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Solid pharmaceutical composition comprising irbesartan

A technology for solid pharmaceutical preparations and mixtures, which is applied in the field of irbesartan hydrochloride and can solve problems such as low solubility

Inactive Publication Date: 2009-02-18
KRKA D D NOVO MESTO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] In general, the specific physical and chemical properties of irbesartan, especially its low solubility in aqueous media, have caused problems in formulating it into formulations suitable for effective oral administration in the past

Method used

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  • Solid pharmaceutical composition comprising irbesartan

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-9

[0112] Tablets are prepared according to the following wet granulation method (A).

[0113] 1) Preparation of particles (1a)-(9a)

[0114] The solid components in the following Table 1 were respectively mixed in a high shear mixer, and ethanol (96 vol.-%) was sprayed on the mixture. The resulting granules are dried at a specific temperature in a drying chamber or in a fluidized bed dryer. The resulting granules were sieved and the loss on drying was determined as previously described. The properties and amounts of solid components and ethanol, drying equipment, drying temperature and drying loss of sieved particles are shown in Table 1.

[0115] Table 1

[0116]

[0117] 1) Is Irbesartan-HCl*1.5H 2 O(86.11g Irbesartan-HCl*1.5H 2 O equivalent to 75g free irbesartan)

[0118] 2) LH-21: commercially available low-substituted hydroxypropyl cellulose

[0119] 3) Klucel-EF: commercially available low-substituted hydroxypropyl cellulose

[0120] 4) DC: drying room

[...

Embodiment 10

[0137] Tablets were prepared according to direct compression method (b) as follows.

[0138] 86.11 g irbesartan-HCl, 40.89 g mannitol and 8 g croscarmellose sodium were mixed in a high shear mixer. Thereto were added 1.50 g of magnesium stearate, 1.5 g of anhydrous silicon dioxide and 12 g of talc, whereby a tableting mixture was obtained. The loss on drying was determined to be 3.1 wt.-% according to the method described above.

[0139] The tableting mixture is compressed into oval tablets with a theoretical weight of 150 mg. The hardness of the tablet core was 45-60N, and its disintegration time in pure water at 37°C was 20 seconds.

[0140] figure 1 Shown to contain 75 mg free irbesartan (equivalent to irbesartan-HCl*1.5H 2 (286.11mg) tablet core (4c)-(9c) of Examples 4-9 of the present invention and the comparison of the dissolution properties of the pharmaceutical dosage form (Aprovel75mg tablet) currently on the market. It can be seen that the pharmaceutical formula...

Embodiment 11-16

[0143] Tablets are prepared according to the following wet granulation method (A), adding hydrochlorothiazide, the steps are as follows: 1) Preparation of granules (11a)-(18a)

[0144] The solid components in the following Table 4 were respectively mixed in a high shear mixer, and ethanol (96 vol.-%) was sprayed on the mixture. The resulting granules are dried in a drying chamber or in a fluid bed drier. The nature and amount of solid components are shown in Table 4.

[0145] Table 4

[0146]

[0147] 1) Is Irbesartan-HCl*1.5H 2 O(86.11g Irbesartan-HCl*1.5H 2 O equivalent to 75g free irbesartan)

[0148] 2) LH-21: commercially available low-substituted hydroxypropyl cellulose

[0149] 3) q.s.: Appropriate amount

[0150] 2) Preparation of tableting mixture (11b)-(18b)

[0151] The ingredients shown in Table 5 below were respectively added to the granules (11a) to (18a) obtained above, followed by mixing in a high shear mixer to obtain a tableting mixture. The amo...

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Abstract

The present invention concerns preferably surfactant-free solid pharmaceutical formulations comprising, as an active ingredient, at least one of irbesartan and pharmaceutically acceptable salts thereof, and at least one disintegrant. Preferably, the active ingredient comprises irbesartan hydrochloride. Also, the present invention is directed to a process for the manufacture of such formulations, including a wet granulation process (A) and a direct granulation process (B).

Description

technical field [0001] The present invention relates to a solid pharmaceutical composition and a preparation method thereof. The solid pharmaceutical composition contains irbesartan and / or a pharmaceutically acceptable salt thereof as an active ingredient, especially irbesartan hydrochloride. The active ingredient is present alone or in combination with a diuretic, preferably hydrochlorothiazide. In particular, the present invention relates to a composition and a method wherein the active ingredient retains its structure and stability. In a preferred mode, the composition is free of surfactants. Background technique [0002] 2-Butyl-3-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1,3-diazaspiro[ 4,4]-non-1-en-4-one (irbesartan) is a non-peptide tetrazole derivative shown in the following structural formula (empirical formula C 25 h 28 N 6 O, molecular weight 428.5g / mol), with angiotensin II type 1 receptor (AT 1 ) antagonistic activity: [0003] [0004] Proc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/415A61K9/16A61P9/12
CPCA61K9/2054A61K9/2027A61K9/2077A61K31/415A61P7/10A61P9/00A61P9/12
Inventor 米哈·弗尔宾克雷娜塔·亚克塞弗兰奇·贝韦茨西尔沃·祖普契奇
Owner KRKA D D NOVO MESTO
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