含左氧氟沙星和法莫替丁的控释双层漂浮泡腾片和非泡腾片

IF 3.4 4区 化学 Q2 POLYMER SCIENCE
Muhammad Tufail, Kifayat Ullah Shah, Ikram Ullah Khan, Kamran Ahmad Khan, Shefaat Ullah Shah, Faisal Rashid, Jahangir Khan, Abdulrahman Alshammari, Abdullah F. Alasmari, Muhammad Shahid Riaz
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The precompression characteristics of tablets depict the suitability of all formulation powder for direct compression. The ATR-FTIR analyses have shown that the components of both effervescent and noneffervescent tablets are compatible with each other. The total weight of each tablet was 600 mg, with a weight variation of about ≤10 mg. Both the layers were smooth and flat with a thickness ranging from <span><svg height=\"8.69875pt\" style=\"vertical-align:-0.3499298pt\" version=\"1.1\" viewbox=\"-0.0498162 -8.34882 32.221 8.69875\" width=\"32.221pt\" xmlns=\"http://www.w3.org/2000/svg\" xmlns:xlink=\"http://www.w3.org/1999/xlink\"><g transform=\"matrix(.013,0,0,-0.013,0,0)\"></path></g><g transform=\"matrix(.013,0,0,-0.013,6.24,0)\"></path></g><g transform=\"matrix(.013,0,0,-0.013,9.204,0)\"></path></g><g transform=\"matrix(.013,0,0,-0.013,15.444,0)\"></path></g><g transform=\"matrix(.013,0,0,-0.013,24.59,0)\"></path></g></svg><span></span><svg height=\"8.69875pt\" style=\"vertical-align:-0.3499298pt\" version=\"1.1\" viewbox=\"35.076183799999995 -8.34882 21.975 8.69875\" width=\"21.975pt\" xmlns=\"http://www.w3.org/2000/svg\" xmlns:xlink=\"http://www.w3.org/1999/xlink\"><g transform=\"matrix(.013,0,0,-0.013,35.126,0)\"></path></g><g transform=\"matrix(.013,0,0,-0.013,41.366,0)\"><use xlink:href=\"#g113-47\"></use></g><g transform=\"matrix(.013,0,0,-0.013,44.33,0)\"><use xlink:href=\"#g113-49\"></use></g><g transform=\"matrix(.013,0,0,-0.013,50.57,0)\"></path></g></svg></span> to <span><svg height=\"8.69875pt\" style=\"vertical-align:-0.3499298pt\" version=\"1.1\" viewbox=\"-0.0498162 -8.34882 32.221 8.69875\" width=\"32.221pt\" xmlns=\"http://www.w3.org/2000/svg\" xmlns:xlink=\"http://www.w3.org/1999/xlink\"><g transform=\"matrix(.013,0,0,-0.013,0,0)\"><use xlink:href=\"#g113-52\"></use></g><g transform=\"matrix(.013,0,0,-0.013,6.24,0)\"><use xlink:href=\"#g113-47\"></use></g><g transform=\"matrix(.013,0,0,-0.013,9.204,0)\"></path></g><g transform=\"matrix(.013,0,0,-0.013,15.444,0)\"><use xlink:href=\"#g113-53\"></use></g><g transform=\"matrix(.013,0,0,-0.013,24.59,0)\"><use xlink:href=\"#g117-37\"></use></g></svg><span></span><span><svg height=\"8.69875pt\" style=\"vertical-align:-0.3499298pt\" version=\"1.1\" viewbox=\"35.0771838 -8.34882 45.523 8.69875\" width=\"45.523pt\" xmlns=\"http://www.w3.org/2000/svg\" xmlns:xlink=\"http://www.w3.org/1999/xlink\"><g transform=\"matrix(.013,0,0,-0.013,35.127,0)\"><use xlink:href=\"#g113-49\"></use></g><g transform=\"matrix(.013,0,0,-0.013,41.367,0)\"><use xlink:href=\"#g113-47\"></use></g><g transform=\"matrix(.013,0,0,-0.013,44.331,0)\"><use xlink:href=\"#g113-49\"></use></g><g transform=\"matrix(.013,0,0,-0.013,50.571,0)\"><use xlink:href=\"#g113-50\"></use></g><g transform=\"matrix(.013,0,0,-0.013,58.986,0)\"></path></g><g transform=\"matrix(.013,0,0,-0.013,69.633,0)\"><use xlink:href=\"#g190-110\"></use></g></svg>.