Artículos de revistas
Study Of Relative Bioavailability/bioequivalence Of Two Formulations Of Rosuvastatin Calcium In Healthy Volunteers For Both Sexes [estudo De Biodisponibilidade Relativa/bioequivalência De Duas Formulações De Rosuvastatina Cálcica Em Voluntários Sadios De Ambos Os Sexos]
Registro en:
Revista Brasileira De Medicina. , v. 69, n. 7, p. 167 - 172, 2012.
347264
2-s2.0-84865319205
Autor
Abib Jr. E.
Duarte L.F.
Pereira R.
Morais D.C.
Lima L.G.
Savio D.
Pengo S.
Institución
Resumen
The study was conducted to compare the bioavailability of two formulations of rosuvastatin calcium 20 mg tablet (rosuvastatin calcium of Aché S/A test formulation and Crestor® from AstraZeneca do Brasil Ltda. reference formulation, Brazil) in 24 volunteers both sexes. This was an open, randomized, two-sequence, two-period, crossover single dose two treatments, in which a group of volunteers received the test formulation and the other reference formulation. Blood samples were obtained throughout a 96 hours interval. The rosuvastatin calcium concentrations were determined by mass spectrometry (UPLC-MS-MS) using atorvastatin as internal standard. From the data obtained, calculate the following pharmacokinetic parameters: AUC 0-t, AUC 0-∞ and Cmax. The geometric mean of rosuvastatin calcium/Crestor® 20 mg were 93,97% for AUC 0-t, 97,43% for AUC 0-∞ and 93,63% for Cmax. The 90% confidence intervals were 82,26-107,34%, 85,82-110,61% and 81,58-107,45%, respectively. Since the confidence intervals 90% for Cmax and AUC 0-t was within the range 80-125% proposed by the FDA and ANVISA (National Agency of Sanitary Surveillance in Brazil), it is concluded that the tablet of rosuvastatin calcium 20 mg was bioequivalent to Crestor® tablet of 20 mg and thus the test product may be considered interchangeable in medical practice. © Copyright Moreira Jr. Editora. 69 7 167 172 Moghadasian, M.H., Experimental atherosclerosis: A historical overview (2002) Life Sci, 70, pp. 855-865 Kritchevsky, D., Dietary protein, cholesterol and atherosclerosis: A review of the early history (1995) J Nutr, 125, pp. 587-593 Lichtman, A.H., Clinton, S.K., Iyama, K., Connelly, P.W., Libby, P., Cybulsky, M.I., Hyperlipidemia and atherosclerotic lesion development in LDL receptor deficient mice fed defined semipurified diets with and without cholate (1999) Arterioscler Thromb Vasc Biol, 19, pp. 1938-1944 Melo, F.S., Toledo, J.C.Y., Coca, A.P., Junior, H.M., Hipertensão arterial, aterosclerose e inflamação: O endotélio como órgäo-alvo (2007) Rev Bras Hipertens, 14, pp. 234-238 Michael, P., Christopher, P., Use of lipid lowering drugs for primary prevention of coronary heart disease: Meta-analysis of randomised trials (2000) BMJ, 321, p. 983 Forti, N., Diament, J., Efeitos indesejáveis dos hipolipemiantes: Condutas na prática clínica (2008) Rev Assoc Med Bras, 54 (357), p. 362 Davignon, J., Beneficial cardiovascular pleiotropic effects of statins (2004) Circulation, 109, pp. 39-43 Wassmann, S., Laufs, U., Baumer, A.T., HMG-CoA reductase inhibitors improve endothelial dysfunction in normocholesterolemic hypertension via reduced production of reactive oxygen species (2001) Hypertension, 37, pp. 1450-1457 Kwak, B., Mulhaupt, F., Myit, S., Mach, F., Statins as a newly recognized type of immunomodulator (2000) Nature Medicine, 6, pp. 1399-1402 Mason, J.C., Statins and their role in vascular protection (2003) Clinical Science, 105, pp. 251-266 Masato, E., Kozai, T., Cosentino, F., Statin prevents tissue factor expression in human endothelial cells. Role of Rho/Rho-kinase and AKT pathways (2002) Circulation, 105, pp. 1756-1759 Ichiki, T., Takeda, K., Todunou, T., Down regulation of angiotensin II type 1 receptor by hydrophobic 3-hydroxy-3-methylglutaryl coenzima A reductase inhibitors in vascular smooth muscle cells (2001) Arterioscl Thromb Vasc Biol, 21, pp. 1896-1901 Walter, D.H., Rittig, K., Bahlmann, F.H., Statin therapy acelerates reendothelization: A novel effect involving mobilization and incorporation of bone marrow-derived endothelial progenitor cells (2002) Circulation, 105, pp. 3017-3024 Harper, C.R., Jacobson, T.A., The broad spectrum of statin myopathy: From myalgia to rhabdomyolysis. Hyperlipidaemia and cardiovascular disease (2007) Current