孟鲁司特钠咀嚼片体外溶出研究

Study on the Dissolution of Montelukast Sodium Chewable Tablets in Vitro

关键词:  孟鲁司特钠  体外溶出  溶解度  胆盐

Key words:  montelukast sodium  in vitro dissolution  solubility  bile salt

摘要:

目的 研究孟鲁司特钠咀嚼片体外溶出行为及其影响因素，为该品种新剂型开发和仿制药一致性评价提供参考。方法 考察pH、胆盐、表面活性剂等因素对孟鲁司特钠咀嚼片溶出的影响。结果 孟鲁司特钠在pH 7.5的介质中，随着胆盐浓度的增加，溶解度明显上升；孟鲁司特钠咀嚼片在pH 1.0盐酸溶液、pH 4.0醋酸盐溶液、pH 6.8磷酸盐溶液的溶出过程中，会迅速析出形成混悬液，而0.5%十二烷基硫酸钠水溶液会抑制其析出。结论 孟鲁司特钠咀嚼片的体外溶出受pH、胆盐、表面活性剂的影响较大，可以为其新型给药系统的开发和质量一致性评价提供参考。

Abstract:

OBJECTIVE To investigate in vitro dissolution behavior and its influencing factors of montelukast sodium chewable tablets, to provide reference for the development of new dosage forms and consistency evaluation of generic drugs. METHODS The effects of pH, bile salts, surfactants and other factors on the dissolution of sodium chewable tablets were investigated. RESULTS In the medium with pH 7.5, the solubility of montelukast sodium increased significantly with the increase of bile salt concentration. The dissolution of montelukast sodium chewable tablets in pH 1.0 hydrochloric acid solution, pH 4.0 acetate solution and pH 6.8 phosphate solution rapidly precipitated to form a suspension, while 0.5% SDS aqueous solution inhibited its precipitation. CONCLUSION The dissolution of montelukast sodium chewable tablets is greatly affected by pH, bile salts and surfactant. It will be the reference and experience of formulation and quality consistency evaluation for generic drugs in future.