</span></span> The diameters of prepared floating tablets were about 15 mm, optimum for oral administration. After adjusting the tablet’s hardness to 6-7 kg/cm<sup>2</sup>, its friability was found to be &lt;0.35 percent. The mean drug content of the formulations was above 90%. The floating lag time of all formulations (F2-F5) was below 25 seconds, except F1 which took almost 50 seconds to start floating on the surface of gastric content due to its higher density. The total floating time of effervescent (F1-F3) and noneffervescent formulations was in the range of 15-25 hours, thereby providing sufficient time to complete drug release and absorption in the gastric area. The total floating time of noneffervescent formulations was higher (<span><svg height=\"11.7782pt\" style=\"vertical-align:-3.42938pt\" version=\"1.1\" viewbox=\"-0.0498162 -8.34882 18.973 11.7782\" width=\"18.973pt\" xmlns=\"http://www.w3.org/2000/svg\" xmlns:xlink=\"http://www.w3.org/1999/xlink\"><g transform=\"matrix(.013,0,0,-0.013,0,0)\"></path></g><g transform=\"matrix(.013,0,0,-0.013,11.342,0)\"></path></g></svg><span></span><span><svg height=\"11.7782pt\" style=\"vertical-align:-3.42938pt\" version=\"1.1\" viewbox=\"22.555183800000002 -8.34882 21.921 11.7782\" width=\"21.921pt\" xmlns=\"http://www.w3.org/2000/svg\" xmlns:xlink=\"http://www.w3.org/1999/xlink\"><g transform=\"matrix(.013,0,0,-0.013,22.605,0)\"><use xlink:href=\"#g113-49\"></use></g><g transform=\"matrix(.013,0,0,-0.013,28.845,0)\"><use xlink:href=\"#g113-47\"></use></g><g transform=\"matrix(.013,0,0,-0.013,31.809,0)\"><use xlink:href=\"#g113-49\"></use></g><g transform=\"matrix(.013,0,0,-0.013,38.049,0)\"><use xlink:href=\"#g113-54\"></use></g></svg>)</span></span> than effervescent formulations due to efficient wettability and swelling characteristics. The release of drugs from both layers of noneffervescent tablets was significantly controlled when compared to the effervescent system, and an anomalous non-Fickian diffusion was found for the drug release. The stability study of the optimized formulation proved the integrity and stability of the developed formulation. Thus, developed formulations are deemed suitable for controlled codelivery of active pharmaceutical ingredients for the effective treatment of <i>H</i>. <i>pylori</i>.","PeriodicalId":14283,"journal":{"name":"International Journal of Polymer Science","volume":"15 1","pages":""},"PeriodicalIF":3.4000,"publicationDate":"2024-01-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Controlled Release Bilayer Floating Effervescent and Noneffervescent Tablets Containing Levofloxacin and Famotidine\",\"authors\":\"Muhammad Tufail, Kifayat Ullah Shah, Ikram Ullah Khan, Kamran Ahmad Khan, Shefaat Ullah Shah, Faisal Rashid, Jahangir Khan, Abdulrahman Alshammari, Abdullah F. 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The ATR-FTIR analyses have shown that the components of both effervescent and noneffervescent tablets are compatible with each other. The total weight of each tablet was 600 mg, with a weight variation of about ≤10 mg. 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引用次数: 0

摘要

