Babar A, Bellete T, Plakogiannis F M
Division of Pharmaceutics and Industrial Pharmacy, Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, New York 11201, USA.
Drug Dev Ind Pharm. 1999 Feb;25(2):241-5. doi: 10.1081/ddc-100102166.
In vitro release of ketoprofen from suppository bases and in vivo absorption in rabbits were studied. Suppositories containing 50 mg of ketoprofen were prepared using theobroma oil, esterified (c10-c18) fatty acids, and polyethylene glycol 1000 bases. The displacement values of the drug were determined and found to be of the order of theobroma oil > esterified (c10-c18) fatty acids and polyethylene glycol 1000 bases. The suppository hardness data revealed that the theobroma oil base produced relatively brittle suppositories. Using the USP dissolution method, the release of ketoprofen was observed to be greatest from polyethylene glycol 1000 suppositories. With the dialysis technique, the maximum release of drug was obtained from theobroma oil suppository containing polysorbate 40 at a 6% level. Selected suppository formulations were evaluated for rectal absorption studies in rabbits. The in vivo data showed that the optimum drug absorption took place from the polyethylene glycol 1000 base and theobroma oil formulation containing 6% polysorbate 40.
研究了酮洛芬从栓剂基质中的体外释放及在兔体内的吸收情况。使用可可脂、酯化（C10 - C18）脂肪酸和聚乙二醇1000基质制备了含50mg酮洛芬的栓剂。测定了药物的置换值，发现其顺序为可可脂>酯化（C10 - C18）脂肪酸和聚乙二醇1000基质。栓剂硬度数据显示，可可脂基质产生的栓剂相对较脆。采用美国药典溶出度方法，观察到聚乙二醇1000栓剂中酮洛芬的释放最大。采用透析技术，在含6%聚山梨酯40的可可脂栓剂中获得了药物的最大释放量。对选定的栓剂配方进行了兔直肠吸收研究评估。体内数据表明，最佳药物吸收发生在聚乙二醇1000基质和含6%聚山梨酯40的可可脂配方中。
