Pharmacological and pharmacokinetic evaluation of celecoxib prodrugs in rats

  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},
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
28 Citations
Oral bioavailability and pharmacokinetics of DRF-4367, a new cox-2 inhibitor in rats
  • 1
hemical and in vitro enzymatic stability of newly synthesized celecoxib ipophilic and hydrophilic amides mjad
  • mjad M. Qandil, Farah H. El Mohtadib, Bassam M. Tashtoushb
  • 2011
A double prodrug system for colon targeting of benzenesulfonamide COX-2 inhibitors.
  • 15
  • PDF
Prodrugs of Nonsteroidal Anti-Inflammatory Drugs (NSAIDs), More Than Meets the Eye: A Critical Review
  • A. Qandil
  • Chemistry, Medicine
  • International journal of molecular sciences
  • 2012
  • 67
  • PDF


Clinical Pharmacokinetics and Pharmacodynamics of Celecoxib
  • 269
  • PDF
Phase I and pharmacokinetic study of etoposide phosphate
  • 14
Pharmacological and biochemical demonstration of the role of cyclooxygenase 2 in inflammation and pain.
  • 1,456
  • PDF
Etoposide phosphate: what, why, where, and how?
  • 89
Mechanism of selective inhibition of the inducible isoform of prostaglandin G/H synthase.
  • 385
  • PDF