 
      21.1 [1.4] years; weight, 62.6 [4.6] kg; height, 171 [5] cm; and body mass index, 
      21.4 [1.3] kg/m(2)). No period or sequence effects were detected. The 90% CIs for 
      the ln-transformed ratios of C(max), AUC(0-24), and AUC(0-infinity) were 96.79 to 
      109.73, 92.14 to 102.93, and 91.64 to 102.60, respectively (all, P < 0.001), 
      meeting the predetermined criterion for bioequivalence. No AEs were reported in 
      this study. CONCLUSIONS: In this small study in these healthy adult male Chinese 
      volunteers, a single 4-mg dose of rosiglitazone hydrochloride appeared to be 
      bioequivalent to rosiglitazone maleate, according to the regulatory definition, 
      based on the rate and extent of absorption. Both formulations were well 
      tolerated.
FAU - Yu, Jia
AU  - Yu J
AD  - Department of Clinical Pharmacology, Zhejiang Provincial People's Hospital, 
      Hangzhou, People's Republic of China.
FAU - Ma, Ke
AU  - Ma K
FAU - Qi, Jinwen
AU  - Qi J
FAU - Jin, Ge
AU  - Jin G
FAU - Wang, Yan
AU  - Wang Y
FAU - Fang, Shungan
AU  - Fang S
FAU - Li, Gonghua
AU  - Li G
LA  - eng
PT  - Comparative Study
PT  - Journal Article
PT  - Randomized Controlled Trial
PT  - Research Support, Non-U.S. Gov't
PL  - United States
TA  - Clin Ther
JT  - Clinical therapeutics
JID - 7706726
RN  - 0 (Hypoglycemic Agents)
RN  - 0 (Tablets)
RN  - 0 (Thiazolidinediones)
RN  - 05V02F2KDG (Rosiglitazone)
SB  - IM
MH  - Adult
MH  - Area Under Curve
MH  - *Asian People
MH  - China
MH  - Chromatography, High Pressure Liquid/methods
MH  - Cross-Over Studies
MH  - Fluorescence
MH  - Half-Life
MH  - Humans
MH  - Hypoglycemic Agents/blood/*pharmacokinetics
MH  - Male
MH  - Rosiglitazone
MH  - Tablets
MH  - Therapeutic Equivalency
MH  - Thiazolidinediones/blood/*pharmacokinetics
MH  - Time Factors
EDAT- 2009/01/27 09:00
MHDA- 2009/03/20 09:00
CRDT- 2009/01/27 09:00
PHST- 2008/10/31 00:00 [accepted]
PHST- 2009/01/27 09:00 [entrez]
PHST- 2009/01/27 09:00 [pubmed]
PHST- 2009/03/20 09:00 [medline]
AID - S0149-2918(08)00437-2 [pii]
AID - 10.1016/j.clinthera.2008.12.011 [doi]
PST - ppublish
SO  - Clin Ther. 2008 Dec;30(12):2272-9. doi: 10.1016/j.clinthera.2008.12.011.