奥氮平双羟萘酸盐长效注射剂体外溶出度的测定

In vitro Dissolution of Olanzapine Pamoate Long-acting Injections

目的：建立奥氮平双羟萘酸盐长效注射剂的体外溶出度方法。方法：采用HPLC法测定奥氮平双羟萘酸盐长效注射剂的溶出度,采用浆法测定药物溶出度,溶出介质为0.5%十二烷基硫酸钠（SLS）模拟肌液（p H 7.0±0.05）,体积为500 ml,分别考察不同转速（25,50,75 r·min^-1）对自制制剂溶出行为的影响。结果：双羟萘酸在2.15-107.40 mg·L^-1（r=0.999 9）内,奥氮平在1.75-87.40 mg·L^-1（r=0.999 9）内浓度与峰面积呈良好的线性关系。奥氮平双羟萘酸盐的平均回收率为99.80%（RSD=0.55%,n=9）;自制制剂和原研制剂在溶出介质中溶出度相似因子f2为70.80。结论：溶出度测定方法能够有效控制该奥氮平双羟萘酸盐长效注射剂的产品质量。

Objective： To develop a dissolution method for olanzapine pamoate long-acting injections. Methods： The in vitro dissolution profile of olanzapine pamoate was detected by an oar method and an HPLC method. The stirring speed respectively was 25,50 and 75 r·min^-1,and 500 ml of sodium lauryl sulfate simulated muscle fluid [0. 5%,with p H of（ 7. 0 ± 0. 05） ]at（ 37 ± 0. 5） ℃was used as the bio-relevant dissolution media. Results： The linearity between the peak areas and the concentrations was observed within the range of 2. 15-107. 40 mg·L^-1（ r = 0. 999 9） for pamoate and 1. 75-87. 40 mg·L^-1（ r = 0. 999 9） for olanzapine,respectively,and the average recovery of olanzapine pamoate was 99. 80%（ RSD = 0. 55%,n = 9）. The f2 for the dissolution in the dissolution medium of shelf-prepared products and the innovation preparations was 70. 80. Conclusion： The dissolution method can be utilized to control the quality of olanzapine pamoate long-acting injections.