GEMCABENE COMBINATIONS FOR THE TREATMENT OF CARDIOVASCULAR DISEASE
The present invention provides pharmaceutical compositions formulated to include a statin and gemcabene, wherein the composition is useful for treating, preventing, or reducing the symptoms of cardiovascular and metabolic indications that involve elevate levels of LDL cholesterol, triglycerides, or both.
1 . 93 . (canceled)
94 . A tablet comprising:
a core, the core comprising a statin or a pharmaceutically acceptable salt thereof; and
an enteric coating comprising a first copolymer or a second copolymer,
the first copolymer is a methyl acrylate, methyl methacrylate and methacrylic acid copolymer, and
the second copolymer is methacrylic acid copolymer type C,
wherein the amount of the enteric coating ranges from about 2% w/w to about 15% w/w of the core.
95 . The tablet of claim 94 , wherein the enteric coating comprises the first copolymer and the second copolymer.
96 . The tablet of claim 94 , wherein the amount of the enteric coating is about 10% w/w of the core.
97 . The tablet of claim 95 , wherein the ratio of the first copolymer to the second copolymer ranges from about 2:1 to about 1:2 by weight.
98 . The tablet of claim 94 , wherein the amount of the first copolymer ranges from 0% w/w to about 10%) w/w of the core.
99 . The tablet of claim 94 , wherein the amount of the second copolymer ranges from 0% w/w to about 10% w/w of the core.
100 . The tablet of claim 94 , further comprising a subcoating between the core and the enteric coating.
101 . The tablet of claim 100 , wherein the amount of the subcoating ranges from about 1% w/w to about 5% w/w of the core.
102 . The tablet of 100 , wherein the subcoating comprises hypromellose.
103 . The tablet of claim 94 , wherein the statin is atorvastatin, simvastatin, pravastatin, mevastatin, rosuvastatin, fluvastatin, lovastatin, pitavastatin, dalvastatin, dihydrocompactin or orcerivastatin.
104 . The tablet of claim 94 , wherein the statin is atorvastatin.
105 . The tablet of claims 94 , wherein the pharmaceutically acceptable salt of the statin is atorvastatin calcium.
106 . The tablet of claim 94 , wherein the amount of the statin or pharmaceutically acceptable salt thereof ranges from about 10% to about 80% w/w of the core.
107 . The tablet of claim 94 , wherein the amount of the statin or pharmaceutically acceptable salt thereof ranges from about 1 mg to about 80 mg.
108 . The tablet of claim 94 , wherein when the tablet is subjected to dissolution testing according to USP <711> Delayed Release Dosage Forms Method A using Apparatus 2 (Paddle Apparatus) at 100 RPM, no more than 5% of the statin is detected in an acidic dissolution medium 2 hours after operation of Apparatus 2, wherein the acidic dissolution medium is 0.1N HCl.
109 . The tablet of claim 94 , wherein the tablet is a microtablet having a diameter ranging from about 10 μm to about 3 mm.
110 . The tablet of claim 94 , further comprising another pharmaceutically active agent.
111 . The tablet of claim 110 , wherein the other pharmaceutically active agent is ezetimibe, gemcabene or a pharmaceutically acceptable salt thereof.
112 . The tablet of claim 110 , wherein the other pharmaceutically active agent is gemcabene calcium.
113 . The tablet of claim 112 , further comprising ezetimibe.
114 . An oral dosage form comprising the tablet of claim 94 and a composition comprising another pharmaceutically active agent.
115 . The oral dosage form of claim 114 , wherein the other pharmaceutically active agent is ezetimibe, gemcabene or a pharmaceutically acceptable salt thereof.
116 . The oral dosage form of claim 114 , wherein the other pharmaceutically active agent is gemcabene calcium.
117 . The oral dosage form of claim 117 , further comprising ezetimibe.
118 . A capsule containing the tablet of claim 94 .
119 . The capsule of claim 118 , further containing another pharmaceutically active agent.
120 . The capsule of claim 119 , wherein the other pharmaceutically active agent is ezetimibe, gemcabene, or a pharmaceutically acceptable salt thereof.
121 . The capsule of claim 119 , wherein the other pharmaceutically active agent is gemcabene or a pharmaceutically acceptable salt thereof.
122 . The capsule of claim 119 , wherein the other pharmaceutically active agent is gemcabene calcium.
123 . The capsule of claim 121 , wherein the gemcabene or pharmaceutically acceptable salt thereof is present in an amount ranging from about 50 mg to about 900 mg per capsule.
124 . The capsule of claim 121 , further containing ezetimibe or a pharmaceutically acceptable salt thereof.
125 . A kit comprising a tablet of claim 94 and instructions for use of the tablet.