地塞米松磷酸钠口服液的制备及其抗大鼠粘连性肠梗阻的初步研究

目的：制备地塞米松磷酸钠口服液并初步考察其抗大鼠粘连性肠梗阻作用。方法：采用高效液相色谱（HPLC）法测定地塞米松磷酸钠的含量、油水分配系数、考察地塞米松磷酸钠稳定性影响因素；采用裘法祖造模法和试剂盒考察其抗大鼠粘连性肠梗阻的作用。结果：在pH 1.0~8.0范围内，地塞米松磷酸钠的油水分配系数均小于零；pH为8.0时药物降解最慢，抗氧剂Na₂SO₃和稳定剂丙二醇联用可增加地塞米松磷酸钠的稳定性。与尾静脉注射给药相比，地塞米松磷酸钠口服液能显著降低粘连性肠梗阻（AIO）大鼠肠道丙二醛（MDA）含量（P<0.05），显著提高超氧化物歧化酶（SOD）和谷胱甘肽过氧化物酶（GSH-PX）的活性（P<0.01，P<0.01）。结论：地塞米松磷酸钠口服液具有抗大鼠粘连性肠梗阻作用且其作用强于注射液。

Preparation of dexamethasone sodium phosphate oral liquid and preliminary research of its anti-adhesive intestinal obstruction in mice

OBJECTIVE To prepare dexamethasone sodium phosphate (DSP) oral liquid and to study its effect of anti-adhesive intestinal obstruction (AIO) in mice. METHODS The content of DSP and the oil-water partition coefficients were determined by HPLC. The factors affecting the stability of DSP were investigated. Qiu Fazu modeling method and kit were used to observe its effect of anti-adhesive intestinal obstruction in mice. RESULTS In the pH range of 1.0-8.0,the oil-water partition coefficients of DSP was less than zero. When pH was 8.0, the degradation of drug was the slowest, antioxidant Na₂SO₃ and stabilizer propylene glycol combination increased the stability of DSP. Compared with the tail vein injection, the AIO mice treated with DSP oral liquid were improved significantly by decreasing the content of malondiadehyde(MDA) (P<0.05) and increasing the activities of supeoxide dismutase(SOD) and glutathlone peroxidase(GSH-PX) (P<0.01, P<0.01). CONCLUSION The dexamethasone sodium phosphate oral liquid is superior to its injection in anti-adhesive intestinal obstruction in mice.