磷酸哌喹片在四种不同pH溶出介质中溶出曲线的比较

Comparative Study on Dissolution Curves of Piperaquine Phosphate Tablets in Four Different pH Dissolution Media

目的:建立磷酸哌喹片中主要成分磷酸哌喹的溶出度HPLC测定方法,为其质量控制和溶出度评价提供依据。方法:参照中国药典2020年版四部通则0931溶出度与释放度项下第二法装置,分别采用4种溶出介质进行溶出实验,用HPLC进行检测,对同一厂家不同批次的磷酸哌喹片在不同的溶出介质中的溶出曲线进行研究。结果:磷酸哌喹在模拟人工胃液(pH=1.2)中溶出最快;在pH=4.0的溶出介质中,溶出效果有所降低;在含有胰酶的模拟肠液(pH=6.8)中,无法溶出;在含有胰酶的模拟肠液中添加乙醇后溶出效果有所提升。结论:所建立溶出测定方法简便、实时、灵敏、结果准确。结果表明,磷酸哌喹片在模拟人工胃液中溶出较好,而在含胰酶的模拟肠液中不易溶解。

Objective:To establish an HPLC method to determine the dissolution of piperaquine phosphate tablets,so as to provide reference for quality control and dissolution evaluation.Methods:Referring to the device of the second method under the item of dissolution and release in the general rule 0931 of Chinese Pharmacopoeia(2020 edition),the dissolution experiments were carried out in four different dissolution media.The dissolution curves of different batches of piperaquine phosphate tablets from the same manufacturer in different dissolution media were studied by HPLC.Results:Piperaquine phosphate dissolved fastest in simulated gastric juice(pH=1.2),while in the medium with pH of 4.0,the dissolution was reduced,and in simulated intestinal fluid containing trypsin(pH=6.8),the drug could not be dissolved out.The dissolution was improved by adding ethanol to the simulated intestinal fluid containing trypsin.Conclusion:This method is simple,real-time,sensitive and accurate.The results showed that piperaquine phosphate tablets dissolved well in simulated gastric juice,while not easily dissolved out in simulated intestinal juice containing trysin.