Evaluation of the effect of milk casein on the pharmacokinetics of rutin

Ravindra Semwal , Ankit Kumar , Ruchi Badoni Semwal , Ashutosh Chauhan , Sunil Kumar Joshi , Kumud Upadhyaya , Deepak Kumar Semwal
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Abstract

Rutin, often referred to as vitamin P, possesses numerous pharmaceutical applications, yet its market availability is restricted due to poor bioavailability. Recent interest has focused on exploiting rutin's therapeutic potential, prompting efforts to enhance its bioavailability. This study aimed to enhance the bioavailability of rutin by formulating tablet dosage forms using cow milk casein as a matrix-forming agent. Tablet formulations containing rutin and milk casein were prepared, and their physicochemical properties were evaluated through in vitro tests, including hardness, friability, and dissolution. Pharmacokinetic studies were conducted using Wistar rat models, analyzing plasma drug concentrations and urine excretion. Stability studies were also performed to assess the tablets' shelf life under various conditions. The results of the study revealed that the incorporation of milk casein significantly improved the bioavailability of rutin, both in vitro and in vivo. Physicochemical evaluations demonstrated satisfactory tablet properties, while pharmacokinetic studies indicated enhanced plasma drug concentrations and reduced urine excretion of rutin with milk casein formulations. Stability studies further supported the suitability of the formulated tablets for long-term storage. In conclusion, milk casein proved effective as a matrix-forming agent for improving the bioavailability of rutin. The formulated tablets exhibited favorable physicochemical properties and enhanced drug absorption characteristics, suggesting the potential utility of milk casein in enhancing the therapeutic efficacy of rutin formulations.
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乳酪蛋白对芦丁药动学影响的评价
芦丁通常被称为维生素P,具有许多制药应用,但由于生物利用度差,其市场供应受到限制。最近的兴趣集中在开发芦丁的治疗潜力,促使努力提高其生物利用度。本研究旨在以牛奶酪蛋白为基质形成剂,通过制定片剂剂型来提高芦丁的生物利用度。制备了含有芦丁和乳酪蛋白的片剂,并通过硬度、脆度、溶出度等体外理化指标对其进行了评价。采用Wistar大鼠模型进行药代动力学研究,分析血浆药物浓度和尿排泄情况。还进行了稳定性研究,以评估片剂在各种条件下的保质期。研究结果表明,乳酪蛋白的掺入显著提高了芦丁的体内和体外生物利用度。理化评价显示令人满意的片剂性质,而药代动力学研究表明,牛奶酪蛋白制剂提高了血浆药物浓度,减少了尿排泄。稳定性研究进一步支持了制剂长期储存的适宜性。综上所述,乳酪蛋白是提高芦丁生物利用度的有效基质形成剂。该制剂具有良好的理化性质和增强的药物吸收特性,提示乳酪蛋白在提高芦丁制剂疗效方面具有潜在的应用价值。
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