Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El-Aini street, Cairo, 11562, Egypt.
Department of Pharmaceutics, National Organization for Drug Control and Research (NODCAR), Giza, Egypt.
AAPS PharmSciTech. 2022 Apr 26;23(5):124. doi: 10.1208/s12249-022-02280-2.
This study aims to prepare drotaverine hydrochloride superporous hydrogel hybrid systems (DSHH systems) to prolong its residence time in the stomach, provide extended release and reduce its frequency of administration. Drotaverine hydrochloride (DRH) is a spasmolytic drug that suffers from brief residence due to intestinal hypermotility during diarrheal episodes associated with gastrointestinal colics resulting in low bioavailability and repeated dosing. Eight DSHH systems were prepared using gas blowing technique. The prepared DSHH systems were evaluated regarding their morphology, incorporation efficiency, density, porosity, swelling ratio, viscoelastic property, erosion percentage and release kinetics. The FH8 formula containing equal proportion of chitosan (3%) /polyvinyl alcohol (3%) as strengthener and crosslinked with tripolyphosphate showed the highest incorporation efficiency (91.83 ± 1.33%), good swelling ratio (28.32 ± 3.15% after 24 h), optimum viscoelastic properties (60.19 ± 3.82 kPa) and sustained release profile (88.03 ± 2.15% after 24 h). A bioequivalence study was done to compare the bioavailability of the candidate formula versus Spasmocure®. Statistical analysis showed significant (P < 0.05) increase in bioavailability 2.7 folds with doubled Tmax (4 h) compared to the marketed product (2 h). These results declared that the superporous hydrogel hybrid systems could be a potential gastroretentive approach for the sustained delivery of drugs with short residence time with enhanced viscoelasticity.
本研究旨在制备盐酸屈他维林超级多孔水凝胶混合系统（DSHH 系统），以延长其在胃中的停留时间，提供延长释放并减少给药频率。盐酸屈他维林（DRH）是一种解痉药物，由于腹泻发作时肠道蠕动过度，其在胃肠道绞痛相关的腹泻发作时停留时间短暂，导致生物利用度低和重复给药。使用吹气技术制备了 8 种 DSHH 系统。对制备的 DSHH 系统进行了形态学、包封效率、密度、孔隙率、溶胀比、粘弹性、侵蚀率和释放动力学评价。含有等量壳聚糖（3%）/聚乙烯醇（3%）作为增强剂并与三聚磷酸交联的 FH8 配方显示出最高的包封效率（91.83±1.33%）、良好的溶胀比（24 小时后 28.32±3.15%）、最佳的粘弹性（60.19±3.82 kPa）和持续释放曲线（24 小时后 88.03±2.15%）。进行了生物等效性研究，以比较候选配方与 Spasmocure®的生物利用度。统计分析显示，与市售产品（2 小时）相比，候选配方的生物利用度显著增加（P<0.05），增加了 2.7 倍，Tmax 延长了 2 倍（4 小时）。这些结果表明，超级多孔水凝胶混合系统可能是一种具有短停留时间和增强粘弹性的药物持续释放的潜在胃滞留方法。
