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Application of nanoparticle containing orlistat in preparing anti-hepatitis B virus medicine

A technology of orlistat and nano-microspheres, applied in the field of medicine, can solve problems such as low solubility of orlistat, inability to be administered orally, and no disclosure of nano-microsphere anti-hepatitis B virus drug technology teachings, etc.

Active Publication Date: 2018-09-14
ZHONGSHAN WANHAN PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The development of orlistat as an anti-HBV drug faces the following two limiting problems: ① The bioavailability of orlistat in conventional oral preparations is extremely low (<2%), making it impossible to use oral administration for the treatment of HBV; Treatment; ② The solubility of orlistat in water is extremely low (<0.001g / 100mL), making it impossible to make liquid preparations for the treatment of HBV by injection
[0007] The prior art does not disclose the technical teaching that nano-microspheres containing orlistat can be used to prepare anti-hepatitis B virus drugs

Method used

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  • Application of nanoparticle containing orlistat in preparing anti-hepatitis B virus medicine
  • Application of nanoparticle containing orlistat in preparing anti-hepatitis B virus medicine
  • Application of nanoparticle containing orlistat in preparing anti-hepatitis B virus medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] Example 1 Preparation and Structure Confirmation of Vitamin A Methacrylate (Compound 3a)

[0064]

[0065] Preparation: Take 28.65g vitamin A (0.100mol), put it in a 500mL three-necked flask, add petroleum ether to it under stirring, until vitamin A is completely dissolved, then add 5mg DCC (N,N'-dicyclohexyldi imine), and then add 13.21g of methacrylic acid (Compound 2, 0.15mol) in saturated petroleum ether solution, slowly raise the temperature to 50°C under stirring for reaction, and use high performance liquid chromatography to track the reaction to the end. Petroleum ether was distilled off under reduced pressure, and the resulting solid was washed with water and freeze-dried to obtain 31.55 g (0.089 mol) of a light yellow solid with a melting point of 51-52° C. and a yield of 89%.

[0066] Structural Confirmation:

[0067] Compound 2: 1 H-NMR (CDCl 3 ) δ (ppm): 6.69 (1H, s), 6.55 (1H, s), 2.03 (3H, s).

[0068] Vitamin A: 1 H-NMR (CDCl 3 )δ (ppm): 6.55 (1...

Embodiment 2

[0070] Example 2 Preparation and Structure Confirmation of Vitamin E Methacrylate (Compound 3b)

[0071]

[0072] Preparation: Take 43.72g of vitamin E (0.100mol), put it in a 500mL three-necked flask, add ether to it under stirring until the vitamin E is completely dissolved, then add 5mg of DMAP (4-dimethylaminopyridine) to it, and then add 13.23 g of methacrylic acid (compound 2, 0.16 mol) in saturated ether solution was slowly raised to 50° C. for reaction under stirring, and the reaction was tracked to the end point by high performance liquid chromatography. Ethyl ether was distilled off under reduced pressure, and the resulting solid was washed with water and then freeze-dried to obtain 45.39 g (0.091 mol) of off-white solid with a melting point of 42-43°C and a yield of 91%.

[0073] Structural Confirmation:

[0074] Compound 2: 1 H-NMR (CDCl 3 ) δ (ppm): 6.69 (1H, s), 6.55 (1H, s), 2.03 (3H, s).

[0075] Vitamin E: 1 H-NMR (CDCl 3 )δ(ppm): 2.74(2H, t), 2.12(3H...

Embodiment 3

[0077] Example 3 Vitamin D 2 Preparation and Structure Confirmation of Methacrylate (Compound 3c)

[0078]

[0079] Preparation: Take 36.69g vitamin D 2 (0.101mol), placed in a 500mL three-necked flask, added diethyl ether therein under stirring until the vitamin E was completely dissolved, then added 5mg DMAP (4-dimethylaminopyridine), and then added 13.22g methacrylic acid (compound 2, 0.15mol) of saturated ether solution, the temperature was slowly raised to 50°C under stirring for reaction, and the reaction was tracked to the end using high performance liquid chromatography. Ethyl ether was distilled off under reduced pressure, and the resulting solid was washed with water and then freeze-dried to obtain 44.15 g (0.095 mol) of off-white solid with a melting point of 85-87° C. and a yield of 95%.

[0080] Structural Confirmation:

[0081] Compound 2: 1H-NMR (CDCl 3 ) δ (ppm): 6.69 (1H, s), 6.55 (1H, s), 2.03 (3H, s).

[0082] Vitamin D 2 : 1 H-NMR (CDCl 3 )δ (pp...

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Abstract

The invention relates to the technical field of medicines, in particular to application of a nanoparticle containing orlistat in preparing an anti-hepatitis B virus (HBV) medicine. The nanoparticle isprepared from the orlistat and a copolymer chosen from a vitamin A methacrylate-2-methacryloyloxyethyl phosphorylcholine copolymer or a vitamin E methacrylate-2-methacryloyloxyethyl phosphorylcholinecopolymer or a vitamin D2 methacrylate-2-methacryloyloxyethyl phosphorylcholine copolymer. The encapsulation efficiency of the nanoparticle is 82.67-93.83%; animal test shows that after oral administration of the nanoparticle, the blood drug concentration is higher, and the sustained-release effect is good; an in-vitro test result shows that the inhibition ratio of extracellular HBV DNA replication is used as an index, and the activity of the nanoparticle for resisting HBV infection is significantly higher than those of the orlistat and a contrast nanoparticle prepared by adopting PMB30W as acarrier.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the use of nanometer microspheres containing orlistat in the preparation of anti-hepatitis B virus drugs. Background technique [0002] Hepatitis B is a potentially fatal liver infectious disease caused by hepatitis B virus (HBV), which can increase the risk of death from liver cirrhosis and liver cancer. According to the World Health Organization (WHO), about 25.7 million people worldwide are infected with HBV, and a total of 887,000 people died of HBV in 2015, most of them died of HBV-induced diseases including liver cirrhosis and hepatocellular carcinoma. Therefore, HBV is a public health challenge faced by countries all over the world. The study by Esser K et al. (Antiviral Res. 2018Jan 5; 151:4-7.) found that lipase inhibitor weight loss drug orlistat (orlistat) can prevent HBV viral life cycle by acting on the early stage infect host cells, [0003] The development of o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K47/32A61K31/365A61P1/16A61P31/20
CPCA61K9/5026A61K31/365A61P1/16A61P31/20
Inventor 向飞杜志博彭韪
Owner ZHONGSHAN WANHAN PHARM CO LTD
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