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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
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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.
出处 《药学实践杂志》 CAS 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)
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 gemcitabine hydrochloride PLGA-PEG-PLGA thermosensitive gel content determination
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