Augustyniak W, Mielcarek J, Milewski M, Szamburska O
Faculty of Chemistry, A. Mickiewicz University, Poznań, Poland.
Drug Dev Ind Pharm. 2001 Nov;27(10):1031-8. doi: 10.1081/ddc-100108365.
Photochemical decomposition of nilvadipine (NV), a derivative of 1,4-dihydropyridine (DHP), was studied. Photodegradation was carried out in the conditions recommended in the first version of the document issued by the International Conference on Harmonization (ICH), currently in force in the studies of photochemical stability of drugs and therapeutic substances. Methanol solutions of NV were irradiated with a high-pressure mercury arc lamp, type HBO 200 (300-400 nm). The maximum absorption of radiation at 365 nm was achieved by applying the interference filter and Wood's filter. The assessment of NV photodegradation was made on the basis of the UV spectrophotometric and high-performance liquid chromatographic (HPLC) methods. Quantitatively, the process was described with the calculated rate constants of decomposition k, time of decomposition of 50% of the compound to 5, and time of decomposition of 10% of the compound t(0.1). The two methods applied allowed a determination of the kinetic parameters of NV photodegradation from the relationship ln c = f(t). Using the Reinecke salt as a chemical actinometer, apparent quantum yields of photodegradation were obtained; after extrapolation to the time of irradiation zero, these gave the actual quantum yield (phi = 7.3 10(-5)). The quantum yield of fluorescence at lambda(exc) = 375 nm was about 9.3 x 10(-4) The methods used for evaluation of NV photodegradation were subjected to validation, and results of the analytical methods were statistically assessed by Snedecor F and Student t tests. The former test revealed no statistically significant difference between the variances obtained by the HPLC and UV spectrophotometric methods. Also, verification of the zero hypothesis of the Student t test on equality of means of the results obtained gave no significant diferences between the two methods.
研究了1,4 - 二氢吡啶(DHP)衍生物尼伐地平(NV)的光化学分解。光降解是在国际协调会议(ICH)发布的第一版文件中推荐的条件下进行的,该条件目前在药物和治疗物质光化学稳定性研究中有效。用HBO 200型高压汞弧灯(300 - 400 nm)照射NV的甲醇溶液。通过应用干涉滤光片和伍德滤光片,实现了在365 nm处的最大辐射吸收。基于紫外分光光度法和高效液相色谱法(HPLC)对NV光降解进行评估。定量地,用计算得到的分解速率常数k、化合物50%分解的时间t(0.5)和化合物10%分解的时间t(0.1)来描述该过程。所应用的两种方法允许根据ln c = f(t)关系确定NV光降解的动力学参数。使用雷氏盐作为化学光量计,获得了光降解的表观量子产率;外推到照射时间为零时,这些产率给出了实际量子产率(φ = 7.3×10⁻⁵)。在λ(exc)= 375 nm处的荧光量子产率约为9.3×10⁻⁴。用于评估NV光降解的方法进行了验证,并且通过斯内德科尔F检验和学生t检验对分析方法的结果进行了统计评估。前一个检验表明,HPLC法和紫外分光光度法获得的方差之间没有统计学上的显著差异。此外,对学生t检验关于所得结果均值相等的零假设的验证表明,这两种方法之间没有显著差异。