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Improving of the accuracy of in vitro-in vivo linear correlation using kinetic models for ultra sustained release theophylline tablets

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Summary

The objective of the current study was to establish and evaluate a new technique to increase the accuracy of the in vitro/in vivo linear correlation of single and multiple dose ultra-sustained release theophylline (USRT) preparation (Xantium®) in hospitalized patients. In vitro, dissolution data for theophylline were collected for 24 h using a USP I (basket) and USP II (paddle) methods. In vivo plasma concentration data were obtained from 8 patients after administration of either single or multiple doses of theophylline. Both in vitro and in vivo results were evaluated by zero-order, first-order, RRSBW, Hixson-Crowell Higuchi, Hopfenberg, Langenbucher, modified Langenbucher and (Bt)a kinetic models. The individual linear correlations between each in vitro and in vivo percent results and their kinetic distributions were established and regression equations were, obtained. The determination coefficient results of the linear kinetic correlations were found to be 0.994 and 0.997 for single and multiple doses by basket method and 0.992 and 0.998 for single and multiple doses by paddle method, respectively. Furthermore, the results of the linear correlations were found as 0.953 and 0.950 for single and multiple doses by basket method and 0.963 and 0.962 for single and multiple doses by paddle method respectively. Therefore, this study suggested that the accuracy of the linear correlation could be improved significantly by using linear kinetic correlation.

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Authors and Affiliations

  1. Center for Drug R&D and Pharmacokinetic Applications, University of Ege, Bornova, Izmir, Turkey

    E. Karasulu & I. Tuglular

  2. Izmir Training Hospital for Thoracic Medicine and Surgery, Yenisehir, Izmir, Turkey

    S. Aktogu

  3. Faculty of Pharmacy, Department of Pharmaceutical Technology, University of Ege, Bornova, Izmir, Turkey

    H. Y. Karasulu & G. Ertan

  4. Department of Biochemistry, Social Insurance Training Hospital, Buca, Izmir, Turkey

    A. Aydogdu

  5. Faculty of Pharmacy, Department of Biopharmacy and Pharmacokinetics, University of Ege, Bornova, 35100, Izmir, Turkey

    E. Karasulu

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  1. E. Karasulu
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  2. S. Aktogu
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  3. H. Y. Karasulu
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Karasulu, E., Aktogu, S., Karasulu, H.Y. et al. Improving of the accuracy of in vitro-in vivo linear correlation using kinetic models for ultra sustained release theophylline tablets. European Journal of Drug Metabolism and Pharmacokinetics 28, 301–307 (2003). https://doi.org/10.1007/BF03220183

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  • DOI: https://doi.org/10.1007/BF03220183

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