Rosuvastatin calcium

Molecular formula 2C22H27pN306S.Ca Molecular weight 1001.14 CAS Registry No 147098-20-2 

Sample preparation Condition a 30 mg Oasis HLB SPE cartridge (in 96 well plate) with 1 mL MeOH and 1 mL 0.5% acetic acid. Mix 500 p,L plasma with 500 ixL 100 mM pH 4 acetate buffer, 50 jrL 150 ng/mL IS in MeOH l M acetic acid 50 50, and 750 lL 1 M acetic acid, vortex for 2 s, centrifuge at 738 g for 7 min, add 1.7 mL of the supernatant to the SPE cartridge, wash with 1 mL MeOH 0.5% acetic acid 30 70, elute with 1 mL 0.5% acetic acid in MeOH. Evaporate the eluate to dryness under a stream of nitrogen at 40°, reconstitute the residue with 130 (aL 0.5% acetic acid, centrifuge at 1700 or 9500 g for 10 min, inject a 100 m-L aliquot. 

Mobile phase MeOH 0.2% formic acid 70 30 (divert first 2 min of run to waste) 

Detector MS, PE Sciex API 365, Turbolonspray 450°, 0.2 mL/min entered detector, positive ion mode, ionspray 3000 V, ring 160 V, orifice 44 V, nebulizer gas nitrogen at 14 units, Turbolonspray gas nitrogen at 7 L/min, coUision gas nitrogen 4 units, curtain gas nitrogen 8 units, deflector —250 V, electron multipher 2900 V, collision energy —47.5 V, m/z 482.2-258.2 

Penman, A.D. Smith, C.K. Martin, P.D. Quantification of rosuvastatin in human plasma by automated solid-phase extraction using tandem mass spectrometric detection, J.Chromatogr.B, 2002, 772, 219 228. 

---

Rosuvastatin calcium (56 Crestor ) Mevastatin Statin NP-derived Microbial Dyslipidemia Inhibits ttie rate-limiting step in hie formation of endogenous cholesterol by HMG-CoA reductase 215-217, 492-495... 

Rosuvastatin calcium (CRESTOR, AstraZeneca Pharmaceuticals LP) is indicated to lower low-density lipoprotein cholesterol (LDL-C), increase high-density lipoprotein cholesterol (HDL-C), and to slow the progression of atherosclerosis in adult patients as part of a treatment plan to decrease cholesterol to a therapeutic goal. 

Crestor (Rosuvastatin calcium). AstraZeneca UK Ltd. UK Summary of product characteristics, June 2007. 

Balakumar, K., Raghavan, C.V., Selvan, N.T., Prasad, R.H., Abdu, S., 2013. Self nanoemulsifying drug delivery system (SNEDDS) of rosuvastatin calcium design, formulation, bioavailabiUty and pharmacokinetic evaluation. Colloids Surf. B Biointerfaces 112, 337—343. 

Rokad, V., Nagda, C., Nagda, C., 2014. Design and evaluation of solid self-emulsifying drug delivery system of rosuvastatin calcium. J. Young Pharm. 6, 37—46. 

The first statins were launched by Merck with lovastatin (Mevacor ) in 1987 and then simvistatin (Zocor ) in 1991. Bristol-Myers launched pravastatin (Pravacol ) in 1991 Pfizer commercialized atorvastatin calcium (Lipitor ) in 1997. As measured by annual sales, Lipitor is the most successful drug in the history of the pharmaceutical industry [13]. Rosuvastatin calcium (Crestor ) is AstraZeneca s top drug with 6.6 billion in annual sales [14]. 

Rosuvastatin calcium is the newest among statins, and it was approved as the cholesterol-lowering drug Crestor (AstraZeneca, London, U.K.) in August 2003. Rosuvastatin has been called a super-statin because it appears to reduce low-density lipoprotein (LDL) cholesterol to a greater degree than rivals in its class without additional adverse effects. 

Quirk J, Thornton M, Kirkpatrick P. Rosuvastatin calcium. Nature Rev. Drug Discov. 2003 2 769-770. 

---