Entecavir solid dispersion, pharmaceutical composition, method for preparing entecavir solid dispersion and pharmaceutical application of entecavir solid dispersion

A solid dispersion, entecavir technology, applied in the field of solid dispersion of entecavir, can solve the problem of organic solvent residues, affecting the quality and safety of entecavir drugs, solid dispersion solubility, dissolution rate and stability can not achieve maximum drug absorption and Use and other problems to achieve the effect of guaranteed quality, good stability and improved water solubility

Active Publication Date: 2014-06-11
BRIGHTGENE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Chinese patent CN101181224B discloses a solid dispersion of entecavir, the preparation method and application technology of its pharmaceutical composition, using poloxamer as the carrier of the solid dispersion; CN10122422A and CN102008447A disclose polyethylene glycol or / and poloxa To improve the solubility of entecavir in water, but the solubility, dissolution rate and stability of the solid dispersion prepared by the above-mentioned technology still cannot meet the requirements of drug maximum absorption and utilization, and the solution used is Organic solvents will produce organic solvent residues during industrial production and preparation, which will affect the quality and safety of entecavir drugs

Method used

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  • Entecavir solid dispersion, pharmaceutical composition, method for preparing entecavir solid dispersion and pharmaceutical application of entecavir solid dispersion
  • Entecavir solid dispersion, pharmaceutical composition, method for preparing entecavir solid dispersion and pharmaceutical application of entecavir solid dispersion
  • Entecavir solid dispersion, pharmaceutical composition, method for preparing entecavir solid dispersion and pharmaceutical application of entecavir solid dispersion

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1. Solid dispersion and preparation of entecavir and lactose (1:500)

[0028] Dissolve 1g of entecavir and 500g of lactose in 1000ml of water, heat to 70°C while stirring. After mixing evenly, it becomes a clear and transparent solution. Freeze-dry for 24 hours to remove water, then dry, cool to 20°C and pulverize, pass through an 80-mesh sieve , the obtained product is solid dispersion of entecavir and lactose.

[0029] Tablet preparation

[0030] The solid dispersion prepared above is mixed with the following pharmaceutical excipients in proportion to prepare tablets:

[0031]

[0032] According to the conventional tablet preparation process, it is compressed into tablets, and each tablet contains 5 mg of entecavir.

Embodiment 2

[0033] Example 2. Solid dispersion and preparation of entecavir and lactose (1:100)

[0034] Dissolve 1g of entecavir and 100g of lactose in 1000ml of water, heat it to 80°C while stirring, and get a clear and transparent solution after mixing evenly, remove the water by spray drying, then dry, cool to 10°C and pulverize, pass through an 80-mesh sieve to obtain The product is entecavir and lactose solid dispersion.

[0035] Preparation of granules

[0036] The solid dispersion prepared above is mixed with the following pharmaceutical excipients in proportion to prepare granules:

[0037]

[0038] According to the conventional preparation process of granules, the granules are prepared, dried and granulated.

Embodiment 3

[0039] Example 3. Solid dispersion and preparation of entecavir and lactose (1:250)

[0040] Dissolve 1g of entecavir and 250g of lactose in 1000ml of water, heat it to 85°C while stirring, and get a clear and transparent solution after mixing evenly, remove the water by spray drying, then dry, cool to 22°C and pulverize, pass through a 80-mesh sieve to obtain The product is entecavir and lactose solid dispersion.

[0041] Preparation of capsules

[0042] The solid dispersion prepared above is mixed with the following pharmaceutical excipients in proportion to prepare capsules:

[0043]

[0044] According to the conventional preparation process of capsules, it is compressed into tablets, and each capsule contains 1 mg of entecavir.

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PUM

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Abstract

The invention belongs to the technical field of pharmacy, and in particular relates to an entecavir solid dispersion, a method for preparing the solid dispersion and a pharmaceutical application of the solid dispersion. The entecavir solid dispersion disclosed by the invention comprises entecavir and lactose or lactose and other additives, wherein the mass ratio of entecavir to lactose or lactose and other additives is 1: (10 to 500) or 1: (100-200): (50-90). The invention further discloses application of a pharmaceutical composition. By the process, the problems that the entecavir preparation with small specification has high content uniformity requirement on pharmaceuticals and stable properties can be effectively solved; and moreover, the entecavir solid dispersion has the characteristics of good water solubility, quick dissolution rate, no organic solvent residue, low production cost and simple process, and is specially suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and in particular relates to a solid dispersion of entecavir, a preparation method and a pharmaceutical application of the solid dispersion. Background technique [0002] Entecavir is a guanosine analog with the chemical name 2-amino-9-[(1S,3R,4S)-4-hydroxy-3-hydroxymethyl-2-methylenecyclopentyl ]-1,9-dihydro-6H-purin-6-one, molecular formula C 12 h 15 N 5 o 3 , molecular weight 277.3. It is mainly used for the treatment of chronic hepatitis B infection in adults with active viral replication and persistently elevated serum transaminases, or active liver histological lesions. [0003] US Patent No. 5,206,244 discloses entecavir and its use for treating hepatitis B virus. WO98 / 09964 and WO04 / 052310 disclose improved synthesis of entecavir. Entecavir is used in a small amount, and generally adults can take 0.5mg or 1mg orally to achieve a good effect. However, such small-scale preparations ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K31/522A61K47/26A61P1/16A61P31/20
Inventor 袁建栋吴洪升毛姝君周丽丽周维娜
Owner BRIGHTGENE PHARMA
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