Pharmacokinetic comparison of controlled-release and immediate-release oral formulations of simvastatin in healthy Korean subjects: A randomized, open-label, parallel-group, single- and multiple-dose study

Clinical Therapeutics

Volumn 32, Issue 1, 2010, Pages 206-216

  Jang, Seong Bok ^a   Lee, Yoon Jung ^a   Lim, Lay Ahyoung ^a   Park, Kyung Mi ^b   Kwon, Bong Ju ^b   Woo, Jong Soo ^b   Kim, Yong IL ^b,c   Park, Min Soo ^a   Kim, Kyung Hwan ^a   Park, Kyungsoo ^a  

^a Yonsei University College of Medicine   (South Korea)

^b Hanmi Pharmaceutical Co Ltd   (South Korea)

^c Yeungnam University   (South Korea)

Author keywords

controlled release formulation; pharmacokinetics; simvastatin; simvastatin acid

Indexed keywords

CALCIUM CHANNEL BLOCKING AGENT; SIMVASTATIN;

ADULT; AREA UNDER THE CURVE; ARTICLE; ASIAN; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DELAYED RELEASE FORMULATION; DOSE RESPONSE; ELECTROCARDIOGRAPHY; FEMALE; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; KOREA; MALE; MIDDLE AGED; ORAL DRUG ADMINISTRATION; RANDOMIZED CONTROLLED TRIAL; REFERENCE VALUE; TANDEM MASS SPECTROMETRY;

ADMINISTRATION, ORAL; ADULT; AREA UNDER CURVE; ASIAN CONTINENTAL ANCESTRY GROUP; CALCIUM CHANNEL BLOCKERS; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; DELAYED-ACTION PREPARATIONS; DOSE-RESPONSE RELATIONSHIP, DRUG; ELECTROCARDIOGRAPHY; FEMALE; HUMANS; KOREA; MALE; MIDDLE AGED; REFERENCE VALUES; SIMVASTATIN; TANDEM MASS SPECTROMETRY; YOUNG ADULT;

MLCS; MLOWN;

EID: 77952316849     PISSN: 01492918     EISSN: 1879114X     Source Type: Journal    
DOI: 10.1016/j.clinthera.2010.01.026     Document Type: Article

References (34)

