Simultaneous determination of kolliphor HS15 and miglyol 812 in microemulsion formulation by ultra-high performance liquid chromatography coupled with nano quantity analyte detector

A novel method for simultaneous determination of kolliphor HS15 and miglyol 812 in microemulsion formulation was developed using ultra-high performance liquid chromatography coupled with a nano quantitation analytical detector （UHPLC-NQAD）. All components in kolliphor HS15 and miglyo1812 were well separated on an Acquity BEH C18 column. Mobile phase A was 0.1% trifluoroacetic acid （TFA） in water and mobile phase B was acetonitrile. A gradient elution sequence was programed initially with 60% organic solvent, slowly increased to 100% within 8 min. The flow rate was 0.7 mL/min. Good linearity （r 〉 0.95） was obtained in the range of 27.6-1381.1 μg/mL for polyoxyl 15 hydroxystearate in kolliphor HS15, 0.8-202.0 μg/mL for caprylic acid triglyceride and 2.7-221.9μg/mL for capric acid triglyceride in miglyol 812. The relative standard deviations （RSD） ranged from 0.6% to 1.7% for intra-day precision and from 0.4% to 2.7% for inter-day precision. The overall recoveries （accuracy） were 99.7%-101.4% for polyoxyl 15 hydroxystearate in kolliphor HS15, 96.7%-99.6% for caprylic acid triglyceride, and 94.1%- 103.3% for capric acid triglyceride in miglyol 812. Quantification limits （QL） were determined as 27.6 μg/ mL for polyoxy115 hydroxystearate in kolliphor HS15, 0.8 μg/mL for caprylic acid triglyceride, and 2.7 μg/ mL for capric acid triglyceride in miglyol 812. No interferences were observed in the retention time ranges of kolliphor HSI5 and miglyol 812. The method was validated in terms of specificity, linearity, precision, accuracy, QL, and robustness. The proposed method has been applied to microemulsion for- mulation analyses with good recoveries （82.2%-103.4%）.

一种以Kolliphor HS 15为增溶剂的参麦注射液的稳定性和安全性研究

目的:制备Kolliphor HS 15(HS 15)参麦注射液,并研究其稳定性和安全性。方法:首先,通过考察灭菌前后p H、粒径和溶液性状的变化,以及冻融实验前后可见异物和粒径的比较,进行稳定性考察。其次,以模拟市售参麦注射液(含0.5%注射用聚山梨酯80)为参照,考察HS 15参麦注射液的稳定性、溶血性和血管刺激性。最后,比较HS 15、注射用聚山梨酯80和普通级聚山梨酯80对大鼠嗜碱性细胞白细胞RBL-2H3的脱颗粒率及与人血清孵育后系统中SC5b-9含量,评价空白辅料及含药制剂的致敏性。结果:0.2%的HS 15参麦注射液的稳定性与模拟市售制剂无显著性差异,但溶血率较低,血管刺激性较小;HS 15的致敏性低于注射用和普通级聚山梨酯80。结论:HS 15具有较高的安全性,可作为增溶剂取代市售参麦注射液中的聚山梨酯80。

右布洛芬脂肪乳注射液的分析方法及处方筛选

为研究右布洛芬脂肪乳注射液并建立分析方法,对右布洛芬原料药稳定性及原辅料相容性等进行研究以筛选处方。建立了一种反相高效液相色谱法,可测定右布洛芬含量及杂质。通过高温、高湿、强光照条件考察原料药及原辅料混合物的有关物质特性。制备含15羟基硬脂酸聚乙二醇酯(Kolliphor HS 15)不同浓度的右布洛芬脂肪乳注射液,考察剂型的质量。结果发现:线性范围为2.0~50.0μg/mL(R^2=0.9999);原料药对热不稳定,原辅料混合物有关物质均小于1.0%;含Kolliphor HS 150.5%的右布洛芬脂肪乳注射液溶液稳定,有关物质小于1.0%。本研究不仅建立了适用于右布洛芬测定的分析方法,还确认了右布洛芬与所选择辅料无配伍禁忌,筛选的处方可满足质量要求,为产品进一步研究提供了数据支持。

三种增溶剂对冠心宁注射液中蛋白质检测的影响

目的:比较3种增溶剂对冠心宁注射液中有关物质蛋白质检测的影响。方法:分别使用泊洛沙姆188(Kolliphor P188)、聚氧乙烯氢化蓖麻油(Kolliphor RH40)、15-羟基硬脂酸聚乙二醇酯(Kolliphor HS15)3种辅料制备冠心宁注射液,进行有关物质蛋白质的检测。结果:其中Poluoshamu 188、Kolliphor RH40对冠心宁注射液蛋白质检测无影响,而含Kolliphor HS15辅料的冠心宁注射液检测蛋白质时易出现假阳性。结论:3种增溶剂对冠心宁注射液蛋白质的检测影响不同;按影响程度由大到小依次是Kolliphor HS15>Poluoshamu 188=Kolliphor RH40。

非离子型表面活性剂HS 15在药剂中的研究进展

KolliphorHS15(HS15)是一种新型注射用增溶剂,具有强大的增溶能力和优良的安全性,可用于提高药物的溶解度、促进吸收以及增加生物利用度。综述HS15在制剂中的应用、临床研究和基础研究进展,为其在药剂中的应用研究提供参考。