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Orlistat liposome and its preparation method and application in antitumor drugs

An orlistat and liposome technology, applied in the field of biomedicine, can solve problems such as orlistat liposomes that are not used for treatment and/or anti-tumor, achieve good medicinal value, increase solubility, reduce stimulating effect

Active Publication Date: 2018-08-21
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 related reports about orlistat liposomes for treatment and / or anti-tumor

Method used

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  • Orlistat liposome and its preparation method and application in antitumor drugs
  • Orlistat liposome and its preparation method and application in antitumor drugs
  • Orlistat liposome and its preparation method and application in antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Weigh soybean lecithin 25mg, distearoylphosphatidylcholine 5mg, mPEG 2000 - 2.5mg of DPPE, 6mg of cholesterol and 4mg of orlistat were uniformly mixed; adding 15ml of absolute ethanol and stirring to dissolve, ultrasonication for 2min to mix evenly, slowly inject the obtained solution into 20ml of PBS buffer, stir at 60°C, The ethanol was removed by pressure, an appropriate amount of PBS was added, and the orlistat liposome L1 was obtained by repeatedly extruding through a 200 nm membrane with a liposome extruder.

Embodiment 2

[0034] Weigh soybean lecithin 24mg, distearoylphosphatidylcholine 4mg, mPEG 2000 - 2mg of DPPE, 7mg of cholesterol and 4mg of orlistat are uniformly mixed; add 12ml of absolute ethanol and stir to dissolve, ultrasonication for 2min to mix evenly, slowly inject the obtained solution into 18ml of PBS buffer, stir at 60°C, and depressurize The ethanol was removed, and an appropriate amount of PBS was added, and the orlistat liposome L2 was obtained by repeatedly extruding through a 200 nm membrane with a liposome extruder.

Embodiment 3

[0036] Weigh soybean lecithin 24mg, distearoylphosphatidylcholine 6mg, mPEG 2000 - 2 mg of DPPE, 5 mg of cholesterol and 5 mg of orlistat are uniformly mixed; add 12 ml of absolute ethanol and stir to dissolve, ultrasonically mix for 2 minutes, slowly inject the obtained solution into 18 ml of PBS buffer, stir at 60°C, and depressurize The ethanol was removed, and an appropriate amount of PBS was added, and the orlistat liposome L3 was obtained by repeatedly extruding through a 200 nm membrane with a liposome extruder.

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Abstract

The invention belongs to the technical field of biomedicines and particularly relates to an orlistat liposome as well as a preparation method and application thereof to an anti-tumor drug. The orlistat liposome provided by the invention comprises orlistat, phospholipid, cholesterol and mPEG200-DPPE; the phospholipid is selected from soybean lecithin and distearyl phosphatidylcholine. According to the preparation method provided by the invention, the orlistat is prepared into the liposome, so that the solubility of the orlistat is increased, the stability of the drug is improved, the drug absorption is promoted, and the stimulation of the drug to a body is reduced; as an orlistat carrier, the orlistat liposome can greatly improve the water solubility of a guest molecule, so that the guest molecule adapts to the requirements for a liquid preparation, the bioavailability of the orlistat is improved, and the medicinal value of the orlistat is better played. The orlistat liposome provided by the invention has good stability, can smoothly enter a tumor cell to play an anti-tumor role and can be used in the preparation of the drug for anti-tumor diseases, thereby having great potential clinical value.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to an orlistat liposome, 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 cavity Th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/365A61K47/24A61P35/00
CPCA61K9/0019A61K9/127A61K31/365A61K47/24
Inventor 邱宗荫肖玉梅李宏伟贺耘于国锋
Owner ZEIN BIOTECHNOLOGY CO LTD
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