Everolimus

A rapid, sensitive, precise, and accurate HPLC method coupled with a photodiode array detector was developed, optimized, and validated for the estimation of everolimus in bulk and tablet dosage forms. The chromatographic separation was achieved using a kromosil C8 column (200 mm × 4.6 mm i.d., 5 μm particle size) at 30°C temperature. The isocratic mobile phase consisted of 0.1M dipotassium hydrogen phosphate and methanol (60:40, v/v). The mobile phase was delivered at 1.0 ml/min and the analyte was monitored at 277 nm. The method was successfully validated in accordance to International Conference on Harmonization. The retention time of everolimus was found to be 3.496 min, and the calibration curve was linear in the concentration range of 50-150 μg/ml (R2 = 0.9992). The limit of detection and the limit of quantitation were found to be 0.109 μg/ml and 0.364 μg/ml, respectively.  The proposed method is accurate (percent recoveries were in the range of 99.56-100.09%) and precise (percent relative standard deviation - 0.047 %). No chromatographic interferences from the tablet excipients and components of mobile phase were found. The proposed method was found to be suitable for the quantitative determination of everolimus in tablet dosage forms.

The present study was undertaken to develop a validated stability-indicating liquid chromatography method for estimating Everolimus in commercial tablet dosage forms. Chromatographic separation was achieved on Kromasil C18column(100mm x 4.6 mm, 5m) with mobile phase containing potassium dihydrogen orthophosphate buffer and acetonitrile taken in the ratio 75:25 v/v. The pH was adjusted to 3.0 with dilute orthophosphoric acid at a flow rate of 1.0 mL/min and the eluent was monitored at 270 nm. The developed method was validated as per International Conference on Harmonization (ICH) guidelines with respect to specificity, precision, linearity, accuracy and robustness. Linearity range was found to be between 5-30 ppm and the linear regression coefficient was not more than 0.999. The values of % RSD are less than 2% indicating that the accuracy and precision of the method are good. Statistical analysis proved that the method was precise, reproducible, selective, specific, and accurate for analysis of Everolimus. All the degradation products formed during forced degradation studies were well separated from the analyte  peak.