体外研究羟丙甲基纤维素对自微乳化给药系统胃肠道行为的影响

Influence of Hydroxypropylmethylcellulose on Digestion of Self-Microemulsifying Drug Delivery System in Gastro-Intestinal Tract in Vitro

目的探究羟丙甲基纤维素对自微乳化给药系统胃肠道行为的影响,为固体自微乳化给药系统的固体载体选择提供依据。方法采用胃模拟分散试验和体外脂解模型测定3种规格的羟丙甲基纤维素(K4M、K15M、K100M)对自微乳化给药系统胃肠道行为的影响。结果 3种规格的羟丙甲基纤维素都可抑制自微乳化给药系统在胃肠道中的分散沉淀;随着羟丙甲基纤维素的黏度增加,自微乳化给药系统的载药能力增强,小肠脂解后分配进入水相的药物浓度也增加。结论羟丙甲基纤维素有利于自微乳化给药系统中药物在胃肠道的吸收,可作为研制固体自微乳化给药系统的固体载体。

OBJECTIVE To study the influence of different viscosity hydroxypropylmethylcellulose（HPMC） on the digestion of self-microemulsifying drug delivery system（S-SMEDDS） in the gastro-intestinal tract,so as to provide basis for the further development of S-SMEDDS.METHODS In vitro experiments including dispersion experime nt and an in vitro lipolysis model were used to evaluate the influence of HPMC of three viscosity grade（K4M,K15M and K100M） on the digestion of S-SMEDDS in gastrointestinal tract.RESULTS All three kinds of HPMC could inhibit the precipitation of drug in gastro-intestinal tract.With the increasing of HPMC viscosity,the solub drug concentration in aqueous phase after intestinal lipolysis were both increased.CONCLUSION HPMC can improve the gastrointestinal absorption of S-SMEDDS and be used as its solid carrier.