结肠癌靶向美洛昔康的新型多粒子系统

E. Ruiz, Covadonga Álvarez, J. Rodriguez, S. Durán, S. Durán, Dellias Pm
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引用次数: 3

摘要

美洛昔康(MLX)是一种非甾体抗炎药(NSAIDs)来自奥昔康家族。这组非甾体抗炎药被广泛用于治疗类风湿关节炎和术后炎症,被认为是良好的抗氧化剂。近年来,它们在化学预防、化学抑制、紫外线敏化和紫外线保护方面的活性也得到了证实。MLX被描述为COX-2选择性抑制剂。它的使用在选择性方面具有一定的优势,即对胃肠道的攻击和抗凝血活性的不良影响较小。由于MLX在结肠中有更好的吸收,其抗结肠癌和结肠炎性疾病的特性正在研究中,研究一种新的MLX结肠给药配方是很有意义的。我们正在研究不同组合制剂在pH值1.2、6.8和7.4时的溶解度和溶出度,以模拟它们在结肠中的吸收。这些配方由不同的赋形剂组成,提供pH值和时间依赖性的递送,如纤维素(Metolose®)和季铵盐基的甲基丙烯酸酯(EUDRAGIT®RS 30D, EUDRAGIT®FS 30D和EUDRAGIT®NM 30D)。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
New Multi-Particle Systems for Colon-Targeted Meloxicam
Meloxicam (MLX) is a non-steroidal anti-inflammatory drug (NSAIDs) from the Oxicam family. This group of NSAIDs has been highly used in the treatment of rheumatoid arthritis and post-operative inflammation and is known as good antioxidants. Recently, their activity in chemoprevention, chemo-suppression, UV-sensitization and UVprotection was also identified. MLX has been described as a COX-2 selective inhibitor. Its use has some advantages regarding to its selectivity, namely, less adverse effects as gastrointestinal aggression and anticlotting activity. As MLX is better absorbed in colon and its properties against colon cancer and colonic inflammatory diseases are being studied, it is interesting to investigate a new MLX formulation for colonic delivery. We are studying the solubility and the dissolution of different combined formulations at pH 1.2, 6.8 and 7.4 to mimic their absorbance in the colon. These formulations are composed by different excipients that provide pH and time-dependent deliveries such as cellulose (Metolose®) and methacrylic acid esters with quaternary ammonium groups (EUDRAGIT® RS 30D, EUDRAGIT® FS 30D and EUDRAGIT® NM 30D).
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