Abstract
A novel, simple, precise, and stability-indicating stereoselective method was developed and validated for the accurate quantification of the enantiomer in the drug substance and pharmaceutical dosage forms of Rosuvastatin Calcium. The method is capable of quantifying the enantiomer in the presence of other related substances. The chromatographic separation was achieved with an immobilized cellulose stationary phase (Chiralpak IB) 250 mm x 4.6 mm x 5.0 μm particle size column with a mobile phase containing a mixture of n-hexane, dichloromethane, 2-propanol, and trifluoroacetic acid in the ratio 82:10:8:0.2 (v/v/v/v). The eluted compounds were monitored at 243 nm and the run time was 18 min. Multivariate analysis and statistical tools were used to develop this highly robust method in a short span of time. The stability-indicating power of the method was established by subjecting Rosuvastatin Calcium to the stress conditions (forced degradation) of acid, base, oxidative, thermal, humidity, and photolytic degradation. Major degradation products were identified and found to be well-resolved from the enantiomer peak, proving the stability-indicating power of the method. The developed method was validated as per International Conference on Harmonization (ICH) guidelines with respect to specificity, limit of detection and limit of quantification, precision, linearity, accuracy, and robustness. The method exhibited consistent, high-quality recoveries (100 ± 10%) with a high precision for the enantiomer. Linear regression analysis revealed an excellent correlation between the peak responses and concentrations (r2 value of 0.9977) for the enantiomer. The method is sensitive enough to quantify the enantiomer above 0.04% and detect the enantiomer above 0.015% in Rosuvastatin Calcium. The stability tests were also performed on the drug substances as per ICH norms.
Highlights
Rosuvastatin Calcium is classified as a statin, a type of agent that inhibits cholesterol production in the liver
We describe the development of a stability-indicating stereoselective method for the quantification of the enantiomer in the drug substance and pharmaceutical dosage forms of Rosuvastatin Calcium
Rosuvastatin Calcium solution was prepared in methanol at a concentration of 100 ppm and scanned in an ultraviolet (UV)-visible spectrometer; Rosuvastatin Calcium had maximum UV absorbances at 210 nm and 243 nm (Figure 2)
Summary
Rosuvastatin Calcium is classified as a statin, a type of agent that inhibits cholesterol production in the liver. Rosuvastatin Calcium is a synthetic lipid-lowering agent approved as a treatment for hypercholesterolemia. The primary site of action of Rosuvastatin is the liver, the target organ for cholesterol lowering. Rosuvastatin reduces cholesterol by increasing the number of low-density lipoprotein (LDL) receptors on the cell surface to enhance uptake and catabolism of LDL. It inhibits hepatic synthesis of hepatic very-low-density lipoprotein (VLDL), which reduces the total number of VLDL and LDL particles. The treatment reduces triglycerides (TG) and produces increases in high-density lipoprotein cholesterol (HDL-C) [1,2,3,4,5,6]
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