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Preparation method and application of nanoparticle microsphere for improving oral bioavailability of poorly soluble drugs

A technology of insoluble drugs and nanoparticles, applied in the field of medicine, can solve the problems of low oral bioavailability, large toxic and side effects, sudden release in the stomach, etc., and achieve the effects of improving oral bioavailability, taking medicines conveniently, and overcoming obstacles.

Active Publication Date: 2016-04-06
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] In view of the above situation, in order to overcome the defects of the prior art, the purpose of the present invention is to provide a preparation method and application of nanoparticle microspheres that improve the bioavailability of insoluble oral drugs, which can effectively solve the problem of low oral bioavailability of existing drugs. , low efficacy, high toxicity and side effects, stomach discomfort caused by sudden drug release

Method used

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  • Preparation method and application of nanoparticle microsphere for improving oral bioavailability of poorly soluble drugs
  • Preparation method and application of nanoparticle microsphere for improving oral bioavailability of poorly soluble drugs

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Embodiment 1

[0015] In the specific implementation of the present invention, the preparation method of nanoparticle microspheres is realized by the following steps:

[0016] (1) At 80°C, 500 mg of glyceryl monostearate and 100 mg of glyceryl behenate (ATO888) were mixed and melted as the oil phase;

[0017] (2) Dissolve 20mg of 2-ME, 100mg of polyethylene glycol 5000-polycaprolactone (PEG-PCL) in 2.5ml of absolute ethanol, heat to 80°C while stirring to dissolve evenly, and add to the oil phase , stir until the absolute ethanol is completely volatilized, forming an oil phase of an alcohol-free mixture;

[0018] (3), under magnetic stirring at 80°C and 900rpm, dissolve 400mg of soybean lecithin (PC-80, phosphatidylcholine content>80%, injection grade) and Tween 80200mg with water to make 10ml of water phase, and phase at 10ml·min -1 The dropping speed is dropped into the oil phase of the alcohol-free mixture. After the dropping is completed, continue to stir for 5 minutes to form colostru...

Embodiment 2

[0022] In the specific implementation of the present invention, the preparation method of nanoparticle microspheres can also be realized by the following steps:

[0023] (1) At 75°C, 400 mg of glyceryl monostearate and 120 mg of glyceryl behenate (ATO888) were mixed and melted as the oil phase;

[0024] (2) Dissolve 2-ME50mg, polyethylene glycol 5000-polycaprolactone 10000 (PEG-PCL) 160mg in 2ml of absolute ethanol, heat to 75°C while stirring to dissolve evenly, add to the oil phase, Stir until the absolute ethanol is completely volatilized, forming an oil phase of an alcohol-free mixture;

[0025] (3), under magnetic stirring at 75°C and 900rpm, dissolve 250 mg of soybean lecithin (PC-80, phosphatidylcholine content > 80%, injection grade) and Tween 80140 mg in water to make 8 ml of water phase, and phase at 10ml·min -1 The dropping rate is dropped into the oil phase of the alcohol-free mixture. After the dropping is completed, continue to stir for 4 minutes to form colost...

Embodiment 3

[0029] In the specific implementation of the present invention, the preparation method of nanoparticle microspheres can also be realized by the following steps:

[0030] (1) At 85°C, 600 mg of glyceryl monostearate and 200 mg of glyceryl behenate (ATO888) were mixed and melted as the oil phase;

[0031] (2) Dissolve 2-ME30mg, polyethylene glycol 5000-polycaprolactone 10000 (PEG-PCL) 200mg in 3ml of absolute ethanol, heat to 85°C while stirring to dissolve evenly, add to the oil phase, Stir until the absolute ethanol is completely volatilized, forming an oil phase of an alcohol-free mixture;

[0032] (3), under magnetic stirring at 85°C and 900rpm, dissolve 400 mg of soybean lecithin (PC-80, phosphatidylcholine content > 80%, injection grade) and Tween 80 to 300 mg in water to make 12 ml of water phase, and phase at 12ml·min -1 The dropping speed is dropped into the oil phase of the alcohol-free mixture. After the dropping is completed, continue to stir for 6 minutes to form ...

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Abstract

The invention relates to a preparation method and application of a nanoparticle microsphere for improving oral bioavailability of poorly soluble drugs, and the microsphere is capable of effectively solving the problems of existing drugs which have low oral bioavailability, poor efficacy, high toxic and side effects and discomfort in stomach due to the burst release of the drugs. The method comprises the following steps: mixing and melting glyceryl monostearate and glyceryl behenate, so that an oil phase is obtained; dissolving 2-ME and polyethylene glycol-polycaprolactone in absolute ethyl alcohol, and adding to the oil phase, so that a mixture oil phase is obtained; dissolving soybean lecithin and Tween-80 in water, so that an aqueous phase is obtained, dropping the aqueous phase to the mixture oil phase so as to obtain a primary emulsion, and filtering by virtue of a microfiltration membrane, so that a solid lipid nanoparticle suspension of the 2-ME is obtained; adding polyacrylic resin to a PBS solution, and adding hydroxypropyl methyl cellulose, so that a microsphere material solution is obtained; and stirring and uniformly mixing the microsphere material solution with the solid lipid nanoparticle suspension of the 2-ME, and spray-drying, so that the nanoparticle microsphere is obtained. According to the invention, the oral bioavailability of the drugs is improved and oral effective rate is increased.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a preparation method and application of nanoparticle microspheres for improving the oral bioavailability of poorly soluble drugs. Background technique [0002] Clinically, some insoluble drugs in water, such as most anticancer drugs, can only be treated by intravenous injection because of their low oral bioavailability. Intravenous administration requires frequent injections, the patient's compliance is poor, and the blood concentration fluctuates greatly, resulting in obvious toxic and side effects. Oral administration patients can self-medicate, and the patient compliance is high. The low bioavailability of these drugs after oral administration may be due to obvious hepatic first-pass effect, gastrointestinal instability or metabolism, intestinal absorption and efflux or absorption saturation and other obstacles. The current common preparations of these drugs (drugs are absorbed in th...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/565A61P35/00
CPCA61K9/0002A61K9/1652A61K31/565
Inventor 郭新红刘欣侯盼盼丁芳郭晓楠陈彩萍郭冀民李丹
Owner ZHENGZHOU UNIV
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