低分子量肝素钙口服制剂的研究

Study on the oral preparation of low molecular weight heparin calcium

目的研究低分子量肝素钙(LMWH-Ca)口服制剂的制备和口服吸收。方法将LMWH-Ca用聚乙二醇制成微囊、β-环糊精(-βCD)包合和在LMWH-Ca口服液中加入促胃肠道黏膜吸收剂N-[10-(2-羟基苯甲酰基)氨基]癸酸钠(SNAD)等方法制备成不同制剂后,SD大鼠采用灌胃给药,用生色底物法测定不同取样时间的药物浓度。结果在试验的LMWH-Ca口服处方中,加入SNAD的处方具有较好的吸收。结论SNAD对LMWH-Ca口服制剂具有优良的促胃肠道黏膜吸收能力,有助于LMWH-Ca口服制剂的深入研究。

Purpose To investigate the oral preparations of low molecular weight heparin calcium（LMWH-Ca） and the absorption of LMWH-Ca in the preparations administered orally. Methods LMWH-Ca preparations were prepared by microeneapsulation with PEG6000, inclusion with β-CD or adding sodium N-[10-（2-hydrox- ybenzoyl）amino]decanoate （SNAD）to enhance the absorption of LMWH-Ca from the gastrointestinal tract, and the concentrations of LMWH-Ca in plasma at varied time after giving the LMWH-Ca preparations to rats intragastrically were determined by chromogenic substrate method. Results Among the preparations of LMWH-Ca, the one containing SNAD had better absorption. Conclusion SNAD has good ability to enhance absorption of oral LMWH-Ca from the gastrointestinal tract. It would be good to have further study on LMWH-Ca oral prepa- rations.