血管活性肠肽化学及生物学稳定性研究  

Chemical and biological stability of vasoactive intestinal peptide

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作  者:崔旭[1] 韩璇[2] 王志敏[1] 曹德英[1] 郑爱萍[3] 

机构地区:[1]河北医科大学药学院,石家庄050017 [2]河北大学医学部基础医学院,保定071000 [3]军事医学科学院毒物药物研究所,北京100850

出  处:《中国新药杂志》2011年第19期1922-1925,共4页Chinese Journal of New Drugs

基  金:河北省自然科学基金(C2009001066)

摘  要: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) for providing a theory basis for pharmaceutical development of VIP. Methods: The stability of VIP in different pH values, ionic strength, temperature, artificial gastric fluid and artificial intestinal fluid was investigated. The concentration of VIP was determined by HPLC method. Results: The stability of VIP was pH-dependent. VIP was stable in acid and neutral solutions; almost no degradation was found in solutions at pH ≤7. However, it was instable in basic solutions and degraded completely at 30 min in solution at pH 13. Ionic strength did not affect its stability. VIP was stable in freezing conditions but degraded at low concentrations after cold storage. Furthermore, VIP was degraded quickly in artificial gastric and intestinal fluids; it was not detected at 0min. Conclusion: The chemical and biological characteristic of VIP is unstable, so it may be not suitable for oral administration.

关 键 词:血管活性肠肽 稳定性 人工胃液 人工肠液 

分 类 号:R978.16[医药卫生—药品]

 

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