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Valsartan-containing solid preparation and preparation method thereof

A technology of valsartan and preparations, which is applied in the field of pharmaceutical preparations and its preparation, and can solve problems such as inconvenience for patients to take, difficulty in tablet disintegration, and slow dissolution rate

Active Publication Date: 2010-09-15
ZHEJIANG HUAHAI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Such a high proportion of disintegrant content will inevitably lead to high hygroscopicity of the product, and the tablet is easy to absorb moisture during storage. As mentioned above, after the tablet absorbs moisture, the raw material of valsartan will become sticky when exposed to water, resulting in increased hardness. Difficulty in tablet disintegration and slow dissolution rate
Therefore, the technology of this patent application is not conducive to ensuring the dissolution stability of the valsartan preparation product, and the high proportion of disintegrant dosage will inevitably lead to an increase in the weight of the preparation product, and the shape of the tablet becomes larger, which is inconvenient for patients to take.

Method used

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  • Valsartan-containing solid preparation and preparation method thereof
  • Valsartan-containing solid preparation and preparation method thereof
  • Valsartan-containing solid preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0082] Embodiment 1: the preparation of valsartan tablet

[0083] The material composition is shown in Table 1;

[0084] Table 1 Material Composition Ratio

[0085]

[0086] *Prescriptions 1 and 2 are here only for comparison and do not belong to the content of the present invention. Prescription 1 comes from Example 7 of the patent application CN1636561A in the background technology, and prescription 2 comes from the prescription in Table 1 of the example of the patent application WO05089720 in the background technology 1.

[0087] Preparation of tablet cores: the prescribed amount of valsartan was granulated by roller compaction (Alexander WP120V), pressure: 40bar, roller speed: 3rpm. The prepared granules are mixed with other auxiliary materials, and then a punch with a suitable size is selected according to the weight of the tablet, and a high-speed tablet press is used to compress the tablet.

[0088] Preparation of coated tablets: Weigh The 85G series coating pow...

Embodiment 2

[0092] Embodiment 2: the preparation of valsartan tablet

[0093] The material composition is shown in Table 3.

[0094] Table 3 Material Composition Ratio

[0095]

[0096]

[0097] Preparation of tablet cores: the prescribed amount of valsartan was granulated by roller compaction (Alexander WP120V), pressure: 60bar, roller speed: 3rpm. Mix the prepared granules with optimized microcrystalline cellulose, crospovidone, low-substituted hydroxypropyl cellulose, and micropowder silica gel in a total mixing tank, then add magnesium stearate and mix evenly, and set aside. Use 14*5.5mm oval shallow concave punching plain tablet.

[0098] Preparation of coated tablets: Weigh 85G series coating powder prepares a coating liquid with a solid content of 20%, and coats plain tablets. Until the sheet has gained about 3% in weight. The indicators of the coated tablets meet the relevant regulations. The specific results are shown in Table 4.

[0099] Table 4 Test results of val...

Embodiment 3

[0101] Embodiment 3: the preparation of valsartan tablet

[0102] The material composition is shown in Table 5.

[0103] Table 5 Material Composition Ratio

[0104]

[0105]

[0106] Preparation of tablet cores: the prescribed amount of valsartan was granulated by roller compaction (Alexander WP120V), pressure: 70bar, roller speed: 3rpm. Mix the prepared granules with powdered cellulose, low-substituted hydroxypropyl cellulose, croscarmellose sodium and silicon dioxide in a mixing tank, then add magnesium stearate and mix evenly, and set aside. A circular shallow concave stamping sheet with a diameter of φ8.0mm is used.

[0107] Preparation of coated tablets: Weigh A coating solution is prepared to coat the plain tablets. Until the sheet has gained about 3% in weight. The results are shown in Table 6.

[0108] Table 6 Test results of valsartan tablets

[0109]

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Abstract

The invention relates to a valsartan-containing medicine preparation which at least comprises valsartan or pharmaceutically acceptable salt thereof that is taken as active ingredient, and at least two disintegrating agents, wherein the proportion of the two disintegrating agents is within the range of 1:2-2:1. The invention also relates to a preparation method of the valsartan-containing medicine preparation, which comprises the steps of: first, pelletizing the valsartan or the pharmaceutically acceptable salt thereof by a roller press way, and then mixing with the at least two disintegrating agents and other pharmaceutic adjuvant; and finally, tabletting or filling into capsules. Compared with the prior art, the valsartan-containing medicine preparation has better stability. The method has simple technique and high production efficiency, and is suitable for industrialized production.

Description

technical field [0001] The invention relates to a pharmaceutical preparation and a preparation method thereof, in particular to a preparation of valsartan or a pharmaceutically acceptable salt thereof and a preparation method thereof. Background technique [0002] Valsartan is a highly specific angiotensin (AT) II receptor antagonist that acts selectively on the AT1 receptor subtype, which responds to the known actions of angiotensin II , AT2 receptor subtypes are not related to cardiovascular effects, and valsartan does not have any partial agonist activity on AT1 receptors. Valsartan has a 20,000-fold stronger affinity for AT1 receptors than for AT2 receptors. The peak time of valsartan after oral administration is 2 to 4 hours, and the absolute bioavailability is about 25%. [0003] Structural formula: [0004] [0005] The original research company of valsartan is Novartis, and the trade name is It was approved for marketing in Europe and the United States in Dec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/41A61K9/30A61K9/48A61K47/38A61K47/36A61K47/32A61K31/5415A61K31/4422
Inventor 高慧燕彭俊清李巧霞胡功允
Owner ZHEJIANG HUAHAI PHARMA CO LTD
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