Enhanced aqueous solubility and bioavailability of capsaicin by the preparation of an inclusion complex
Enhanced aqueous solubility and bioavailability of capsaicin by the preparation of an inclusion complex
复制标题
通过制备包合物提高辣椒素的水溶性和生物利用度
DOI：
10.1055/s-0031-1296327
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发表时间：
2010-01-01
影响因子：
--
通讯作者：
Gong, Tao
中科院分区：
文献类型：
--
作者：
Chen, Xiaoyu;Sun, Xun;Gong, Tao
针对辣椒碱（CAS 404-86-4）水溶性差、生物利用度低的问题，研究了羟丙基-β-环糊精（HP-β-CD）对辣椒碱水溶性的影响及其药代动力学特征。采用饱和水溶液法制备了辣椒碱/HP-β-CD（摩尔比为1：1）包合物，并用差示扫描量热法和X射线衍射法对其进行了表征。由于HP-β-CD的增溶活性，与HP-β-CD的络合显著增加了辣椒碱的溶出速率。研究了辣椒碱及其复合物经皮下给药后的吸收行为和生物利用度。c.）注射到大鼠体内。辣椒碱与HP-β-CD形成包合物后，其皮下组织吸收速率和生物利用度显著提高。目前的结果表明，利用HP-β-CD，以提高辣椒素的皮下吸收和生物利用度的潜力。
To increase the aqueous solubility and poor bioavailability of capsaicin (CAS 404-86-4), in this paper, the effects of hydroxypropyl-beta-cyclodextrin (HP-beta-CD) on the aqueous solubility and the pharmacokinetic characteristics of capsaicin were investigated. The corresponding inclusion complex of capsaicin/HP-beta-CD at the molar ratio of 1:1 was obtained by the method of saturated aqueous solution and characterized by differential scanning calorimetry and X-ray diffractometry. The dissolution rate of capsaicin was significantly increased by the complexation with HP-beta-CD, due to its solubilizing activity. The absorption behavior and bioavailability of capsaicin and its complexation were evaluated after their subcutaneous (s. c.) injection in rats. The absorption rates of capsaicin across subcutaneous tissues and its bioavailability were significantly enhanced by the formation of an inclusion complex with HP-beta-CD. The present results indicate the potential of utilizing HP-beta-CD to improve the subcutaneous absorption and bioavailability of capsaicin.