Gai M N, Pezoa R, Corbeaux J, Arancibia A
Departamento de Ciencias y Tecnología Farmacéutica, Facultad de Ciencias Químicas y Farmacéuticas, Universidad de Chile, Santiago.
Farmaco. 1989 Nov;44(11):1119-26.
A 300 mg controlled-release theophylline formulation was developed as a tablet prepared by wet granulation using the acrylic resins Eudragit S 100R and Eudragit RSPMR. The tablet was compared with a marketed controlled-release capsule using in vivo and in vitro tests. The in vitro dissolution of theophylline from the tablets followed an apparent zero order kinetics. The in vivo comparison was performed in a cross over fashion in four healthy volunteers who received one tablet or capsule every 12 hours during seven days. The results showed no statistically significant differences in AUC, tmax and in plasma theophylline concentrations at the different times. Nevertheless, concentrations were lower after the administration of the tablets than when the volunteers received the capsules. On the other hand, the apparent elimination half lives obtained after the tablets were longer than with the capsules. An excessive retardation in the release of theophylline from the tablet could be responsible for this fact.
研发了一种300毫克的控释茶碱制剂，制成片剂，采用丙烯酸树脂Eudragit S 100R和Eudragit RSPMR通过湿法制粒制备。通过体内和体外试验将该片剂与市售控释胶囊进行比较。茶碱从片剂中的体外溶出遵循明显的零级动力学。体内比较以交叉方式在四名健康志愿者中进行，他们在七天内每12小时服用一片片剂或一粒胶囊。结果显示，AUC、tmax以及不同时间的血浆茶碱浓度无统计学显著差异。然而，服用片剂后的浓度低于志愿者服用胶囊时的浓度。另一方面，服用片剂后获得的表观消除半衰期比服用胶囊时长。茶碱从片剂中释放的过度延迟可能是造成这一现象的原因。
