海藻多糖植物空心胶囊体内生物利用度与生物等效性研究

采用三交叉、自身对照的方法,研究了3种药用空心胶囊的体内相对利用度,并评估了其生物等效性,以检验本实验室研发的海藻多糖空心胶囊替代动物明胶空心胶囊的可行性。实验选择了12名志愿者,以布洛芬为模型药物,采用高效液相色谱法(HPLC)检测志愿者体内的血药浓度变化,用DAS2.0计算主要药动学参数,并评价其生物利用度及生物等效性。结果显示,海藻多糖植物空心胶囊替代动物明胶空心胶囊并不影响人体内药物吸收;海藻多糖植物空心胶囊布洛芬胶囊剂与日本Qualicaps布洛芬胶囊剂(相对生物利用度94.9%)、明胶布洛芬胶囊剂(相对生物利用度97.5%)均具有生物等效性。

BIOAVAILABILITY AND BIOEQUIVALENCE OF ALGAL POLYSACCHARIDE CAPSULES IN HUMAN

Capsules are used to encapsulate drugs. Consequently, the quality of the capsule shells is crucial for the bioavailability of the encapsulated drugs. Our laboratory developed a new plant-based capsule shell called Algal Polysaccharide Vegetable Capsule (APPC). It was composed of algal polysaccharide and cellulose. Studies on the bioavailability and bioequivalence of three types of capsules (APPC, Qualicaps, and gelatin) were conducted. Ibuprofen was adopted as model drug, and its plasma concentrations of 12 healthy volunteers were determined by high performance liquid chromatography (HPLC). Pharmacokinetic parameters are calculated on the basis of plasma concentrations with the software DAS 2.0, and the bioavailability and bioequivalence of the three types of capsules were evaluated. The aim of this paper was to compare the absorption of the drug in the capsules of APPC, Qualicaps and gelatin. The results showed that the substitution of gelatin capsules with algal polysaccharide vegetable capsules would not affect the in vivo drug absorption. Algal polysaccharide capsule met the criteria of bioequivalence with Qualicaps (relative bioavailability of 94.9%) and gelatin capsules (relative bioavailability of 97.5%).