激光浊度法与高效液相色谱法测定布洛芬及其2-羟丙基-对环糊精包合物溶解度的比较

IF 0.8 4区 化学 Q4 CHEMISTRY, MULTIDISCIPLINARY South African Journal of Chemistry-Suid-Afrikaanse Tydskrif Vir Chemie Pub Date : 2022-01-01 DOI:10.17159/0379-4350/2022/v76a08
Frank Ssengooba, Thashree Marimuthu, E. Olivier, P. Demana, Y. Choonara
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引用次数: 1

摘要

药物溶解度差是阻碍新药发现和开发的主要问题。需要快速和廉价的技术来获取可靠的药物溶解度数据。本研究以低溶解度模型药物布洛芬及其2-羟丙基-对环糊精包合物(ic)为研究对象,探讨了激光浊度法测定溶解度的适用性。本研究涉及用共沉淀法制备布洛芬-环糊精(1:1)并进行表征。热分析和分子振动评估证实了包合物的存在。采用摇瓶法在酸性和碱性介质中进行测试,并采用高效液相色谱(HPLC)验证溶解度数据。浊度测定结果显示,布洛芬在酸性(0.565 mg ml-1)和碱性(7.5 mg ml-1)介质中的溶解度都相对增强,这是通过包合物的形成实现的。HPLC结果与浊度测定结果相似,在酸性(0.454 mg ml-1)和碱性(201.73 mg ml-1)介质中的溶解度值均有所增加。激光浊度法是测定母体药物及其载体体系溶解度的一种快速、经济的方法。关键词:环糊精,布洛芬,包合物,激光比浊法,溶解度
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Comparison of laser nephelometric and HPLC techniques for efficient determination of solubility of ibuprofen and its 2-hydroxypropyl-p-cyclodextrin inclusion complex
ABSTRACT Poor drug solubility is a major problem that hinders the discovery and development of new drugs. There is a need for rapid and inexpensive techniques for acquiring reliable drug solubility data. In this study, the suitability of laser nephelometry for the determination of solubility was investigated using ibuprofen, as a model drug of low solubility, and its 2-hydroxypropyl-p-cyclodextrin inclusion complex (ic). This investigation involved the preparation of ibuprofen-ic-cyclodextrin (1:1) using coprecipitation and characterisation. Thermal analysis and assessment of molecular vibrations confirmed the existence of the inclusion complex. The shake flask testing method was employed and carried out in acidic and alkaline media, and solubility data were verified against high-performance liquid chromatography (HPLC). Results obtained via nephelometry showed relative enhanced solubility of ibuprofen in both acidic (0.565 mg ml-1) and basic (7.5 mg ml-1) media, respectively, which was enabled via inclusion complex formation. Relative to nephelometry data, HPLC results showed a similar trend with increased solubility values in acidic (0.454 mg ml-1) and basic (201.73 mg ml-1) media, respectively. The application of laser nephelometry proved to be a quick and relatively cost-effective technique for solubility measurements of the parent drug and its carrier system. Keywords: cyclodextrin, ibuprofen, inclusion complex, laser nephelometry, solubility
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来源期刊
CiteScore
3.10
自引率
0.00%
发文量
6
审稿时长
>12 weeks
期刊介绍: Original work in all branches of chemistry is published in the South African Journal of Chemistry. Contributions in English may take the form of papers, short communications, or critical reviews.
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