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Pharmacokinetic Exploration of Sublingual Route for the Enhanced Bioavailability of Tacrolimus with Rabbit as Animal Model

1, 2★, 1, 3★ Corresponding author

  1. 1Department of Pharmacy, College of Pharmaceutical Sciences, Government Medical College, Thiruvananthapuram, Kerala, INDIA.
  2. 2Department of Pharmaceutics, Sri Ramachandra Faculty of Pharmacy, Sri Ramachandra Institute of Higher Education and Research, Porur, Chennai, Tamil Nadu, INDIA.
  3. 3Department of Pharmaceutics, SRM College of Pharmacy, SRM University, Kattankulathur, Tamil Nadu, INDIA.

CORRESPONDENCE

Gopinath Subramaniyan

Department of Pharmaceutics, Sri Ramachandra Faculty of Pharmacy, Sri Ramachandra Institute of Higher Education and Research, Porur, Chennai, Tamil Nadu, INDIA.

gopinath.s@sriramachandra.edu.in

Received: 21-06-2023; Revised: 07-08-2023; Accepted: 07-10-2023.

Volume 14, Issue 1 · pp. 180-185 · 2023 · DOI: 10.5530/ijpi.14.1.23

ABSTRACT

Introduction: The study aimed to assess the bioavailability of two sublingual formulations i.e., fast-dissolving films and tablets of the poorly bioavailable immunosuppressant drug, tacrolimus, and to compare with its marketed oral capsule formulation.Materials and Methods: Optimized film and tablet formulations of tacrolimus for sublingual administration were developed. Stability studies were performed at room temperature as well as at 40±2°C/75±2% relative humidity for 6 months. The in vivo pharmacokinetic studies were performed with rabbits as the animal model. Different pharmacokinetic parameters like tmax, Cmax, AUC, t1/2 and Ke were established and they were analyzed statistically by the student t-test.Results: The stability analysis showed a satisfactory stability profile of all the dosage forms in a six-month study. The in vivo study of the developed formulations showed better pharmacokinetic performance when compared with the marketed oral formulation. There was approximately a 2 and 1.8-fold increase in the relative bioavailability of the film and the tablet formulations respectively.Conclusion: The development of tacrolimus into sublingual dosage forms could improve the in vivo performance of the drug candidate.

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    Mohanan, J., Subramaniyan, G., Kuttalingam, A., & Narayanasamy, D. (2023). Pharmacokinetic Exploration of Sublingual Route for the Enhanced Bioavailability of Tacrolimus with Rabbit as Animal Model. International Journal of Pharmaceutical Investigation, 14(1), 180-185. https://doi.org/10.5530/ijpi.14.1.23

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    © 2023 Author(s)

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