申请人:Rariy V. Roman
公开号:US20070116757A1
公开(公告)日:2007-05-24
Pharmaceutical compositions comprising a fatty acid salt, a dicarboxylic acid salt, an alkyl sulfate salt, an aryl sulfate salt or an alkyl aryl sulfonate salt of methylene blue or a derivative of methylene blue are described herein. The compositions are preferably administered orally and can be administered as tablets, soft or hard shell capsules (e.g. soft gelatin capsules), suspensions or solutions. The composition can also be formulated as a suppository or enema or rectal administration. The compositions further comprise a pharmaceutically acceptable carrier and optionally one or more pharmaceutically acceptable excipients. Suitable excipients include diluents, binders, plasticizers, lubricants, disintegrants, colorants, stabilizers, surfactants, and combinations thereof. The fatty acid salts, alkyl sulate salts, aryl sulfate salts or alkyl aryl sulfonate salts can be co-mixed or co-melted with one or more fatty acids to make more hydrophobic compositions, which may result in less staining formulations. The compositions can be formulated for immediate release, controlled release such as extended release, delayed release, and pulsatile release, or combinations thereof. In one embodiment, the derivative of methylene blue is methylene dodecylsulfate.
本文描述了包含脂肪酸盐、二羧酸盐、烷基硫酸盐、芳基硫酸盐或烷基芳基磺酸盐的甲蓝或甲蓝衍生物的制药组合物。这些组合物最好是口服给药,可以制成片剂、软壳或硬壳胶囊(例如软明胶胶囊)、悬浮液或溶液进行给药。该组合物也可以制成栓剂或灌肠剂或直肠给药。这些组合物还包括一种药用可接受载体,以及可选地一种或多种药用可接受的辅料。适用的辅料包括稀释剂、粘结剂、增塑剂、润滑剂、崩解剂、色素、稳定剂、表面活性剂以及它们的组合。脂肪酸盐、烷基硫酸盐、芳基硫酸盐或烷基芳基磺酸盐可以与一种或多种脂肪酸共混或共熔,制成更疏水的组合物,这可能导致更少的染色配方。这些组合物可以制成即时释放、控制释放(如延长释放)、延迟释放和脉冲释放,或者以上述的组合形式。在一个实施例中,甲蓝的衍生物是十二烷基硫酸甲蓝。