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Vinpocetine solid liposome nano-particle and its preparation technology

A technology of solid lipid nanometer and vinpocetine, which is applied in liposome delivery, cardiovascular system diseases, nervous system diseases, etc., and can solve problems such as low absolute bioavailability and liver first-pass effect

Inactive Publication Date: 2006-08-30
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the strong metabolism of vinpocetine by liver cells in the human body, there is a serious first-pass effect in the liver, and the drug is mainly metabolized into apovincine, and the absolute bioavailability of oral absorption is extremely low, and the effect is non-selective

Method used

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  • Vinpocetine solid liposome nano-particle and its preparation technology
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  • Vinpocetine solid liposome nano-particle and its preparation technology

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Prescription: Vinpocetine 5mg

[0043] Phospholipids 100-300mg

[0044] Poloxamer-188 100-300mg

[0045] Glyceryl monostearate 150-400mg

[0046] Water 10-20mL

[0047] Preparation method: ①Dissolve vinpocetine in a hot solution containing glyceryl monostearate, stir evenly, add the aqueous solution containing phospholipids and poloxamer 188 dropwise into the oil phase under gentle stirring to make a microemulsion.

[0048] ②Under mild mechanical mixing conditions, the microemulsion is dispersed in a cold water phase medium (2-3° C.) to form a solid lipid nanoparticle suspension.

Embodiment 2

[0050] Prescription: Vinpocetine 5mg

[0051] Phospholipids 100-300mg

[0052] Polyoxyethylene hydrogenated castor oil 100-300mg

[0053] Glyceryl Tristearate 150-400mg

[0054] Water 10-20mL

[0055] Preparation method: ① Dissolve vinpocetine in a hot solution containing glyceryl tristearate, stir evenly, add the aqueous solution containing phospholipids and Cremophor RH 40 into the oil phase and mix well to form colostrum, then crush the cells machine ultrasound.

[0056] ②Through the homogenizer cycle and homogenize for 3-5 times, cool down to form a solid lipid nanoparticle suspension.

Embodiment 3

[0058] Prescription: Vinpocetine 5mg

[0059] Phospholipids 100-300mg

[0060] Tween-80 100-300mg

[0061] Glyceryl Behenate 150-400mg

[0062] Water 10-20mL

[0063] Preparation method: ① Dissolve vinpocetine in a hot solution containing glyceryl behenate, stir evenly, add the aqueous solution containing phospholipids and Tween-80 into the oil phase and fully mix it into colostrum, then pass through a cell pulverizer ultrasound.

[0064]②After cooling, the solid lipid nanoparticle suspension is formed.

[0065] ③ Add freeze-dried support agent (trehalose, mannitol, dextran, sorbitol, lactose, sucrose, etc.) to prepare freeze-dried powder injection.

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Abstract

A solid lipid nanoparticle of vinpocetin used for preparing orally taken medicine or injection for treating the circulatory disturbance type cerebrovascular diseases including cerebral infarction, sequelae of encephalorrhagia, cerebral arteriosclerosis, etc, improving cerebral function and delaying cerebral senility is prepared from xinpocetin, phosphatide, emulsifier and additive.

Description

technical field [0001] The invention relates to a medicinal compound vinpocetine, which has the function of improving cerebral circulation, and vinpocetine solid lipid nanoparticles prepared from the drug for oral or injection use and a preparation process thereof. Background technique [0002] Vinpocetine is a cerebral circulation metabolism improving agent developed by Gedeon Richter Company in Hungary in the 1970s. As the drug of choice for improving cerebral circulation, it is mainly used to treat various types of cerebral infarction, sequelae of cerebral hemorrhage and cerebral arteriosclerosis. It has a remarkable effect on circulatory disorders and cerebrovascular diseases, and can be used to improve brain function, enhance memory, improve mood, improve aging auditory and visual abnormalities, delay brain aging, and has high long-term application safety and tolerance. However, due to the strong metabolism of vinpocetine by liver cells in the human body, there is a ser...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/475A61K9/127A61K9/08A61K9/19A61P9/10A61P25/00
Inventor 罗轶凡陈大为
Owner SHENYANG PHARMA UNIVERSITY
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