Investigating the Effect of Basic Amino Acids and Glucosamine on the Solubility of Ibuprofen and Piroxicam.

IF 3.1 Q2 PHARMACOLOGY & PHARMACY
Hadi Valizadeh, Somayeh Mahdinloo, Negin Zakeri, Muhammad Sarfraz, Saeed Nezafat, Parvin Zakeri-Milani
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Abstract

Purpose: Poor aqueous solubility hampers the development of several compounds as pharmacological agents. Hence, preparing novel formulations with augmented absorption is a challenge in pharmaceutical industries. In this paper, we have examined the effect of basic amino acids including arginine (ARG), lysine (LYS), and glucosamine (GlucN) on the solubility of ibuprofen (IBU) and piroxicam (PXM) as drugs with limited solubility. We have also studied the effect of the dissolution media with the pH values 1.2 to 7.4.

Methods: The saturation shake-flask method was used for solubility studies in the presence of amino acids. Briefly, buffer solutions containing different concentrations of amino acids were prepared. Then, an excess amount of each drug with these buffers was shaken to reach equilibrium. After 48 hours, the upper phase was separated, and solubility was calculated by reading their UV-Vis absorbance.

Results: The results illustrated that amino acids increased solubility of both drugs with different ratios, which were pH and concentration-dependent. Solubility improved as the amount of amino acids went up, and this upward pattern was more robust with ARG than LYS. The presence of GlucN in citrate buffer significantly enhanced IBU solubility. The solubility of PXM in accompany of GlucN in water did not change significantly while in citrate buffer solubility enhanced specially at pH 6.

Conclusion: Overall, GlucN in citrate buffer and ARG in phosphate buffer could be introduced as the most suitable media for IBU and PXM solubility improvement, respectively.

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碱性氨基酸和氨基葡萄糖对布洛芬和吡洛昔康溶解度的影响。
目的:水溶性差阻碍了一些化合物作为药物的发展。因此,制备具有增强吸收的新型制剂是制药工业的一个挑战。本文研究了精氨酸(ARG)、赖氨酸(LYS)和葡萄糖胺(GlucN)等碱性氨基酸对布洛芬(IBU)和吡罗西康(PXM)溶解度的影响。我们还研究了pH值为1.2 ~ 7.4的溶解介质的影响。方法:采用饱和摇瓶法研究氨基酸存在下的溶解度。简单地说,制备了含有不同浓度氨基酸的缓冲溶液。然后,用这些缓冲液摇动过量的每种药物以达到平衡。48小时后,分离上相,通过读取其UV-Vis吸光度计算溶解度。结果:氨基酸对两种药物的溶解度均有不同比例的提高,且呈pH和浓度依赖性。溶解度随着氨基酸含量的增加而提高,而ARG的这种上升模式比LYS更强。柠檬酸缓冲液中葡聚糖的存在显著提高了IBU的溶解度。PXM与葡聚糖在水中的溶解度变化不明显,而在柠檬酸盐缓冲液中的溶解度在pH 6时增强。结论:总体而言,柠檬酸缓冲液中的葡糖苷和磷酸盐缓冲液中的ARG可分别作为改善IBU和PXM溶解度的最合适培养基。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Advanced pharmaceutical bulletin
Advanced pharmaceutical bulletin PHARMACOLOGY & PHARMACY-
CiteScore
6.80
自引率
2.80%
发文量
51
审稿时长
12 weeks
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