Orlistat nano-microspheres, preparation method thereof and application in antitumor drugs

A technology of orlistat and nano-microspheres, applied in the field of biomedicine, can solve problems such as orlistat nano-microspheres that are not used for treatment and/or anti-tumor

Active Publication Date: 2018-08-07
ZEIN BIOTECHNOLOGY CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] All of the above are oral medications, and all of them use orlistat for weight loss and treatment of metabolic syndrome, and there are no reports about orlistat nanospheres used for treatment and / or anti-tumor

Method used

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  • Orlistat nano-microspheres, preparation method thereof and application in antitumor drugs
  • Orlistat nano-microspheres, preparation method thereof and application in antitumor drugs
  • Orlistat nano-microspheres, preparation method thereof and application in antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Embodiment 1 Preparation of orlistat nano-microspheres

[0052] Take 40g mPEG respectively 2000 -PCL 2000 (M.W: mPEG 2000, M.W: PCL 2000),

[0053] mPEG 2000 -PCL 5000 , mPEG 5000 -PCL 5000 , mPEG 5000 -PCL 10000 , mPEG 2000 -PCL 10000 and mPEG 2000 -PCL 20000 Dissolve in 12mL of a mixed solvent of acetone and dichloromethane (1:1 by volume) to prepare a drug-loaded material solution. Take 120g orlistat respectively and disperse it in 7 kinds of above-mentioned drug-loading material solutions with a high-speed disperser (12000r / min, 1min) to obtain a mixed solution; take 0.4g of carbon fatty alcohol polyoxyethylene ether and 0.08g of chlorinated The sodium is fully soluble in the water medium, and the mixed solution is added dropwise to 180mL carbon-containing fatty alcohol polyoxyethylene ether and sodium chloride aqueous solution under the condition of 600r / min mechanical stirring, fully mixed, stirred for 4 hours, filtered, and vacuum freeze-dried.

[00...

Embodiment 2

[0056] The preparation of embodiment 2 orlistat nano microspheres

[0057] Take 100g mPEG 2000 -PCL 20000 Dissolve in 30mL of acetone and dichloromethane (volume ratio: 1:1) mixed solvent to prepare drug-loaded material solution; take 33g orlistat and disperse it on the carrier with a high-speed disperser (12000r / min, 1min). In the medicinal material solution, a mixed solution was obtained; 1.65g of carbon fatty alcohol polyoxyethylene ether and 0.33g of sodium chloride were fully dissolved in the aqueous solution, and the mixed solution was added dropwise to 450mL of carbon-containing fatty alcohol polyoxyethylene ether under 600r / min mechanical stirring condition. In an aqueous solution of oxyethylene ether and sodium chloride, fully mix, stir for 4 hours, filter, and vacuum freeze-dry to obtain orlistat nanospheres.

Embodiment 3

[0058] Embodiment 3 Preparation of orlistat nano-microspheres

[0059] Take 80g mPEG 2000 -PCL 10000 Dissolve in 20mL of acetone and dichloromethane (volume ratio: 1:1.5) mixed solvent to prepare drug-loaded material solution, take 20g orlistat and disperse it on the carrier with a high-speed disperser (12000r / min, 1min). In the medicinal material solution, a mixed solution was obtained; 1.6 g of carbon fatty alcohol polyoxyethylene ether and 1 g of sodium chloride were fully dissolved in an aqueous solution, and the mixed solution was added dropwise to 200 mL of carbon fatty alcohol polyoxyethylene ether under 600 r / min mechanical stirring. In an aqueous solution of vinyl ether and sodium chloride, fully mix, stir for 4.5 hours, filter, and vacuum freeze-dry to obtain orlistat nanospheres.

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Abstract

The invention belongs to the technical field of bio-medicine, and in particular relates to an orlistat nano-microsphere as well as a preparation method and an application thereof in anti-tumor drugs. The orlistat nano-microsphere provided by the invention is prepared by mixing orlistat and a drug-carrying material, wherein the drug-carrying material is polyethylene glycol-polycaprolactone (mPEG-PCL); the mass ratio of the orlistat to the mPEG-PCL is at (1-2) to (3-10); and the molecular weight ratio of mPEG to PCL is at 2000 to 10000 or 2000 to 20000. The polymer nano-microsphere provided by the invention is prepared by loading the orlistat on the nano-material, so that a hydrophobic property of the nano-microsphere is changed; and through the sustained-release property of the microsphere, the microsphere can be used for preparing drugs for resisting tumor diseases; therefore, the nano-microsphere is huge in potential clinical value.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to an orlistat nano-microsphere, a preparation method thereof and an application in antitumor drugs. Background technique [0002] Orlistat (Orlistat) chemical name: N-formyl-L-leucine (s)-1 [(2s, 3s) 3-hexyl-4 oxy-2-epoxypropylmethyl] ten Diester, also known as tetrahydrolipstatin (THL), is a semi-synthetic lipstatin derivative with the following structural formula: [0003] [0004] Orlistat is currently internationally recognized as a new type of weight-loss and lipid-lowering drug. The product name on the market is Xenical. It was first launched in New Zealand in 1998, and the sales volume reached US$146 million that year. Orlistat is a long-acting and potent specific gastrointestinal lipase inhibitor, white or off-white powder at room temperature, insoluble in water, soluble in chloroform, easily soluble in ethanol, through the stomach and small intestine ca...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K47/34A61K47/10A61K47/02A61K31/365A61P35/00
CPCA61K9/5115A61K9/5146A61K9/5153A61K31/365
Inventor 邱宗荫肖玉梅李宏伟贺耘于国锋
Owner ZEIN BIOTECHNOLOGY CO LTD
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