混合疏水法增强难水溶性药物扎尔托洛芬的溶解度

Kate Ba, Phulzalke Sb, Deshmukh Mt
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引用次数: 3

摘要

本研究可能是最早尝试采用混合亲水性和混合溶解度方法来提高扎尔托洛芬溶解度的研究。选择扎尔托洛芬作为模型药物是因为它几乎不溶于水,因此需要增加溶解度以更好地吸收和提高治疗效果。在处方前研究中,筛选了药物赋形剂的物理相容性,并观察了Zaltoprofen与选定的增溶剂的相容性。在药物增溶剂干扰研究中,对Zaltoprofen的紫外分光光度分析没有观察到增溶剂存在的干扰。Zaltoprofen的溶解度为0.028 mg/ml。根据溶解度增强比,选择乙酸钠、苯甲酸钠、水杨酸钠、乙醇、PEG 600、无水哌嗪等增溶剂进行增溶研究。在柠檬酸钠、柠檬酸、尿素、peg6000、peg4000、peg200、peg400、丙二醇和甘油中的溶解度增强比选定的增溶剂要小。室温下对药物在亲水溶液中的溶解度进行了测定,不同亲水溶液的增溶力可分为:无水哌嗪>水杨酸钠>苯甲酸钠>乙酸钠> PEG 600。从Zaltoprofen在增溶剂中的平衡溶解度曲线可以看出,Zaltoprofen的溶解度随增溶剂浓度的增加呈非线性函数关系。关键词:混合亲和性,扎尔托洛芬,溶解度,选择性COX2抑制剂
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Solubility Enhancement of Poorly Water Soluble Drug Zaltoprofen by Mixed Hydrotropy Approach
The present study is probably the earliest attempt to enhance Solubility of Zaltoprofen by using mixed hydrotropy and mixed solvency approaches.  Zaltoprofen is selected as model drug because it is practically insoluble in water hence there is need to increase the solubility for better absorption and improved therapeutic efficacy. In the preformulation study physical compatibility of the drug-excipient was screened  and compatibility was observed between Zaltoprofen and selected solubilizers. In the drug solubilizers interference study no interference was observed in UV spectrophometric analysis of Zaltoprofen in presence of employed solubilizers. Aqueous solubility of Zaltoprofen was found 0.028 mg/ml. The solubilizers sodium acetate, sodium benzoate and sodium salicylate, ethanol, PEG 600, piperazine anhydrous, were selected for solubilization studies on the basis of solubility enhancement ratio. The solubility enhancement ratio in sodium citrate, citric acid, urea, PEG 6000, PEG 4000, PEG 200, PEG 400, propylene glycol and glycerin were found to be less as compare to selected solubilizers. The solubility determination of drug in hydrotropic solutions was carried out at room temperature and solubilizing power of different hydrotropes could be ranked as: Piperazine anhydrous > sodium salicylate > sodium benzoate > sodium acetate > PEG 600. From the equilibrium solubility curves of Zaltoprofen in solubilisers it was concluded that increase in the solubility was nonlinear function with respect to the hydrotrope concentration. Keywords: Mixed hydrotropy, Zaltoprofen, solubility, selective COX2 inhibitor
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