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Solid self-microemulsifying formulation for candesartan cilexetil.

Vijaykumar Nekkanti1, Pradeep Karatgi, Raghavendra Prabhu

  • 1NCE Product Development, Integrated Product Development Organization, Dr Reddy's Laboratories Limited, Innovation Plaza, Bachupally, Qutubullapur, Hyderabad 500072, India.

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|December 17, 2009
PubMed
Summary
This summary is machine-generated.

Developing self-microemulsifying drug delivery systems (SMEDDS) for candesartan cilexetil improved its solubility and dissolution. Solid SMEDDS formulations demonstrated enhanced drug release compared to commercial tablets, showing potential for increased bioavailability.

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Physical Pharmacy

Background:

  • Poorly water-soluble drugs like candesartan cilexetil present bioavailability challenges.
  • Developing effective drug delivery systems is crucial for enhancing therapeutic efficacy.

Purpose of the Study:

  • To develop and characterize self-microemulsifying drug delivery systems (SMEDDS) of candesartan cilexetil.
  • To evaluate the potential of SMEDDS for improving drug solubility, dissolution, and bioavailability.
  • To convert liquid SMEDDS into a solid dosage form for capsule filling.

Main Methods:

  • Solubility studies of candesartan cilexetil in various non-aqueous carriers.
  • Construction of pseudoternary phase diagrams to identify self-microemulsification regions.
  • Formulation and characterization of liquid SMEDDS, including droplet size and zeta potential.
  • Conversion of liquid SMEDDS to solid intermediates by adsorption onto a carrier.
  • Dissolution testing of solid SMEDDS capsules compared to liquid and commercial formulations.

Main Results:

  • Optimized SMEDDS formulations were successfully prepared.
  • The conversion of liquid SMEDDS to solid intermediates did not affect self-emulsifying properties.
  • Solid SMEDDS formulations exhibited comparable dissolution rates to liquid SMEDDS.
  • Drug dissolution from solid SMEDDS was significantly higher than from the commercial tablet.

Conclusions:

  • SMEDDS are a viable approach for enhancing the solubility and dissolution of candesartan cilexetil.
  • The conversion to a solid form maintains the self-emulsifying characteristics and improves drug release.
  • This approach holds promise for improving the oral bioavailability of poorly soluble drugs.