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HIV-1 integrase inhibitor solution agent, preparation process and applications thereof

An integrase inhibitor, HIV-1 technology, applied in antiviral agents, pharmaceutical formulations, medical preparations with non-active ingredients, etc., can solve the problems of limiting oral absorption, clinical application and dosage form development, and achieve exposure Low, improved bioavailability, easy preparation

Inactive Publication Date: 2018-08-24
TIANJIN INT JOINT ACADEMY OF BIOTECH & MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, HIV-A5 is a water-insoluble compound, and its water solubility limits its oral absorption, which limits its clinical application and formulation development.

Method used

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  • HIV-1 integrase inhibitor solution agent, preparation process and applications thereof
  • HIV-1 integrase inhibitor solution agent, preparation process and applications thereof
  • HIV-1 integrase inhibitor solution agent, preparation process and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Embodiment 1: the preparation of HIV-1 integrase inhibitor (HIV-A5) solution

[0018] Weigh 0.10g HIV-A5 raw material, add 15mL propylene glycol, stir to dissolve; continue to add 15mL ethanol, 8mL Tween 80, 8mL glycerin and 15mL Poloxamer 188 and continue to stir until completely dissolved; add distilled water to 100mL, add to the above solution Slowly add 0.02g of β-carotene and 0.02g of sorbitol and stir until completely dissolved; subpackage and label.

Embodiment 2

[0019] Embodiment 2: the preparation of HIV-1 integrase inhibitor (HIV-A5) solution

[0020] Weigh 0.10g HIV-A5 raw material, add 15mL ethanol, stir to dissolve; continue to add 10mL propylene glycol, 3mL Tween 80, 8mL glycerin and 10mL Poloxamer 188 and continue to stir until completely dissolved; add distilled water to 100mL, add to the above solution Slowly add 0.02g of β-carotene and 0.02g of sorbitol and stir until completely dissolved; subpackage and label.

Embodiment 3

[0021] Embodiment 3: the preparation of HIV-1 integrase inhibitor (HIV-A5) solution

[0022] Weigh 0.10g of HIV-A5 raw material, add 35mL of ethanol, stir to dissolve; continue to add 10mL of glycerin, 30mL of poloxamer 188 continue to stir until completely dissolved; add distilled water to 100mL, slowly add 0.06g of β-carotene and Stir 0.1g of mannitol until completely dissolved; subpackage and label.

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Abstract

The invention provides an HIV-1 integrase inhibitor solution agent, a preparation process and applications thereof, wherein the HIV-1 integrase inhibitor HIV-A5 solution agent comprises: HIV-A5, wherein the mass concentration (g / ml) of the HIV-A5 in the solution agent is 0.3-5%; a solvent, wherein the solvent comprises at least one selected from 10-50% of ethanol, 5-15% of propylene glycol and 1-10% of glycerol and at least one selected from 1-10% of Tween 80 and 10-35% of Poloxamer 188; and optionally a coloring agent and a flavoring agent, wherein the mass concentrations (g / ml) of the coloring agent and the flavoring agent in the solution agent respectively are 0.01-0.09% and 0.01-0.1%. According to the present invention, the preparation process is simple; the drug is uniformly dispersedin the form of small molecules in the solvent, and is quickly absorbed by the body after the drug enters the body so as to quickly enter the tissue, the in vivo absorption capacity is improved, the bioavailability is high, the drug can be taken orally, and the medication is convenient.

Description

technical field [0001] The invention relates to a pharmaceutical preparation of an HIV-1 integrase inhibitor, more specifically, a solution of HIV-A5 as an HIV-1 integrase inhibitor 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 occur, and severe cases can lead to death. . The replication cycle of ...

Claims

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Application Information

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IPC IPC(8): A61K31/506A61K9/08A61K47/10A61K47/26A61P31/18
CPCA61K47/10A61K47/26A61K9/08A61K31/506
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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