本研究旨在设计双层浮动片剂,以提高药物在胃中的浓度,从而增强疗效。片剂由上层的左氧氟沙星(466.5 毫克)和下层的法莫替丁(133.5 毫克)组成。通过使用羟丙基甲基纤维素等级(K4M、K15M 和 K100M)和 Carbopol 934,开发出了五种配方(F1-F5)。在泡腾体系(F1-F3)中,加入了碳酸氢钠以增加片剂的浮力;而在非泡腾配方(F4 & F5)中,加入了瓜尔豆胶和黄原胶以诱导漂浮和膨胀,并延缓药物的释放。片剂的预压缩特性表明所有配方粉末都适合直接压缩。ATR-FTIR 分析表明,泡腾片和非泡腾片的成分相互兼容。每片片剂的总重量为 600 毫克,重量差异约为≤10 毫克。制备的浮动片剂直径约为 15 毫米,最适合口服。将片剂的硬度调整到 6-7 kg/cm2 后,发现其易碎性为 0.35%。制剂的平均药物含量高于 90%。所有制剂(F2-F5)的上浮滞后时间都低于 25 秒,只有 F1 由于密度较大,需要近 50 秒才开始在胃内容物表面上浮。泡腾制剂(F1-F3)和非泡腾制剂的总漂浮时间在 15-25 小时之间,因此有足够的时间在胃部完全释放和吸收药物。由于高效的润湿性和溶胀特性,非泡腾制剂的总漂浮时间()高于泡腾制剂。与泡腾体系相比,非泡腾片两层的药物释放量都得到了明显的控制,并发现药物释放存在异常的非费克式扩散。对优化配方的稳定性研究证明了所开发配方的完整性和稳定性。因此,所开发的制剂被认为适用于控制活性药物成分的联合给药,以有效治疗幽门螺杆菌。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Controlled Release Bilayer Floating Effervescent and Noneffervescent Tablets Containing Levofloxacin and Famotidine
The present study is aimed at designing bilayer-floating tablets to improve the drug concentration in the stomach for enhanced therapeutic efficacy. The tablets are comprised of an upper layer of levofloxacin (466.5 mg) and a lower layer of famotidine (133.5 mg). Five formulations (F1-F5) were developed by using hydroxypropyl methylcellulose grades (K4M, K15M, and K100M) along with Carbopol 934. In the case of the effervescent system (F1-F3), sodium bicarbonate was added to impart buoyancy to the tablets; while in the case of noneffervescent formulations (F4 & F5), guar gum and xanthan gum were incorporated to induce flotation and swelling and retard the release of a drug. The precompression characteristics of tablets depict the suitability of all formulation powder for direct compression. The ATR-FTIR analyses have shown that the components of both effervescent and noneffervescent tablets are compatible with each other. The total weight of each tablet was 600 mg, with a weight variation of about ≤10 mg. Both the layers were smooth and flat with a thickness ranging from to . The diameters of prepared floating tablets were about 15 mm, optimum for oral administration. After adjusting the tablet’s hardness to 6-7 kg/cm2, its friability was found to be <0.35 percent. The mean drug content of the formulations was above 90%. The floating lag time of all formulations (F2-F5) was below 25 seconds, except F1 which took almost 50 seconds to start floating on the surface of gastric content due to its higher density. The total floating time of effervescent (F1-F3) and noneffervescent formulations was in the range of 15-25 hours, thereby providing sufficient time to complete drug release and absorption in the gastric area. The total floating time of noneffervescent formulations was higher () than effervescent formulations due to efficient wettability and swelling characteristics. The release of drugs from both layers of noneffervescent tablets was significantly controlled when compared to the effervescent system, and an anomalous non-Fickian diffusion was found for the drug release. The stability study of the optimized formulation proved the integrity and stability of the developed formulation. Thus, developed formulations are deemed suitable for controlled codelivery of active pharmaceutical ingredients for the effective treatment of H. pylori.
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来源期刊
CiteScore
6.10
自引率
0.00%
发文量
55
审稿时长
>12 weeks
期刊介绍: The International Journal of Polymer Science is a peer-reviewed, Open Access journal that publishes original research articles as well as review articles on the chemistry and physics of macromolecules.
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