Sinha V R, Kumria Rachna
University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India.
Drug Dev Ind Pharm. 2004 Feb;30(2):143-50. doi: 10.1081/ddc-120028709.
Matrix tablets were prepared using xanthan gum (XG) and guar gum (GG) in varying proportions, and the suitability of the prepared tablets was evaluated for colon specific drug delivery. Indomethacin was used as a model drug. The ability of the prepared matrices to retard drug release in the upper gastrointestinal tract (GIT) and to undergo enzymatic hydrolysis by the colonic bacteria was evaluated. For this, drug release studies were carried out in the presence of rat cecal content. Further cecal content of rats with induced enzymatic activity were used. To ascertain the role of bacterial flora in carrying out the hydrolysis of the tablet, cecal content of rats treated with antibiotics were used in the dissolution media. Presence of XG in combination with GG in the tablets could retard drug release in the conditions of the upper GIT. However, the presence of GG and starch made these matrices microbially degradable. Guar gum alone as a drug release-retarding excipient in the matrices does not achieve the desired retardation. Presence of XG in the tablets not only retards the initial drug release from the tablets, but due to high swelling, makes them more vulnerable to digestion by the microbial enzymes in the colon.
采用不同比例的黄原胶(XG)和瓜尔胶(GG)制备了基质片剂,并对所制备片剂用于结肠特定药物递送的适用性进行了评估。吲哚美辛用作模型药物。评估了所制备基质在上消化道(GIT)中延缓药物释放以及被结肠细菌进行酶解的能力。为此,在大鼠盲肠内容物存在的情况下进行了药物释放研究。还使用了具有诱导酶活性的大鼠的盲肠内容物。为确定细菌菌群在片剂水解过程中的作用,在溶出介质中使用了用抗生素处理过的大鼠的盲肠内容物。片剂中XG与GG联用可在上消化道条件下延缓药物释放。然而,GG和淀粉的存在使这些基质可被微生物降解。单独使用瓜尔胶作为基质中药物释放延缓辅料无法达到所需的延缓效果。片剂中XG的存在不仅延缓了药物从片剂中的初始释放,而且由于其高膨胀性,使其更容易被结肠中的微生物酶消化。