Dexibuprofen enteric film-coated tablets: design, characterization and pharmacokinetic analysis in human volunteers

Pharm Dev Technol. 2024 Oct;29(8):832-840. doi: 10.1080/10837450.2024.2398537. Epub 2024 Sep 4.

Abstract

Objective: This study aimed to develop a stable and scalable enteric film-coated tablet for the gastric irritant dexibuprofen.

Methods: Utilizing direct compression with super-disintegration (crospovidone), the optimal core batches were coated with Opadry white seal coat and enterically coated with Eudragit®L100 with pigment (Talc), demonstrating a 12% weight increase; release and integrity were assessed using specific pH buffers and SEM, with stability testing confirming a six-month shelf life at 40 °C and 75% RH.

Results: The optimized formulation achieved 99.87% release in phosphate buffer within 60 min, maintained integrity for 120 min in acidic conditions, and exhibited superior bioavailability compared to Innovifen with relative bioavailability ≈of 121% and elevated Cmax (18.35 µg/ml compared to 11.1 µg/ml).

Conclusion: These results highlight the potential of this formulation to enhance patient safety and efficacy through delayed enteric technology and fast intestinal release.

Keywords: Dexibuprofen; Eudragit®L-100; Opadry ®II; direct compression; enteric tablets; pharmacokinetics.

MeSH terms

  • Adult
  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics
  • Biological Availability*
  • Chemistry, Pharmaceutical / methods
  • Drug Liberation
  • Drug Stability
  • Healthy Volunteers
  • Humans
  • Ibuprofen* / administration & dosage
  • Ibuprofen* / analogs & derivatives
  • Ibuprofen* / chemistry
  • Ibuprofen* / pharmacokinetics
  • Male
  • Polymethacrylic Acids / chemistry
  • Polymethacrylic Acids / pharmacokinetics
  • Tablets, Enteric-Coated*
  • Young Adult

Substances

  • Tablets, Enteric-Coated
  • Ibuprofen
  • dexibuprofen
  • Anti-Inflammatory Agents, Non-Steroidal
  • methylmethacrylate-methacrylic acid copolymer
  • Polymethacrylic Acids