| 中文摘要 |
岩黃連在民間多用於治療肝炎、肝硬化以及肝癌，生物鹼為其主要活性成分。已有研究顯示，岩黃連生物鹼在水中溶解性差，與靜脈注射相比，口服生物利用度僅為10%左右。本文以聚乙二醇PEG 4000與聚乙烯?咯烷酮PVP K30為基質，採用固體分散技術製備岩黃連生物鹼提取物的固體分散體，通過提高其水溶性進一步提高其生物利用度。結果顯示，以7倍量的PEG 4000為基質，可以顯著提高岩黃連生物鹼在水、pH 1.2鹽酸以及pH 7.2磷酸鹽緩衝液中的溶解度，DSC與X-衍射檢測結果顯示，與物理混合物的存在狀態不同，生物鹼以溶解分散或無定形狀態存在。採用新建立的LC/DAD分析方法，基於尿藥累積法對該配方進行大鼠口服生物利用度的研究，與口服混懸液相比，大鼠口服固體分散體後3個主要生物鹼（dehydrocavidine , coptisine, dehy-droapocavidine）的生物利用度在0-24 h提高了約1倍（p < 0.05）。" |
| 英文摘要 |
Corydalis saxicola Bunting, also named Yanhuanglian in China, is widely used in folk prescriptions to treat hepatitis, hepato-cirrhosis and hepatic cancer. Its active components consists mainly of alkaloids, which have poor solubility in water. The previous study showed that the absolute bioavailabilities (BA) of the alkaloids were only about 10% after oral administration to rats, compared to intravenous administration. In this paper, the solid dispersion (SD) method was used to improve the BAs of dehydro-cavidine (YHL-1), coptisine (YHL-2), and dehydroapocavidine (YHL-3), the main alkaloids of the extract of Corydalis saxicola Bunting, by improving their solubility. The results showed that using PEG 4000 as a carrier at an amount equivalent to 7 folds of the extract could significantly improve the solubility of the compounds in water, pH 1.2 HCl and pH 7.2 PBS. DSC and X-ray detection indicated that the drug might be in a dissolved or amorphous state in SD, which was different from that in the physical mixture. The formulation was further studied in terms of BA enhancement by cumulative urinary excretion after oral administration to rats. A new method using high performance liquid chromatography (HPLC) coupled to a diode-array detector (DAD) was established. The results showed that the relative BAs (RE BAs) of YHL-1, YHL-2 and YHL-3 were all significantly improved by about 1 fold after oral administration of SD solution, compared to the extract suspension (p < 0.05). |
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