V. Patole, Harshad S Kapare, J. Mahore, Rachana Bhimanwar, Devyani Awari, Pranali Jadhav
{"title":"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","authors":"V. Patole, Harshad S Kapare, J. Mahore, Rachana Bhimanwar, Devyani Awari, Pranali Jadhav","doi":"10.29228/jrp.472","DOIUrl":null,"url":null,"abstract":": 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.","PeriodicalId":17096,"journal":{"name":"Journal of Research in Pharmacy","volume":"141 1","pages":""},"PeriodicalIF":0.6000,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Development and evaluation of gastro retentive drug delivery system of monoammonium glycyrrhizinate for the management of gastric ulcer\",\"authors\":\"V. Patole, Harshad S Kapare, J. Mahore, Rachana Bhimanwar, Devyani Awari, Pranali Jadhav\",\"doi\":\"10.29228/jrp.472\",\"DOIUrl\":null,\"url\":null,\"abstract\":\": 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.\",\"PeriodicalId\":17096,\"journal\":{\"name\":\"Journal of Research in Pharmacy\",\"volume\":\"141 1\",\"pages\":\"\"},\"PeriodicalIF\":0.6000,\"publicationDate\":\"2023-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Research in Pharmacy\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.29228/jrp.472\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Research in Pharmacy","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.29228/jrp.472","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
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.