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Pharmaceutical composition containing lycopene and preparation method thereof

A technology for lycopene and solid pharmaceutical preparations is applied in the field of lycopene-containing pharmaceutical compositions and their preparation, and can solve the problems of low bioavailability, low solubility of lycopene, poor dissolution and the like

Inactive Publication Date: 2009-05-27
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no report of preparing lycopene into a preparation with high solubility, fast dissolution and stability. CN200610037859.5 discloses a "β-cyclodextrin and hydroxypropyl-β-cyclodextrin mixed clathrate tomato Composition of lycopene and its preparation method", this method improves the solubility of lycopene to a certain extent by preparing lycopene into a cyclodextrin inclusion compound, the maximum is 14 μg / ml, and increases the stability , but the degree to which the invention increases the solubility of lycopene is still small
In addition, for the existing commercially available preparation lycopene oil capsules, only lycopene is suspended in oil, the dissolution in vitro is poor, and the bioavailability in vivo is low.

Method used

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  • Pharmaceutical composition containing lycopene and preparation method thereof
  • Pharmaceutical composition containing lycopene and preparation method thereof
  • Pharmaceutical composition containing lycopene and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Preparation of Lycopene Solid Dispersion and Its Tablets

[0046] Take 5g of lycopene and 1885g of poloxamer, add 600ml of tetrahydrofuran to ultrasound to dissolve, evaporate most of the solvent on a rotary evaporator, water bath temperature of 40℃, put it in vacuum for 24h, grind the dried product to obtain a solid dispersion .

[0047] Mix 256 g of lactose with the solid dispersion first, then add 5.6 g of differential silica gel, 2.8 g of cross-linked polyvinylpyrrolidone, and 5.6 g of magnesium stearate, mix well, and press 1000 tablets.

[0048] The tablets dissolve 75% in water in 45 minutes (n=6).

Embodiment 2

[0050] Preparation of Lycopene Solid Dispersion and Its Tablets

[0051] Take 5g of lycopene and 18815g of poloxamer, add 600ml of tetrahydrofuran to ultrasonically dissolve, and evaporate most of the solvent on a rotary evaporator. The temperature of the water bath is 40℃, and it is dried in vacuum for 24h. The dried product is ground to obtain a solid dispersion. .

[0052] Mix 251.6g of lactose with the solid dispersion first, 2.8g of cross-linked polyvinylpyrrolidone and 5.6g of magnesium stearate, mix evenly, and press 1000 tablets.

[0053] The tablets dissolve 76% in water in 45 minutes (n=6).

Embodiment 3

[0055] Preparation of Lycopene Solid Dispersion and Its Tablets

[0056] Take 5g of lycopene and 18825g of poloxamer, add 600ml of tetrahydrofuran to ultrasonically dissolve, evaporate most of the solvent on a rotary evaporator, water bath temperature of 40℃, put it in vacuum for 24h, grind the dried product to obtain a solid dispersion .

[0057] Mix 241.6g of lactose with the solid dispersion, dry granulation and granulate, add 2.8g of cross-linked polyvinylpyrrolidone and 5.6g of magnesium stearate, mix well, and press 1000 tablets.

[0058] The tablet can dissolve 83% in water in 45 minutes (n=6).

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Abstract

The invention relates to the pharmaceutical preparation field, in particular to a pharmaceutical composition with lycopene. The pharmaceutical composition is characterized in that poloxamer 188 is added so as to greatly improve the water solubility of the lycopene; in particular, after the lycopene and the poloxamer 188 are prepared into solid dispersion or, together with cyclodextrin, are prepared into a cyclodextrin iclusion complex, bioavailability of the lycopene is remarkably improved.

Description

Technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a pharmaceutical composition containing lycopene and a preparation method thereof. Background technique [0002] Lycopene, molecular formula C 40 H 36 , With a molecular weight of 536.85, is a kind of carotenoid. Among all carotenoids, it has the strongest function of eliminating singlet oxygen and eliminating free radicals. Its ability to eliminate singlet oxygen is carotene 2 times, 100 times that of vitamin E; it can slow down the oxidation of low-density lipoprotein, reduce cholesterol in plasma, and prevent cardiovascular disease; it can effectively inhibit the growth of cancer cells, has anti-cancer and anti-cancer effects, especially for prostate cancer It has a very good therapeutic effect. In addition, it has the function of activating immune cells, which can enhance the body's immunity and anti-aging. Lycopene has such a wide range of effects and has such unparalle...

Claims

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Application Information

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IPC IPC(8): A61K31/01A61K47/34A61P39/06A61K47/10A61K47/40
Inventor 平其能吕文莉戎飞毛毛
Owner CHINA PHARM UNIV
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