Laboratory for Polymer Analysis, Biomedical Technology Wing, Sree Chitra Tirunal Institute for Medical Sciences & Technology, Poojapura, Trivandrum 695012, Kerala, India.
J Chromatogr B Analyt Technol Biomed Life Sci. 2010 Mar 1;878(7-8):709-12. doi: 10.1016/j.jchromb.2010.01.023. Epub 2010 Jan 25.
Prior understanding on the in vitro release profile of the drug from drug eluting devices such as stent (DES) is crucial in designing and optimizing the drug embedded coating or matrices. In fact, assessing in vitro release profile is a mandatory requirement prior to the clinical evaluation of DES. The in vitro release is also employed to estimate parameters such as T1/2. The release profile largely depends on the release medium selected for the studies. Normally PBS with a pH of 7.4 is used for assessing the release kinetics of the drug. Often drug undergoes irreversible changes such as hydrolysis in PBS leading to erroneous assessment of the release profile. This is particularly true in the case of sirolimus, one of the widely used drugs in various applications. We studied the influence of various media on the release profile of sirolimus from DES. The data generated suggested that a release medium consisting of 9:1 (v/v) of normal saline and isopropanol is a most suitable one for assessing in vitro the release kinetics of sirolimus from DES.
在设计和优化药物嵌入涂层或基质之前，了解药物洗脱器械（如支架）中药物的体外释放情况至关重要。事实上，评估体外释放情况是 DES 临床评估之前的强制性要求。体外释放也可用于估计 T1/2 等参数。释放曲线在很大程度上取决于研究中选择的释放介质。通常使用 pH 值为 7.4 的 PBS 来评估药物的释放动力学。药物通常会发生不可逆的变化，如在 PBS 中水解，从而导致对释放曲线的错误评估。对于西罗莫司（广泛用于各种应用的药物之一）尤其如此。我们研究了不同介质对 DES 中西罗莫司释放曲线的影响。生成的数据表明，由生理盐水和异丙醇 9:1（v/v）组成的释放介质是评估 DES 中西罗莫司体外释放动力学的最适合介质。
