In this paper, rectal absorption and tissue tolerance of amoxicillin sodium (AS) suppositories prepared in a hydrophilic base, polyethylene glycol (PEG) or lipophilic base, Suppocire® NA 15 (SNA 15), were investigated. Following in vitro characterization, including drug distribution in the suppository bases, drug-base interactions and drug release, pharmacokinetics were investigated in rabbits to determine absolute bioavailability (F) at two dose levels (100 mg and 200 mg). Both types of suppositories were found uniform in weight and content. Powder X-ray diffraction (XRD) and differential scanning calorimetry indicated that AS existed as solid dispersion or anhydrous crystalline dispersion in both suppositories at different ratios without changing melting points of the bases. This was supported by Fourier transform infrared (FTIR) spectroscopy and scanning electron microscopy conjugated with energy dispersive X-ray (SEM/EDX). In dissolution medium, melting and spreading of SNA 15 and dissolution of PEG suppositories accounted for their different drug release kinetics and mean dissolution time (MDT). A rapid and complete amoxicillin absorption (F close to 100%) with a double peak pharmacokinetic profile was observed alongside minimal signs of tissue irritation in rabbits treated with SNA 15 suppositories at both dose levels. In contrast, the F of amoxicillin from PEG suppositories was 59%, increasing to 77.3% as AS dose doubled from 100 mg to 200 mg, reflected in the slower release predominately controlled by erosion of the base. An in vitro – in vivo correlation was observed (MDT vs F; p < 0.01). AS was stable in SNA 15 suppositories at least for three months at 20 ± 0.2 °C. This research highlighted the advantages of SNA 15 suppositories over the PEG suppositories in providing rapid and complete rectal absorption of AS and tissue compatibility.

在本文中，研究了在亲水性基质、聚乙二醇 (PEG) 或亲脂性基质 Suppocire® NA 15 (SNA 15) 中制备的阿莫西林钠 (AS) 栓剂的直肠吸收和组织耐受性。体外继表征，包括栓剂基质中的药物分布、药物-基质相互作用和药物释放、在兔中研究药代动力学以确定两个剂量水平（100mg 和 200mg）的绝对生物利用度 (F)。发现两种栓剂的重量和含量均一。粉末 X 射线衍射 (XRD) 和差示扫描量热法表明，AS 以固体分散体或无水结晶分散体的形式存在于两种栓剂中，以不同的比例存在而不改变基质的熔点。这得到了傅里叶变换红外 (FTIR) 光谱和与能量色散 X 射线 (SEM/EDX) 共轭的扫描电子显微镜的支持。在溶解介质中，SNA 15 的熔化和扩散以及 PEG 栓剂的溶解解释了它们不同的药物释放动力学和平均溶解时间 (MDT)。在用两种剂量水平的 SNA 15 栓剂治疗的兔子中，观察到快速和完全的阿莫西林吸收（F 接近 100%），具有双峰药代动力学特征，同时组织刺激的迹象最小。相比之下，PEG 栓剂中阿莫西林的 F 为 59%，随着 AS 剂量从 100 mg 增加到 200 mg，增加到 77.3%，反映在主要由基质侵蚀控制的缓慢释放中。一个 PEG 栓剂中阿莫西林的 F 为 59%，随着 AS 剂量从 100 mg 增加到 200 mg，增加到 77.3%，反映在主要由基质侵蚀控制的缓慢释放中。一个 PEG 栓剂中阿莫西林的 F 为 59%，随着 AS 剂量从 100 mg 增加到 200 mg，增加到 77.3%，反映在主要由基质侵蚀控制的缓慢释放中。一个观察到体外-体内相关性（MDT vs F；p  < 0.01）。AS 在 SNA 15 栓剂中在 20 ± 0.2 °C 下至少稳定三个月。该研究强调了 SNA 15 栓剂在提供 AS 的快速和完全直肠吸收和组织相容性方面优于 PEG 栓剂的优势。