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Preparation method of tenofovir disoproxil fumarate oral tablets

A technology of tenofovir fumarate and disoproxil, which is applied in the directions of non-active ingredient medical preparations, medical preparations containing active ingredients, and pill delivery, etc. It can reduce the difficulty of swallowing, increase the drug dissolution rate, and reduce the particle size.

Inactive Publication Date: 2016-06-15
广东京豪生物制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The dosage forms of tenofovir disoproxil fumarate currently on the market are mainly oral tablets with large specifications, each containing 300 mg of the main drug, which is relatively viscous and disintegrates slowly during taking. Affect the body's absorption
Different preparation methods of the same pharmaceutical preparation may have significant differences in the dissolution rate of the drug, which will affect the absorption and metabolism process of the drug in the body, so that its bioavailability may also have significant differences

Method used

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  • Preparation method of tenofovir disoproxil fumarate oral tablets
  • Preparation method of tenofovir disoproxil fumarate oral tablets
  • Preparation method of tenofovir disoproxil fumarate oral tablets

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Effect test

Embodiment 1

[0015] prescription:

[0016]

[0017] Preparation method: (1) Weigh each material separately, micronize, pass tenofovir disoproxil fumarate raw material through a 100-mesh sieve, microcrystalline cellulose, lactose, pregelatinized starch, cross-linked carboxymethyl Sodium cellulose is passed through a 80-mesh sieve, magnesium stearate and Opadry coating mixed powder are passed through a 40-mesh sieve for subsequent use;

[0018] (2) Take the prescription amount of 60% ethanol (v / v) solution, add the above prescription amount of micronized pregelatinized starch, and prepare a pregelatinized starch suspension with a concentration of 10% (w / v), and set aside ;

[0019] (3) Mix tenofovir disoproxil fumarate, lactose, microcrystalline cellulose, and croscarmellose sodium (75% prescription amount) evenly with the suspension treated in step (2), Soft materials are prepared in a fluidized bed, granulated through 18 mesh, dried at an air inlet temperature of 45°C, and the moistur...

Embodiment 2

[0024] prescription:

[0025]

[0026] Preparation method: (1) Weigh each material separately, micronize, pass tenofovir disoproxil fumarate raw material through a 100-mesh sieve, microcrystalline cellulose, lactose, pregelatinized starch, cross-linked carboxymethyl Sodium cellulose is passed through a 80-mesh sieve, magnesium stearate and Opadry coating mixed powder are passed through a 40-mesh sieve for subsequent use;

[0027] (2) Take the prescription amount of 75% ethanol (v / v) solution, add the above prescription amount of micronized pregelatinized starch, and prepare a pregelatinized starch suspension with a concentration of 15% (w / v), and set aside ;

[0028] (3) Mix tenofovir disoproxil fumarate, lactose, microcrystalline cellulose, and croscarmellose sodium (75% prescription amount) evenly with the suspension treated in step (2), Soft materials are prepared by fluidized bed, granulated through 30 mesh, dried at air inlet temperature of 50°C, and moisture content...

Embodiment 3

[0033] prescription:

[0034]

[0035] Preparation method: (1) Weigh each material separately, micronize, pass tenofovir disoproxil fumarate raw material through a 100-mesh sieve, microcrystalline cellulose, lactose, pregelatinized starch, cross-linked carboxymethyl Sodium cellulose is passed through a 80-mesh sieve, magnesium stearate and Opadry coating mixed powder are passed through a 40-mesh sieve for subsequent use;

[0036] (2) Take the 70% ethanol (v / v) solution of the prescription amount, add the micronized pregelatinized starch of the above prescription amount, and prepare a pregelatinized starch suspension with a concentration of 20% (w / v), and set aside ;

[0037] (3) Mix tenofovir disoproxil fumarate, lactose, microcrystalline cellulose, and croscarmellose sodium (75% prescription amount) evenly with the suspension treated in step (2), Fluidized bed preparation of soft materials, granulation through 20 mesh, air inlet temperature 55 ℃ drying, control moisture ...

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Abstract

The invention discloses a preparation method of tenofovir disoproxil fumarate oral tablet, which comprises micronization of raw and auxiliary materials, preparation of pregelatinized starch suspension and fluidized bed granulation and tableting process technical processing, thereby reducing particle size, tablet weight, and difficulty in swallowing, making it easier for patients to accept, and at the same time speeding up its disintegration rate, and improving oral administration of tenofovir disoproxil Bioavailability of esters.

Description

technical field [0001] The invention relates to a preparation method of medicine, in particular to a preparation method of tenofovir disoproxil fumarate oral tablet. Background technique [0002] Tenofovir Disoproxil Fumarate (Tenofovir Disoproxil Fumarate) is an ester prodrug of tenofovir, which belongs to a new type of nucleotide reverse transcriptase inhibitor. It is hydrolyzed into tenofovir after oral administration, and then Phosphorylated by cellular kinases to produce a pharmacologically active metabolite tenofovir diphosphate, which competes with 5'-deoxyadenosine triphosphate and participates in the synthesis of viral DNA. After entering the viral DNA, due to the lack of 3'-OH group Agglomerates, resulting in blocked DNA elongation, which in turn blocks viral replication. TDF was developed by Gilead, and was approved by the US FDA in October 2001 and 2008 for the treatment of AIDS and chronic hepatitis B (CHB) in adults. At present, more than 100 countries includ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K31/675A61K47/38A61K47/36A61K47/26A61P31/18A61P31/20A61P31/12
CPCA61K31/675A61K9/2018A61K9/205A61K9/2054A61K9/2866
Inventor 卢晓露陈文彪郑辉
Owner 广东京豪生物制药有限公司
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