Caduet (Amlodipine Besylate / Atorvastatin Calcium) - Description

DESCRIPTION

CADUET® (amlodipine besylate and atorvastatin calcium) tablets combine the long-acting calcium channel blocker amlodipine besylate with the synthetic lipid-lowering agent atorvastatin calcium.

The amlodipine besylate component of CADUET is chemically described as 3-Ethyl-5-methyl (±)-2-[(2-aminoethoxy)methyl]-4-(o-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate, monobenzenesulphonate. Its empirical formula is C₂₀H₂₅ClN₂O₅•C₆H₆O₃S.

The atorvastatin calcium component of CADUET is chemically described as [R-(R*, R*)]-2-(4-fluorophenyl)-β, δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid, calcium salt (2:1) trihydrate. Its empirical formula is (C₃₃H₃₄FN₂O₅)₂Ca•3H₂O.

The structural formulae for amlodipine besylate and atorvastatin calcium are shown below.

CADUET contains amlodipine besylate, a white to off-white crystalline powder, and atorvastatin calcium, also a white to off-white crystalline powder. Amlodipine besylate has a molecular weight of 567.1 and atorvastatin calcium has a molecular weight of 1209.42. Amlodipine besylate is slightly soluble in water and sparingly soluble in ethanol. Atorvastatin calcium is insoluble in aqueous solutions of pH 4 and below. Atorvastatin calcium is very slightly soluble in distilled water, pH 7.4 phosphate buffer, and acetonitrile; slightly soluble in ethanol, and freely soluble in methanol.

CADUET tablets are formulated for oral administration in the following strength combinations:

Table 1. CADUET Tablet Strengths

	2.5 mg/ 10mg	2.5 mg/ 20mg	2.5 mg/ 40mg	5 mg/10 mg	5 mg/20 mg	5 mg/40 mg	5 mg/80 mg	10 mg/ 10 mg	10 mg/ 20 mg	10 mg/ 40 mg	10 mg/ 80 mg
amlodipine equivalent (mg)	2.5	2.5	2.5	5	5	5	5	10	10	10	10
atorvastatin equivalent (mg)	10	20	40	10	20	40	80	10	20	40	80

Each tablet also contains calcium carbonate, croscarmellose sodium, microcrystalline cellulose, pregelatinized starch, polysorbate 80, hydroxypropyl cellulose, purified water, colloidal silicon dioxide (anhydrous), magnesium stearate, Opadry® II White 85F28751 (polyvinyl alcohol, titanium dioxide, PEG 3000 and talc) or Opadry® II Blue 85F10919 (polyvinyl alcohol, titanium dioxide, PEG 3000, talc and FD&C blue #2). Combinations of atorvastatin with 2.5 mg and 5 mg amlodipine are film coated white, and combinations of atorvastatin with 10 mg amlodipine are film coated blue.