Bourie C, Paillard B, Goutay E, Avan J L, Combal J P, Bougaret J, Aiache J M, Jacquinet J C
Pierre Fabre Research Institute, Boulogne, France.
J Biomater Appl. 1998 Jan;12(3):201-21. doi: 10.1177/088532829801200302.
Several studies have been devoted to cross-linked sodium chondroitin sulphate (SCS), in the context of numerous strategies attempting to target the colon for the absorption or the therapeutic action of a drug. SCS, a glycosaminoglycan presenting a specific degradation in the colon, is in fact soluble in water and its use as drug carrier at such a distance from the digestive tube necessitates its hydrophobisation. One method described in the literature consists in manufacturing a three-dimensional network by cross-linking with bifunctional compounds. However, all the structural characterisations carried out on the products resulting from the catalysed treatments of SCS with diaminoalkanes demonstrate that there are no cross-linking bridges between the polymer chains. Moreover, treated SCS-based tablets containing theophylline as model drug lead in vitro to dissolution profiles which are identical to those obtained with the non-treated SCS. We were therefore unable to find the announced results using the method described.
在众多试图使药物靶向结肠以实现吸收或治疗作用的策略背景下，已有多项研究致力于交联硫酸软骨素钠（SCS）。SCS是一种在结肠中会发生特定降解的糖胺聚糖，实际上它可溶于水，而要在离消化道如此远的地方将其用作药物载体，就需要对其进行疏水化处理。文献中描述的一种方法是通过与双功能化合物交联来制造三维网络。然而，对用二氨基烷烃催化处理SCS所得到的产物进行的所有结构表征表明，聚合物链之间不存在交联桥。此外，含有茶碱作为模型药物的经处理的SCS基片剂在体外产生的溶出曲线与未处理的SCS所获得的溶出曲线相同。因此，我们无法通过所描述的方法得到宣称的结果。
