The influence of natural polymers on loratadine's solubility and dissolution profiles.

Q3 Medicine Journal of Medicine and Life Pub Date : 2024-03-01 DOI:10.25122/jml-2023-0529

Hussein Alkufi, Suad Lateef Ibrahim, Lina Salim Hussein

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Abstract

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.

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天然聚合物对氯雷他定溶解度和溶解曲线的影响

第二代三环 H1 抗组胺药物氯雷他定（LTD）具有高渗透性、低水溶性，口服吸收率取决于其在胃肠道中的溶解速度。改善药物溶解度和溶解速率的一种方法是天然固体分散剂（NSD）。本研究评估了亲水性天然聚合物海藻酸钠（SA）、透明质酸（HA）和木聚糖（XG）在天然固体分散体中的使用情况，以提高 LTD 的溶解度和溶解速率。共生产了 12 种不同药物与聚合物比例的制剂，并对其产量百分比、水溶性和体外溶解率进行了分析。在所有配方中，LTD 的溶解度都有所提高。NSD1（LTD：SA 1:0.25）取得了极佳的效果，产量高（99%），溶解度（0.187）优于纯氯雷他定（0.0021），30 分钟内溶解速度快（98%）。这些研究表明，SA、HA 和 XG 等天然聚合物可显著提高氯雷他定的溶解度。当引入 NSD 时，这些聚合物可有效提高 LTD 的溶解速率，为提高生物利用度和疗效带来了诱人的前景。

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来源期刊

Journal of Medicine and Life Medicine-Medicine (all)

CiteScore

1.90

自引率

0.00%

发文量

202

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.