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硝苯吡啶广泛用作为钙拮抗剂。在水中几乎不溶,且对光具有高度敏感性。市售制剂一般为硬胶囊和软胶囊,但该药的注射剂无效。本文采用增溶技术,设计制备了硝苯吡啶的水性注射液,考察了热压、温度和光线对硝苯吡啶稳定性的影响。经大鼠体内初步试验证实;硝苯吡啶注射液有效。本文分别以苯甲酸钠、水杨酸钠为增溶剂。25±1℃时硝苯吡啶在30%W/V的苯甲酸钠溶液和30%W/V的水杨酸钠溶液中的溶解度分别增加85和135倍,37℃时则分别增加76和107倍。由此将注射液的规格设计为含硝苯吡啶1 mg/5 ml和1 mg/2 ml。用UV法测定硝苯吡啶含量,测定波长分别为340 nm(以苯甲酸钠为增溶剂)、350nm(以水杨酸钠为增溶剂)
Nifedipine is widely used as a calcium antagonist. Almost insoluble in water, and highly sensitive to light. Commercial formulations are generally hard and soft capsules, but the drug injection is invalid. In this paper, an aqueous injection of nifedipine was designed and prepared by solubilization technology. The effects of hot pressing, temperature and light on the stability of nifedipine were investigated. The initial test in rats confirmed; nifedipine injection effective. In this paper, sodium benzoate, sodium salicylate as solubilizer. The solubilities of nifedipine in 30% w / v sodium benzoate solution and 30% w / v sodium salicylate solution increased by 85 and 135 times at 25 ± 1 ℃ and increased by 76 and 107 times at 37 ℃, respectively . The injection was therefore designed to contain nifedipine 1 mg / 5 ml and 1 mg / 2 ml. Determination of nifedipine content by UV method, the measured wavelength was 340 nm (sodium benzoate as solubilizer), 350nm (sodium salicylate as a solubilizer)