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用于消化性溃疡空间给药的新型姜黄素漂浮片

Novel Curcumin Floating Tablets for Spatial Delivery in Peptic Ulcer.

作者信息

Gupta Chitra, Sahu Girdhar Kumar, Parashar Ashish Kumar, Singh Kalpana, Bukke Sarad Pawar Naik, Udom Godswill James

机构信息

Department of Pharmaceutics, Lloyd Institute of Management and Technology, Greater Noida, 201306, India.

Department of Pharmaceutics and Pharmaceutical Technology, Kampala International University, Western Campus, Ishaka-Bushenyi, PO Box 71, Uganda.

出版信息

Biomed Res Int. 2025 Jul 23;2025:6622146. doi: 10.1155/bmri/6622146. eCollection 2025.


DOI:10.1155/bmri/6622146
PMID:40741132
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12310316/
Abstract

Peptic ulcers, caused by factors like infection and NSAID overuse, are often treated with drugs that can have significant downsides. Curcumin, a natural compound with high therapeutic potential, faces challenges due to poor solubility and instability. Innovative delivery systems are key to unlocking curcumin's full benefits for effective peptic ulcer treatment. To address the challenge of curcumin's limited bioavailability, a novel drug delivery system was developed. The system employed a twofold strategy: enhancing curcumin's solubility via complexation with methyl--cyclodextrin, and formulating effervescent, gastroretentive tablets composed of hypromellose and gas-generating agents. This approach is aimed at achieving sustained gastric retention and localized drug release, thereby maximizing curcumin's therapeutic potential. The formulated tablets exhibited excellent pharmaceutical properties, meeting all required standards for hardness, friability, and drug content. Importantly, the tablets demonstrated rapid flotation in simulated gastric fluid (buoyancy achieved within 20 s) and maintained buoyancy for approximately 16 h, indicating successful gastroretention. dissolution studies confirmed sustained drug release (73.92% within 9 h) following a quasi-Fickian diffusion mechanism, as per the Korsmeyer-Peppas model. This study presents a novel approach to enhance peptic ulcer treatment using floating tablets designed to optimize curcumin delivery. These tablets leverage cyclodextrin complexation for enhanced solubility, while their effervescent, gastroretentive properties allow for prolonged gastric residence time and targeted drug release. This strategy shows promise in improving curcumin's bioavailability and therapeutic efficacy, addressing a significant unmet need in peptic ulcer management.

摘要

由感染和非甾体抗炎药过度使用等因素引起的消化性溃疡,通常使用具有显著副作用的药物进行治疗。姜黄素是一种具有高治疗潜力的天然化合物,但由于其溶解性差和稳定性低而面临挑战。创新的给药系统是充分发挥姜黄素对消化性溃疡有效治疗作用的关键。为应对姜黄素生物利用度有限的挑战,开发了一种新型药物递送系统。该系统采用了双重策略:通过与甲基-β-环糊精络合提高姜黄素的溶解度,并制备由羟丙甲纤维素和产气剂组成的泡腾胃滞留片。这种方法旨在实现药物在胃中的持续滞留和局部释放,从而最大限度地发挥姜黄素的治疗潜力。所制备的片剂表现出优异的药学性质,符合硬度、脆碎度和药物含量的所有要求标准。重要的是,这些片剂在模拟胃液中迅速漂浮(20秒内实现漂浮)并保持漂浮约16小时,表明胃滞留成功。溶出度研究证实,根据Korsmeyer-Peppas模型,药物按照准Fickian扩散机制持续释放(9小时内释放73.92%)。本研究提出了一种使用漂浮片优化姜黄素递送以增强消化性溃疡治疗的新方法。这些片剂利用环糊精络合提高溶解度,同时其泡腾胃滞留特性可延长胃停留时间并实现靶向药物释放。该策略在提高姜黄素的生物利用度和治疗效果方面显示出前景,满足了消化性溃疡治疗中一个重大的未满足需求。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f082/12310316/9bfa3913718d/BMRI2025-6622146.005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f082/12310316/c73edcb914a3/BMRI2025-6622146.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f082/12310316/79dc55210524/BMRI2025-6622146.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f082/12310316/e8ae1b74e915/BMRI2025-6622146.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f082/12310316/cd6b2cdfe0ba/BMRI2025-6622146.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f082/12310316/9bfa3913718d/BMRI2025-6622146.005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f082/12310316/c73edcb914a3/BMRI2025-6622146.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f082/12310316/79dc55210524/BMRI2025-6622146.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f082/12310316/e8ae1b74e915/BMRI2025-6622146.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f082/12310316/cd6b2cdfe0ba/BMRI2025-6622146.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f082/12310316/9bfa3913718d/BMRI2025-6622146.005.jpg

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Novel Curcumin Floating Tablets for Spatial Delivery in Peptic Ulcer.

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本文引用的文献

[1]
Curcumin and proton pump inhibitors for functional dyspepsia: a randomised, double blind controlled trial.

BMJ Evid Based Med. 2023-11-22

[2]
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Chin Herb Med. 2020-12-5

[3]
Study of Orally Disintegrating Tablets Using Erythritol as an Excipient Produced by Moisture-Activated Dry Granulation (MADG).

Pharmaceuticals (Basel). 2022-8-15

[4]
Improved Dermal and Transdermal Delivery of Curcumin with SmartFilms and Nanocrystals.

Molecules. 2021-3-15

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Therap Adv Gastroenterol. 2019-3-11

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[8]
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Gut. 2016-10-5

[9]
Design and In-vitro Evaluation of Sustained Release Floating Tablets of Metformin HCl Based on Effervescence and Swelling.

Iran J Pharm Res. 2016

[10]
The Stability, Sustained Release and Cellular Antioxidant Activity of Curcumin Nanoliposomes.

Molecules. 2015-8-5

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