PMID- 30336808
OWN - NLM
STAT- MEDLINE
DCOM- 20190805
LR  - 20190805
IS  - 0946-1965 (Print)
IS  - 0946-1965 (Linking)
VI  - 57
IP  - 1
DP  - 2019 Jan
TI  - Pharmacokinetics and safety of transdermal and oral granisetron in healthy 
      Chinese subjects: An open-label, randomized, crossover study
.
PG  - 24-31
LID - 10.5414/CP203327 [doi]
AB  - AIMS: To examine the pharmacokinetics and safety of granisetron during 
      transdermal delivery and oral administration to healthy Chinese male subjects. 
      MATERIALS AND METHODS: A single 34.3 mg/52 cm(2) transdermal delivery patch of 
      granisetron and the 1-mg tablet of granisetron were dosed to subjects in an 
      open-label, randomized, crossover study. Two dosing schemes were established: 
      scheme 1, in which the 5-day oral administration phase of the tablet (the OA 
      phase) (twice daily every 12 hours) was conducted, followed by the 6-day 
      transdermal delivery phase of the patch (the TD phase); and scheme 2, in which 
      these two phases were conducted in reverse order. Plasma concentrations of 
      granisetron were measured according to high-performance liquid chromatography, 
      and the following pharmacokinetic parameters were determined: C(avg) 
      [AUC(0-24,ss) (day 5)/24 for OA and AUC(24-144)/120 for TD], C(max), t(max), AUC, 
      and T(1/2). RESULTS: All of the subjects completed the TD phase, and 1 subject 
      withdrew from the study due to increased alanine aminotransferase. The C(avg) 
      values for OA and TD were 2.95 +/- 1.60 ng/mL and 2.83 +/- 1.43 ng/mL, respectively. 
      The C(max) values at steady state for OA and TD were 5.98 +/- 2.27 ng/mL and 
      3.91 +/- 2.23 ng/mL, respectively. The incidences of adverse events (AEs) possibly 
      or definitely related to OA and TD were 45.83% and 37.5%, respectively. No 
      serious AEs were found in the two dosing schemes. CONCLUSION: The C(avg) values 
      determined through TD and OA were equivalent, indicating similar drug exposures. 
      Therefore, the granisetron patch may be an alternative formulation for oral 
      granisetron in Chinese individuals.
.
FAU - Chen, Rui
AU  - Chen R
FAU - Chen, Xia
AU  - Chen X
FAU - Wang, Hongyun
AU  - Wang H
FAU - Zhong, Wen
AU  - Zhong W
FAU - Oh, Eun Sil
AU  - Oh ES
FAU - Park, Min Soo
AU  - Park MS
FAU - Kumagai, Yuji
AU  - Kumagai Y
FAU - Zhou, Li
AU  - Zhou L
FAU - Nagahama, Fumiko
AU  - Nagahama F
FAU - Hu, Pei
AU  - Hu P
LA  - eng
PT  - Journal Article
PT  - Randomized Controlled Trial
PL  - Germany
TA  - Int J Clin Pharmacol Ther
JT  - International journal of clinical pharmacology and therapeutics
JID - 9423309
RN  - 0 (Tablets)
RN  - WZG3J2MCOL (Granisetron)
MH  - Administration, Oral
MH  - Area Under Curve
MH  - Chromatography, High Pressure Liquid
MH  - Cross-Over Studies
MH  - Granisetron/*administration & dosage/*pharmacokinetics
MH  - Humans
MH  - Male
MH  - *Tablets
MH  - *Transdermal Patch
EDAT- 2018/10/20 06:00
MHDA- 2019/08/06 06:00
CRDT- 2018/10/20 06:00
PHST- 2018/12/13 00:00 [accepted]
PHST- 2018/10/20 06:00 [pubmed]
PHST- 2019/08/06 06:00 [medline]
PHST- 2018/10/20 06:00 [entrez]
AID - 17704 [pii]
AID - 10.5414/CP203327 [doi]
PST - ppublish
SO  - Int J Clin Pharmacol Ther. 2019 Jan;57(1):24-31. doi: 10.5414/CP203327.