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Vinpocetine oral administration self-microemulsifying pellet as well as preparation method and application thereof

A vinpocetine, self-micro-emulsifying technology, applied in the directions of pill delivery, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., can solve slow absorption, long disintegration time, low bioavailability, etc. problems, to achieve the effect of increasing dissolution, improving clinical efficacy, and improving dissolution and absorption

Inactive Publication Date: 2010-02-17
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Because vinpocetine is almost insoluble in water, there are many vinpocetine tablets currently used clinically, but the preparation type is relatively traditional. Traditional preparations have long disintegration time, slow absorption, and low bioavailability, which affect the curative effect; How to overcome these shortcomings is that the rapid onset of the drug has become a subject of active research. Therefore, a new technical solution is sought to improve the solubility and dissolution rate of the drug, and eliminate the impact of food on the absorption and bioavailability of vinpocetine. Drugs can be better applied clinically is the direction that those skilled in the art are working hard to study

Method used

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  • Vinpocetine oral administration self-microemulsifying pellet as well as preparation method and application thereof
  • Vinpocetine oral administration self-microemulsifying pellet as well as preparation method and application thereof
  • Vinpocetine oral administration self-microemulsifying pellet as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Pill Core Prescription

[0035] Vinpocetine 0.5%

[0036] PEG-8-Glyceryl Caprylic Acid 10%

[0037] Ethylene glycol monoethyl ether 10%

[0038] Ethyl Oleate 25%

[0039] Microcrystalline Cellulose pH101 25%

[0040] Lactose 5%

[0041] Silica 20%

[0042]Sodium Chloride 4.5%

[0043] Preparation Process:

[0044] The fat-soluble drug is dissolved in the prescribed amount of oil phase, emulsifier, or co-emulsifier or its mixture, and then the rest of the prescribed amount of solvent is added, vortexed, and mixed uniformly to prepare drug-containing self-emulsifying oil. Mix absorbent and other auxiliary materials evenly, use self-emulsifying oil as a binder, make a soft material, prepare pellets by extrusion and spheronization, and pack them into capsules.

Embodiment 2

[0046] Pill Core Prescription

[0047] Vinpocetine 0.2%

[0048] Polyoxyethylene castor oil 15%

[0049] Propylene Glycol 50%

[0050] Olein Glycerides 10%

[0051] Sucrose 3%

[0052] Calcium Phosphate 20%

[0053] Mannitol 1.8%

[0054] Preparation Process:

[0055] The fat-soluble drug is dissolved in the prescribed amount of oil phase, emulsifier, or co-emulsifier or its mixture, and then the rest of the prescribed amount of solvent is added, vortexed, and mixed uniformly to prepare drug-containing self-emulsifying oil. Mix absorbent and other auxiliary materials evenly, use self-emulsifying oil as adhesive, make soft material, prepare pellets by extrusion and spheronization, and tablet.

Embodiment 3

[0057] Pill Core Prescription

[0058] Vinpocetine 0.5%

[0059] Polyoxyethylene Triglycerides 20%

[0060] Propylene carbonate 10%

[0061] soybean oil 10%

[0062] Starch 5%

[0063] Magnesium Oxide 50%

[0064] Sorbitol 4.5%

[0065] Preparation Process:

[0066] The fat-soluble drug is dissolved in the prescribed amount of oil phase, emulsifier, or co-emulsifier or its mixture, and then the rest of the prescribed amount of solvent is added, vortexed, and mixed uniformly to prepare drug-containing self-emulsifying oil. Mix absorbent and other auxiliary materials evenly, use self-emulsifying oil as a binder, make a soft material, prepare pellets by extrusion and spheronization, and pack them into capsules.

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Abstract

The invention relates to a vinpocetine oral administration self-microemulsifying pellet preparation. After being uniformly mixed, vinpocetine self-microemulsifying concentrated liquor and a common auxiliary material are made into a soft material and further made into a pellet, and an insoluble medicine in the prepared solid preparation can be rapidly dissolved till completion, wherein the vinpocetine self-microemulsifying concentrated liquor comprises the following components in percentage by volume in the preferable range: 1-10 percent of vinpocetine, 10-60 percent of oil phase, 10-70 percentof emulsifying agent and 0-50 percent of assistant emulsifying agent. The pellet prepared in the way can be used for further preparing a medicine release system with properties of slow release and controlled release. The prepared insoluble medicine pellet is rapidly dissolved and can lead about 100 percent of medicines to be released in an hour, and a method is safe and reproducible. The pellet can carry out self-microemulsifying in vivo to form micro-emulsion with the particle diameter of 10-100nm after oral administration, and the dissolution and the absorption of the vinpocetine in water are improved; and the bioavailability of the vinpocetine is improved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a vinpocetine oral self-microemulsification pellet and a preparation method thereof, and also relates to its application in preparing a preparation containing the pellet. Background technique [0002] Vinpocetine (Vinpocetine) is a derivative of indole alkaloid vincamine extracted from Apocynaceae plant Vinca minor. It is a brain circulation metabolism improving agent, which can improve the blood circulation of the brain and promote the energy metabolism of the brain. It has a good curative effect on the prevention and treatment of cerebral arteriosclerosis, sequelae of cerebral hemorrhage and hyperviscosity of hypertensive coronary heart disease, and can be used to improve brain function, enhance memory, improve mood, and improve aging auditory and visual abnormalities , Delay brain aging, long-term application safety and high tolerance. [0003] Because vinpo...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K9/20A61K9/48A61K31/4375A61K47/44A61K47/34A61K47/24A61K47/14A61P25/00A61P9/10A61P7/00
Inventor 潘卫三崔淑霞聂淑芳杨星钢关津张世忠
Owner SHENYANG PHARMA UNIVERSITY
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