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

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

Examples

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Example Embodiment

[0014] Example 1

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

[0016] (1) Mix and melt 500 mg of glyceryl monostearate and 100 mg of glyceryl behenate (ATO888) at 80°C as the oil phase;

[0017] (2). Dissolve 2-ME20mg, polyethylene glycol 5000-polycaprolactone 10000 (PEG-PCL) 100mg in 2.5ml of absolute ethanol, stir and heat to 80℃ to dissolve evenly, add to the oil phase , Stir until the absolute ethanol is completely volatilized to form an alcohol-free mixture oil phase;

[0018] (3) Under 80℃, 900rpm magnetic stirring, soy lecithin (PC-80, phosphatidylcholine content> 80%, injection grade) 400mg, Tween 80200mg dissolved in water to make 10ml water phase, the water phase 10ml·min -1 Drop into the oil phase of the alcohol-free mixture at the rate of dropping, continue to stir for 5 minutes to form colostrum, shear the colostrum at a shear rate of 10000 rpm for 3 minutes, and...

Example Embodiment

[0021] Example 2

[0022] In the specific implementation of the present invention, the preparation method of nano-particle 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 an oil phase;

[0024] (2). Dissolve 2-ME50mg, polyethylene glycol 5000-polycaprolactone 10000 (PEG-PCL) 160mg in 2ml of absolute ethanol, stir and heat to 75℃ to dissolve evenly, then add to the oil phase, Stir until the absolute ethanol is completely volatilized to form an alcohol-free mixture oil phase;

[0025] (3), under 75℃, 900rpm magnetic stirring, soy lecithin (PC-80, phosphatidylcholine content> 80%, injection grade) 250mg, Tween 80140mg dissolved in water to make 8ml water phase, the water phase is 10ml·min -1 Drop into the non-alcoholic mixture oil phase at the rate of drop, continue stirring for 4 minutes to form colostrum, shear the colostrum at a shear speed of 9000 rpm for ...

Example Embodiment

[0028] Example 3

[0029] In the specific implementation of the present invention, the preparation method of nano-particle 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 an oil phase;

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

[0032] (3) Under 85℃, 900rpm magnetic stirring, soy lecithin (PC-80, phosphatidylcholine content> 80%, injection grade) 400mg, Tween 80300mg dissolved in water to make 12ml of water phase, the water phase is 12ml·min -1 Drop into the oil phase of the alcohol-free mixture at the rate of dropping. After the addition is complete, continue to stir for 6 minutes to form colostrum. The colostrum...

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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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