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Orlistat nano-microsphere as well as preparation method and application thereof in anti-tumor 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: 2017-12-01
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-microsphere as well as preparation method and application thereof in anti-tumor drugs
  • Orlistat nano-microsphere as well as preparation method and application thereof in anti-tumor drugs
  • Orlistat nano-microsphere as well as preparation method and application thereof in anti-tumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Example 1 Preparation of Orlistat Nanospheres

[0052] Take 40g mPEG separately 2000 -PCL 2000 (M.W: mPEG 2000, M.W: PCL 2000), mPEG 2000 -PCL 5000 , MPEG 5000 -PCL 5000 , MPEG 5000 -PCL 10000 , MPEG 2000 -PCL 10000 And mPEG 2000 -PCL 20000 Dissolved in 12 mL of a mixed solvent of acetone and dichloromethane (volume ratio 1:1) to prepare a drug-carrying material solution. Take 120g of orlistat and disperse it in 7 kinds of the above-mentioned drug-carrying 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 Sodium is fully soluble in water medium, and the mixed solution is added dropwise to 180 mL of carbon-containing fatty alcohol polyoxyethylene ether and sodium chloride aqueous solution under 600r / min mechanical stirring, thoroughly mixed, stirred for 4h, filtered, and vacuum freeze-dried.

[0053] The respectively obtained substances were observed un...

Embodiment 2

[0054] Example 2 Preparation of Orlistat Nanospheres

[0055] Take 100g mPEG 2000 -PCL 20000 Dissolve in 30mL acetone and dichloromethane (volume ratio 1:1) mixed solvent to prepare the drug-carrying material solution; take 33g orlistat and use a high-speed disperser (12000r / min, 1min) to disperse it on the carrier In the medicinal material solution, a mixed solution is obtained; 1.65g carbon fatty alcohol polyoxyethylene ether and 0.33g sodium chloride are fully dissolved in the aqueous solution, and the mixed solution is added dropwise to 450mL carbon-containing fatty alcohol polyoxyethylene under the condition of 600r / min mechanical stirring. In the aqueous solution of oxyethylene ether and sodium chloride, mix well, stir for 4 hours, filter, and freeze-dry in vacuum to obtain orlistat nanospheres.

Embodiment 3

[0056] Example 3 Preparation of Orlistat Nanospheres

[0057] Take 80g mPEG 2000 -PCL 10000 Dissolve it in a mixed solvent of 20 mL of acetone and dichloromethane (volume ratio 1:1.5) to prepare a drug-carrying material solution. Take 20 g of orlistat and disperse it on the carrier with a high-speed disperser (12000r / min, 1min). In the medicinal material solution, a mixed solution is obtained; 1.6g of carbon fatty alcohol polyoxyethylene ether and 1g of sodium chloride are fully dissolved in the aqueous solution, and the mixed solution is added dropwise to 200mL of carbon-containing fatty alcohol polyoxygen under the condition of 600r / min mechanical stirring. In the aqueous solution of vinyl ether and sodium chloride, mix well, stir for 4.5 hours, filter, and freeze-dry in vacuum 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 specifically relates to an orlistat nano-microsphere, a preparation method thereof, and an application in an anti-tumor medicine. Background technique [0002] Orlistat (Orlistat) chemical name: N-formyl-L-leucine (s)-1[(2s, 3s)3-hexyl-4oxy-2-epoxypropylmethyl] ten The diester, also called tetrahydrolipostatin (THL), is a semi-synthetic lipostatin derivative with the following structural formula: [0003] [0004] Orlistat is a new type of weight-loss and lipid-lowering drug that is currently internationally recognized. Its product name is Xenical. It was first listed in New Zealand in 1998 and its sales reached 146 million US dollars that year. Orlistat is a long-acting and potent specific gastrointestinal lipase inhibitor. It is a white or off-white powder at room temperature, insoluble in water, soluble in chloroform, and easily soluble in ethanol. It passes through the stomach and small int...

Claims

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Application Information

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Patent Type & Authority Applications(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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