| 摘要: |
| 为了解决阿苯达唑的溶解性和口服吸收难题，借助高分子活性剂的稳定作用，利用反溶剂法-高压匀质法制备阿苯达唑纳米混悬剂，并考察该制剂的药学特征及稳定性；研究该制剂在大鼠体内的药代动力学。研究创制的纳米混悬液在电镜下药物形状大小均一，中位粒径为358.1nm。其药学特征符合《兽药质量标准》（2017版）中对混悬液的质量要求。6个月加速试验表明，该制剂外观色泽、含量、pH值、沉降体积比、重分散性均未发生明显变化，且放置6个月后粒径没有显著变化。该阿苯达唑纳米混悬液的Cmax为5.895μg/mL，显著高于参比制剂阿苯达唑伊维菌素粉、佛山正典阿苯达唑混悬液的2.804和2.053μg/mL。与阿苯达唑伊维菌素粉、佛山正典阿苯达唑混悬液相比，该制剂的相对生物利用度分别为214% 和299.74% ，表明该阿苯达唑纳米混悬液能显著提高阿苯达唑的吸收，将有助于提高临床治疗效果。 |
| 关键词: 阿苯达唑、纳米晶体、混悬液、药动学、生物利用度 |
| DOI： |
| 投稿时间：2021-11-25修订日期：2022-03-07 |
| 基金项目: |
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| Preparation and Evaluation of Albendazole Nanosuspensions |
|
| (Shenyang Vica Animal Biotechnology Technology Co., Ltd) |
| Abstract: |
| In order to solve the problem of the solubility and oral absorption of albendazole, this study used the anti-solvent method-high pressure homogenization
method to prepare the albendazole nano-suspension with the help of the stabilizing effect of the polymer active agent, and investigated the pharmacy of the preparation
Characteristics and stability; study its pharmacokinetics in rats. Under the electronmicroscope, the nano-suspension created by the research was uniform in shape and size, and the median diameter was 358.1nm. The pharmaceutical characteristics of this nanosuspension meeted the quality requirements of the suspension in the "Quality Standards for Veterinary Drugs" (2017 edition). The 6-month accelerated test showed that the appearance, color, content, pH value, sedimentation volume ratio, and re-dispersibility of the preparation did not change significantly, and the particle size after 6 months of storage did not change significantly. The Cmax of the albendazole nano-suspension was 5.895 μg/mL, which was significantly higher than the 2.804 and 2.053 μg/mL of the reference preparation albendazole and ivermectin powder and Foshan Zhengdian albendazole suspension. Compared with albendazole ivermectin powder and Foshan Zhengdian albendazole suspension, the relative bioavailability of the preparation was 214% and 299.74%, respectively； indicating that the albendazole nano-suspension can significantly improve the absorption of albendazole and
will help improve the clinical treatment effect. |
| Key words: Albendazole, nanocrystals, suspension, pharmacokinetics, bioavailability |
