Moretti M D, Gavini E, Juliano C, Pirisino G, Giunchedi P
Dipartimento di Scienze del Farmaco, Università di Sassari, Italy.
J Microencapsul. 2001 Jan-Feb;18(1):111-21. doi: 10.1080/026520401750038647.
In this study, microspheres were prepared by a spray-drying technique using solutions of ketoprofen and two polymers, cellulose acetate butyrate (CAB) and hydroypropylmethylcellulose phthalate (HPMCP), in different weight ratios. Different total concentrations were used in the feed solutions: 3, 6 and 9% w/v. The spray-dried microparticles were characterized in terms of shape (SEM), size (light scattering method), production yield and encapsulation efficiency. They were formulated into capsules; tablets were prepared by direct compression of the microparticles mixed with maltose and, in some cases, hydroypropylmethylcellulose (HPMC). In vitro release studies were performed both at acidic and neutral pHs. The spray-drying process of solutions of ketoprofen with polymeric blends of cellulose derivatives leads to microparticles which, depending on their final formulation (capsules or tablets), can give a rapid or prolonged drug release. The formulations here described can be proposed for the oral administration of NSAIDs.
在本研究中，采用喷雾干燥技术，使用酮洛芬与两种聚合物（醋酸丁酸纤维素（CAB）和邻苯二甲酸羟丙基甲基纤维素（HPMCP））以不同重量比配制的溶液制备微球。进料溶液中使用了不同的总浓度：3%、6%和9%（w/v）。通过形状（扫描电子显微镜）、尺寸（光散射法）、产率和包封效率对喷雾干燥的微粒进行表征。将它们制成胶囊；通过直接压制与麦芽糖混合的微粒来制备片剂，在某些情况下还会加入羟丙基甲基纤维素（HPMC）。在酸性和中性pH值条件下进行体外释放研究。酮洛芬与纤维素衍生物聚合物共混物溶液的喷雾干燥过程会产生微粒，根据其最终剂型（胶囊或片剂），这些微粒可以实现药物的快速或长效释放。本文所述的制剂可用于非甾体抗炎药的口服给药。
