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
{"title":"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","authors":"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","doi":"10.1155/2024/1243321","DOIUrl":null,"url":null,"abstract":"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 <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 <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":null,"pages":null},"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. Alasmari, Muhammad Shahid Riaz\",\"doi\":\"10.1155/2024/1243321\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"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 <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 <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\":null,\"pages\":null},\"PeriodicalIF\":3.4000,\"publicationDate\":\"2024-01-11\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"International Journal of Polymer Science\",\"FirstCategoryId\":\"5\",\"ListUrlMain\":\"https://doi.org/10.1155/2024/1243321\",\"RegionNum\":4,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"POLYMER SCIENCE\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"International Journal of Polymer Science","FirstCategoryId":"5","ListUrlMain":"https://doi.org/10.1155/2024/1243321","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"POLYMER SCIENCE","Score":null,"Total":0}
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.
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.