通过制备包合物提高辣椒素的水溶性和生物利用度。
Enhanced aqueous solubility and bioavailability of capsaicin by the preparation of an inclusion complex.
作者信息
Chen Xiaoyu, Sun Xun, Ren Ke, Zhang Xiaoning, Zhang Zhirong, Gong Tao
机构信息
Key Laboratory of Drug Targeting and Drug Delivery Systems, Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu, Sichuan, PR China.
出版信息
Arzneimittelforschung. 2010;60(9):571-4. doi: 10.1055/s-0031-1296327.
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.
为提高辣椒素（CAS 404 - 86 - 4）的水溶性及改善其较差的生物利用度，本文研究了羟丙基-β-环糊精（HP-β-CD）对辣椒素水溶性及药代动力学特征的影响。采用饱和水溶液法制备了摩尔比为1:1的辣椒素/HP-β-CD相应包合物，并通过差示扫描量热法和X射线衍射法对其进行表征。由于HP-β-CD的增溶活性，辣椒素与HP-β-CD络合后其溶解速率显著提高。在大鼠皮下（s.c.）注射辣椒素及其络合物后，对其吸收行为和生物利用度进行了评价。与HP-β-CD形成包合物显著提高了辣椒素经皮下组织的吸收速率及其生物利用度。目前的结果表明利用HP-β-CD改善辣椒素皮下吸收和生物利用度的潜力。
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