Anti-HIV compound preparation and preparation method and application thereof

A compound preparation and excipient technology, which is applied in the directions of antiviral agents, medical preparations without active ingredients, and medical preparations containing active ingredients, etc. Many problems, to achieve the effect of excellent activity, reducing drug resistance, and a wide range of safe doses

Active Publication Date: 2017-06-20
YANGZHOU AIDEA BIOTECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But existing above-mentioned preparation also has some defects, for example in Atripla (containing emtricitabine, tenofovir disoproxil fumarate, efavirenz) the consumption of efavirenz is many, and daily consumption has re...

Method used

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  • Anti-HIV compound preparation and preparation method and application thereof
  • Anti-HIV compound preparation and preparation method and application thereof
  • Anti-HIV compound preparation and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Table 1 Example 1 prescription component table

[0053]

[0054] The preparation steps are as follows:

[0055] (1) Preparation of tenofovir disoproxil fumarate (TDF) granules: weigh tenofovir disoproxil fumarate and excipient II according to the above formula ratio, pass through a 20-mesh sieve and mix evenly, add the above raw and auxiliary materials 20-60% of the total weight of water is used for wet granulation, and then air blast or fluidized bed drying is used until the moisture content of the granules is less than 5%, and the granules are passed through a 10-mesh sieve to obtain tenofovir disoproxil fumarate granules;

[0056] (2) Preparation of ACC007 granules: Weigh ACC007 and excipient III according to the above formula ratio, pass through a 20-mesh sieve and mix evenly, add 20-60% of the total weight of the above raw and auxiliary materials for wet granulation, and then use air blast Or fluidized bed drying until the moisture content of the granules is le...

Embodiment 2

[0061] Table 2 embodiment 2 prescription component list

[0062]

[0063] The preparation steps are as follows:

[0064] (1) Preparation of tenofovir disoproxil fumarate (TDF) granules: weigh tenofovir disoproxil fumarate and excipient II according to the above formula ratio, pass through a 100-mesh sieve and mix evenly, add the above raw and auxiliary materials 20-60% of the total weight of water is used for wet granulation, and then air blast or fluidized bed drying is used until the moisture content of the granules is less than 4%, and the granules are passed through a 40-mesh sieve to obtain tenofovir disoproxil fumarate granules;

[0065] (2) Preparation of ACC007 granules: Weigh ACC007 and excipient III according to the above formula ratio, pass through a 100-mesh sieve and mix evenly, add 20-60% of the total weight of the above raw and auxiliary materials for wet granulation, and then use air blast Or fluidized bed drying until the moisture content of the granules i...

Embodiment 3

[0069] Table 3 Example 3 prescription component table

[0070]

[0071] The preparation steps are as follows:

[0072] (1) Preparation of tenofovir disoproxil fumarate (TDF) granules: weigh tenofovir disoproxil fumarate and excipient II according to the above formula ratio, pass through a 50-mesh sieve and mix evenly, add the above raw and auxiliary materials 20-60% of the total weight of water is used for wet granulation, and then air blast or fluidized bed drying is used until the moisture content of the granules is less than 3%, and the granules are passed through a 20-mesh sieve to obtain tenofovir disoproxil fumarate granules;

[0073] (2) Preparation of ACC007 granules: Weigh ACC007 and excipient III according to the above formula ratio, pass through a 50-mesh sieve and mix evenly, add 20-60% of the total weight of the above raw and auxiliary materials for wet granulation, and then use air blast Or fluidized bed drying until the moisture content of the granules is le...

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Abstract

The invention discloses anti-HIV compound preparation. The anti-HIV compound preparation is prepared from the following ingredients in weight percentage: 10 to 35% of lamivudine, 10 to 35% of fumaric acid tenofovir ester, 5 to 20% of 3-((3-ethyl-2,6-dioxo-5-(propyl-2-radical)-1,2,3,6-tetrahydropyrimidine-4-radical)carbonyl)-5-tolunitrile and 10 to 75% of excipient. The anti-HIV compound preparation disclosed by the invention is single-layer tablet or double-layer tablet; in preparation, the fumaric acid tenofovir ester and compound of the 3-((3-ethyl-2,6-dioxo-5-(propyl-2-radical)-1,2,3,6-tetrahydropyrimidine-4-radical)carbonyl)-5-tolunitrile are independently pelletized and then totally mixed and compressed into tablets. The anti-HIV compound preparation disclosed by the invention has the advantages of good stability, a simple preparation technology and controllable quality, can restrain HIV virus from different targets, improves a treating effect of single drug use to AIDS, avoids side effects on a nervous system and has small toxicity and a wide safety dosage range.

Description

technical field [0001] The invention belongs to compound preparations, in particular to a combined preparation (triple compound) containing compounds with antiviral activity (more specifically anti-HIV properties), its preparation method and application. Background technique [0002] Acquired Immunodeficiency Syndrome (Human Acquired Immunodeficiency Syndrome, AIDS), referred to as AIDS, is a systemic infectious disease caused by human immunodeficiency virus (human immunodeficiency virus, HIV). Since the first HIV infection was discovered in the United States in 1981, more than 34 million people have died so far. According to statistics from the World Health Organization (WHO) and the United Nations Program on AIDS (UNAIDS), by the end of 2014, an estimated 36.9 million people worldwide were living with HIV, with an estimated 2 million new infections and 1.2 million deaths in 2014. According to statistics from the Chinese Center for Disease Control and Prevention (CDC), by ...

Claims

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Application Information

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IPC IPC(8): A61K9/36A61K47/20A61K31/513A61K31/675A61P31/18
CPCA61K9/2013A61K9/2077A61K9/2086A61K9/2095A61K9/2866A61K31/513A61K31/675A61K2300/00
Inventor 沈小宁傅和亮李文全胡雄林孙建华吴蓉蓉袁玉刘三侠陈希颜
Owner YANGZHOU AIDEA BIOTECH
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