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Stable pharmaceutical composition containing amlodipine and valsartan

A technology of amlodipine and valsartan granules, which can be applied in directions such as drug combinations, medical preparations containing active ingredients, active ingredients of heterocyclic compounds, etc., can solve the problems of not allowing the preparation of bioequivalents, etc. favorable effect

Inactive Publication Date: 2018-12-11
ZENTIVA AS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Dry granulation of the active substance and pharmaceutically acceptable excipients known from application WO2007 / 022113A does not allow the preparation of a bioequivalent single component containing higher doses of valsartan (greater than 160 mg) and amlodipine single layer tablet

Method used

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  • Stable pharmaceutical composition containing amlodipine and valsartan
  • Stable pharmaceutical composition containing amlodipine and valsartan
  • Stable pharmaceutical composition containing amlodipine and valsartan

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1 - Monolayer tablet made from valsartan containing granules (wet granulation) and powdered amlodipine. Values ​​are expressed in mg.

[0041] Table 1

[0042] Composition of 1 film tablet

Prototype 1

Valsartan

160.0

Amlodipine

13.9

Silicified microcrystalline cellulose

67.0

Sorbitol

18.5

Calcium Carbonate + Pregelatinized Starch

18.5

pregelatinized starch

6.0

povidone

15.0

Sodium stearyl fumarate

8.0

sodium lauryl sulfate

2.0

Crospovidone

26.0

Colloidal silica

4.0

Coating layer (polyethylene glycol, hypromellose, titanium dioxide, talc, iron oxide)

10.0

total

348.9

[0043] Valsartan together with sorbitol, crospovidone, silicified microcrystalline cellulose, povidone and sodium lauryl sulfate was homogenized in a granulator and subsequently kneaded by means of water as wetting agent. Granulation. Once the desired...

Embodiment 2

[0045] Example 2 - Monolayer tablet made from granules containing valsartan together with amlodipine (wet granulation). Values ​​are expressed in mg.

[0046] Table 2

[0047] Composition of 1 film tablet

[0048] Valsartan together with amlodipine, sorbitol, crospovidone, silicified microcrystalline cellulose, povidone and sodium lauryl sulfate was homogenized in a granulator and subsequently passed through with the aid of water as a wetting agent. The agent is kneaded and granulated. Once the desired granulation is achieved, the mixture is dried to a resulting granule moisture of 1% to 3%. Other excipients - ie another portion of crospovidone, pregelatinized starch, calcium carbonate and microcrystalline cellulose, sodium stearyl fumarate sieved through a sieve with a mesh size of maximum 1.0 mm and colloidal silicon dioxide, added to granules. After final homogenization, the tableting blend is compressed into a solid block with a strength of at least 30N. Aft...

Embodiment 3

[0049] Example 3 - Monolayer tablet made from valsartan containing granules (wet granulation) and compacted amlodipine.

[0050] table 3

[0051] Composition of 1 film tablet

[0052] Valsartan together with sorbitol, crospovidone, silicified microcrystalline cellulose, povidone and sodium lauryl sulfate was homogenized in a granulator and subsequently kneaded by means of water as wetting agent. Granulation. Once the desired granulation is achieved, the mixture is dried to a resulting granule moisture of 1% to 3% by weight. Amlodipine besylate together with microcrystalline cellulose, crospovidone, colloidal silicon dioxide and sodium stearyl fumarate were sieved through a sieve with a mesh size of 1.0 mm and the mixture was compacted Compacted in the machine. The compacted material is mixed together with the remaining excipients - ie the remaining portion of crospovidone, pregelatinized starch, calcium carbonate with microcrystalline cellulose, sodium stearyl fum...

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Abstract

The present invention relates to stable pharmaceutical compositions in the form of monolayer tablets. The composition contains valsartan, amlodipine or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable excipient. The pharmaceutical composition according to the invention may contain hydrochlorothiazide as a further active ingredient.

Description

technical field [0001] The present invention relates to a stable pharmaceutical composition comprising valsartan and amlodipine in the form of a monolayer tablet. Background technique [0002] Patent application WO2000 / 02543A describes the use of the AT1 receptor antagonist (S)-N-(1-carboxy-2-methylpropan-1-yl)-N-pentanoyl-N-[2'(1H-tetrazole -5-yl)biphenyl-4-ylmethyl]amine (valsartan) or its pharmaceutically acceptable salt and calcium channel blocker (4RS)-2-[(2-aminoethoxy)methanol Base]-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylic acid 3-ethyl-5-methyl ester (amlodipine) or its pharmaceutical Acceptable salt for combination therapy in hypertension. [0003] A fixed combination comprising valsartan and amlodipine in single dosage form is described in patent application WO2007 / 022113A. The invention relates to the drug in the form of a monolayer tablet in the case of lower doses of valsartan (less than or equal to 160 mg) or in the form of a bilayer t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K9/28A61K31/41A61K31/4422
CPCA61K9/205A61K9/2054A61K9/2059A61K9/2095A61K31/41A61K31/4422A61K31/549A61P43/00A61P9/12A61K2300/00
Inventor J·萨拉多瓦L·克伦姆霍尔科瓦T·瓦里洛瓦M·普拉辛那L·库卡科瓦A·巴尔图纳克
Owner ZENTIVA AS