Uner Melike, Gönüllü Umit, Yener Gülgün, Altinkurt Turan
Faculty of Pharmacy, Department of Pharmaceutical Technology, Istanbul University, Beyazit, 34119 Istanbul, Turkey.
Farmaco. 2005 Jan;60(1):27-31. doi: 10.1016/j.farmac.2004.08.008. Epub 2004 Nov 5.
Solid lipid ketoprofen micropellets (SLKM) at different drug/beeswax ratios [(1:1) and (1:2)] were prepared by emulsion congealing technique and then compressed into tablets. Ketoprofen in solid state was incorporated into the melted beeswax at 90 degrees C and the mixture was emulsified in the hot aqueous Tween 80 solution by stirring at a constant rate. The SLKM were obtained by cooling the coarse emulsion down to room temperature and filtering. Drug entrapment efficiency and particle size analysis by laser diffractometry (LD) were determined, and existence of a drug-lipid interaction was investigated by differential scanning calorimetry (DSC) on the SLKM, before being compressed into the tablets by direct compression method. Finally, in vitro release studies were performed and the release kinetics of the waxy tablets were calculated. A commercial ketoprofen retard tablet (reference: Profenid Retard 200 mg) was also examined to compare the release properties. While the data obtained from DSC were indicating absence of drug-lipid interaction in the SLKM, it was determined that 28.62% (+/-2.08), 38.60% (+/-1.91) and 47.00% (+/-1.82) of ketoprofen was released from the tablets containing (1:2) and (1:1) SLKM and Profenid Retard 200 mg in pH 7.4 phosphate buffer solution after 8 h, respectively.
采用乳化冷凝技术制备了不同药物/蜂蜡比例(1:1和1:2)的固体脂质酮洛芬微丸(SLKM),然后将其压制成片剂。将固态酮洛芬在90℃下加入到熔化的蜂蜡中,通过恒速搅拌在热的吐温80水溶液中乳化该混合物。通过将粗乳液冷却至室温并过滤得到SLKM。在通过直接压片法将SLKM压制成片剂之前,测定了药物包封率并通过激光衍射法(LD)进行了粒度分析,并通过差示扫描量热法(DSC)研究了SLKM中药物-脂质相互作用的存在。最后,进行了体外释放研究并计算了蜡质片剂的释放动力学。还检测了市售的酮洛芬缓释片(对照:Profenid Retard 200 mg)以比较释放特性。虽然从DSC获得的数据表明SLKM中不存在药物-脂质相互作用,但发现在pH 7.4的磷酸盐缓冲溶液中,含(1:2)和(1:1)SLKM的片剂以及Profenid Retard 200 mg的片剂在8小时后分别释放了28.62%(±2.08)、38.60%(±1.91)和47.00%(±1.82)的酮洛芬。