Pharmacological and pharmacokinetic evaluation of celecoxib prodrugs in rats

@article{Mamidi2002PharmacologicalAP,
  title={Pharmacological and pharmacokinetic evaluation of celecoxib prodrugs in rats},
  author={R. Mamidi and R. Mullangi and J. Kota and Ravikanth Bhamidipati and Ansar A. Khan and K. Katneni and Srinivasaraju Datla and Sunil K. Singh and Koteswar Y. Rao and C. Seshagiri Rao and N. Srinivas and R. Rajagopalan},
  journal={Biopharmaceutics & Drug Disposition},
  year={2002},
  volume={23}
}
This study demonstrates the utility of an in vitro – in vivo correlative approach in the selection and optimization of a prodrug candidate of celecoxib (CBX), a COX2 inhibitor. As an initial screening step, a comparative single oral dose pharmacokinetic study was conducted in rats for CBX and its three aliphatic acyl water‐soluble prodrugs viz., CBX‐acetyl (CBX‐AC), CBX‐propionyl (CBX‐PR) and CBX‐butyryl (CBX‐BU) at high equimolar dose, 100 mg/kg. Only CBX‐BU and CBX‐PR converted rapidly to CBX… Expand
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