Improvement of absorption enhancing effects of n-dodecyl-β-D-maltopyranoside by its colon-specific delivery using chitosan capsules
Improvement of absorption enhancing effects of n-dodecyl-β-D-maltopyranoside by its colon-specific delivery using chitosan capsules
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DOI：
10.1016/j.ijpharm.2004.12.017
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发表时间：
2005-04-11
影响因子：
5.8
通讯作者：
Yamamoto, A
中科院分区：
文献类型：
--
作者：
Fetih, G;Lindberg, S;Yamamoto, A
一般而言，各种吸收促进剂的吸收促进作用在大肠中大于在小肠区域中。因此，如果这些吸收促进剂可以在口服给药后与一些吸收不良的药物一起被递送到大肠，则预期会显著观察到这些吸收促进剂的有效性。因此，在这项研究中，我们研究了壳聚糖胶囊是否有效的结肠特异性递送某种吸收促进剂，并可以提高口服给药后的吸收促进剂的吸收促进作用。以5（6）-羧基荧光素（CF）为模型药物，采用原位闭环方法研究了不同吸收促进剂的部位依赖性效应。以甘氨胆酸钠（NaGC）、正十二烷基-β-D-吡喃麦芽糖苷（LM）、水杨酸钠（NaSal）和癸酸钠（NaCap）为吸收促进剂模型。总的来说，这些促进剂对CF的肠吸收的吸收促进作用在结肠中比在空肠和回肠中更大。特别是，在本研究中测试的这些促进剂中，LM在结肠中显示出比在空肠和回肠中大得多的吸收促进作用。因此，选择LM作为模型吸收促进剂，以检查壳聚糖胶囊对LM吸收促进作用的影响。壳聚糖胶囊灌胃给药后，CF和LM的血药浓度明显高于其他剂型（溶液剂和胶囊剂）。因此，壳聚糖胶囊可能是有用的载体，用于结肠特异性递送LM，从而增加其从肠膜的吸收促进作用。(c)2005 Elsevier B. V.保留所有权利。
In general, absorption enhancing effects of various absorption enhancers were greater in the large intestine than those in the small intestinal regions. Therefore, the effectiveness of absorption enhancers is expected to be remarkably observed, if these enhancers can be delivered to the large intestine with some poorly absorbable drugs after oral administration. In this study, therefore, we examined whether chitosan capsules were effective for the colon-specific delivery of a certain absorption enhancer and can improve the absorption enhancing action of the absorption enhancer after oral administration. 5(6)-Carboxyfluorescein (CF) was used as a model drug to investigate the site-dependent effectiveness of various absorption enhancers by an in situ closed loop method. Sodium glycocholate (NaGC), n-dodecyl-beta-D-maltopyranoside (LM), sodium salicylate (NaSal) and sodium caprate (NaCap) were used as models of absorption enhancers in this study. overall, the absorption enhancing effects of these enhancers for intestinal absorption of CF were greater in the colon than those in the jejunum and the ileum. Especially, among these enhancers tested in this study, LM showed much greater absorption enhancing effect in the colon than in the jejunum and the ileum. Therefore, LM was selected as a model absorption enhancer to examine the effect of chitosan capsules on the absorption enhancing effect of LM. When CF and LM were orally administered to rats using chitosan capsules, the plasma concentration of CF was much higher than those in other dosage forms including solution and gelatin capsules. Therefore, chitosan capsules may be useful carriers for colon-specific delivery of LM, thereby increasing its absorption enhancing effect from the intestinal membranes. (c) 2005 Elsevier B.V. All rights reserved.