治疗胃溃疡的甘草酸单铵胃内保留给药系统的研制与评价

IF 0.6 Q4 PHARMACOLOGY & PHARMACY Journal of Research in Pharmacy Pub Date : 2023-01-01 DOI:10.29228/jrp.472
V. Patole, Harshad S Kapare, J. Mahore, Rachana Bhimanwar, Devyani Awari, Pranali Jadhav
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引用次数: 0

摘要

甘草酸一铵(MAG)是甘草酸的一种盐,据报道可有效治疗胃疾病。该工作旨在设计和开发一种胃保留性药物递送系统,通过开发具有足够强度和酸中和电位的稳定筏体来延迟MAG在胃中的释放。初步进行了MAG与胃质子泵中存在的天然配体(Vonoprazan,一种潜在的质子泵抑制剂)的硅分子对接研究。对接研究预测MAG可以结合Vonoprazan结合位点,表明其具有抑制胃质子泵的能力。优选出的MAG筏形片最佳处方为满意度(0.819)。优化后的配方筏体强度为8.61±0.06 g,酸中和能力为11.19±0.03 mEq, MAG体外释放量为69.11±0.61% (8h),表明其是一种潜在的胃保留筏体形成递送系统。优化后的配方能显著降低幽门结扎引起的胃溃疡动物模型胃酸产量,提高胃pH值(p< 0.001),显著降低溃疡指数(p< 0.001)。所研制的MAG木筏形片剂有望替代现有的合成药物治疗胃溃疡。
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Development and evaluation of gastro retentive drug delivery system of monoammonium glycyrrhizinate for the management of gastric ulcer
: Monoammonium glycyrrhizinate (MAG), a salt of glycyrrhizin, is reported for effective treatment of gastric disorders. The work was aimed to design and develop a gastro-retentive drug delivery system for MAG to delay its release in stomach by developing a stable raft with sufficient strength and acid-neutralizing potential. Preliminary, in-silico molecular docking study of MAG with the native ligand (Vonoprazan, a potential proton pump inhibitor) present in the gastric proton pump was performed. Docking studies predicted that MAG could bind to Vonoprazan binding site, indicating its ability to inhibit the gastric proton pump. The most desirable optimal formulation of raft forming tablets of MAG was anticipated with the desirability (0.819). The optimized formulation showed raft strength (8.61 ± 0.06 g), acid neutralizing capacity (11.19 ± 0.03 mEq) and in vitro release of MAG (69.11 ± 0.61% over 8h) indicating its suitability as a potential Gastro-retentive raft forming delivery system. The optimized formulation decreased gastric acid production and elevated gastric pH (p< 0.001.) in pylorus ligation induced gastric ulcers in animal model and demonstrated significant decrease in ulcer index (p< 0.001.) The developed raft-forming tablet of MAG could be a promising alternative to the existing synthetic agents to treat gastric ulcers.
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来源期刊
Journal of Research in Pharmacy
Journal of Research in Pharmacy PHARMACOLOGY & PHARMACY-
CiteScore
1.00
自引率
12.50%
发文量
80
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