Faculty of Pharmacy, Federal University of Rio Grande do Sul , Porto Alegre - RS , Brazil.
Drug Dev Ind Pharm. 2014 Apr;40(4):488-93. doi: 10.3109/03639045.2013.768633. Epub 2013 Apr 24.
Lodenafil carbonate is a phosphodiesterase type 5 inhibitor used for the treatment of erectile dysfunction. Currently, there is no dissolution test reported for lodenafil carbonate and this drug is not listed in any pharmacopoeia.
The present study focused on the development and validation of a dissolution test for lodenafil carbonate tablets, using a simulated absorption profile based on in vivo data.
The appropriate conditions were determined after testing sink conditions. Different conditions as medium, surfactant concentration and rotation speed were evaluated. The percentage of dose absorbed was calculated by deconvolution, using the Wagner-Nelson method.
According to the obtained results, the use of 0.1 M HCl + 1.5% SLS (900 mL, at 37 + 0.5 °C) as the dissolution medium, paddles at 25 rpm were considered adequate. The samples were quantified by UV spectroscopy at 295 nm and the validation was performed according to international guidelines. The method showed specificity, linearity, accuracy and precision, within the acceptable range. Kinetics of drug release was better described by the first-order model.
The proposed dissolution test can be used for the routine quality control of lodenafil carbonate in tablets.
碳酸洛地那非是一种用于治疗勃起功能障碍的磷酸二酯酶 5 抑制剂。目前，尚未报道碳酸洛地那非的溶出度试验，且该药未列入任何药典。
本研究旨在根据体内数据的模拟吸收曲线，开发并验证碳酸洛地那非片的溶出度试验方法。
在测试溶出度条件后，确定了合适的条件。考察了不同的介质、表面活性剂浓度和转速条件。采用 Wagner-Nelson 法进行解卷积计算，计算吸收的剂量百分比。
根据结果，使用 0.1 M HCl + 1.5% SLS（900 mL，37 ± 0.5°C）作为溶出介质，桨板转速为 25 rpm 被认为是合适的。采用 UV 光谱法在 295nm 处对样品进行定量分析，并根据国际指南进行了验证。该方法具有专属性、线性、准确性和精密度，均在可接受范围内。药物释放的动力学更好地用一级模型描述。
所提出的溶出度试验可用于碳酸洛地那非片的常规质量控制。
