PMID- 24495314
OWN - NLM
STAT- MEDLINE
DCOM- 20140617
LR  - 20140430
IS  - 0946-1965 (Print)
IS  - 0946-1965 (Linking)
VI  - 52
IP  - 5
DP  - 2014 May
TI  - Effects of food on the pharmacokinetics of gemigliptin/metformin 
      sustained-release 50/1,000 mg (25/500 mg x 2 tablets) fixeddose combination 
      tablet in healthy male volunteers.
PG  - 381-91
LID - 10.5414/CP202038 [doi]
AB  - OBJECTIVES: For patient convenience, a gemigliptin/metformin sustainedrelease 
      fixed-dose combination (FDC) tablet was developed. This study was conducted to 
      investigate the effects of food on the pharmacokinetic (PK) profile of the FDC 
      tablets. MATERIALS AND METHODS: This was an open-label, randomized, single dose, 
      2-period, 2-sequence crossover study in 24 healthy male volunteers. The FDC 
      tablets (25/500 mg x 2 tablets) were administered in high-fat fed and fasted 
      states on separate occasions, and each subject was randomly allocated to each 
      sequence with a 7-day washout period. PK blood samplings were conducted from 
      predose to 48 hours after dosing. Tolerability assessments were performed 
      throughout the study. RESULTS: Nine adverse events (AEs) of mild intensity were 
      reported from 8 subjects after study drug administration, and the AE frequency 
      was similar between treatments. No serious AEs were reported. The PK parameters 
      of gemigliptin and metformin were compared between fasting and fed states. For 
      gemigliptin, the geometric mean ratios (GMRs) (fed : fasted state) of the Cmax 
      and AUClast were 0.886 (90% confidence interval (CI) 0.781 - 1.006) and 1.021 
      (90% CI 0.949 - 1.099), respectively. For metformin, the GMRs of the Cmax and 
      AUClast were 0.811 (90% CI 0.712 - 0.923) and 1.144 (90% CI 1.013 - 1.291), 
      respectively. A prolonged tmax for metformin was observed. These results are 
      similar to the effects of food on each component. CONCLUSION: The FDC tablet may 
      have a similar PK profile as that of individual drugs and is generally tolerable 
      when administered with food. These results indicate that the FDC tablet can be 
      administered in the same dosing regimen as each component, especially that of 
      metformin sustained-release.
FAU - Choi, Hee Youn
AU  - Choi HY
FAU - Noh, Yook-Hwan
AU  - Noh YH
FAU - Kim, Yo Han
AU  - Kim YH
FAU - Kim, Mi Jo
AU  - Kim MJ
FAU - Lee, Shi Hyang
AU  - Lee SH
FAU - Kim, Jeong-Ae
AU  - Kim JA
FAU - Kim, Bogyeong
AU  - Kim B
FAU - Lim, Hyeong-Seok
AU  - Lim HS
FAU - Bae, Kyun-Seop
AU  - Bae KS
LA  - eng
PT  - Journal Article
PT  - Randomized Controlled Trial
PT  - Research Support, Non-U.S. Gov't
PL  - Germany
TA  - Int J Clin Pharmacol Ther
JT  - International journal of clinical pharmacology and therapeutics
JID - 9423309
RN  - 0 (Delayed-Action Preparations)
RN  - 0 (Drug Combinations)
RN  - 0 (Hypoglycemic Agents)
RN  - 0 (LC15-0444)
RN  - 0 (Piperidones)
RN  - 0 (Pyrimidines)
RN  - 0 (Tablets)
RN  - 9100L32L2N (Metformin)
SB  - IM
MH  - Administration, Oral
MH  - Adult
MH  - Area Under Curve
MH  - Cross-Over Studies
MH  - Delayed-Action Preparations
MH  - Drug Administration Schedule
MH  - Drug Combinations
MH  - Fasting/blood
MH  - *Food-Drug Interactions
MH  - Half-Life
MH  - Healthy Volunteers
MH  - Humans
MH  - Hypoglycemic Agents/administration & dosage/adverse 
      effects/blood/*pharmacokinetics
MH  - Male
MH  - Metabolic Clearance Rate
MH  - Metformin/administration & dosage/adverse effects/blood/*pharmacokinetics
MH  - Piperidones/administration & dosage/adverse effects/blood/*pharmacokinetics
MH  - Postprandial Period
MH  - Pyrimidines/administration & dosage/adverse effects/blood/*pharmacokinetics
MH  - Republic of Korea
MH  - Sex Factors
MH  - Tablets
MH  - Young Adult
EDAT- 2014/02/06 06:00
MHDA- 2014/06/18 06:00
CRDT- 2014/02/06 06:00
PHST- 2014/04/29 00:00 [accepted]
PHST- 2014/02/06 06:00 [entrez]
PHST- 2014/02/06 06:00 [pubmed]
PHST- 2014/06/18 06:00 [medline]
AID - 11244 [pii]
AID - 10.5414/CP202038 [doi]
PST - ppublish
SO  - Int J Clin Pharmacol Ther. 2014 May;52(5):381-91. doi: 10.5414/CP202038.