孟鲁司特钠口腔崩解片的制备和质量评价研究

Preparation and quality evaluation of montelukast sodium orally disintegrating tablets

目的 对冷冻干燥技术制备孟鲁司特钠口腔崩解片的处方和工艺进行优化并对自研制剂进行溶出相似性评价。方法通过单因素实验和Box-Behnken效应面法对孟鲁司特钠口腔崩解片的辅料种类、用量和冻干工艺进行考察和优化,并以外观性状、崩解时限、水分和口感等为指标,对自研制剂的质量进行初步评价。参照《中国药典》2020年版溶出度测定方法,用HPLC法对孟鲁司特钠在4种溶出介质中的溶出行为进行评价。结果确定孟鲁司特钠口腔崩解片的处方为:孟鲁司特钠10 mg、甘露醇9 mg、麦芽糖糊精3 mg、交联聚维酮3 mg、明胶8 mg、阿斯帕坦1 mg、薄荷香精0.2 mg。自研孟鲁司特钠口腔崩解片与原研孟鲁司特钠咀嚼片溶出行为相似。结论该处方及工艺合理稳定,为后续孟鲁司特钠口腔崩解片的研究开发奠定了基础。

Objective To prepare montelukast sodium orally disintegrating tablets by using freeze-drying technology,and to optimize its formulation and process and evaluate the dissolution similarity of the tablets.Methods Single factor experiments and the Box-Behnken design method were used to determine the type and dosage of the tablet excipients and optimize its freeze-drying process.The appearance characteristics,disintegration time,moisture content and taste of the tablets were evaluated.The dissolution behaviors of the tablets in 4 dissolution media were evaluated by HPLC according to the dissolution determination method of Chinese Pharmacopoeia 2020.Results Formulation of the tablets was determined as follows:montelukast sodium 10 mg,mannitol 9 mg,maltodextrin 3 mg,crospovidone 3 mg,gelatin 8 mg,aspartame 1 mg,and peppermint flavor 0.2 mg.The dissolution behaviors of the self-developed tablets were similar to those of the original drugs.Conclusion The formulation and process are reasonable and stable for further research and development of the tablets.