Browse Prior Art Database

COMBINATION OF ANGIOTENSIN II RECEPTOR ANTAGONIST WITH OTHER ACTIVE SUBSTANCES

IP.com Disclosure Number: IPCOM000237823D
Publication Date: 2014-Jul-15
Document File: 5 page(s) / 93K

Publishing Venue

The IP.com Prior Art Database

This text was extracted from a Microsoft Word document.
This is the abbreviated version, containing approximately 20% of the total text.

COMBINATION OF ANGIOTENSIN II RECEPTOR ANTAGONIST WITH OTHER ACTIVE SUBSTANCES

The present disclosure relates to the field of pharmaceutical compositions and methods of preparing said compositions. Specifically, this disclosure relates to combination compositions comprising at least one angiotensin II receptor antagonist and at least one calcium channel blocker and optionally other active substance(s). Patients with hypertension, cardiovascular disease or other similar diseases usually require two or more antihypertensive drugs to achieve the desired blood pressure. Therefore, there exists the constant need for the preparation of combination composition that can effectively treat, prevent and manage the high blood pressure.

2,3-dihydroxy-2-butenyl 4(1-hydroxy-1-methylethyl)-2-propyl-1-[p-(o-1H-tetrazol-5-ylphenyl)benzyl]imidazole5-carboxylate, cyclic 2,3-carbonate (olmesartan medoxomile) is a well-known oral antihypertensive drug which acts as angiotensin II receptor antagonist used to treat high blood pressure. Olmesartan medoxomile used in the combination compositions of the present disclosure can be prepared according to any method known in the state of the art.

3-ethyl-5-methyl (¬Ī)-2-[(2-aminoethoxy)methyl]- 4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate, monobenzenesulphonate (amlodipine besylate) is a well-known dihydropyridine calcium-channel blocker used in the treatment of hypertension. ¬†Amlodipine besylate used in the combination compositions of the present disclosure can be prepared according to any method known in the state of the art.

6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide; 6-chloro-3,4-dihydro-7-sulfamoyl-2H-1,2,4-benzothiadiazine 1,1-dioxide (hydrochlorothiazide - HCTZ) is a well-known thiazide diuretic used to treat high blood pressure. HCTZ used in the combination compositions of the present disclosure can be prepared according to any method known in the state of the art.

Composition tablets comprising combination of olmesartan medoxomile and amlodipine besylate (proposed w/w % of each ingredient in formulation is defined) were produced by direct compression method by mixing olmesartan medoxomile (10-20 %), amlodipine besylate (1-10%), diluent such as for example Microcrystalline Cellulose of any type for direct compression, wet or dry granulation as defined by the manufacturer, Silicified Microcrystalline Cellulose, Lactose Monohydrate of any type for direct compression, wet or dry granulation as defined by the manufacturer, Lactose Anhydrous of any type for direct compression, wet or dry granulation as defined by the manufacturer, Mannitol of any type for direct compression, wet or dry granulation as defined by the manufacturer, Pregelatinized starch, Xylitol of any type for direct compression, wet or dry granulation as defined by the manufacturer, or any mixture thereof (65-85%) and disintegrant e.g. Low-substituted Hydroxypropylcellulose of any type for direct compres...