Pharmaceutical Technology: Controlled Drug Release, Volume 2

6
Controlled release matrix tablets of ketoprofen
Paola Mura and Giampiero Bramanti
Department of Pharmaceutical Sciences, Via G.Capponi 9, Firenze, Italy
Luca Fabbri
Pharmaceutical Technology Laboratory, Menarini SaS, Via Sette Santi 3, Firenze, Italy
Maurizio Valleri
Pharmaceutical Technology Laboratory, Malesci SpA, Via Paisiello 8, Firenze, Italy
SUMMARY
To obtain a prolonged action dosage form of ketoprofen, three different techniques for delaying
drug release from hydrophilic matrices of hydroxypropylmethylcellulose were evaluated. They
were incorporation of glyceryl monostearate, as a release controller, partial coating with an
impermeable covering of cellulose acetate phthalate, and pan-spray coating with a mixture of
insoluble (Eudragit) and soluble (PEG 400) polymers. The in vitro release profiles of each
formulation were studies using the USP basket method. Pan-spray coating with the Eudragit-PEG
mixture was found to be the best technique, enabling the desired release profile to be obtained
through variation of the coating thickness.
INTRODUCTION
Ketoprofen (2-(3-benzoylphenyl)propionic acid), one of the most active non-steroidal antiinflammatory
drugs, is employed in the long-term treatment of rheumatoid arthritis and also as an
analgesic in the treatment of pain of varying origins [1]. Clinical use, however, requires a dose
schedule of 100–200 mg 3–4 times a day, the duration of action of a single oral dose being only 6–
8 h [2].
Development of a prolonged action dosage form of ketoprofen will bring about several
desirable therapeutic advantages: improvement of patient compliance; minimization of blood
level fluctuations; reduction of the total amount of drug administered; reduction of incidence of
both local and systemic adverse side effects [3].