Romero A J, Rhodes C T
Université de Rhode Island, Faculté de Pharmacie, Département de Pharmacie Galénique et Biopharmacie, Kingston 02881.
J Pharm Belg. 1993 Jan-Feb;48(1):27-32.
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.
为不断优化布洛芬抗炎治疗，已开展了布洛芬活性立体异构体的研发研究。研究了药物加工对消旋体（消旋布洛芬）和对映体（S(+)-布洛芬）的影响。采用湿法制粒无法制备新的立体特异性系统制剂。采用直接压片法开发S(+)-布洛芬似乎是解决这一问题的切实可行方案。所得片剂的生物药剂学性质完全符合药典要求。然而，将S(+)-布洛芬与辅料混合会导致熔融焓下降，压片后差示扫描量热法吸热曲线上出现低温低共熔物。老化研究表明，S(+)-布洛芬的原料和药物混合物应在严格控制的条件下储存或立即进行加工。
