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目的:以血浆抗Xa活性及体内抗静脉血栓形成为指标,考察了低分子肝素(LMWH)溶液及乳剂在麻醉大鼠胃肠道的吸收情况。方法:LNWH溶液和乳剂给大鼠灌服或十二指肠直接注入给药,颈动脉插管取血、生色底物法测血浆抗Xa活性,并考察对实验性颈静脉血栓形成的预防作用。结果:在5000Anti-Xa IU/kg的剂量下,LMWH溶液灌胃给药时血浆抗Xa活性与空白对照没有显著差别,而与油酸、胆盐制成乳剂后灌服则血浆抗Xa活性明显升高,可达0.508±0.18Anti-Xa IU/ml的峰值,并有显著抗静脉血栓作用;同样剂量十二指肠给药,两种剂型都有显著吸收,在给药后1h左右达到血药峰值,分别为1.12±0.916Anti-Xa IU/ml(溶液),1.25±0.526Anti-Xa IU/ml(乳剂),与100 Anti-Xa IU/kg剂量下LHWH注射液静脉给药后0.5h的血药水平相当,并显示明显的抗静脉血栓形成活性。结论:LMWH在胃液中可能被破坏,在十二指肠能够有所吸收,与油酸、胆盐制成乳剂可保护并促进LMWH的吸收。
OBJECTIVE: To investigate the anti-Xa activity of plasma and anti-venous thrombosis in vivo as an index, the absorption of low molecular weight heparin (LMWH) solution and emulsion in the gastrointestinal tract of anesthetized rats was investigated. Methods: LNWH solution and emulsion were administered orally or intraduodenally to rats. Carotid arteries were cannulated for blood and the anti-Xa activity was measured by chromogenic substrate method. The experimental jugular thrombosis prevention was also investigated effect. Results: At the dose of 5000 Anti-Xa IU / kg, there was no significant difference in anti-Xa activity between the LMWH solution and the blank control group when orally administered with LMWH solution. However, Increased up to 0.508 ± 0.18Anti-Xa IU / ml peak, and significant anti-venous thrombosis; the same dose of duodenal administration, both formulations have significant absorption, at about 1h after administration to reach the blood (Peak) were 1.12 ± 0.916Anti-Xa IU / ml (solution) and 1.25 ± 0.526Anti-Xa IU / ml (emulsion) respectively. After 0.5h injection of LHWH injection at 100 Anti-Xa IU / The level of blood drug equivalent, and showed significant anti-venous thrombosis activity. CONCLUSION: LMWH may be destroyed in gastric juice and absorbed in the duodenum. Emulsions prepared with oleic acid and bile salts can protect and promote LMWH absorption.