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Pharmaceutical compositions of amlodipine and atorvastatin

A technology of atorvastatin and atorvastatin calcium, which is applied in the field of pharmaceutical compositions of amlodipine and atorvastatin, and can solve problems such as inability to prove complete normalization of cardiovascular mortality

Inactive Publication Date: 2005-05-18
WARNER LAMBERT CO LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, the hypertension intervention trial could not demonstrate complete normalization of cardiovascular mortality due to coronary heart disease

Method used

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  • Pharmaceutical compositions of amlodipine and atorvastatin
  • Pharmaceutical compositions of amlodipine and atorvastatin
  • Pharmaceutical compositions of amlodipine and atorvastatin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0216] General Process for Manufacture of Atorvastatin Calcium / Amlodipine Besylate Dual Therapy Tablets

[0217] [A] Atorvastatin granulation method

[0218] Step 1. - Dissolve polysorbate 80 in purified water at 50°C and add hydrated hydroxypropylcellulose. The solution was allowed to cool to room temperature.

[0219] Step 2.- Mix atorvastatin calcium, calcium carbonate, microcrystalline cellulose, starch 1500 and croscarmellose sodium in a fluid bed granulator / dryer (FBG / D) or high shear mixer / granulator .

[0220] Step 3.- Granulate the powder mixture from step 2 and the solution from step 1 in a FBG / D or high shear mixer / granulator.

[0221] Step 4.- Dry the granules in FBG / D or other drying equipment to a moisture content (loss on drying, LOD) less than or equal to 2.0%.

[0222] [B] final preparation

[0223] Step 1.- Add amlodipine besylate, microcrystalline cellulose, croscarmellose sodium and silicon dioxide to the atorvastatin granules obtained in step [A].

...

Embodiment 2

[0251] A Single-Dose Bioequivalence Study of 5-mg Amlodipine / 10-mg Atorvastatin Dual Therapy Tablets Compared with Coadministered 5-mg Amlodipine and 10-mg Atorvastatin Tablets

[0252] Protocol: A randomized single-dose two-way crossover study in 36 healthy volunteers. Following an overnight fast, each subject received a single 5-mg amlodipine and 10-mg atorvastatin tablet as a dual treatment and co-administered separate tablets on Days 1 and 15.

[0253] Blood samples were collected before and for 168 consecutive hours after each dose. Plasma samples were collected and stored frozen at -70°C until analysis. Plasma amlodipine and atorvastatin concentrations were determined by validated methods. Pharmacokinetic parameter values ​​were evaluated from concentration-time curves by non-compartmental methods. ANOVA (Analysis of Variance) results of the log-transformed Cmax and AUC values ​​were used to calculate 90% confidence intervals for the proportion of means with the least...

Embodiment 3

[0269] A Single-Dose Bioequivalence Study of 10-mg Amlodipine / 40-mg Atorvastatin Dual Therapy Tablets Compared with Coadministered 10-mg Amlodipine and 40-mg Atorvastatin Tablets

[0270] Protocol: A randomized single-dose two-way crossover study in 36 healthy volunteers. Following an overnight fast, each subject received a single 10-mg amlodipine and 40-mg atorvastatin as a dual treatment tablet and co-administered separate tablets on Days 1 and 15.

[0271] Blood samples were collected before and for 168 consecutive hours after each dose. Plasma samples were collected and stored frozen at -70°C until analysis. Plasma amlodipine and atorvastatin concentrations were determined by validated methods. Pharmacokinetic parameter values ​​were evaluated from concentration-time curves by non-compartmental methods. ANOVA results of log-transformed Cmax and AUC values ​​were used to calculate 90% confidence intervals for the proportion of mean values ​​of the least variance treatmen...

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Abstract

The present invention describes a pharmaceutical composition comprising two components: (a) a component comprising granules of atorvastatin or a pharmaceutically acceptable salt thereof and a carrier, including an alkalizing agent to form a pH greater than 5; and (b) Two components comprising amlodipine or a pharmaceutically acceptable salt thereof and a carrier, excluding an alkalizing agent for forming a pH greater than 5, wherein the two components are mixed to form a final composition in solid dosage form, and a method of preparing the composition, A kit containing such a composition, and the use of a therapeutically effective amount of the pharmaceutical composition to treat angina pectoris, atherosclerosis, hypertension and hyperlipidemia complications and / or hypercholesterolemia and to treat heart disease risk signs.

Description

field of invention [0001] The present invention relates to the pharmaceutical composition containing amlodipine (amlodipine) and its pharmaceutically acceptable salt, and atorvastatin (atorvastatin) and its pharmaceutically acceptable salt, the preparation method of this composition, the reagent that comprises such composition Kit, and use of such compositions for the treatment of patients with angina pectoris, atherosclerosis, hypertension and hyperlipidemia and / or hypercholesterolemia and for the presence of cardiac risk signs, including human subjects methods of patient treatment. Background of the invention [0002] In an early and rate-limiting step in the cholesterol biosynthetic pathway, 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) is converted to mevalonate. This step is catalyzed by HMG-CoA reductase. Inhibins inhibit HMG-CoA reductase from catalyzing this conversion. Because of this, statins are effective lipid-lowering agents. [0003] Atorvastatin calcium ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61J3/06A61K9/16A61K9/20A61K31/40A61K31/401A61K31/44A61K31/4422A61K47/02A61K47/04A61P3/06A61P9/00A61P9/08A61P9/10A61P9/12A61P9/14A61P43/00
CPCA61K9/1611A61K9/1652A61K9/2009A61K9/2054A61K9/2059A61K9/2081A61K31/40A61K31/401A61K31/4422A61P3/06A61P43/00A61P9/00A61P9/08A61P9/10A61P9/12A61P9/14A61P3/10A61K2300/00A61K31/4418
Inventor L·阿拉尼S·U·克汉T·M·麦克奈尔N·A-H·穆哈迈德
Owner WARNER LAMBERT CO LLC
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