{"title":"天然聚合物对氯雷他定溶解度和溶解曲线的影响","authors":"Hussein Alkufi, Suad Lateef Ibrahim, Lina Salim Hussein","doi":"10.25122/jml-2023-0529","DOIUrl":null,"url":null,"abstract":"<p><p>Second-generation tricyclic H1 antihistamine loratadine (LTD) has a high permeability, low water solubility, and an oral absorption rate dependent on the rate at which it dissolves in the gastrointestinal tract. One approach suggested for improving the drug's solubility and rate of dissolution is natural solid dispersion (NSD). The present study evaluated the use of hydrophilic natural polymers, sodium alginate (SA), hyaluronic acid (HA), and xyloglucan (XG), in natural solid dispersion to enhance LTD solubility and dissolution rate. A total of 12 formulations comprising varied drug-to-polymer ratios were produced and analyzed for percentage yield, water solubility, and in vitro dissolution rate. The solubility of LTD was improved in all formulations. Excellent results were achieved with NSD1 (LTD: SA 1:0.25), with a high yield (99%), superior solubility (0.187) compared to pure loratadine (0.0021), and a speedy dissolution rate (98%) within 30 minutes. These studies suggest natural polymers like SA, HA, and XG can considerably increase LTD solubility. When introduced into NSD, these polymers effectively augment LTD dissolving rates, presenting attractive prospects for better bioavailability and therapeutic efficacy.</p>","PeriodicalId":16386,"journal":{"name":"Journal of Medicine and Life","volume":"17 3","pages":"305-308"},"PeriodicalIF":0.0000,"publicationDate":"2024-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11262610/pdf/","citationCount":"0","resultStr":"{\"title\":\"The influence of natural polymers on loratadine's solubility and dissolution profiles.\",\"authors\":\"Hussein Alkufi, Suad Lateef Ibrahim, Lina Salim Hussein\",\"doi\":\"10.25122/jml-2023-0529\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Second-generation tricyclic H1 antihistamine loratadine (LTD) has a high permeability, low water solubility, and an oral absorption rate dependent on the rate at which it dissolves in the gastrointestinal tract. One approach suggested for improving the drug's solubility and rate of dissolution is natural solid dispersion (NSD). The present study evaluated the use of hydrophilic natural polymers, sodium alginate (SA), hyaluronic acid (HA), and xyloglucan (XG), in natural solid dispersion to enhance LTD solubility and dissolution rate. A total of 12 formulations comprising varied drug-to-polymer ratios were produced and analyzed for percentage yield, water solubility, and in vitro dissolution rate. The solubility of LTD was improved in all formulations. Excellent results were achieved with NSD1 (LTD: SA 1:0.25), with a high yield (99%), superior solubility (0.187) compared to pure loratadine (0.0021), and a speedy dissolution rate (98%) within 30 minutes. These studies suggest natural polymers like SA, HA, and XG can considerably increase LTD solubility. When introduced into NSD, these polymers effectively augment LTD dissolving rates, presenting attractive prospects for better bioavailability and therapeutic efficacy.</p>\",\"PeriodicalId\":16386,\"journal\":{\"name\":\"Journal of Medicine and Life\",\"volume\":\"17 3\",\"pages\":\"305-308\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2024-03-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11262610/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Medicine and Life\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.25122/jml-2023-0529\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"Medicine\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Medicine and Life","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.25122/jml-2023-0529","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"Medicine","Score":null,"Total":0}
The influence of natural polymers on loratadine's solubility and dissolution profiles.
Second-generation tricyclic H1 antihistamine loratadine (LTD) has a high permeability, low water solubility, and an oral absorption rate dependent on the rate at which it dissolves in the gastrointestinal tract. One approach suggested for improving the drug's solubility and rate of dissolution is natural solid dispersion (NSD). The present study evaluated the use of hydrophilic natural polymers, sodium alginate (SA), hyaluronic acid (HA), and xyloglucan (XG), in natural solid dispersion to enhance LTD solubility and dissolution rate. A total of 12 formulations comprising varied drug-to-polymer ratios were produced and analyzed for percentage yield, water solubility, and in vitro dissolution rate. The solubility of LTD was improved in all formulations. Excellent results were achieved with NSD1 (LTD: SA 1:0.25), with a high yield (99%), superior solubility (0.187) compared to pure loratadine (0.0021), and a speedy dissolution rate (98%) within 30 minutes. These studies suggest natural polymers like SA, HA, and XG can considerably increase LTD solubility. When introduced into NSD, these polymers effectively augment LTD dissolving rates, presenting attractive prospects for better bioavailability and therapeutic efficacy.
期刊介绍:
The Journal of Medicine and Life publishes peer-reviewed articles from various fields of medicine and life sciences, including original research, systematic reviews, special reports, case presentations, major medical breakthroughs and letters to the editor. The Journal focuses on current matters that lie at the intersection of biomedical science and clinical practice and strives to present this information to inform health care delivery and improve patient outcomes. Papers addressing topics such as neuroprotection, neurorehabilitation, neuroplasticity, and neuroregeneration are particularly encouraged, as part of the Journal''s continuous interest in neuroscience research. The Editorial Board of the Journal of Medicine and Life is open to consider manuscripts from all levels of research and areas of biological sciences, including fundamental, experimental or clinical research and matters of public health. As part of our pledge to promote an educational and community-building environment, our issues feature sections designated to informing our readers regarding exciting international congresses, teaching courses and relevant institutional-level events.