1. Alberts, AW, Chen, J, Kuron, G, et al. Mevinolin: A highly potent competitive inhibitor of hydroxymethylglutarylcoenzyme A reductase and a cholesterol-lowering agent. Proc Natl Acad Sci U S A 77 (1980), 3957–3961.
2. Tobert, JA, New developments in lipid-lowering therapy: The role of inhibitors of hydroxymethylglutaryl-coenzyme A reductase. Circulation 76 (1987), 534–538.
3. Vickers, S, Duncan, CA, Vyas, KP, et al. In vitro and in vivo biotransformation of simvastatin, an inhibitor of HMG CoA reductase. Drug Metab Dispos 18 (1990), 467–483.
4. Randomised trial of cholesterol lowering in 4444 patients with coronary heart disease: The Scandinavian Simvastatin Survival Study (4S). Lancet 344 (1994), 1383–1389.
5. Sacks, FM, Pfeffer, MA, Moye, LA, et al., Cholesterol and Recurrent Events Trial investigators. The effect of pravastatin on coronary events after myocardial infarction in patients with average cholesterol levels. N Engl J Med. 335 (1996), 1001–1009.
6. Vickers, S, Duncan, CA, Chen, IW, et al. Metabolic disposition studies on simvastatin, a cholesterol-lowering prodrug. Drug Metab Dispos 18 (1990), 138–145.
7. Christians, U, Jacobsen, W, Floren, LC, Metabolism and drug interactions of 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors in transplant patients: Are the statins mechanistically similar?. Pharmacol Ther. 80 (1998), 1–34.
8. Lilja, JJ, Neuvonen, M, Neuvonen, PJ, Effects of regular consumption of grapefruit juice on the pharmacokinetics of simvastatin. Br J Clin Pharmacol 58 (2004), 56–60.
9. Raal, FJ, Pilcher, GJ, Illingworth, DR, et al. Expanded-dose simvastatin is effective in homozygous familial hypercholesterolaemia. Atherosclerosis 135 (1997), 249–256.
10. Brinton, EA, Newer HMG-CoA reductase inhibitor (statin) therapies. Clin Cardiol 24:Suppl II (2001), II-10–II-13.
11. Sacher, J, Weigl, L, Werner, M, et al. Delineation of myotoxicity induced by 3-hydroxy-3-methylglutaryl CoA reductase inhibitors in human skeletal muscle cells. J Pharmacol Exp Ther. 314 (2005), 1032–1041.
12. Bradford, RH, Shear, CL, Chremos, AN, et al. Expanded Clinical Evaluation of Lovastatin (EXCEL) study results. I. Efficacy in modifying plasma lipoproteins and adverse event profile in 8245 patients with moderate hypercholesterolemia. Arch Intern Med. 151 (1991), 43–49.
13. Shepherd, J, Cobbe, SM, Ford, I, et al., West of Scotland Coronary Prevention Study Group. Prevention of coronary heart disease with pravastatin in men with hypercholesterolemia. N Engl J Med. 333 (1995), 1301–1307.
14. Curran, MP, Goa, KL, Lovastatin extended release: A review of its use in the management of hypercholesterolaemia. Drugs 63 (2003), 685–699.
15. East, C, Alivizatos, PA, Grundy, SM, et al. Rhabdomyolysis in patients receiving lovastatin after cardiac transplantation. N Engl J Med. 318 (1988), 47–48.
16. Corpier, CL, Jones, PH, Suki, WN, et al. Rhabdomyolysis and renal injury with lovastatin use. Report of two cases in cardiac transplant recipients. JAMA 260 (1988), 239–241.
17. Barilla, D, Prasad, P, Hubert, M, Gumbhir-Shah, K, Steadystate pharmacokinetics of fluvastatin in healthy subjects following a new extended release fluvastatin tablet, Lescol XL. Biopharm Drug Dispos 25 (2004), 51–59.
18. http://www.hanmipharm.com/business_product_view.asp?prd_idx=325&pageNum=1&prd_gubun=1 Simvast CR tablets, 2004. Hanmi Pharmaceutical Co, Ltd. Accessed January 7, 2010.
19. http://www.merck.com/product/usa/pi_circulars/z/zocor/zocor_pi.pdf Zocor (simvastatin) tablets. Merck Sharpe & Dohme. Accessed January 7, 2010.
20. Lim, SK, Kang, HC, Kim, JN, Guidance for Dietary Prescription, 5th ed., 2004, Nutrition Management Committee of Severance Hospital, Seoul, Korea.
21. García, MJ, Reinoso, RF, Sánchez Navarro, A, Prous, JR, Clinical pharmacokinetics of statins. Methods Find Exp Clin Pharmacol 25 (2003), 457–481.
22. Najib, NM, Idkaidek, N, Adel, A, et al. Pharmacokinetics and bioequivalence evaluation of two simvastatin 40 mg tablets (Simvast and Zocor) in healthy human volunteers. Biopharm Drug Dispos 24 (2003), 183–189.
23. Shah, VP, Midha, KK, Dighe, S, et al. Analytical methods validation: Bioavailability, bioequivalence and pharmacokinetic studies. Conference report. Eur J Drug Metab Pharmacokinet 16 (1992), 249–255.
24. Shargel, L, Wu-Pong, S, Yu, ABC, Applied Biopharmaceutics & Pharmacokinetics, 5th ed., 2005, Appleton & Lange Reviews/ McGraw-Hill, Medical Pub. Division, New York, NY, 170–171.
25. Isaacsohn, JL, LaSalle, J, Chao, G, Gonasun, L, Comparison of treatment with fluvastatin extendedrelease 80-mg tablets and immediaterelease 40-mg capsules in patients with primary hypercholesterolemia. Clin Ther. 25 (2003), 904–918.
26. Davidson, MH, Lukacsko, P, Sun, JX, et al. A multiple-dose pharmacodynamic, safety, and pharmacokinetic comparison of extended- and immediate-release formulations of lovastatin. Clin Ther. 24 (2002), 112–125.
27. Sun, JX, Niecestro, R, Phillips, G, et al. Comparative pharmacokinetics of lovastatin extended-release tablets and lovastatin immediate-release tablets in humans. J Clin Pharmacol 42 (2002), 198–204.
28. Olsson, AG, Pauciullo, P, Soska, V, et al., Fluvastatin Study Group. Comparison of the efficacy and tolerability of fluvastatin extendedrelease and immediate-release formulations in the treatment of primary hypercholesterolemia: A randomized trial. Clin Ther. 23 (2001), 45–61.
29. Ziviani, L, Da Ros, L, Squassante, L, et al. The effects of lacidipine on the steady/state plasma concentrations of simvastatin in healthy subjects. Br J Clin Pharmacol 51 (2001), 147–152.
30. Wang, A, Yu, BN, Luo, CH, et al. Ile118Val genetic polymorphism of CYP3A4 and its effects on lipidlowering efficacy of simvastatin in Chinese hyperlipidemic patients. Eur J Clin Pharmacol 60 (2005), 843–848.
31. Fiegenbaum, M, da Silveira, FR, Van der Sand, CR, et al. The role of common variants of ABCB1, CYP3A4, and CYP3A5 genes in lipid-lowering efficacy and safety of simvastatin treatment. Clin Pharmacol Ther. 78 (2005), 551–558.
32. Kim, RB, Leake, BF, Choo, EF, et al. Identification of functionally variant MDR1 alleles among European Americans and African Americans. Clin Pharmacol Ther. 70 (2001), 189–199.
33. Kajinami, K, Brousseau, ME, Ordovas, JM, Schaefer, EJ, Polymorphisms in the multidrug resistance-1 (MDR1) gene influence the response to atorvastatin treatment in a genderspecific manner. Am J Cardiol 93 (2004), 1046–1050.
34. Tachibana-Iimori, R, Tabara, Y, Kusuhara, H, et al. Effect of genetic polymorphism of OATP-C (SLCO1B1) on lipid-lowering response to HMG-CoA reductase inhibitors. Drug Metab Pharmacokinet 19 (2004), 375–380.