Opinion in Lipidology, 18, pp. 401-408 Taggart, F., Buckett, L., Davidson, R., Holdgate, G., McCormick, A., Schneck, D., Preclinical and clinical pharmacology of rosuvastatin, a new 3-hydroxy-3-methylglutaryl coenzyme A reducatase inhibitor (2001) Am J Cardiol, 87, pp. 28-32 Buckett, L., Ballard, P., Davidson, R., Dunkley, C., Martin, L., Stafford, J., Selectivity of ZD4522 for inhibition of cholesterol synthesis in hepatic versu non-hepatic cells (2000) Atherosclerosis Supplements, 141, p. 151 Brown, C.D.A., Windass, A., Bleasby, A., Lauffart, B., Rosuvastatin is a high affinity substrate of hepatic organic anion transporter OATP-C (2001) Atherosclerosis Supplements, 2, p. 90 Smith, G., Davidson, R., Bloor, S., Burns, K., Calnam, C.C., Aulay, P.M.C., Pharmacological properties of ZD4522 - A new HMG-CoA reductase inhibitor (2000) Atherosclerosis Supplements, 139, p. 151 Schuster, H., Rosuvastatin-a highly effective new 3-hydroxy-3-methylglutaryl Coenzyme. A reductase inhibitor: Review of clinical trial data at 10-40 mg doses in dyslipidemic patients (2003) Cardiology, 99, pp. 126-139 Jones, P.H., Davidson, M.H., Stein, E.A., Bays, H.E., Mckenney, J.M., Miller, E., Comparison of efficacy and safety of rosuvastatin versus atorvastatin. Simvastatin, and pravastatin across doses (2003) Am J Cardiol, 92, pp. 152-160 Chapman, M.J., Taggart, F., Optimizing the pharmacology of statins: Characteristics of rosuvastatin (2002) Atherosclerosis Supplements, 2, pp. 33-36 Cooper, K.J., Martin, P.D., Dane, A.L., Warwick, M.J., Raza, A., Schneck, D.W., Lack of effect of ketoconazole on the pharmacokinetics of rosuvastatin in healthy subjects (2003) Br J Clin Pharmacol, 55, pp. 94-99 Schneck, D.W., Knopp, R.H., Ballantyne, C.M., McPherson, R., Chitra, R.R., Simonson, S.G., Comparative effects of rosuvastatin and atorvastatin across their dose ranges in patients with hypercholesterolemia and without active arterial disease (2003) Am J Cardiol, 91, pp. 33-41 Blasetto, J.W., Stein, E.A., Brown, W.V., Chitra, R., Raza, A., Efficacy of rosuvastatin compared with other statins at selected starting doses in hypercholesterolemia patients and in special population groups (2003) Am J Cardiol, 91, pp. 3-10 Shepherd, J., Hunninghake, D.B., Barter, P., McKenney, J.M., Hutchinson, H.G., Guidelines for lowering lipids to reduce coronary artery disease risk: A comparison of rosuvastatin with atorvastatin, pravastatin, and simvastatin for achieving lipid lowering goals (2003) Am J Cardiol, 91, pp. 11-19 Davidson, M., Ma, P., Stein, E.A., Gotto, A.M., Raza, J.A., Chitra, R., Comparison of effects on low-density lipoprotein cholesterol and high-density lipoprotein cholesterol with rosuvastatin versus atorvastatin in patients with type IIa or Iib hypercholesterolemia (2002) Am J Cardiol, 89, pp. 268-275 Ballantyne, C.M., Stein, E.A., Paoletti, R., Southworth, H., Blasetto, J.W., Efficacy of rosuvastatin 10mg in patients with the metabolic syndrome (2003) Am J Cardiol, 91, pp. 25-28 Moghadasian, M.H., Mancini, G.B.J., Frohlich, J.J., Pharmacotherapy of hyperchcholesterolaemia: Statins in clinical practice (2000) Exp Opin Pharmacother, 1, pp. 683-695 Rader, D.J., Davidson, M.H., Caplan, R.J., Pears, J.S., Lipid and apolipoprotein ratios:association with coronary artery disease and effects of rosuvastatin compared with atorvastatin, pravastatin and simvastatin (2003) Am J Cardiol, 91, pp. 20-24 Istvan, E.S., Deisenhofer, J., Structural Mechanism for statin inhibition of HMG-CoA reductase (2001) Science, 292, pp. 1160-1164 Oliveira, C.M., Dislipidemias (2011) RBM. Rev. Bras. Med., 68, pp. 42-60 Cheung, B.M.Y., Lauder, I.J., Lau, C., Rumana, C.R., Meta-analysis of large randomized controlled trials to evaluate the impact of statins on cardiovascular outcomes (2004) Br J Clin Pharmacol, 57, pp. 640-651 Cheng-Lai, A., Rosuvastatin: A new HMG-CoA reductase inhibitor for the treatment of hypercholesterolemia (2003) Heart Disease, 5, pp. 72-78 Kemp, J., Martin, P., Olive, M.D., Coadministration of rosuvastatin does not alter the pharmacokinetics of digoxin (2001) Pharmacotherapy, 21, p. 1255 Coelho, V.G., Perfil lipídico e fatores de risco para doenças cardiovasculares em estudantes de medicina (2005) Arq Bras Cardiol, 85, pp. 57-62