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HIV-1 (human immunodeficiency virus-1) integrase inhibitor tablet and preparation method thereof

An integrase inhibitor, HIV-1 technology, applied in pill delivery, antiviral agents, pharmaceutical formulations, etc., to achieve the effects of simple preparation process, high dissolution rate, and portability

Inactive Publication Date: 2017-08-11
TIANJIN INT JOINT ACADEMY OF BIOTECH & MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

HIV-1 integrase inhibitor HIV-A5 bulk drug is insoluble in water, and there is still no suitable HIV-A5 preparation in the report

Method used

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  • HIV-1 (human immunodeficiency virus-1) integrase inhibitor tablet and preparation method thereof
  • HIV-1 (human immunodeficiency virus-1) integrase inhibitor tablet and preparation method thereof
  • HIV-1 (human immunodeficiency virus-1) integrase inhibitor tablet and preparation method thereof

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preparation example Construction

[0023] The preparation method for preparing HIV-1 integrase inhibitor tablet provided by the invention comprises the following steps:

[0024] First, HIV-1 integrase inhibitor HIV-A5 is mixed with pharmaceutically acceptable auxiliary materials to obtain a drug mixture. In this step, the HIV-1 integrase inhibitor HIV-A5 and pharmaceutically acceptable auxiliary materials are first dried and sieved (usually 50-80 mesh, 60 mesh is used below), and then mixed , wherein the auxiliary material is a combination of one or more of fillers, disintegrants, binders and lubricants, therefore, preferably, by weight, 25 to 500 parts of HIV-1 integrase inhibitor HIV-A5, 50-600 parts of filler, 6-30 parts of disintegrating agent, 5-20 parts of binder and 1-6 parts of lubricant are mixed to obtain the drug mixture.

[0025] Wherein, the chemical formula of HIV-1 integrase inhibitor HIV-A5 is:

[0026] wherein, Bz represents a benzoyl group.

[0027] Wherein, the filler is a combination of...

Embodiment 1

[0034] Embodiment 1: the preparation of HIV-1 integrase inhibitor (HIV-A5) tablet

[0035]Sieve the HIV-1 integrase inhibitor and pharmaceutically acceptable excipients separately, weigh 300g of lactose, 10g of low-substituted hydroxypropyl cellulose, 10g of hydroxypropyl cellulose, 5g of magnesium stearate, mix, and then add 550 g of HIV-1 integrase inhibitor HIV-A were mixed; the above drug mixture was compressed into tablets, and the hardness of the HIV-1 integrase inhibitor tablet was controlled at 50N to obtain HIV-1 integrase inhibitor tablet. The HIV-1 integrase inhibitor tablet is packaged and labeled with polyoxyethylene blister + double-sided composite aluminum film bag.

Embodiment 2

[0036] Embodiment 2: the preparation of HIV-1 integrase inhibitor (HIV-A5) tablet

[0037] Sieve the HIV-1 integrase inhibitor and pharmaceutically acceptable auxiliary materials separately, weigh 150g of lactose, 150g of pregelatinized starch, 12g of crospovidone, 6g of hydroxypropyl cellulose, 5g of magnesium stearate, Mix, then add HIV-1 integrase inhibitor HIV-A5 50g and mix; The above drug mixture is compressed into tablets, and the hardness of the HIV-1 integrase inhibitor tablet is controlled at 60N to obtain HIV-1 integrase inhibitor tablet agent. The HIV-1 integrase inhibitor tablet is packaged and labeled with polyoxyethylene blister + double-sided composite aluminum film bag.

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Abstract

The invention provides an HIV-1 (human immunodeficiency virus-1) integrase inhibitor tablet and a preparation method thereof. The preparation method includes the steps: mixing an HIV-1 integrase inhibitor HIV-A5 with pharmaceutically acceptable auxiliary materials; pressing the materials to prepare the HIV-1 integrase inhibitor tablet. The method is simple in preparation process, mechanical in production, high in automation degree, large in output and low in cost, and the prepared HIV-1 integrase inhibitor tablet is high in dissolubility, short in disintegration time, stable in quality and convenient to carry, transport and store and is a solid preparation.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to an HIV-1 integrase inhibitor tablet and a preparation method thereof. Background technique [0002] AIDS (acquired immunodeficiency syndrome, referred to as AIDS) has developed into a global disease since it was first diagnosed in the United States in 1981. So far, AIDS has become one of the most important epidemic diseases in the world. According to the latest statistics from UNAIDS, there are 35.3 million people living with AIDS worldwide, and 1.6 million people died of AIDS-related diseases in 2012. In 1983, Montgnier Bare-Sinoussi and others confirmed that the pathogen of AIDS is human immunodeficiency virus (human immunodeficiency virus, referred to as HIV), by killing or destroying the human immune system, a series of opportunistic infections and tumors are concurrent, and severe cases can lead to die. The replication cycle of HIV is divided into adsorption, penetration, uncoatin...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K47/38A61K47/36A61K47/26A61K31/506A61P31/18
CPCA61K9/2018A61K9/2054A61K9/2059A61K31/506
Inventor 饶子和杨诚郭宇马海秋蔡岩汪颖王淑艳李玉彩张玉普左臣强张金敏
Owner TIANJIN INT JOINT ACADEMY OF BIOTECH & MEDICINE
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