Alrabiah Haitham, Aljohar Haya I, Bakheit Ahmed Hassan, Homoda Atef Ma, Mostafa Gamal Abdel-Hafiz
Pharmaceutical Chemistry Department, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
Micro-analytical Laboratory, Applied Organic Chemistry Department, National Research Center, Dokki, Cairo, Egypt.
Drug Des Devel Ther. 2019 Jul 11;13:2283-2293. doi: 10.2147/DDDT.S201907. eCollection 2019.
Trazodone (TRZ) is a second-generation non-tricyclic antidepressant derived from a triazolopyridine derivative, which is mainly used to treat emotional disorders and conditions related to depressive disorders.
This study investigated the design, development and characteristics of polyvinyl chloride (PVC) membrane sensors for trazodone HCl (TRZ).
The developed sensing membranes were constructed using β-cyclodextrin (β-CD; sensor 1), γ-cyclodextrin (γ-CD; sensor 2) or 4--butylcalix[8]arene (-BC8; sensor 3) ionophores as sensing materials in addition to ionic sites and dioctyl phthalate in the PVC matrix.
Sensors 1, 2 and 3 displayed fast, stable and near-Nernstian response over a relatively wide trazodone concentration range (7.0×10-1×10, 5.0×10-1×10and 8.0×10-1.0×10 M, respectively), with detection limits of 2.2×10, 1.5×10 and 2.42×10 M, respectively in the pH range of 3.0-6.0. The sensors demonstrated good selectivity for TRZ in the presence of different ionic compounds. The accuracy and precision of the proposed sensors were assessed by the determination of 40.7 μg/ml of TRZ, which showed average recoveries of 99.6%, 99.1% and 98.5% with mean relative standard deviations of 2.4%, 2.5% and 2.6% for sensor 1, 2 and 3 respectively. Molecular modeling was used to calculate the host-guest binding energy. The lowest free binding energy was -6.243, -5.752 and -5.7105 kcal/mol for 1:1 stoichiometry host-guest complexes of trazodone and β-CD, γ-CD and -BC8, respectively, which was in-line with a Nernstian response.
The investigated methods can be applied for the determination of TRZ in pharmaceutical preparations. The results of investigated dosage-form of TRZ show good agreement with those using the US Pharmacopeia method.
曲唑酮(TRZ)是一种源自三唑并吡啶衍生物的第二代非三环类抗抑郁药,主要用于治疗情绪障碍和与抑郁症相关的病症。
本研究考察了盐酸曲唑酮(TRZ)聚氯乙烯(PVC)膜传感器的设计、开发及特性。
所开发的传感膜除了在PVC基质中含有离子位点和邻苯二甲酸二辛酯外,还使用β-环糊精(β-CD;传感器1)、γ-环糊精(γ-CD;传感器2)或4-丁基杯[8]芳烃(-BC8;传感器3)离子载体作为传感材料构建而成。
传感器1、2和3在相对较宽的曲唑酮浓度范围(分别为7.0×10⁻¹×10、5.0×10⁻¹×10和8.0×10⁻¹.0×10 M)内显示出快速、稳定且接近能斯特响应,在pH值为3.0 - 6.0范围内的检测限分别为2.2×10、1.5×10和2.42×10 M。在存在不同离子化合物的情况下,这些传感器对TRZ表现出良好的选择性。通过测定40.7 μg/ml的TRZ评估了所提出传感器的准确性和精密度,结果显示传感器1、2和3的平均回收率分别为99.6%、99.1%和98.5%,平均相对标准偏差分别为2.4%、2.5%和2.6%。采用分子建模计算主客体结合能。曲唑酮与β-CD、γ-CD和 -BC8的1:1化学计量主客体配合物的最低自由结合能分别为 -6.243、-5.752和 -5.7105 kcal/mol,这与能斯特响应一致。
所研究的方法可用于药物制剂中TRZ的测定。所研究的TRZ剂型结果与采用美国药典方法的结果显示出良好的一致性。