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目的:考察血管活性肠肽(vasoactive intestinal peptide,VIP)的化学及生物学的稳定性,为VIP的制剂学研究提供依据。方法:考察VIP在不同pH值(2.0,4.0,7.0,9.0,11.0,13.0)、不同离子强度溶液、不同温度以及人工胃液和人工肠液中的稳定性,用HPLC法检测VIP含量变化。结果:VIP的稳定性具有pH依赖性,VIP在酸性及中性条件下稳定,pH≤7时几乎无降解,但VIP在碱性条件下不稳定,pH=13时30min已完全降解;离子强度对其稳定性无影响;VIP在冷冻条件下稳定性良好,在冷藏条件下低浓度存在降解;VIP在人工胃液和人工肠液中降解迅速,0 min即完全降解,无法检测到主药峰。结论:VIP化学及生物学的稳定性差,口服无效。
OBJECTIVE: To investigate the chemical and biological stability of vasoactive intestinal peptide (VIP), and to provide a basis for the study of pharmaceutics of VIP. Methods: The stability of VIP in different pH values (2.0, 4.0, 7.0, 9.0, 11.0, 13.0), different ionic strength solutions, different temperatures and artificial gastric juice and artificial intestinal juice were investigated. Results: The stability of VIP was pH-dependent. VIP was stable under acidic and neutral conditions and hardly degraded when pH≤7. However, VIP was not stable under alkaline conditions and completely degraded at pH = 13 and 30 min. The ionic strength Had no effect on its stability. VIP had good stability under freezing condition and degraded at low concentration under refrigerated conditions. VIP degraded rapidly in artificial gastric juice and artificial intestinal juice, completely degraded at 0 min, and the main drug peak could not be detected. Conclusions: VIP chemistry and biology are poorly stable and orally ineffective.