Orlistat-contained nanoparticles as well as preparation method and application thereof

A technology of nano-microspheres and orlistat, applied in the field of medicine, can solve the problems of insufficient oral bioavailability for disease treatment, low growth inhibition rate of gastric cancer and liver cancer cells, etc., to improve oral bioavailability and inhibit tumor cells Effect of growth and inhibition of cancer cell growth

Active Publication Date: 2018-11-23
ZHONGSHAN WANHAN PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the oral bioavailability of the above two nanospheres containing orlistat cannot meet the needs of disease treatment, and the growth inhibition rate of gastric cancer and liver cancer cells is low

Method used

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  • Orlistat-contained nanoparticles as well as preparation method and application thereof
  • Orlistat-contained nanoparticles as well as preparation method and application thereof
  • Orlistat-contained nanoparticles as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0051] Preparation and Structure Confirmation of Copolymer

[0052] 1. Preparation of Copolymer 1a

[0053] (1) Reaction path:

[0054] When x=10, the present invention obtains the copolymer 1a through the following reaction pathway.

[0055]

[0056] (2) Preparation steps:

[0057] Step ①: Take 0.252g of compound 2a (1mmol), dissolve it in 5ml of dichloromethane, stir at -10°C for 5min, slowly add dropwise 5ml of dichloromethane solution containing 0.087ml of oxalyl chloride (1mmol), for 20min After the internal drop is completed, add another drop of N,N-dimethylformamide, and continue to stir for 2 hours at -10°C to obtain solution A; take another 0.063ml of aminoethanol (1.05mmol) and dissolve it in 5ml of dichloromethane , then add 0.276ml triethylamine (2mmol) dropwise therein, and stir evenly at -10°C to obtain solution B, slowly add solution A dropwise to solution B, and continue stirring at -10°C for 2h , the reaction solution was washed with 10% of 10% sodium ...

Embodiment 1

[0121] Example 1 Nanospheres comprising orlistat and copolymer 1a (m:n=76:24)

[0122] S1. Take the copolymer 1a with an m:n value of 76:24 and dissolve it in chloroform, prepare an oil phase matrix solution with a copolymer concentration of 125mg / ml, and then add the copolymer with a mass ratio of 1:5.5 Orlistat was stirred at a speed of 450rpm for 20min to make it evenly mixed to obtain solution A;

[0123] S2. Take Tween 80 and dissolve it in water, and prepare it into an aqueous solution with a mass concentration of surfactant of 2.75%, to obtain solution B;

[0124] S3. Add solution A obtained in step S1 dropwise to solution B obtained in step S2, so that the volume of solution B is 12 times that of solution A, stir at 1250rpm for 12h, then centrifuge at 10000rpm for 15min, disperse and centrifuge the precipitate with distilled water for 5 times and wash Net Tween 80, and finally freeze-dry the precipitate, that is.

Embodiment 2

[0125] Example 2 Nanospheres comprising orlistat and copolymer 1b (m:n=76:24)

[0126] The difference from Example 1 is that the copolymer in Example 2 is replaced by Copolymer 1b (m:n=76:24), and the remaining parameters and operations refer to Example 1.

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to orlistat-contained nanoparticles as well as a preparation method and application thereof. According to the orlistat-contained nanoparticles as well as the preparation method and application thereof, orlistat and a copolymer are mixed to prepare the nanoparticles, so that the nanoparticles can be dissolved in anaqueous solution so as to be prepared into an oral preparation or an injection, in addition, the defect that the oral bioavailability of the orlistat is low can be overcome, the bioavailability is improved to 75% or above, the inhibition rate on hepatocellular carcinoma BEL-7402 cell strains and gastric carcinoma BGC-823 cell strains can reach 20% or above, and the orlistat-contained nanoparticlescan be widely applied to cancer therapies.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a nano-microsphere containing orlistat, a preparation method and application thereof. Background technique [0002] Fatty acid synthase (FAS) is a key enzyme in fatty acid synthesis, which is in a state of low expression and low activity in normal cells, but in breast cancer, prostate cancer, melanoma, pancreatic cancer, retinoblastoma And other tumor tissues have a higher expression level, therefore, FAS is currently widely considered to be an ideal target for anti-tumor therapy. [0003] Orlistat is a lipase inhibitor weight-loss drug that was launched in Europe and the United States in the late 1990s and in China at the beginning of this century. It has the activity of a lipase inhibitor, so the anti-tumor effect of the drug has been to receive more and more attention. Chen Shaobo et al. (Chen Shaobo, Zhang Houde. Orlistat anti-tumor research progress [J]. Medic...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/32A61K31/365A61P35/00
CPCA61K9/5138A61K31/365A61P35/00
Inventor 向飞杜志博彭韪
Owner ZHONGSHAN WANHAN PHARM CO LTD
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