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Unbiased membrane permeability parameters for gabapentin using boundary layer approach

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Abstract

The present study was performed to determine the relative contribution of both passive and nonpassive transport processes in jejunal absorption of gabapentin. The oral absorption of gabapentin was studied using in situ single pass intestinal perfusion technique in fasted rats. Unbiased intrinsic membrane absorption parameters such as maximal flux, Michaelis constant, carrier permeability, and membrane permeability were calculated using a modified boundary layer model. Gabapentin intestinal perfusion results indicate that its jejunal absorption in rats occurs via a nonpassive process, with no significant passive absorption kinetics and its concentration-dependent permeability. A good correlation (r 2=0.88) between observed human absorption fraction and calculated (from in situ rat intestine) human absorption fraction was obtained.

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Author notes

  1. Jitender Madan

    Present address: Division of Pharmaceutics, Central Drug Research Institute, Chattar Manzil Place, 226001, Lucknow, India

Authors and Affiliations

  1. Department of Pharmaceutical Technology (Formulations), National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, S.A.S. Nagar, 160 062, Punjab, India

    Jitender Madan, Garima Chawla & Arvind K. Bansal

  2. Ranbaxy Research Laboratories, Plot No. 20, Sector 18, Udyog Vihar Industrial Area, 122 001, Gurgaon, Haryana, India

    Vinod Arora & Rajiv Malik

Authors
  1. Jitender Madan
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  2. Garima Chawla
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  3. Vinod Arora
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  4. Rajiv Malik
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  5. Arvind K. Bansal
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Corresponding author

Correspondence to Arvind K. Bansal.

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Published: September 2, 2005

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Madan, J., Chawla, G., Arora, V. et al. Unbiased membrane permeability parameters for gabapentin using boundary layer approach. AAPS J 7, 21 (2005). https://doi.org/10.1208/aapsj070121

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  • DOI: https://doi.org/10.1208/aapsj070121

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