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基于淫羊藿黄酮苷的肠道水解代谢规律和骨质疏松病理状态下的肠道吸收特征,制备了添加有少量外源性水解酶(蜗牛酶)的仿生酶解肠溶胶囊,探索该胶囊提高淫羊藿总黄酮口服生物利用度的可行性。建立了骨质疏松大鼠模型,再分别灌胃给予淫羊藿总黄酮提取物及其仿生酶解肠溶胶囊(以淫羊藿总黄酮计剂量为500 mg/kg)。采用HPLC法测定淫羊藿总黄酮提取物中原型苷(朝藿定A、朝藿定B、朝藿定C、淫羊藿苷)及其代谢产物(箭藿苷A、箭藿苷B、2’’-O-鼠李糖基淫羊藿次苷Ⅱ、宝藿苷Ⅰ、淫羊藿苷元)的血药浓度,绘制药-时曲线。结果显示,各原型苷及代谢产物在骨质疏松模型大鼠体内的药-时曲线均呈双峰现象。计算了各原型苷及代谢产物的药动学参数,并对其进行整合和比较。结果表明,淫羊藿总黄酮仿生酶解肠溶胶囊的AUC_(0→t)显著提高(P<0.01),但其他药动学参数未见明显变化。
Based on the rules of intestinal glycogen metabolism and intestinal absorption of osteoporosis under pathological conditions of Epimedium glycoside, a biomimetic enzyme-solubilized enteric-coated capsule with a small amount of exogenous hydrolase (snail enzyme) was prepared, and the capsule Feasibility of Increasing Oral Bioavailability of Epimedium Flavonoids. A rat model of osteoporosis was established. The total flavonoids of Herba Epimedii and the biomimetic enzyme-solubilized enteric-coated capsules were given by gavage respectively. The total flavonoids of Herba Epimedii were 500 mg / kg. The content of aristotechin (Epimedin A, Epimedin B, Epimedin C, Icariin) and their metabolites (Icariin A, Icariin B, 2 "- O - rhamnosyl icariin Ⅱ, treasure glycosides Ⅰ, icariin) blood concentration, draw the drug - time curve. The results showed that each prototype glycosides and metabolites in osteoporosis model rat body-time curve showed a bimodal phenomenon. The pharmacokinetic parameters of each prototype glycosides and metabolites were calculated and integrated and compared. The results showed that the AUC_ (0 → t) of biomimetic enzyme digestion solution of Epimedium sagittatum flavonoids was significantly increased (P <0.01), but the other pharmacokinetic parameters showed no significant changes.