Influence of choline-based ionic liquids as neoteric green solvents on aqueous solubility of lamotrigine and piroxicam drugs

Q4 Pharmacology, Toxicology and Pharmaceutics

Infarma Pharmaceutical Sciences Pub Date : 2022-03-14 DOI:10.34172/ps.2022.12

H. Shekaari, Negar Basteholia, Masumeh Mokhtarpour, M. T. Zafarani-Moattar

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Abstract

Background: The low aqueous solubility of three important drugs (betamethasone (BETA), meloxicam (MEL) and piroxicam (PIR)) have been increased by use of deep eutectic solvents (DESs) based choline chloride/urea (ChCl/U), choline chloride/ethylene glycol (ChCl/EG) and choline chloride/glycerol (ChCl/G) as new class of solvents at T = (298.15 to 313.15) K. Methods: DESs were prepared by combination of the ChCl/EG, U and G with the molar ratios: 1:2. The solubility of drugs in the aqueous DESs solutions was measured at different temperatures with shake flask method. Results: The solubility of the investigated drugs increased with increasing the weight fraction of DESs. The solubility data were correlated by e-NRTL and Wilson models. Also, the thermodynamic functions, Gibbs energy, enthalpy, and entropy of dissolution were calculated. Conclusion: At the same composition of co-solvents and temperature, the BETA, PIR and MEL solubility was highest in (ChCl/U + water), (ChCl/U + water) and (ChCl/EG + water) respectively. The calculated solubility based on these models was in good agreement with the experimental values. In addition, the results show that, the main contribution for drugs solubility in the aqueous DES solutions is the enthalpy.

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胆碱基离子液体作为新绿色溶剂对拉莫三嗪和吡罗康类药物水溶性的影响

背景:在T = (298.15 ~ 313.15) k时，以氯化胆碱/尿素(ChCl/U)、氯化胆碱/乙二醇(ChCl/EG)和氯化胆碱/甘油(ChCl/G)为新溶剂，采用深度共晶溶剂(DESs)，提高了三种重要药物倍他米松(BETA)、美洛昔康(MEL)和吡洛昔康(PIR)的低水溶性。方法:将ChCl/EG、U、G按摩尔比1:2组合制备DESs。用摇瓶法测定了不同温度下药物在DESs水溶液中的溶解度。结果:随着DESs质量分数的增加，所研究药物的溶解度增加。溶解度数据通过e-NRTL和Wilson模型进行相关性分析。同时，计算了溶解的热力学函数、吉布斯能、焓和熵。结论:在相同助溶剂组成和温度下，β、PIR和MEL分别在(ChCl/U +水)、(ChCl/U +水)和(ChCl/EG +水)中溶解度最高。模型计算的溶解度与实验值吻合较好。另外，研究结果表明，影响药物在DES水溶液中溶解度的主要因素是焓。

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