高压均质机提高替莫唑胺水溶性的方法研究
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摘要
目的探究提高替莫唑胺药物水溶性的方法。方法在酸性条件下,以紫外分光光度法测定替莫唑胺在水中的溶解度,通过单因素和正交优化试验法确定最佳方案工艺,并对其样品进行粒径和Zeta、电位、红外光谱表征。结果由正交优化试验得出最佳方案为:选用烟酰胺为表面活性剂,替莫唑胺与水的比例为8∶1,高压均质压力为60 psi,经过15次高压均质处理后,替莫唑胺的溶解度与未经高压均质机作用相比溶解度提高了95.11%,平均粒径减小257 nm,Zeta电位为-26.7 mV。结论经最佳工艺处理后的样品溶解度提高了95.11%,分散均匀,稳定性较好,对替莫唑胺的进一步应用提供了理论基础。
Objective To explore the method of increasing the solubility of temozolomide.Methods The solubility of temozolomide was determined by UV spectrophotometry under acid condition.The best solution process was optimized through single factors and orthogonal.The samples were tested by infrared spectrum,particle size and Zeta potential.Results The optimal extraction conditions were obtained as follows:the surfactant was nicotinamide,the temozolomide to water ratio was 8∶1,the pressure was 60 psi and times were 15 in high pressure homogenizer.Under this condition,the solubility of TMZ was increased by 95.11%,compared with TMZ without homogenizer.The average size was 257 nm,Zeta potential was 26.7 mv.Conclusion After optimum treatment,the solubility increases 3.36 mg/ml,and TMZ has uniform dispersion and good stability.This provides a theoretical basis for the further application of temozolomide.
Objective To explore the method of increasing the solubility of temozolomide.Methods The solubility of temozolomide was determined by UV spectrophotometry under acid condition.The best solution process was optimized through single factors and orthogonal.The samples were tested by infrared spectrum,particle size and Zeta potential.Results The optimal extraction conditions were obtained as follows:the surfactant was nicotinamide,the temozolomide to water ratio was 8∶1,the pressure was 60 psi and times were 15 in high pressure homogenizer.Under this condition,the solubility of TMZ was increased by 95.11%,compared with TMZ without homogenizer.The average size was 257 nm,Zeta potential was 26.7 mv.Conclusion After optimum treatment,the solubility increases 3.36 mg/ml,and TMZ has uniform dispersion and good stability.This provides a theoretical basis for the further application of temozolomide.
引文
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[3] 赵彩霞,刘军.替莫唑胺治疗脑胶质瘤的临床应用进展[J].临床误诊误治,2009,2(03):70-73.
[4] 马逾英,钟世红,贾敏如,等.紫外分光光度法测定川白芷中总香豆素类成分的含量[J].华西药学杂志,2005,20(02):159-160.
[5] 艾德平.高压均质技术在化工行业中的应用[J].江西化工,2008(04):194-196.
[6] 张吉祥,欧来良.正交试验法优化超声提取枣核总黄酮[J].食品科学,2012(04):18-21.
[7] 王玮,程黎,赵辉,等.拉曼光谱法与经典方法验证对乙酰氨基酚固体分散体[J].光散射学报,2011,23(03):263-270.