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采用往复圆筒法对美沙拉嗪肠溶片溶出度进行体外评价。

In vitro evaluation of mesalazine enteric-coated tablet dissolution by the reciprocating cylinder method.

作者信息

Wang Jinxiang, Zhao Yanqing, He Gaihua, Guo Bin, Zhang Hui

机构信息

Jinzhou Medical University, Jinzhou city, 121000, China.

Elite Pharmatech Company, Shanghai city, 201210, China.

出版信息

Sci Rep. 2025 Jul 1;15(1):22066. doi: 10.1038/s41598-025-05936-8.

Abstract

Mesalazine formulations are first-line treatments for ulcerative colitis. However, the drug release mechanisms of currently available mesalazine formulations on the market vary, and different in vitro dissolution methods have been used to characterize their in vivo absorption. Thus, there is an urgent need for more in-depth research on in vitro dissolution methods for mainstream mesalazine enteric-coated tablets. The goal of this study is to determine more scientifically rigorous testing methods to enhance the discriminatory power of in vitro dissolution testing of these products. Dissolution tests were performed using the reciprocating cylinder method with a small 250 ml vessel, a reciprocating frequency of 10 cycles/min, a sample volume of 5 ml, and UV spectrophotometric detection. The absorbance values of the dissolution solutions at different pH values were measured using cuvettes with path lengths of 1 cm and 1 mm and at detection wavelengths of 303 nm and 332 nm, respectively. In pH 1.2, 4.5, 5.5, and 6.0 solutions, the linear concentration range was from 5 to 30 µg/ml. In contrast, the linear concentration range in pH 6.8 media was 90 to 660 µg/ml. Method accuracy was tested at levels of 5%, 50%, 100%, and 120%, and the average recovery rates were 105.8%, 102.8%, 100.9%, and 101.2%, respectively. Moreover, the differences in the dissolution data did not exceed 2% with different instruments or analysts or on different days. Using the reciprocating cylinder method, we continuously measured the dissolution of mesalazine enteric-coated tablets in media with various pH values that simulate different sections of the human digestive system. Furthermore, in pH 6.8 dissolution media, drug release from both the homemade and the reference formulations followed zero-order kinetics. The established reciprocating cylinder method for determining the dissolution of mesalazine enteric-coated tablets is suitable for quality control of this type of product.

摘要

美沙拉嗪制剂是溃疡性结肠炎的一线治疗药物。然而,目前市场上可用的美沙拉嗪制剂的药物释放机制各不相同,并且已使用不同的体外溶出方法来表征它们的体内吸收情况。因此,迫切需要对主流美沙拉嗪肠溶片的体外溶出方法进行更深入的研究。本研究的目的是确定更科学严谨的测试方法,以增强这些产品体外溶出测试的区分能力。使用250 ml小容器的往复圆筒法进行溶出试验,往复频率为10次/分钟,样品体积为5 ml,并采用紫外分光光度法检测。分别使用光程为1 cm和1 mm的比色皿,在303 nm和332 nm的检测波长下测量不同pH值下溶出溶液的吸光度值。在pH 1.2、4.5、5.5和6.0的溶液中,线性浓度范围为5至30 μg/ml。相比之下,pH 6.8介质中的线性浓度范围为90至660 μg/ml。在5%、50%、100%和120%的水平下测试方法准确性,平均回收率分别为105.8%、102.8%、100.9%和101.2%。此外,不同仪器、分析人员或不同日期的溶出数据差异不超过2%。使用往复圆筒法,我们连续测量了美沙拉嗪肠溶片在模拟人体消化系统不同部位的各种pH值介质中的溶出情况。此外,在pH 6.8溶出介质中,自制制剂和参比制剂的药物释放均符合零级动力学。所建立的用于测定美沙拉嗪肠溶片溶出度的往复圆筒法适用于此类产品的质量控制。

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