BIOMAT Database Logo BIOMAT Database Logo

Efficacy of a new topical gel-spray formulation of ketoprofen lysine salt in the rat: percutaneous permeation in vitro and in vivo and pharmacological activity. 1998

S Porzio, and G Caselli, and L Pellegrini, and V Pallottini, and M Del Rosario, and A Coppola, and L Boltri, and M Gentile, and G Clavenna, and G Melillo
Dompé S.p.A., Research Center, L'Aquila, Italy.

The aim of this study was to evaluate the percutaneous permeation of a new topical Gel-Spray formulation, containing 15% of ketoprofen lysine salt (KLS), both in vitro, using the Franz-type diffusion cells and in vivo, by evaluating urinary recovery after topical administration and to correlate the absorption data with KLS pharmacological activity in the rat. Concentrations of ketoprofen free acid (KFA) were determined by HPLC in the receptor compartment (in vitro), or in urine (in vivo). The permeation of ketoprofen evaluated in vitro after the application of KLS Gel-Spray was higher than that observed with the marketed formulation Profénid gel (containing KFA at 2.5%). The same evidence was found in vivo, except when the ratio between the administered dose and the area treated was higher than 1 mg cm-2. Thus, the difference between the two formulations seems to be the resultant of two opposing components: a positive gradient of concentration that favours the absorption of ketoprofen from KLS Gel-Spray and the presence of the enhancer ethanol that could favour the efficacy of Profénid gel. Under our conditions the former prevailed. As for the efficacy, evaluated in the carrageenan-induced oedema and hyperalgesia model, KLS Gel-Spray confirmed the data obtained for in vivo absorption, being more efficient than the reference standard Profénid gel. The observed inhibitory effects were due only to dermal absorption, oral absorption was excluded by an Elizabethan collar applied around the neck of the rat. In these experimental conditions, no significant damage of the rat stomach mucosa was observed. These results indicate that KLS Gel-Spray, due to its high KLS concentration, allows a very high efficiency in delivering ketoprofen to the inflamed area using a minimal amount of formulation, even in the absence of permeation enhancers.

UI MeSH Term Description Entries
D007249 Inflammation A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function. Innate Inflammatory Response,Inflammations,Inflammatory Response, Innate,Innate Inflammatory Responses
D007660 Ketoprofen An IBUPROFEN-type anti-inflammatory analgesic and antipyretic. It is used in the treatment of rheumatoid arthritis and osteoarthritis. Benzoylhydratropic Acid,19,583 RP,2-(3-Benzoylphenyl)propionic Acid,Alrheumat,Alrheumum,Orudis,Profenid,RP-19583,RP 19583,RP, 19,583,RP19583
D008239 Lysine An essential amino acid. It is often added to animal feed. Enisyl,L-Lysine,Lysine Acetate,Lysine Hydrochloride,Acetate, Lysine,L Lysine
D005260 Female Females
D005782 Gels Colloids with a solid continuous phase and liquid as the dispersed phase; gels may be unstable when, due to temperature or other cause, the solid phase liquefies; the resulting colloid is called a sol.
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000894 Anti-Inflammatory Agents, Non-Steroidal Anti-inflammatory agents that are non-steroidal in nature. In addition to anti-inflammatory actions, they have analgesic, antipyretic, and platelet-inhibitory actions. They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins. Inhibition of prostaglandin synthesis accounts for their analgesic, antipyretic, and platelet-inhibitory actions; other mechanisms may contribute to their anti-inflammatory effects. Analgesics, Anti-Inflammatory,Aspirin-Like Agent,Aspirin-Like Agents,NSAID,Non-Steroidal Anti-Inflammatory Agent,Non-Steroidal Anti-Inflammatory Agents,Nonsteroidal Anti-Inflammatory Agent,Anti Inflammatory Agents, Nonsteroidal,Antiinflammatory Agents, Non Steroidal,Antiinflammatory Agents, Nonsteroidal,NSAIDs,Nonsteroidal Anti-Inflammatory Agents,Agent, Aspirin-Like,Agent, Non-Steroidal Anti-Inflammatory,Agent, Nonsteroidal Anti-Inflammatory,Anti-Inflammatory Agent, Non-Steroidal,Anti-Inflammatory Agent, Nonsteroidal,Anti-Inflammatory Analgesics,Aspirin Like Agent,Aspirin Like Agents,Non Steroidal Anti Inflammatory Agent,Non Steroidal Anti Inflammatory Agents,Nonsteroidal Anti Inflammatory Agent,Nonsteroidal Anti Inflammatory Agents,Nonsteroidal Antiinflammatory Agents
D012867 Skin The outer covering of the body that protects it from the environment. It is composed of the DERMIS and the EPIDERMIS.
D012869 Skin Absorption Uptake of substances through the SKIN. Absorption, Skin,Intracutaneous Absorption,Intradermal Absorption,Percutaneous Absorption,Transcutaneous Absorption,Transdermal Absorption,Absorption, Intracutaneous,Absorption, Intradermal,Absorption, Percutaneous,Absorption, Transcutaneous,Absorption, Transdermal,Absorptions, Intracutaneous,Absorptions, Intradermal,Absorptions, Percutaneous,Absorptions, Skin,Absorptions, Transcutaneous,Absorptions, Transdermal,Intracutaneous Absorptions,Intradermal Absorptions,Percutaneous Absorptions,Skin Absorptions,Transcutaneous Absorptions,Transdermal Absorptions
D013270 Stomach An organ of digestion situated in the left upper quadrant of the abdomen between the termination of the ESOPHAGUS and the beginning of the DUODENUM. Stomachs

