磷酸哌喹分散片的处方前研究
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摘要
目的阐明磷酸哌喹原料药的基本理化性质,为设计分散片优良的处方提供依据。方法采用HPLC测定磷酸哌喹含量,分别进行磷酸哌喹的平衡溶解度、油水分配系数、吸湿性考察、破坏性试验和稳定性试验等处方前研究。结果磷酸哌喹原料药的溶解度随pH值增大呈减小趋势;磷酸哌喹在pH(1.0～4.5)中的油水分配系数<0,在pH(5.8～8.0)中的油水分配系数>0;在25℃,RH80%条件下吸湿性较小;磷酸哌喹在酸、碱、氧化溶液中相对稳定,高温、高湿条件下也相对稳定,光照易变色。结论本研究结果可为磷酸哌喹分散片处方设计及工艺研究提供实验依据。
Objective To elucideat the basic physiochemical properties of piperaquine phosphate and provide evidence for designing dispersible tablets.Methods The content of piperaquine phosphate was determined by high performance liquid chromatography(HPLC).The preformulation studies on the equilibrium solubility,oil-water partition coefficient,hygroscopicity,destructive test and stability test of piperaquine phosphate were carried out respectively.Piperaquine phosphate is relatively stable in acid,alkali and oxidation solutions,and is relatively stable under high temperature and humidity conditions,and the light is easily discolored.Results The solubility of piperaquine phosphate active pharmaceutical ingredient(API)decreased with the increase of pH value.The oilwater partition coefficient of piperaquine phosphate was less than zero when the pH value was between 1.0 and 4.5 and greater than zero when the pH value was between 5.8 and 8.0.Its hygroscopicity is small under the condition of RH80% at the temperature of 25°C.Piperaquine phosphate was relatively stable in the acid,alkali,and oxidation solutions and it was also relatively stable under the condition of high temperature and high humidity.The color of piperaquine phosphate was easily changed under light.Conclusion The results of this study can provide experimental evidence for the formulation design and process research of piperaquine phosphate dispersible tablets.
Objective To elucideat the basic physiochemical properties of piperaquine phosphate and provide evidence for designing dispersible tablets.Methods The content of piperaquine phosphate was determined by high performance liquid chromatography(HPLC).The preformulation studies on the equilibrium solubility,oil-water partition coefficient,hygroscopicity,destructive test and stability test of piperaquine phosphate were carried out respectively.Piperaquine phosphate is relatively stable in acid,alkali and oxidation solutions,and is relatively stable under high temperature and humidity conditions,and the light is easily discolored.Results The solubility of piperaquine phosphate active pharmaceutical ingredient(API)decreased with the increase of pH value.The oilwater partition coefficient of piperaquine phosphate was less than zero when the pH value was between 1.0 and 4.5 and greater than zero when the pH value was between 5.8 and 8.0.Its hygroscopicity is small under the condition of RH80% at the temperature of 25°C.Piperaquine phosphate was relatively stable in the acid,alkali,and oxidation solutions and it was also relatively stable under the condition of high temperature and high humidity.The color of piperaquine phosphate was easily changed under light.Conclusion The results of this study can provide experimental evidence for the formulation design and process research of piperaquine phosphate dispersible tablets.
引文
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[2]郭毅新,张元杰,丁涛.HPLC法测定双氢青蒿素哌喹片中的PQP含量[J].药学研究,2014,33(6):332-333.
[3]秦斌,殷果,闫研,等.HPLC法测定青蒿素哌喹片中哌喹的含量及相关物质[J].世界科学技术-中医药现代化,2014,16(8):1747-1753.
[4]周琳.HPLC测定双氢青蒿素哌喹片中的PQP及有关物质[J].华西药学杂志,2015,30(5):610-612.
[5]徐结红,高莹,曹青日.右布洛芬缓释干混悬剂的处方前研究[J].中国当代医药,2018,25(1):16-18.
[6]国家药典委员会.中华人民共和国药典:二部[M].北京:中国医药科技出版社,2015:1576.
[7]廖灿城,许丹翘,刘晓红.芒柄花素平衡溶解度和油水分配系数的测定[J].佛山科学技术学院学报(自然科学版),2017,35(6):71-75.
[8]孙磊,冯军,雷艳丽.黄芩苷-盐酸小檗碱复合物的溶解度与油水分配系数测定[J].中国实验方剂学杂志,2017,23(21):35-38.
[9]李朝,夏新华,周宇.黄芩苷的处方前研究[J].湖南中医药大学学报,2016,(7):51-54.
[10]陈淑圻,李悦山.洛伐他汀缓释微丸型片剂处方前研究[J].中国医药导报,2011,8(16):72-74.
[11]张睿智,王晓宇,陈超,等.盐酸吉西他滨的处方前研究[J].沈阳药科大学学报,2010,27(8):595-598.