Entecavir tablet and preparation method thereof

A technology for entecavir and cavir tablets, applied in the field of entecavir tablets and their preparation, can solve the problems of complex technological process and difficulty in industrialized production, and achieve the effects of good product quality, rapid dissolution rate, and good content uniformity

Inactive Publication Date: 2012-09-05
ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the process of preparing solid dispersion is relatively complicated, and the industrial production is more difficult.

Method used

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  • Entecavir tablet and preparation method thereof
  • Entecavir tablet and preparation method thereof
  • Entecavir tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033]

[0034] 0.532 g of entecavir monohydrate is equivalent to 0.5 g of entecavir.

[0035] Preparation method: mix entecavir monohydrate (d(0.9)=8.6μm) with mannitol and cornstarch evenly, add purified water to granulate, granulate, and dry in a fluidized bed to obtain dry granules, and add colloidal dioxide to the dry granules Silicone and magnesium stearate are mixed and compressed into tablets.

[0036] Stability test

[0037] The product of embodiment 1 and the product of comparative example 2 (0.1N hydrochloric acid is solvent) are placed on 60 ℃, under the condition of 75% relative humidity, in 5 days, 10 days sampling uses HPLC to detect content and related substance, and with 0 The results are shown in Table 1 below.

[0038] Table 1:

[0039]

[0040] It can be seen that the addition of hydrochloric acid can lead to a significant change in product stability.

Embodiment 2

[0042]

[0043] 1.064g of entecavir monohydrate is equivalent to 1.0g of entecavir.

[0044] Preparation method: Entecavir monohydrate is micronized to a particle size of d(0.9)=47.3 μm, mixed evenly with entecavir monohydrate, lactose monohydrate, pregelatinized starch, and cross-linked povidone, and then added into povidone aqueous solution to granulate , granulated, and dried in a fluidized bed to obtain dry granules, which are mixed with magnesium stearate and compressed into tablets.

Embodiment 3

[0046]

[0047] 0.532 g of entecavir monohydrate is equivalent to 0.5 g of entecavir.

[0048] Preparation method: Entecavir monohydrate is micronized to a particle size of d(0.9)=11.8 μm, 0.532 g of entecavir monohydrate and about 6 g of lactose monohydrate are mixed uniformly in equal increments, and then mixed with the remaining lactose monohydrate , microcrystalline cellulose, and half of the amount of crospovidone are mixed evenly, and the povidone aqueous solution is added to granulate, granulated, and dried in a fluidized bed to obtain dry granules, and the remaining crospovidone and stearin are added to the dry granules Magnesium acid mixed, compressed into tablets.

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Abstract

The invention relates to an Entecavir tablet. The Entecavir tablet contains 0.2-1% of Entecavir monohydrate, 85-98% of filler, 0-5% of binder, 0-10% of disintegrating agent, 0-2% of flow aid and 0.5-2% of lubricating agent by weight, wherein the Entecavir monohydrate is added in the form of powder. The invention also relates to a preparation method of the Entecavir tablet.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to entecavir tablets and a preparation method thereof. Background technique [0002] Entecavir (Entecavir) is a kind of guanosine nucleoside analog, has the following chemical structure, molecular formula is C 12 h 15 N 5 o 3 , molecular weight 277.3, entecavir usually contains a molecule of crystal water, and the molecular formula of its monohydrate is C 12 h 15 N 5 o 3 ·H 2 O, the molecular weight is 295.3. [0003] [0004] Entecavir tablets were first developed by the Billy Stoll-Myers Squibb Company of the United States, and the product on the market is called Bolu (Baraclude) The doses of Entecavir tablets are 0.5 mg and 1.0 mg, and the tablet weights are about 206 mg and about 412 mg respectively, that is, the proportion of Entecavir in the pharmaceutical composition is only about 0.25%. Therefore, it is crucial to ensure the content uniformity of the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/522A61P1/16A61P31/20
Inventor 胡李斌彭俊清李巧霞胡功允
Owner ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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