Iranian Journal of Pharmaceutical Sciences

Vol. 10 No. 1 (2014)

Pharmacokinetics and Bioavailability Comparison of two oral Tablet Formulations of Escitalopram 20 mg: A Single-Dose, Open-Label, Two-Period Crossover Study in Healthy Indian Adult Subjects Bio-equivalence of Escitalopram in Healthy Indian subjects

Iranian Journal of Pharmaceutical Sciences, Vol. 10 No. 1 (2014), 15 January 2014 , Page 27-36
https://doi.org/10.22037/ijps.v10.40832

Abstract

This study was undertaken to assess bioequivalence between test and reference formulations of escitalopram oxalate 20 mg in healthy Indian male subjects. This single-dose, randomized, open-label, 2-period crossover study was carried out in 12 Healthy Indian Male volunteers aged 18 to 55 years under fasting conditions with a wash out of 14 days. The subjects were randomly assigned to receive the test formulation followed by the reference formulation, and then vice versa. Blood samples were collected for up to 156 h postdose. Quantification was carried out using a validated LC-MS/MS method. Maximum plasma concentrations Cmax of 26.386 ± 5.54 ng/mL (test) and 24.430 ± 3.52 ng/mL (reference) were achieved. Areas under the plasma concentration-time curve AUC0-inf of 854.241 ± 91.22 ng. hr/mL (test) and 825.135 ± 1.37 ng. hr/mL (reference), AUC0-t of 848.766 ± 93.26 ng. hr/mL (test), 819.504 ± 1.91 ng. hr/mL (reference) were calculated. The median Tmax was 4.00 hr for test and reference formulation, respectively. Plasma elimination half-lives T1/2 of 19.26 ± 5.95 hr (test), 20.94 ± 2.88 hr (reference) were determined. Both formulations were well tolerated. The 90% confidence intervals obtained by analysis of variance were 94.49-120.68% for Cmax and 98.22-108.18% for AUC0-t which were within the predefined regulatory acceptance limit of 80.00-125.00%.

Keywords:
  • Bioavailability
  • Bioequivalence
  • Escitalopram
  • Human volunteers
  • Pharmacokinetics
  • Psychiatric disorders

How to Cite

Kotakonda Harish Kaushik, S.Vijay Kumar, Y. Narasimha Reddy, & M.Nagulu. (2014). Pharmacokinetics and Bioavailability Comparison of two oral Tablet Formulations of Escitalopram 20 mg: A Single-Dose, Open-Label, Two-Period Crossover Study in Healthy Indian Adult Subjects: Bio-equivalence of Escitalopram in Healthy Indian subjects. Iranian Journal of Pharmaceutical Sciences, 10(1), 27–36. https://doi.org/10.22037/ijps.v10.40832

References

[1] Sa´nchez, C., P. B. F. Bergqvist, L. T. Brennum, S. Gupta, S. Hogg, A. Larsen & O. Wiborg: Escitalopram, the S-(+)-enantiomer of citalopram, is a selective serotonin reuptake inhibitor with potent effects in animal models predictive of antidepressant and anxiolytic activities. Psychopharmacology (2003a) 167: 353–362.
[2] Auquier, P., S. Robitail, P. M. Llorca & B. Rive. Comparison of escitalopram and citalopram efficacy: a meta-analysis. Int. J.Psych. Clin. Pract. (2003) 7: 259–268.
[3] Cremers, T. I. F. H. & B. H. C. Westerink. Pharmacological difference between escitalopram and citalopram. Int. J. Psychiatry Clin. Pract (2003) 7: 306.
[4] Niranjan Rao. The clinical pharmacokinetics of escitalopram, Clin Pharmacokinet (2007) 46(4) 281-90.
[5] Sonu Sundd Singh, Hiten Shah, Sapna Gupta, Manish Jain, Kuldeep Sharma, Purav Thakkar, Ruchy Shah, Liquid chromatography–electrospray ionisation mass spectrometry method for the determination of escitalopram in human plasma and its application in bioequivalence study. Journal of Chromatography B (2004) 811: 209–215.
[6] Chow SC, Liu JP. Statistical methods for average bioavailability. Chow SC, Liu JP (2nd ed) In: Design and Analysis of Bioavailability and Bioequivalence Studies.. Marcel Dekker New York, NY (2007) 79-124.
[7] US Dept of Health and Human Services (HHS), Food and Drug Administration (FDA), Center for Drug Evaluation and Research (CDER). Guidance for Industry. Bioavailability and bioequivalence studies for orally administered drug products—general considerations. http://www.fda.gov/downloads/Drugs/DevelopmentApprovalProcess/How Drugs are Developed and Approved/Approval Applications/ Abbreviated New Drug Application ANDA Generics/ UCM154838.pdf. (Accessed on Jan 12, 2014)
[8] Central Drugs Standard Control Organization, Directorate General of Health Services, Ministry of Health & Family Welfare. Guidelines for bioavailability & bioequivalence studies.
http://www.cdsco.nic.in/htmL/BE%20Guidelines%20Draft%20Ver10%20March%2016,%2005.pdf. (Accessed on Jan 12, 2014)
[9] Nakai K, Fujita M, Ogata H. International harmonisation of bioequivalence studies and issues shared in common. Yakugaku Zasshi (2000) (120):1193–1200.
[10] G.D. Mendes,T. Babadopulos et al, Comparative bioavailability of two escitalopram formulations in healthy human volunteers, Int. Journal of Clinical Pharmacology and Therapeutics (2010) 48(8): 554-62.
[11] Jing Li ,Yuan Tian , Zun-jian Zhang et al, Pharmacokinetics and Bioequivalence Study of Escitalopram Oxalate Formulations after Single-dose Administration in Healthy Chinese Male Volunteers, Arzneimittelforschung (2009) 59(5): 228-232.
[12] S.Almeida, P.Pedroso, A.Flipe et al, Bioequivalence of Two Formulations of Escitalopram , Arzneimittelforschung (2012) 62(7): 307-312.
  • Abstract Viewed: 416 times
  • IJPS_Volume 10_Issue 1_Pages 27-36 Downloaded: 352 times

Download Statastics

Developed By

Open Journal Systems

Information