# US 8,785,432 B2 · Pharmaceutical compositions of amlodipine and valsartan

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- Number: US 8,785,432 B2
- Document ID: US8785432B2
- Status: Granted
- Kind: B2
- Application number: 12/810,662
- Filed: 2008-02-21
- Published: 2010-10-28
- Granted: 2014-07-22
- Earliest claimed: 2007-12-31
- Assignees: Lupin Limited
- Applicants: Anirudha Bhagirath Kute; Nikhil Prabhakar Malewar; Makarand Krishnakumar Avachat
- Inventors: Anirudha Bhagirath Kute; Nikhil Prabhakar Malewar; Makarand Krishnakumar Avachat
- Web page: https://patentgrep.com/patent/US8785432B2

## CPC

- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 31/41: having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K 31/4422: 1,4-Dihydropyridines, e.g. nifedipine, nicardipine
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 9/12: Antihypertensives
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

A single layer pharmaceutical composition comprising active agent(s) amlodipine or a pharmaceutically acceptable salt thereof and valsartan or a pharmaceutically acceptable salt thereof wherein the composition exhibits bioequivalence to the commercially available bilayer tablet dosage form comprising amlodipine besylate and valsartan; when administered to human subject, under the bioequivalence parameters of a 90% Confidence Interval for AUC which is between 80% and 125%, and a 90% Confidence Interval for Cmax, which is between 80% and 125%.

## Claims

### Claim 1

A single layer pharmaceutical composition comprising active agent(s)
(a) amlodipine or a pharmaceutically acceptable salt thereof and
(b) valsartan or a pharmaceutically acceptable salt thereof
wherein:
(i) the composition exhibits bioequivalence to the commercially available bilayer tablet dosage form comprising amlodipine besylate and valsartan; when administered to a human subject, under the bioequivalence parameters of: (a) a 90% Confidence Interval for AUC which is between 80% and 125%, and (b) a 90% Confidence Interval for Cmax, which is between 80% and 125%; and
(ii) wherein valsartan is present in an amount less than 35% by weight, based on the total weight of the pharmaceutical composition.

### Claim 2 (depends on 1)

A single layer pharmaceutical composition according to claim 1, wherein valsartan is present in a unit dose in amount ranging from about 250 mg to about 640 mg.

### Claim 3 (depends on 1)

A single layer pharmaceutical composition according to claim 1, wherein active agent is present in an amount less than 35% by weight, based on the total weight of the pharmaceutical composition.

### Claim 4 (depends on 1)

A single layer pharmaceutical composition according to claim 1, comprising pharmaceutically acceptable additives selected from the group comprising fillers or diluents, binders, lubricants, glidants and disintegrants.

### Claim 5 (depends on 4)

A single layer pharmaceutical composition of claim 4, wherein the diluent is one or more selected from the group comprising confectioner's sugar, compressible sugar, dextrates, dextrin, dextrose, lactitol, fructose, mannitol, sucrose, starch, lactose, dibasic or tribasic calcium phosphate, calcium carbonate, calcium sulphate, xylitol, sorbitol, talc, micro-crystalline cellulose or mixtures thereof.

### Claim 6 (depends on 4)

A single layer pharmaceutical composition claim 4, wherein the binder is one or more selected from the group comprising methyl cellulose, hydroxypropylcellulose, low substituted hydroxypropylcellulose, hydroxypropyl methylcellulose, sodium carboxymethylcellulose, ethyl cellulose, microcrystalline cellulose, potato starch, wheat starch, corn starch, pregelatinised maize starch, polyvinylpyrrolidone, acacia, alginic acid, guar gum; liquid glucose, dextrin, povidone, syrup, polyethylene oxide and mixtures thereof.

### Claim 7 (depends on 4)

A single layer pharmaceutical composition of claim 4, wherein the lubricant is one or more selected from the group comprising Mg, Al, Zn or Ca stearate, polyethylene glycol, mineral oil, sodium stearyl fumarate, stearic acid, hydrogenated vegetable oil, glyceryl behenate, talc and mixtures thereof.

### Claim 8 (depends on 4)

A single layer pharmaceutical composition of claim 4, wherein the glidant is one or more selected from the group comprising silicon dioxide, colloidal silica, powdered cellulose, talc, tribasic calcium phosphate and mixtures thereof.

### Claim 9 (depends on 4)

A single layer pharmaceutical composition of claim 4, wherein the disintegrant is one or more selected from the group comprising cross linked polyvinylpyrrolidone, maize starch, dried starch, pregelatinized starch, sodium starch glycolate, alginic acid, sodium alginate, guar gum, croscarmellose sodium, microcrystalline cellulose and its salts, microfine cellulose, low substituted hydroxypropylcellulose, ion exchange resins and mixtures thereof.

### Claim 10 (depends on 1)

A pharmaceutical composition described in claim 1, which is in the form of tablets, capsules, granules, microparticles, minitablets and pellets.

### Claim 11 (depends on 1)

A pharmaceutical composition of claim 1 is further coated.