大黄泻下的大肠靶向给药之我见

目的 :从药剂学的角度出发阐明大黄作为泻下剂应大肠靶向给药的观点。方法 :根据近 6 0年国内外药理学、药剂学及临床实验研究 ,论述了结合蒽醌、特别是游离蒽醌对大肠蠕动和转运时间的影响和它们的吸收特点 ,以及大黄提取、浓缩、干燥过程中成分的损失情况。结果及结论 :大黄提取物中的游离蒽醌应视为有效泻下成分 ;不仅应注意大黄提取、浓缩、干燥过程中游离蒽醌的损失 ,更应注意游离蒽醌在上消化道转运过程中的损失 ;大肠靶向给药可阻止游离蒽醌在上消化道的吸收 ,将有利于提高疗效和降低用量。

Opinion of Colon-targeting Delivery about Rhubarb Extract as a Purgative

Objective: To elucidate that rhubarb extract as a purgative should be delivered to colon from a pharmaceutical point of view. Method: Effects of anthranoids and free anthraquinones as purgatives on the colon motility and transit time, the absorption in vivo, and the loss in the processes of extraction, concentration and dryness were reviewed, based on the recent 60 years pharmacological, pharmaceutical and clinical experimental studies at home and abroad. Result and Conclusion: Free anthraquinones in rhubarb extract should be regarded as purgative principles. Close attention should be paid to the loss of free anthraquinones not only in the processes of extraction, concentration and dryness,but also in the process of transit in the upper gastrointestinal tract. Colon-targeting delivery of rhubarb extract, as a purgative, may prevent absorption of free anthraquinones in the upper gastrointestinal tract, thus improving clinical effects and lowering dosage.