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Entecavir oral solid composition and preparation method thereof

A solid composition, entecavir technology, applied in the directions of drug combination, heterocyclic compound active ingredient, pharmaceutical formula, etc., can solve the problems of high compression moldability, high material flowability, and poor particle moldability, etc. Enhanced quality control and cost savings, reduced heat and humidity processes, fast and easy micronization of raw materials

Active Publication Date: 2015-04-15
YAOPHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are two prominent problems. One is that the compression formability of the material is high, otherwise the particle formability is not good, and the obtained product (especially the tablet) has low hardness and is easy to wear
Second, there is a high requirement for the fluidity of the material. If the proportion of the raw material in the prescription is small or the fluidity is poor, it will make it difficult to mix evenly. The material may also be stratified during the tableting process, and there is a risk of uneven product content.
[0013] Therefore, it is necessary to develop a new process to solve the problem of uneven content that is easy to occur during the preparation of entecavir oral solid preparations by dry granulation, so that qualified entecavir solid preparations can be produced by adopting dry granulation processes in large-scale industrial production.

Method used

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  • Entecavir oral solid composition and preparation method thereof
  • Entecavir oral solid composition and preparation method thereof
  • Entecavir oral solid composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Preparation of 0.5mg Entecavir Tablets

[0051]

[0052] First, crush Entecavir to d(0.5)=12μm, d(0.9)=38μm, pre-mix with microcrystalline cellulose for dispersion, then add microcrystalline cellulose and lactose for internal use into the mixture, mix well and add internal Add magnesium stearate and mix well. The resulting mixture is then fed into a dry granulator for dry granulation. The prepared granules are uniformly mixed with microcrystalline cellulose for external use and cross-linked povidone, and finally magnesium stearate is added, mixed uniformly, and compressed into tablets. The prepared tablet was placed in a coating pan, sprayed into Opady series coating solution, film coated, and the weight of the coating increased by 3%, to obtain the product.

Embodiment 2

[0054] Preparation of 1.0mg Entecavir Tablets

[0055]

[0056] First, crush Entecavir until the material d(0.5)=30μm, d(0.9)=50μm, pre-mix with microcrystalline cellulose for dispersion, then add microcrystalline cellulose and mannitol for internal addition to the mixture, and mix well Add magnesium stearate for internal use and mix well. The resulting mixture is then fed into a dry granulator for dry granulation. The prepared granules are uniformly mixed with microcrystalline cellulose for external use and sodium carboxymethyl starch, and finally magnesium stearate is added, mixed uniformly, and compressed into tablets. The prepared tablet was placed in a coating pan, sprayed into Opady series coating solution, film coated, and the weight of the coating increased by 6%, to obtain the product.

Embodiment 3

[0058] Preparation of 0.1mg Entecavir Tablets

[0059]

[0060]

[0061] First, crush Entecavir to d(0.5)=1μm, d(0.9)=13μm, pre-mix with microcrystalline cellulose for dispersion, then add microcrystalline cellulose for internal addition to the mixture, mix well and then add for internal addition magnesium stearate, mix well. The resulting mixture is then fed into a dry granulator for dry granulation. The prepared granules are uniformly mixed with microcrystalline cellulose for external use and cross-linked povidone, and finally magnesium stearate is added, mixed uniformly, and compressed into tablets. The prepared tablet was put into a coating pan, sprayed into Opady series coating solution, film coated, and the weight of the coating increased by 2%, to obtain the product.

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PUM

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Abstract

The invention discloses an entecavir oral solid composition prepared with dry granulating and a preparation method thereof. The entecavir oral solid composition disclosed by the invention comprises entecavir, a dispersing agent, a disintegrating agent and a lubricating agent; the particle size of the entecavir is controlled in a certain range by micronizing; the entecavir is uniformly dispersed in the composition; and the entecavir oral solid composition is prepared with dry granulating. The entecavir oral solid composition has a simple preparation method, is easy to control, and is suitable for large-scale industrial production; and a prepared product has uniform content and high stability.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to an oral solid composition of Entecavir and a preparation method thereof, in particular to an oral solid composition of Entecavir prepared by dry granulation. Background technique [0002] Hepatitis B is one of the three obstinate diseases in the world, and it is widespread, but the intensity of HBV prevalence varies greatly in different regions. According to the report of the World Health Organization, about 2 billion people in the world have been infected with hepatitis B virus (HBV), of which 350 million are chronic HBV infected people, and about 1 million people die of liver failure and cirrhosis caused by HBV infection every year and primary hepatocellular carcinoma (HCC). my country is a high-endemic area of ​​HBV. According to expert estimates, there are currently 20 to 30 million chronic hepatitis B patients in the country, and about 300,000 people die of chronic liver disease every...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K9/48A61K31/522A61K47/32A61K47/38A61P1/16A61P31/20
Inventor 以盛张旭陈剑锋王小霞黄兴锟
Owner YAOPHARMA CO LTD