European Journal of Clinical Pharmacology

, Volume 74, Issue 5, pp 561–569 | Cite as

Evaluation of pharmacokinetic and pharmacodynamic parameters following single dose of sitagliptin in healthy Indian males

  • Ganesh V. SangleEmail author
  • Mohan Patil
  • Nitin J. Deshmukh
  • Sushant A. Shengule
  • Shantibhushan Kamble
  • Kiran Kumar Vuppalavanchu
  • Sushil Kale
  • Mirza Layeeq Ahmed Baig
  • Geetchandra Singh
  • Javed Shaikh
  • Jitendra Tripathi
  • P. Aravindababu



Sitagliptin, a dipeptidyl peptidase (DPP)-IV inhibitor approved for the treatment of type 2 diabetes, is reported to be more efficacious in Indian patients than non-Indian patient population. The objective of the study was to evaluate pharmacokinetic and pharmacodynamic (PK/PD) parameters of single-dose sitagliptin 100 mg (Januvia) in healthy Indian male participants.


In a randomised, single-dose, open-label, three-treatment, three-period, three-sequence, crossover bioavailability study, 18 healthy male participants received single-dose of sitagliptin under fasted and fed conditions. PK parameters (Cmax, Tmax, AUC0-∞ and t1/2) were determined using Phoenix WinNonlin software. PD parameters [DPP-IV inhibition, active glucagon-like peptide-1 (GLP-1) and insulin] were determined using established methods.


PK parameters expressed in mean (SD) were Cmax 491.7 (135.9) ng/mL; AUC0-∞ 4256.1 (509.9) ng· hr/mL, Tmax 2.9 (1.0) hr and t1/2 10.4 (3.0) hr. The weighted average (WA) plasma DPP-4 inhibition over 24 h was 89.6% and WA of plasma active GLP-1 over 2 h after standardised meal (geometric mean ratio) was 11.1 (9.9) pM/L which is two- to- four fold higher compared to that reported in other populations. The mean average (SD) AUC of plasma insulin over 2 h of standardised meal was 47.9 (24.9) μIU/mL.


Although, there are differences in pharmacokinetic parameters, no clinically meaningful differences were observed with respect to DPP-IV inhibition between Indian and non-Indian population.


Sitagliptin Pharmacodynamics Pharmacokinetics Incretins DPP-IV inhibitors 



The authors thank clinical researchers and participants who participated in this study. We acknowledge Dr. Sai Krishnaveni Chevooru (for editorial support) during the development of the manuscript. Wockhardt Limited (Mumbai, India) funded the study.

Compliance with ethical standards

Conflict of interest

The authors declare that they have no conflict of interest.

Supplementary material

228_2018_2433_MOESM1_ESM.docx (14 kb)
ESM 1 (DOCX 14 kb)


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Copyright information

© Springer-Verlag GmbH Germany, part of Springer Nature 2018

Authors and Affiliations

  • Ganesh V. Sangle
    • 1
    Email author
  • Mohan Patil
    • 1
  • Nitin J. Deshmukh
    • 1
  • Sushant A. Shengule
    • 1
  • Shantibhushan Kamble
    • 2
  • Kiran Kumar Vuppalavanchu
    • 2
  • Sushil Kale
    • 2
  • Mirza Layeeq Ahmed Baig
    • 2
  • Geetchandra Singh
    • 2
  • Javed Shaikh
    • 2
  • Jitendra Tripathi
    • 2
  • P. Aravindababu
    • 2
  1. 1.Diabetes Research Lab, New Drug DiscoveryWockhardt Research CentreAurangabadIndia
  2. 2.Clinical Pharmacokinetics and Biopharmaceutics DepartmentWockhardt Research CentreAurangabadIndia

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