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Arzneimittelforschung 2012; 62(03): 145-148
DOI: 10.1055/s-0031-1298024
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

Comparative Bioequivalence Study of Leflunomide Tablets in Indian Healthy Volunteers

S. Agarwal
1   Bioequivalence Study Centre, Department of Pharmaceutical Technology, Jadavpur University, Kolkata, India
,
A. Das
1   Bioequivalence Study Centre, Department of Pharmaceutical Technology, Jadavpur University, Kolkata, India
,
D. Ghosh
1   Bioequivalence Study Centre, Department of Pharmaceutical Technology, Jadavpur University, Kolkata, India
,
A. K. Sarkar
1   Bioequivalence Study Centre, Department of Pharmaceutical Technology, Jadavpur University, Kolkata, India
,
T. K. Chattaraj
2   Department of Pharmacology, N.R.S. Medical College & Hospital, Kolkata, India
,
T. K. Pal
1   Bioequivalence Study Centre, Department of Pharmaceutical Technology, Jadavpur University, Kolkata, India
› Author Affiliations
Further Information

Publication History

received 14 October 2011

accepted 07 December 2011

Publication Date:
25 January 2012 (online)

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Abstract

Objective:

The pharmacokinetics of teriflunomide [CAS No. 163451-81-8], the metabolite of leflunomide [CAS No. 75706-12-6] has been evaluated in adult human volunteers after oral administration of tablet formulation. However, no published data is available regarding the bioavailability of this in the Indian population. In light of the above, a study was designed to carry out a bioequivalence study of 2 preparations of leflunomide 20 mg in healthy Indian male volunteers.

Methods:

24 healthy male volunteers (age, 25±4.1 years; weight, 57.58±7.01 kg) were enrolled in this study. Each subject received a test and reference formulation in a single dose, fasting 2 period, 2 way crossover study with a wash out period of 4 weeks. Analysis of teriflunomide from plasma samples was done by a simple and sensitive HPLC method using UV detection developed in our laboratory. An analysis of variance was performed on the pharmacokinetic parameters Cmax, AUC0-t, AUC0–∞ using GLM procedures in which sources of variation were subject, formulation, and period.

Results:

The results indicated that there are no statistically significant differences between the 2 products in either the mean concentration-time profiles or in the obtained pharmacokinetic parameters. 90% confidence limits for the log transformed data of Cmax, AUC0–t, AUC0–∞. were within the acceptable range of 0.80–1.25.

Conclusion:

The results indicate that the 2 products are bioequivalent in terms of rate and extent of drug absorption. Both the preparations were well tolerated with no adverse reactions throughout the study.

Key words

bioavailability - bioequivalence - leflunomide - teriflunomide - active metabolite
 

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