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Entecavir granule formulation and preparation method thereof

A technology of entecavir and granules, which is applied in the field of entecavir soluble granules and its preparation, can solve the problems of affecting the bioavailability of active components and poor solubility of granules, and achieve solid and non-brittle granules, fast onset of action, good taste effect

Active Publication Date: 2012-03-28
HUNAN WARRANT PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The prepared granules have poor solubility properties, which may affect the bioavailability of the active ingredient

Method used

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  • Entecavir granule formulation and preparation method thereof
  • Entecavir granule formulation and preparation method thereof
  • Entecavir granule formulation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Preparation Components of Entecavir Granules:

[0051]

[0052] The preparation method of entecavir granules:

[0053] (1) Pulverize entecavir, lactose and mannitol respectively, pass entecavir through a 120-mesh sieve, and lactose and mannitol pass through a 100-mesh sieve;

[0054] (2) prepare 5% soluble starch slurry;

[0055] (3) First mix mannitol and lactose evenly, then weigh the above excipient mixture equivalent to entecavir, grind it with entecavir for 15 minutes, then add the mixture of mannitol and lactose in increments, mix evenly, and finally use 5% wet granules made of soluble starch slurry;

[0056] (4) The wet granules obtained in step (3) were dried at 55° C., and then sized to obtain the entecavir granules.

Embodiment 2

[0058] Preparation components of entecavir granules (specification: 0.5mg / bag):

[0059]

[0060] The preparation method of entecavir granules:

[0061] (1) Pulverize entecavir, sucrose and soluble starch respectively, pass entecavir through a 120 mesh sieve, and sucrose and soluble starch pass through a 100 mesh sieve respectively;

[0062] (2) prepare 3% hypromellose aqueous solution;

[0063] (3) firstly mix sucrose and soluble starch evenly, then, mix entecavir with the above-mentioned mixture uniformly in increments, and finally use 3% hypromellose aqueous solution to make wet granules;

[0064] (4) The wet granules obtained in step (3) were dried at 55° C., and then sized to obtain the entecavir granules.

Embodiment 3

[0066] Preparation components of Entecavir granules (specification: 1mg / bag):

[0067]

[0068] The preparation method of entecavir granules:

[0069] (1) Pulverize entecavir, xylitol and lactose respectively, pass entecavir through a 120 mesh sieve, and xylitol and lactose pass through a 100 mesh sieve respectively;

[0070] (2) prepare 5% hypromellose 50% ethanol solution;

[0071] (3) Mix xylitol and lactose uniformly first, then mix entecavir and the above-mentioned mixture uniformly in equal increments, and finally use 5% hypromellose 50% ethanol solution to prepare wet granules;

[0072] (4) The wet granules obtained in step (3) were dried at 55° C., and then sized to obtain the entecavir granules.

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Abstract

The invention provides an entecavir granule formulation and a preparation method thereof. The raw materials of the granule formulation comprise the following components according to the part by weight: 0.001 to 0.5 of entecavir, 90 to 99.5 of a diluent and 0.5 to 5.0 of a binder. The granule formulation has a simple auxiliary composition and has a good palatability. no additional flavoring or essence or pigment is required. The granule formulation is well molded, and forms a clear solution with no chips or impurities after being dissolved in hot water.

Description

technical field [0001] The invention relates to an entecavir granule, in particular to an entecavir soluble granule and a preparation method thereof. Background technique [0002] Chronic viral hepatitis B (CH-B) is a common disease that seriously endangers human health. The prevention and treatment of chronic hepatitis B is a global public health problem, which has attracted the attention of all countries in the world. Hundreds of millions of people around the world have been infected with hepatitis B virus, among which there are about 400 million chronic hepatitis B virus carriers. Among infected patients, about 15% to 40% will develop cirrhosis, liver failure or liver cancer. Among the carriers of hepatitis B virus, 50% to 75% of them have chronic hepatitis B with active virus replication, and the estimated incidence rate of progression from chronic hepatitis B to cirrhosis in 5 years is 2% to 20%; from compensated cirrhosis to Liver decompensation is 20% to 23%; from c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/522A61P1/16A61P31/20A61P31/22
Inventor 谢安云
Owner HUNAN WARRANT PHARMA
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