Effects of a new foam formulation of ketoprofen lysine salt in experimental models of inflammation and hyperalgesia

Arzneimittelforschung. 1995 May;45(5):590-4.

Abstract

The anti-inflammatory and analgesic profile of a new topical foam formulation of ketoprofen lysine salt (CAS 57469-78-0, Artrosilene Schiuma, KLS-foam) was characterized in comparison with marketed gel formulations containing KLS (KLS-gel) or diclofenac diethylammonium salt (DCF-gel). KLS-foam dose-dependently inhibited oedema formation and hyperalgesia induced by subplantar injection of carrageenan or substance P, being more potent than KLS-gel. At equieffective anti-inflammatory doses, KLS-foam provided a more pronounced analgesic effect than DCF-gel. KLS-foam also markedly inhibited exudate formation and prostaglandin production induced by subcutaneous implantation of carrageenan soaked sponges. In carrageenan induced paw inflammation, KLS-foam provided the same anti-inflammatory effect as orally administered KLS, but induced significantly less gastric damages. Oral administration of KLS resulted in sustained systemic absorption of ketoprofen, whereas after topical application of KLS-foam no appreciable ketoprofen plasma levels were detected. These data support the anti-inflammatory and particularly the analgesic effectiveness of the new foam formulation of KLS, a finding that, together with the high gastric tolerability, further emphasizes the usefulness of KLS-foam in the treatment of localized flogistic diseases and associated pain.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics
  • Anti-Inflammatory Agents, Non-Steroidal / therapeutic use*
  • Carrageenan
  • Diclofenac / pharmacology
  • Exudates and Transudates / drug effects
  • Female
  • Gastric Mucosa / drug effects
  • Gels
  • Hyperalgesia / chemically induced
  • Hyperalgesia / drug therapy*
  • Hyperalgesia / pathology
  • Inflammation / chemically induced
  • Inflammation / drug therapy*
  • Inflammation / pathology
  • Ketoprofen / administration & dosage
  • Ketoprofen / analogs & derivatives*
  • Ketoprofen / pharmacokinetics
  • Ketoprofen / therapeutic use
  • Lysine / administration & dosage
  • Lysine / analogs & derivatives*
  • Lysine / pharmacokinetics
  • Lysine / therapeutic use
  • Male
  • Prostaglandins / biosynthesis
  • Rats
  • Rats, Sprague-Dawley
  • Substance P / metabolism

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Gels
  • Prostaglandins
  • Diclofenac
  • Substance P
  • ketoprofen lysine
  • Carrageenan
  • Ketoprofen
  • Lysine