吉西他滨温敏凝胶注射剂的制备及其含量测定  

Gemcitabine hydrochloride thermosensitive gel injection preparation and contents determination

作　　者：韦忠明 莫冬海 黄启斌 丁雪鹰[2] 

机构地区：[1]桂林华诺威基因药业有限公司,广西桂林541004 [2]上海交通大学附属第一人民医院临床药学科,上海200080

出　　处：《药学实践杂志》2016年第1期36-40,共5页Journal of Pharmaceutical Practice

基　　金：国家自然科学基金(81472349);上海市自然科学基金(14ZR1433300)

摘　　要：目的 制备吉西他滨温敏凝胶注射剂,并建立其含量测定方法。方法 以聚乙二醇/聚酯嵌段共聚物（PLGAPEG-PLGA）为载体,制备吉西他滨温敏凝胶注射剂,采用1 H NMR、FT-IR对其结构进行表征,HPLC法测定其中药物的含量。结果 吉西他滨温敏凝胶注射剂中,PLGA-PEG-PLGA的质量分数为20%,吉西他滨含量为40 mg/ml,胶凝温度为（37±0.15）℃,在接近人体温度时黏度最大;吉西他滨在5~500μg/ml范围内线性关系良好（r=0.999 8）,精密度和重复性良好,溶液24h内稳定性良好,低、中、高浓度的吉西他滨的回收率分别为（99.5±3.2）%、（100.4±2.4）%、（102.1±2.4）%,n=3。3批样品中吉西他滨的平均含量分别为标示量的（101.87±2.95）%、（99.4±2.73）%、（98.98±0.71）%,n=3。结论 采用PLGA-PEG-PLGA聚合物为载体制备的吉西他滨温敏凝胶注射剂质量可控,是一种很有开发前景的抗胰腺癌制剂。Objective To prepare gemcitabine hydrochloride thermosensitive gel injection and to stablish the determina- tion methods of its contents. Methods Gemcitabine hydrochloride thermosensitive gel injection was prepared using PLGA- PEG-PLGA as thermosensitive viecle. The contents of gemcitabine hydrochloride were determined by HPLC. Results The formulation contained 40 mg/m1 gemcitabine and 20% （wt） PLGA-PEG-PLGA with phase-transition temperature of （37± 0.15） C ,showing the best viscosity around human body temperature. Gemcitabine hydrochloride presented a good linearity in the range of 5-500 μg/ml（r=0. 999 8）, which had good precision and reproducibility. The recovery rate of low, middle and high concentrations of gemcitabine hydroehloride were （99.5±3.2） %, （100.4±2.4） %, （102.1±2.4） % ,n=3, respectively. The average contents of gemcitabine hydrochioride in three batches of sample were （ 101.87 ± 2.95 ）%, （99.4 ± 2.73 ）% , （98.98±0.71） %, n=3, respectively. Conclusion The quality of gemcitabine hydrochloride thermosensitive gel injection with PLGA-PEG-PLGA as matrix could be controlled. It is a promising new drug for pancreatic cancer.

关 键 词：吉西他滨 聚乙二醇/聚酯嵌段共聚物 温敏凝胶 含量测定 

分 类 号：R979.1[医药卫生—药品]