[Efforts toward the formulation of the therapeutic stereoisomer of ibuprofen].
In an on going effort to optimize ibuprofen antiinflammatory therapy, development studies on the active stereoisomer of ibuprofen have been conducted. The effects of pharmaceutical processing on the racemate (RAC-ibuprofen) and the enantiomer (S(+)-ibuprofen) were investigated. The formulation of the new stereospecific system, was impossible using wet granulation. The pharmaceutical development of S(+)-ibuprofen using direct compression appeared as a practical solution to this problem. The biopharmaceutical properties of the resulting tablets were well within pharmacopeia requirements. Nevertheless, mixing S(+)-ibuprofen with the excipients induced a drop in the enthalpy of fusion and after compaction, a low temperature eutectic appeared on the differential scanning calorimetry endotherms. Aging studies indicated that the raw material and pharmaceutical mixtures of S(+)-ibuprofen should be stored under strictly controlled conditions or processed immediately.
Romero
A J
AJ
Université de Rhode Island, Faculté de Pharmacie, Département de Pharmacie Galénique et Biopharmacie, Kingston 02881.
Rhodes
C T
CT
D007052:Ibuprofen / Q000008:administration & dosage / Q000737:chemistry*; D013237:Stereoisomerism
D007052:Ibuprofen
Efforts de formulation du stéréoisomère thérapeutique de l'ibuprofène.