Following the preparation of inclusion complex of cetirizine (CTZ) and β-cyclodextrin (β-CD), the compound was investigated to assess the possibility of modifying the physicochemical properties (solubility, release, stability, permeability) of CTZ after complexation that are vital for subsequent formulation studies involving the said complex. Changes in FT-IR/Raman spectra, DSC thermograms and XRD diffractograms confirmed the formation of a CTZ–β-CD system. Hydrophilic interaction chromatography with a DAD detector was employed to determine alterations of the CTZ concentration during studies following complexation. An analysis of a phase-solubility diagram of cCTZ = fcβ-CD indicated a linear rise in the solubility of CTZ as the concentration of β-CD increased. The inclusion of CTZ in a system with β-CD significantly reduced the instability of CTZ in the presence of oxidizing factors. It was also found that regardless of the pH of the acceptor fluids used in the release studies an increase was observed in the concentration of CTZ in CD system compared to its free form. The ability to permeate artificial biological membranes manifested by CTZ after complexation was enhanced as well. In summary, CD has significant potential to mask the bitter taste of CTZ and to counter the instability induced by oxidizing factors.

中文翻译：

---

β-环糊精中加入盐酸西替利嗪的影响

在制备西替利嗪 (CTZ) 和 β-环糊精 (β-CD) 的包合物后，对该化合物进行了研究，以评估在络合后改变 CTZ 的重要理化性质（溶解度、释放、稳定性、渗透性）的可能性用于涉及所述复合物的后续制剂研究。FT-IR/Raman 光谱、DSC 热谱图和 XRD 衍射图的变化证实了 CTZ-β-CD 系统的形成。使用带有 DAD 检测器的亲水相互作用色谱法来确定复合后研究期间 CTZ 浓度的变化。对 cCTZ = fcβ-CD 的相溶解度图的分析表明，随着 β-CD 浓度的增加，CTZ 的溶解度呈线性上升。在具有 β-CD 的系统中包含 CTZ 显着降低了 CTZ 在氧化因子存在下的不稳定性。还发现，无论释放研究中使用的受体流体的 pH 值如何，都观察到 CD 系统中 CTZ 浓度与其游离形式相比有所增加。复合后CTZ表现出的对人工生物膜的渗透能力也增强了。总之，CD 具有掩盖 CTZ 苦味和对抗氧化因素引起的不稳定性的巨大潜力。复合后CTZ表现出的对人工生物膜的渗透能力也增强了。总之，CD 具有掩盖 CTZ 苦味和对抗氧化因素引起的不稳定性的巨大潜力。复合后CTZ表现出的对人工生物膜的渗透能力也增强了。总之，CD 具有掩盖 CTZ 苦味和对抗氧化因素引起的不稳定性的巨大潜力。