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Tenofovir disoproxil fumarate fine granules

A technology of tenofovir disoproxil fumarate and fine particles, which is applied in the field of fine particles of tenofovir disoproxil fumarate, which can solve the problem of extremely bitter taste of tenofovir disoproxil fumarate and poor patient compliance problems, to achieve the effect of improving drug compliance and simple preparation process

Active Publication Date: 2014-12-03
SHINEWAY PHARMA GRP LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The present invention aims to provide an oral dosage form of tenofovir disoproxil fumarate with excellent taste-masking effect to solve the problems of extremely bitter taste and poor patient compliance of tenofovir disoproxil fumarate

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Weigh 4g of tenofovir disoproxil fumarate, 16g of mannitol and mix evenly, then add 80g of Kollidon VA64 (copolyvinylpyrrolidone / vinyl acetate) and mix evenly, and extrude the mixture through a hot-melt extruder. The extrusion temperature of the extruder is set to 140°C. After 20 minutes of equilibrium, the screw speed is set to 40r / min, the extrusion screws rotate in the same direction, and the extrusion torque is 40-45Ncm. After standing for 4 hours, it is pulverized by a secondary crusher, and the pulverized material passes through a 30-mesh sieve, and the materials above the 30-mesh sieve continue to pass through the secondary crusher for secondary crushing, so that all materials finally pass through a 30-mesh sieve to obtain a fine-grained agent.

Embodiment 2

[0041] Weigh tenofovir disoproxil fumarate 4g, xylitol 24g and mix evenly, then add Kollidon VA64 120g mix evenly, and the mixture is extruded by a hot melt extruder, and the extrusion temperature of the hot melt extruder is set at 130 ℃, after balancing for 20 minutes, set the screw speed to 25r / min, the extrusion screw to rotate in the same direction, and the extrusion torque to be 30-35Ncm. Pulverize, pass through a 30-mesh sieve, and the materials above the 30-mesh sieve continue to pass through a secondary crusher for secondary crushing so that all materials finally pass through a 30-mesh sieve to obtain a fine-grained agent.

Embodiment 3

[0043] Weigh 4g of tenofovir disoproxil fumarate, 20g of mannitol and mix evenly, then add Kollidon VA6484g and mix evenly, and extrude the mixture through a hot-melt extruder, and the extrusion temperature of the hot-melt extruder is set at 140°C , after balancing for 20 minutes, set the screw speed to 35r / min, the extrusion screw to rotate in reverse, and the extrusion torque to be 45 to 50Ncm, and the obtained strips are placed at room temperature for 4 hours, and then pulverized by a secondary crusher , the pulverized matter passes through a 30-mesh sieve, and the materials above the 30-mesh sieve continue to pass through the secondary crusher for secondary crushing, so that all materials finally pass through the 30-mesh sieve to obtain a fine-grained agent.

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Abstract

The invention relates to tenofovir disoproxil fumarate fine granules. The tenofovir disoproxil fumarate fine granules are formed by the following steps of: mixing tenofovir and a sweetening agent according to a mass ratio of 1: (0-6); mixing the mixture with a polymer for hot melting extrusion according to a mass ratio of 1: (2-15); then carrying out hot melting extrusion through a hot melting extruder; and crushing into the fine granules with the grain diameter less than or equal to 30 meshes. The tenofovir disoproxil fumarate fine granules disclosed by the invention overcome the disadvantages that the taste of tenofovir disoproxil fumarate is very bitter and the taste masking effect of an existing preparation is not enough, and the medicine-taking compliance of a patient is greatly improved.

Description

technical field [0001] The invention relates to a fine granule of tenofovir disoproxil fumarate, which belongs to the field of pharmaceutical preparations. Background technique [0002] Tenofovir disoproxil fumarate (tenofovir disoproxil fumarate, Tenofovir disoproxil fumarate) is an ester prodrug of tenofovir, which is a non / low drug resistance, low toxicity Anti-HBV and anti-HIV drugs. It is a new type of nucleotide reverse transcriptase inhibitor, which is hydrolyzed into tenofovir after oral administration, and then phosphorylated by cellular kinases to generate a pharmacologically active metabolite tenofovir diphosphate, which interacts with 5 '-Deoxyadenosine triphosphate competes and participates in the synthesis of viral DNA. After entering the viral DNA, due to the lack of 3'-OH group, the DNA elongation is blocked, thereby blocking the replication of the virus. [0003] Tenofovir disoproxil fumarate has a very bitter taste, and it is technically difficult to mask...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K31/675A61P31/20A61P31/18A61J3/02
Inventor 胡向青武勇刘军锋周学刚
Owner SHINEWAY PHARMA GRP LTD
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