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目的:制备羟基喜树碱凝胶并建立质量控制方法。方法:采用正交设计法,以凝胶的成型性、涂展性、pH和黏度为指标,对基质处方进行优化;对HPLC检测羟基喜树碱进行方法学考察并检测羟基喜树碱在制剂中的含量。结果:羟基喜树碱凝胶最佳基质处方为(质量体积比):卡波姆-934 0.5%、甘油15%、月桂氮芯卓酮2%、三乙醇胺0.3%,此处方制备的凝胶均匀、细腻、易于涂布,测得其pH为6.90,黏度为35 Pa·s;羟基喜树碱在0.187 7~117.3μg·mL-1范围内线性关系良好(R2=0.999 8),精密度和准确度良好,重复性和稳定性的相对标准偏差为1.96%和1.95%,80%、100%和120%,制剂的加样回收率分别为(95±1)%,(96±2)%,(94±1)%。3批样品中羟基喜树碱的平均含量分别为标示量的104.8%、105.0%和100.6%。结论:采用卡波姆为基质制备羟基喜树碱凝胶工艺简单、质量可控,凝胶的水性基质可以增加患者的依从性,具有良好的开发前景。
Objective: To prepare hydroxy camptothecin gel and establish quality control method. Methods: Orthogonal design method was used to optimize the formulation of matrix with gel formability, spreadability, pH and viscosity as indexes. The HPLC method was used to detect hydroxycamptothecin, and hydroxycamptothecin In the content. Results: The optimal formulation of hydroxycamptothecin gel was (mass volume ratio): 0.5% carbomer -934, 15% glycerol, 2% laurel azithromycin, 0.3% triethanolamine. Uniform, delicate and easy to apply. The pH value was 6.90 and the viscosity was 35 Pa · s. The linearity of hydroxycamptothecin in the range of 0.187 7 ~ 117.3 μg · mL-1 was good (R2 = 0.999 8) The relative standard deviations (RSDs) were 1.96% and 1.95%, 80%, 100% and 120% respectively. The recoveries of the preparations were (95 ± 1)% and (96 ± 2) %, (94 ± 1)%. The average contents of hydroxycamptothecin in the three batches of samples were 104.8%, 105.0% and 100.6% of the indicated amounts, respectively. CONCLUSION: The preparation of hydroxy camptothecin gel with carbomer is a simple, controlled and gel-based aqueous matrix which can increase patient compliance and has good development prospect.