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Bioavailability, bioequivalence, and in vitro–in vivo correlation of oxybutynin transdermal patch in rabbits

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Abstract

The first objective of the proposed research work includes comparative bioavailability and bioequivalence evaluation of oxybutynin transdermal patch with respect to different permeation enhancers. The second objective was to evaluate different in vitro methods along with synthetic membranes toward development of an in vitro–in vivo correlation. Oleic acid (fatty acid), Soluphor P (2-pyrrolidone, cosolvent), menthol (volatile oil), and dipropylene glycol (plasticizer) were selected as representatives from different classes of permeation enhancers. A random, crossover, single-dose pharmacokinetic study was carried out on male New Zealand white rabbits to determine bioavailability and bioequivalence. The obtained pharmacokinetic data were correlated with in vitro drug release using convolution–deconvolution approach. All developed formulations were found to be bioequivalent with respect to the marketed patch (Oxytrol®) on the basis of level of C max, AUC0–96, and AUCtotal (0.8–1.25). A biphasic linear correlation was obtained pertaining to differential diffusion behavior of the drug in vivo during the experimental timeframe. Because of close resemblance to skin, Cuprophan® membrane was found to be more suitable for developing an IVIVC than Millipore® membrane.

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Acknowledgments

The authors would like to acknowledge the All India Council for Technical Education (AICTE) and TEQIP Phase II for providing lab facilities. The authors would like to thank CSIR, Govt. of India, for providing funding (letter no. 9/991 (0019) 2K12-EMR-I dated 28/02/2012). The authors would also like to thank Dr. Rahul Choudhari and Mahindra Ganu for teaching rabbit handling, physiology, and blood sampling from the ear vein of rabbits. The authors are also thankful to Watson Pharma, India, for providing the gift sample of oxybutynin.

Conflict of interest

This research work is part of doctoral studies of Mr. Achyut Sharad Khire. The authors declare no conflict of interest. The authors declare that the experiments performed on laboratory animals comply with the guidelines of the institutional animal ethics committee.

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  1. Center for Novel Drug Delivery Systems, Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Elite Status & Centre of Excellence—Govt. of Maharashtra, Matunga (E), Mumbai, 400019, India

    Achyut Khire & Pradeep Vavia

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  1. Achyut Khire
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  2. Pradeep Vavia
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Correspondence to Pradeep Vavia.

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Khire, A., Vavia, P. Bioavailability, bioequivalence, and in vitro–in vivo correlation of oxybutynin transdermal patch in rabbits. Drug Deliv. and Transl. Res. 4, 105–115 (2014). https://doi.org/10.1007/s13346-013-0170-y

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