Related Publications

S Porzio, and G Caselli, and L Pellegrini, and V Pallottini, and M Del Rosario, and A Coppola, and L Boltri, and M Gentile, and G Clavenna, and G Melillo
Effect of formulation variables on the percutaneous permeation of ketoprofen from gel formulations.
January 2000, Drug delivery,
S Porzio, and G Caselli, and L Pellegrini, and V Pallottini, and M Del Rosario, and A Coppola, and L Boltri, and M Gentile, and G Clavenna, and G Melillo
[Pharmacologic and pharmacokinetic activity of ketoprofen lysine salt for topical administration].
February 1983, Il Farmaco; edizione pratica,
S Porzio, and G Caselli, and L Pellegrini, and V Pallottini, and M Del Rosario, and A Coppola, and L Boltri, and M Gentile, and G Clavenna, and G Melillo
Effects of a new foam formulation of ketoprofen lysine salt in experimental models of inflammation and hyperalgesia.
May 1995, Arzneimittel-Forschung,
S Porzio, and G Caselli, and L Pellegrini, and V Pallottini, and M Del Rosario, and A Coppola, and L Boltri, and M Gentile, and G Clavenna, and G Melillo
Physical characteristics, pharmacological properties and clinical efficacy of the ketoprofen patch: a new patch formulation.
July 2011, European review for medical and pharmacological sciences,
S Porzio, and G Caselli, and L Pellegrini, and V Pallottini, and M Del Rosario, and A Coppola, and L Boltri, and M Gentile, and G Clavenna, and G Melillo
Formulation development, in vitro and in vivo evaluation of microemulsion-based gel loaded with ketoprofen.
January 2015, Drug delivery,
S Porzio, and G Caselli, and L Pellegrini, and V Pallottini, and M Del Rosario, and A Coppola, and L Boltri, and M Gentile, and G Clavenna, and G Melillo
Formulation and in vitro/in vivo evaluation of chitosan-based film forming gel containing ketoprofen.
November 2017, Drug delivery,
S Porzio, and G Caselli, and L Pellegrini, and V Pallottini, and M Del Rosario, and A Coppola, and L Boltri, and M Gentile, and G Clavenna, and G Melillo
Formulation of meloxicam gel for topical application: In vitro and in vivo evaluation.
June 2010, Acta pharmaceutica (Zagreb, Croatia),
S Porzio, and G Caselli, and L Pellegrini, and V Pallottini, and M Del Rosario, and A Coppola, and L Boltri, and M Gentile, and G Clavenna, and G Melillo
Unexpected Salt/Cocrystal Polymorphism of the Ketoprofen-Lysine System: Discovery of a New Ketoprofen-l-Lysine Salt Polymorph with Different Physicochemical and Pharmacokinetic Properties.
June 2021, Pharmaceuticals (Basel, Switzerland),
S Porzio, and G Caselli, and L Pellegrini, and V Pallottini, and M Del Rosario, and A Coppola, and L Boltri, and M Gentile, and G Clavenna, and G Melillo
[Efficacy and tolerability of ketoprofen lysine salt foam for topical use in the treatment of traumatic pathologies of the locomotor apparatus].
September 1992, La Clinica terapeutica,
S Porzio, and G Caselli, and L Pellegrini, and V Pallottini, and M Del Rosario, and A Coppola, and L Boltri, and M Gentile, and G Clavenna, and G Melillo
Ketoprofen lysine salt inhibits disuse-induced osteopenia in a new non-traumatic immobilization model in the rat.
January 1996, Pharmacological research,
Copied contents to your clipboard!