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Tenofovir alafenamide fumarate tablet, preparation method thereof and detection method of related substances

A technology of tenofovir fumarate and tenofol fumarate, which is applied in the field of tenofovir fumarate and tenofovir fumarate tablets and its preparation, can solve the problems of slow product dissolution, cumbersome process, poor consistency and the like , to achieve the effects of high drug stability, volume reduction, and narrow particle size distribution

Active Publication Date: 2021-02-09
NORTH CHINA PHARMA HUAKUN HEBEI BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Referring to the European marketing review report, it can be seen that the preparation process of the original preparation is dry granulation, which is cumbersome and consumes a lot of energy. In addition, obvious material crushing dust will be generated during the preparation process, which is not conducive to environmental protection.
In the prior art, some researchers have tried to prepare tenofovir alafenamide fumarate tablets by direct powder compression. The product obtained by direct powder compaction has higher hardness, slower dissolution rate, and poor consistency with the original research. And the impurity increases greatly during the storage process

Method used

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  • Tenofovir alafenamide fumarate tablet, preparation method thereof and detection method of related substances
  • Tenofovir alafenamide fumarate tablet, preparation method thereof and detection method of related substances
  • Tenofovir alafenamide fumarate tablet, preparation method thereof and detection method of related substances

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Comparison scheme
Effect test

Embodiment 1

[0042] The present embodiment provides a tenofovir alafenamide fumarate tablet, and the prescription dosage is as shown in the table below:

[0043]

[0044]

[0045] The preparation method of above-mentioned tenofovir alafenamide fumarate tablet is as follows:

[0046]The tenofovir alafenamide fumarate raw material is crushed through a 100-mesh sieve for later use, and other auxiliary materials are passed through an 80-mesh sieve for later use. According to the principle of the main drug after the auxiliary material first, each component is weighed according to the prescription amount, and the weighed tenofovir alafenamide fumarate, 65wt% prescription amount hydroxypropyl cellulose, lactose, sodium carboxymethyl starch , calcium hydrogen phosphate and 68wt% prescription amount of sodium stearyl fumarate are mixed evenly, and the fluidized bed granulation is carried out. The temperature of the air inlet is controlled at 20 ° C. After the granulation is completed, add the...

Embodiment 2

[0050] The present embodiment provides a tenofovir alafenamide fumarate tablet, and the prescription dosage is as shown in the table below:

[0051]

[0052]

[0053] The preparation method of above-mentioned tenofovir alafenamide fumarate tablet is as follows:

[0054] The tenofovir alafenamide fumarate raw material is crushed through a 100-mesh sieve for later use, and other auxiliary materials are passed through an 80-mesh sieve for later use. According to the principle of the main drug after the auxiliary material first, each component is weighed according to the prescription amount, and the weighed tenofovir alafenamide fumarate, 70wt% prescription amount hydroxypropyl cellulose, lactose, sodium carboxymethyl starch , calcium hydrogen phosphate and 65wt% prescription amount of sodium stearyl fumarate are mixed evenly, and the fluidized bed granulation is carried out. The temperature of the air inlet is controlled at 30 ° C. After the granulation is completed, add th...

Embodiment 3

[0058] The present embodiment provides a tenofovir alafenamide fumarate tablet, and the prescription dosage is as shown in the table below:

[0059] components Dosage per tablet / mg tenofovir alafenamide fumarate 28 Hypromellose 31 lactose 106 Sodium carboxymethyl starch 15 Sodium stearyl fumarate 6 Calcium hydrogen phosphate 11 Gastric film coating premix 10

[0060] The preparation method of above-mentioned tenofovir alafenamide fumarate tablet is as follows:

[0061] The tenofovir alafenamide fumarate raw material is crushed through a 100-mesh sieve for later use, and other auxiliary materials are passed through an 80-mesh sieve for later use. According to the principle of the main drug after the auxiliary material first, each component is weighed according to the prescription amount, and the weighed tenofovir alafenamide fumarate, 68wt% prescription amount hydroxypropyl cellulose, lactose, sodium carboxymethyl starch...

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Abstract

The invention relates to the technical field of pharmaceutical preparations, and particularly discloses a tenofovir alafenamide fumarate tablet and a preparation method thereof. The tenofovir alafenamide fumarate tablet comprises the following components in percentage by weight: 12%-14% of tenofovir alafenamide fumarate, 10%-15% of a cross-linking agent, 45%-58% of a diluent, 5%-12% of a disintegrating agent, 1%-5% of sodium stearyl fumarate and 5%-15% of calcium hydrophosphate. The tenofovir alafenamide fumarate tablet is prepared from the raw materials and auxiliary materials with a fluidized bed granulation method. The tenofovir alafenamide fumarate tablet prepared by steps of selecting the auxiliary materials and matching the optimized auxiliary material proportion with the fluidized bed granulation process is high in in-vitro dissolution rate, low in impurity content and good in stability, the safety of clinical application is improved, the tenofovir alafenamide fumarate tablet can be consistent with an original ground product in four dissolution media, besides, the preparation process is simple, and the tablet is suitable industrial production.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a tenofovir alafenamide fumarate tablet, a preparation method thereof and a detection method for related substances. Background technique [0002] Viral hepatitis B (hepatitis B) is caused by hepatitis B virus (HBV) infection, with fatigue, loss of appetite, nausea, vomiting, oily, hepatomegaly and abnormal liver function as the main clinical symptoms. It is a systemic infectious disease with high morbidity, strong infectivity, and serious harm to human health. At present, about 2 billion people in the world have been infected with hepatitis B virus, of which 350 million people have become chronic HBV carriers, and 1 million patients worldwide die of chronic hepatitis B-related diseases every year. Hepatitis B has become a serious threat to human health. Therefore, it is very important to develop a drug for the treatment of hepatitis B virus. [0003] Tenofo...

Claims

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Application Information

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IPC IPC(8): A61K9/28A61K31/675A61K47/38A61K47/36A61K47/26A61K47/02A61K47/12A61P1/16A61P31/20G01N30/02G01N30/16G01N30/30G01N30/32G01N30/34
CPCA61K9/2893A61K9/2054A61K9/2059A61K9/2018A61K9/2009A61K9/2013A61K31/675A61P1/16A61P31/20G01N30/02G01N30/16G01N30/30G01N30/32G01N30/34G01N2030/324Y02A50/30
Inventor 高彩杰刘建芬郭慧娟魏松波任风芝张向彬李丽红王彩肖
Owner NORTH CHINA PHARMA HUAKUN HEBEI BIOTECH
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