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Vincamine sustained-release pellet preparation and preparation method thereof

A technology of slow-release pellets and vincamine, which is applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, and devices that make drugs into special physical or taking forms, and can solve the problems of intestinal absorption and drug utilization. Not high, unfavorable for the release of O'Brien, etc., to achieve the effect of solving pH value dependence, convenient drug use, and good stability

Inactive Publication Date: 2012-09-12
上海智同医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As a result, patients can only absorb the drug in the acidic stomach after taking the drug, while the alkaline intestinal tract is not conducive to the release of O'Brien, resulting in inability to absorb the drug in the intestinal tract, which in turn leads to low utilization of the drug

Method used

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  • Vincamine sustained-release pellet preparation and preparation method thereof
  • Vincamine sustained-release pellet preparation and preparation method thereof
  • Vincamine sustained-release pellet preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Prescription ratio of vincamine sustained-release pellet preparation:

[0041]

[0042] Preparation:

[0043] (1) Material preparation:

[0044] a The main drug vincamine is micronized, with an average particle size range of 5 μm;

[0045] B, add 60g ethanol in povidone, be mixed with solution, add vincamine, make the solution containing medicine, standby;

[0046] c, add 140g water in tartaric acid, be mixed with organic acid solution, set aside;

[0047] (2) Preparation of acidic blank cores: get blank cores and put them in a fluidized bed, spray the organic acid solution obtained by c on the blank cores to make acidic blank cores;

[0048] (3) Prepare drug-loaded pellet cores: take acidic blank pellet cores and put them in a fluidized bed, spray the drug-containing solution obtained in b on the acidic blank pellet cores to make drug-loaded pellet cores;

[0049] (4) Prepare slow-release drug-loaded pellets: take the drug-loaded pellet core and put it in a flui...

Embodiment 2

[0053] Prescription ratio of vincamine sustained-release pellet preparation:

[0054]

[0055] Preparation:

[0056] (1) Material preparation:

[0057] a The main drug vincamine is micronized, with an average particle size range of 20 μm;

[0058] B, add 60g ethanol, 100g water in copovidone, be mixed with solution, add vincamine, make the solution containing medicine, standby;

[0059] c. Add 40g of water to the citric acid to prepare an organic acid solution for subsequent use;

[0060] (2) Prepare acidic blank cores: get blank cores and put them in a coating pan, spray the organic acid solution obtained in c on blank cores to make acidic blank cores;

[0061] (3) Preparation of drug-loaded pellet cores: take acidic blank pellet cores and put them in a coating pan, spray the drug-containing solution obtained in b on the acidic blank pellet cores to make drug-loaded pellet cores;

[0062] (4) Prepare slow-release drug-loaded pellets: take the drug-loaded pellet core and ...

Embodiment 3

[0066] Prescription ratio of vincamine sustained-release pellet preparation:

[0067]

[0068] Preparation:

[0069] (1) Material preparation:

[0070] a The main drug vincamine is micronized, with an average particle size range of 15 μm;

[0071] B, add 380g water in hydroxypropyl methylcellulose, starch, be mixed with solution, add vincamine, make the solution containing medicine, standby;

[0072] c. Add 120g of water to tartaric acid and malic acid to prepare an organic acid solution for subsequent use;

[0073] (2) Preparation of acidic blank core: take the blank core and put it in extrusion spheronization, spray the organic acid solution obtained by c on the blank core to make an acidic blank core;

[0074] (3) Prepare drug-loaded pellet cores: take acidic blank pellet cores and place them in extrusion spheronization, spray the drug-containing solution obtained in b on the acidic blank pellet cores to make drug-loaded pellet cores;

[0075] (4) Preparation of slow...

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Abstract

The invention discloses a vincamine sustained-release pellet preparation, which comprises main medicines of vincamine, acid blank pellet cores, an adhesive and a diluent in a weight ratio of (1-10): (10-20): (1-10): (20-200), wherein the acid blank pellet cores consist of blank pellet cores and an organic acid covered on the blank pellet cores. The invention provides the vincamine preparation which can be stably released under the pH of 1.5-7.4, the release pH dependency of the conventional vincamine sustained-release preparation is solved, the vincamine preparation can be released stably and slowly in stomach and intestinal tracts, and the pharmaceutical effect is lasting. Moreover, the invention also discloses a preparation method for the vincamine sustained-release pellet preparation. The preparation method is simple, good in repeatability, high in production efficiency and suitable for industrialized mass production. The prepared medicine-carrying pellets are smooth and round, are released uniformly under the pH of 1.5-7.4, and are high in stability.

Description

technical field [0001] The invention relates to a sustained-release pellet preparation in the field of pharmaceutical preparations, in particular to a vincamine sustained-release pellet preparation and a preparation method thereof. Background technique [0002] Vincamine is a biological substance isolated from oleander plants Vinca major, V.minor, V.erecta, and V.dilormis. Alkali, whose chemical name is (3α, 14β, 16α)-14,15-dihydro-14-hydroxyivorene-14-carboxylic acid methyl ester, is soluble in acidic solution and can be semi-synthesized at present. The chemical structural formula is shown in (I). [0003] [0004] Vincamine can pass through the blood-brain barrier, maintain and restore the oxidative catabolism of glucose in the brain tissue of the diseased area, restore the production of lactic acid and the release of carbon dioxide to normal, thereby dilating small cerebral blood vessels and improving cerebral circulation; The blood flow in the normal brain area of ​...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/48A61K31/4375A61P9/10A61P9/12A61P25/00A61J3/06
Inventor 陈挺汤爱斌张继全
Owner 上海智同医药科技有限公司
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