HIV-1 integrase inhibitor phospholipid complex, preparation method and applications thereof

An integrase inhibitor, HIV-1 technology, applied in the direction of drug delivery, antiviral agent, pill delivery, etc., can solve the problems of clinical application and dosage form development restrictions, restrictions on oral absorption, etc., to improve in vivo absorption capacity, biological affinity Good performance, suitable for industrial scale-up production requirements

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

Benefits of technology

This patented new formulation called Phoslinum BP-40 was developed that contains certain substances found naturally occurring within it which prevent viruses from infecting their host cells through binding them with specific receptors located inside they's cell membranes. These agents are effective at slow down virus replication without causing damage to other organs such as kidneys. They also have strong bacterial adhesion properties making them ideal candidates for use in medical treatments where target tissues may be affected.

Problems solved by technology

This patents discuss how different types of agents called antivirals play their role during this pandemic period - specifically against certain parts of the Human Immunodefusion Complex Virus ("Human IF"). They were discovered through experiments conducted over several decades ago but did find them difficult to develop due to poor aquatic dissolution properties such as low bioavailability and difficulty in delivering these medications effectively throughout the entire life span.

Method used

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  • HIV-1 integrase inhibitor phospholipid complex, preparation method and applications thereof
  • HIV-1 integrase inhibitor phospholipid complex, preparation method and applications thereof
  • HIV-1 integrase inhibitor phospholipid complex, preparation method and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1: Preparation and thermal analysis of HIV-1 integrase inhibitor (HIV-A5) phospholipid complex.

[0022] Weigh 0.15g of HIV-A5 raw material, 0.56g of egg yolk lecithin, add 8mL of chloroform, and react at 40°C for 3 hours until clarification. The chloroform was evaporated to dryness by rotary evaporation under reduced pressure, and dried in vacuum for 24 hours to obtain 0.71 g of phospholipid complex. Seal the package and store in a refrigerator at 4°C. From the differential thermal analysis in Figure 1, it can be observed that Figure 1C The absorption peak of HIV-A5 still exists, indicating that HIV-A5 and phospholipids exist in the form of physical mixture. Figure 1D Compared with the peak of the mixture, the peak in the peak changes greatly, and the melting point peak of HIV-A5 disappears, indicating that HIV-A5 forms a complex with phospholipids.

Embodiment 2

[0023] Embodiment 2: Preparation of HIV-1 integrase inhibitor (HIV-A5) phospholipid complex

[0024] Weigh 0.15 g of HIV-A5 raw materials, 0.56 g of egg yolk lecithin, add 8 mL of dichloromethane, and react at 40°C for 0.5 hours until clarification. Dichloromethane was evaporated to dryness by rotary evaporation under reduced pressure, and vacuum-dried for 24 hours to obtain 0.71 g of phospholipid complex. Seal the package and store in a refrigerator at 4°C.

Embodiment 3

[0025] Embodiment 3: the preparation of HIV-1 integrase inhibitor (HIV-A5) phospholipid complex

[0026] Weigh 0.15g of HIV-A5 raw material, 0.56g of egg yolk lecithin, add 8mL of cyclohexane, and react at 60°C for 3 hours until clarification. The cyclohexane was evaporated to dryness by rotary evaporation under reduced pressure, and vacuum-dried for 24 hours to obtain 0.71 g of phospholipid complex. Seal the package and store in a refrigerator at 4°C.

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Abstract

The invention provides an HIV-1 integrase inhibitor phospholipid complex, a preparation method and applications thereof, wherein a mass ratio of the HIV-1 integrase inhibitor to the phospholipid is 1:1-20. According to the present invention, the complex formed by HIV-A5 and phospholipid can effectively improve the hydrophilicity and the lipophilicity of drugs, the phospholipid has good biologicalaffinity, the in vivo absorption capacity is improved, and the bioavailability is improved.

Description

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Claims

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Application Information

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Owner TIANJIN INT JOINT ACADEMY OF BIOTECH & MEDICINE
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