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Pharmacokinetics of colon-specific pH and time-dependent flurbiprofen tablets

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Abstract

Present research deals with the development of compression-coated flurbiprofen colon-targeted tablets to retard the drug release in the upper gastro intestinal system, but progressively release the drug in the colon. Flurbiprofen core tablets were prepared by direct compression method and were compression coated using sodium alginate and Eudragit S100. The formulation is optimized based on the in vitro drug release study and further evaluated by X-ray imaging and pharmacokinetic studies in healthy humans for colonic delivery. The optimized formulation showed negligible drug release (4.33 ± 0.06 %) in the initial lag period followed by progressive release (100.78 ± 0.64 %) for 24 h. The X-ray imaging in human volunteers showed that the tablets reached the colon without disintegrating in the upper gastrointestinal tract. The C max of colon-targeted tablets was 12,374.67 ng/ml at T max 10 h, where as in case of immediate release tablets the C max was 15,677.52 ng/ml at T max 3 h, that signifies the ability of compression-coated tablets to target the colon. Development of compression-coated tablets using combination of time-dependent and pH-sensitive approaches was suitable to target the flurbiprofen to colon.

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Acknowledgments

The authors acknowledge FDC Limited, Mumbai, India and Matrix laboratories, Hyderabad, India for gift sample of Flurbiprofen, Sodium alginate and Eudragit S100. The authors also thank the Principal and Management, Jangaon Institute of Pharmaceutical Sciences for providing the facilities.

Conflict of interest

The authors report no conflicts of interest.

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Authors and Affiliations

  1. Department of Pharmaceutics, Chaitanya College of Pharmacy Education and Research, Kishanpura, Hanamkonda, Warangal, 506001, Andhra Pradesh, India

    Sateesh Kumar Vemula, Prabhakar Reddy Veerareddy & Venkat Ratnam Devadasu

  2. Department of Pharmaceutics, Jangaon Institute of Pharmaceutical Sciences, Yeshwanthapur, Jangaon, Warangal, 506167, Andhra Pradesh, India

    Sateesh Kumar Vemula

  3. College of Pharmacy Palamuru University, Mahabubnagar, Andhra Pradesh, India

    Prabhakar Reddy Veerareddy

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  1. Sateesh Kumar Vemula
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  2. Prabhakar Reddy Veerareddy
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  3. Venkat Ratnam Devadasu
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Correspondence to Sateesh Kumar Vemula.

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Vemula, S.K., Veerareddy, P.R. & Devadasu, V.R. Pharmacokinetics of colon-specific pH and time-dependent flurbiprofen tablets. Eur J Drug Metab Pharmacokinet 40, 301–311 (2015). https://doi.org/10.1007/s13318-014-0210-0

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  • DOI: https://doi.org/10.1007/s13318-014-0210-0

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