摘要
目的制备氯雷他定自乳化制剂,并对其质量进行评价。方法通过测定药物在不同油相中的溶解度,研究油相与各种乳化剂、助乳化剂的配伍对自乳化效率的影响,并结合伪三元相图,筛选氯雷他定自乳化制剂的处方。考察该制剂经水稀释后形成的微乳的外观、粒径和Zeta电位,测定药物的油水分配系数及溶解度,并通过加速实验评价制剂的稳定性。结果自乳化介质处方为油酸乙酯-吐温80-正丁醇(10∶54∶36);氯雷他定自乳化制剂稀释50倍后仍为澄清透明液体,粒径为(13.9±3.2)nm,ζ电位为(16.7±0.8)mv,药物的油水分配系数(logP)和在自乳化介质中的溶解度分别为2.30和256.2 mg.mL-1;加速实验表明氯雷他定自乳化制剂的各项指标稳定。结论氯雷他定自乳化制剂制备简单,质量稳定,能显著提高药物的溶解度。
Objective To prepare the loratadine self-emulsifying formulation and to evaluate its quality. Methods The loratadine selfemulsifying formulation was optimized based on the loratadine solubility in different oils, and the self-emulsifying efficiency of various combinations of emulsifier and co-emulsifier was evaluated using the pseudo-ternary phase diagram. The appearance, size and zeta potential of loratadine self-emulsifying drug were examined. The oil-water partition coefficient and solubility in the self-emulsifying system were tested. The formulation stability was investigated by accelerated experiment. Results The blank selfemulsifier was composed of ethylolerte / Tween80 / butanol with weight ratio of 10 ： 54 ： 36. After being diluted with water, the appearance of selfemulsifying drug was clear liquid. The particle size and the Zeta potential were （13.9±3.2） nm, and （16.7±0.8） my, respectively. The oil-water partition coefficient （log P） and the solubility of loratadine in selfemulsifying formulation were 2.30 and 256. 2 mg · mL^-1 , respectively. The quality of loratadine self-emulsifying formulation was stable during the 3 month storage at 40 ℃.Conclusion The solubility of loratadine is significantly increased in selfemulsifying system and the formulation is sta ble and easy to prepare.
出处
《中南药学》
CAS
2008年第4期414-416,共3页
Central South Pharmacy
关键词
氯雷他定
自乳化
质量评价
伪三元相图
分配系数
loratadine
self-emulsifying
quality evaluation
pseudo-ternary phase diagram
oil-water partition coefficient
