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Orlistat inclusion compound and preparation method and application thereof in antineoplastic medicines

A technology of orlistat and cyclodextrin inclusion compound is applied to orlistat sulfobutyl ether-β-cyclodextrin inclusion compound and preparation thereof, and the application field of antitumor drugs can solve the problem of For the treatment and/or anti-tumor orlistat inclusion complex and other problems, to achieve the effects of good medicinal value, improved bioavailability, and good biosafety

Active Publication Date: 2017-07-14
CHONGQING ZEN PHARMACEUTICAL 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 inclusion compounds used for treatment and / or anti-tumor

Method used

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  • Orlistat inclusion compound and preparation method and application thereof in antineoplastic medicines
  • Orlistat inclusion compound and preparation method and application thereof in antineoplastic medicines
  • Orlistat inclusion compound and preparation method and application thereof in antineoplastic medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1 Preparation of orlistat sulfobutyl ether-β-cyclodextrin inclusion compound

[0044] Preparation of orlistat sulfobutyl ether-β-cyclodextrin inclusion compound by grinding method comprises the following steps:

[0045] Take 10g of sulfobutyl ether-β-cyclodextrin, add it into 30mL of water medium, and grind it evenly; take 0.8g of orlistat and dissolve it in 2.4mL of ethanol to obtain an ethanol solution of orlistat; His ethanol solution is slowly added to the well-ground sulfobutyl ether-β-cyclodextrin, fully ground and then dried to obtain orlistat sulfobutyl ether-β-cyclodextrin inclusion compound.

Embodiment 2

[0046] Example 2 Preparation of orlistat sulfobutyl ether-β-cyclodextrin inclusion compound

[0047] Ultrasonic method prepares orlistat sulfobutyl ether-β-cyclodextrin inclusion compound, comprises the following steps:

[0048] Dissolve 25g of sulfobutyl ether-β-cyclodextrin in water medium to make a saturated solution; dissolve 1g of orlistat in acetone, slowly add it to the saturated solution of sulfobutyl ether-β-cyclodextrin, mix well After homogenization, ultrasonic treatment was performed for 6 hours, filtered, washed and dried to obtain orlistat sulfobutyl ether-β-cyclodextrin inclusion compound.

Embodiment 3

[0057] Example 3 Preparation of orlistat sulfobutyl ether-β-cyclodextrin inclusion compound

[0058] Preparation of orlistat sulfobutyl ether-β-cyclodextrin inclusion compound by grinding method comprises the following steps:

[0059] Take 10g of sulfobutyl ether-β-cyclodextrin, add it to 30mL of water medium, and grind it evenly; take 5g of orlistat and dissolve it in 15mL of ethanol to obtain an ethanol solution of orlistat; The ethanol solution is slowly added to the well-ground sulfobutyl ether-β-cyclodextrin, thoroughly ground and then dried to obtain the orlistat sulfobutyl ether-β-cyclodextrin inclusion compound.

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Abstract

The invention belongs to the technical field of biological medicines, and particularly relates to an Orlistat inclusion compound and a preparation method and application thereof in antineoplastic medicines. The Orlistat inclusion compound disclosed by the invention is an Orlistat-sulfobutylether-beta-cyclodextrin inclusion compound, and the weight ratio of Orlistat to sulfobutylether-beta-cyclodextrin is 1:1-1:25. The invention prepares Orlistat into the inclusion compound, and sulfobutylether-beta-cyclodextrin can increase the solubility of Orlistat, enhance the stability of a medicine, promote medicine absorption and reduce the stimulation of the medicine to the body; as a carrier for Orlistat, sulfobutylether-beta-cyclodextrin can greatly improve the water solubility of guest molecules, so that Orlistat can be adapted to the requirement of liquid preparation and the bioavailability of Orlistat can be increased, and thereby the medicinal value of Orlistat can be better exerted; and the Orlistat inclusion compound can be used in the preparation of antineoplastic medicines, and has great potential clinical value.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to an orlistat sulfobutyl ether-β-cyclodextrin inclusion compound, 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 ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K31/365A61P35/00
CPCA61K31/365
Inventor 邱宗荫肖玉梅李宏伟贺耘于国锋
Owner CHONGQING ZEN PHARMACEUTICAL CO LTD
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