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(-)-epigallocatechin gallate-calcium complex solid dispersion and its prepn and application

A technology of solid dispersion and complex, applied in the field of pharmaceutical compositions, can solve the problems of unsatisfactory curative effect of osteoporosis, and achieve the effects of significant curative effect, enhanced pharmacological action, and improved water solubility.

Active Publication Date: 2008-01-16
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the present invention is to provide a kind of EGCG-calcium complex solid dispersion with remarkable curative effect in view of the problem of unsatisfactory curative effect generally existing in the existing senile disease osteoporosis treatment

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] The preparation of embodiment 1 EGCG-calcium complex solid dispersion

[0019] EGCG, with a purity of 99.6%, was provided by the Laboratory of Traditional Chinese Medicine and Marine Medicine, School of Pharmacy, Sun Yat-sen University. Polyvinylpyrrolidone PVP k30 (referred to as PVP), imported and repackaged, provided by Guangzhou Chemical Reagent Wholesale Department.

[0020] Dissolve 10 g of EGCG in 20 ml of deionized water, add saturated CaCl dropwise 2 Solution, stirring while adding dropwise, nitrogen protection, until the precipitation is complete, centrifuge at 5000rpm for 5min, collect the precipitate, resuspend with 200ml deionized water, centrifuge at 5000rpm for 5min, collect the precipitate, then suspend with 200ml deionized water, centrifuge at 5000rpm 5min (repeated 3 times), 6.9 grams of EGCG-Ca was obtained. 6.9 grams of EGCG-Ca and 40 grams of PVP were mixed and dissolved in 300 ml of water, protected by nitrogen, homogenized by a high-pressure hom...

Embodiment 2

[0021] The preparation of embodiment 2 EGCG-calcium complex solid dispersion

[0022] EGCG, with a purity of 99.6%, was provided by the Laboratory of Traditional Chinese Medicine and Marine Medicine, School of Pharmacy, Sun Yat-sen University. Polyvinylpyrrolidone PVP k30 (referred to as PVP), imported and repackaged, provided by Guangzhou Chemical Reagent Wholesale Department.

[0023] Dissolve 10 g of EGCG in 20 ml of deionized water, add saturated CaCl dropwise 2 Solution, while stirring while adding dropwise, until the precipitation is complete, centrifuge at 5000rpm for 5min, collect the precipitate, re-suspend with 200ml deionized water, centrifuge at 5000rpm for 5min, collect the precipitate, then suspend with 200ml deionized water, and centrifuge at 5000rpm for 5min (repeat 3 times), to get 6.9 grams of EGCG-Ca. 6.9 g of EGCG-Ca and 95 g of PVP were mixed and dissolved in 600 ml of water, protected by nitrogen, homogenized by a high-pressure homogenizer, filtered, an...

Embodiment 3

[0024] Embodiment 3 Preparation of EGCG-calcium complex solid dispersion

[0025] EGCG, with a purity of 99.6%, was provided by the Laboratory of Traditional Chinese Medicine and Marine Medicine, School of Pharmacy, Sun Yat-sen University. Polyvinylpyrrolidone PVP k30 (referred to as PVP), imported and repackaged, provided by Guangzhou Chemical Reagent Wholesale Department.

[0026] Dissolve 10 grams of EGCG in 20ml of deionized water, add saturated calcium acetate solution dropwise, stir while adding, and protect with nitrogen until the precipitation is complete, centrifuge at 5000rpm for 5min, collect the precipitate, resuspend with 200ml of deionized water, and centrifuge at 5000rpm After 5 minutes, the precipitate was collected, suspended in 200 ml of deionized water, and centrifuged at 5000 rpm for 5 minutes (repeat 3 times) to obtain 7.2 grams of EGCG-Ca. 7.2 grams of EGCG-Ca and 180 grams of PVP were mixed and dissolved in 2000 ml of water, protected by nitrogen, homog...

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Abstract

The present invention discloses one kind of (-)-epigallocatechin gallate (EGCG)-Ca complex solid dispersion and its preparation and application. The EGCG-Ca complex solid dispersion contains EGCG-Ca complex and PVP-k30 in the weight ratio of 1 to 4-25, optimally 1 to 7-12. The preparation process of the EGCG-Ca complex solid dispersion includes dissolving EGCG in deionized water, dropping saturated calcium salt solution while stirring and introducing protecting nitrogen until complete precipitation, collecting the precipitate, suspending and washing with deionized water, centrifuging to collect precipitate as the EGCG-Ca complex, mixing EGCG-Ca complex and PVP-k30 in required ratio, dissolving the mixture in water while introducing protecting nitrogen, high pressure homogenizing, filtering, spray drying the filtrate to obtain the EGCG-Ca complex solid dispersion, which is used in treating senile osteoporosis in high curative effect.

Description

technical field [0001] The invention relates to the field of pharmaceutical compositions, in particular to a solid dispersion of (-)-epigallocchinin gallate-calcium complex, a preparation method and a medical application thereof. Background technique [0002] (-)-Epigallocatechin-3-gallate [(-)-Epigallocatechin-3-gallate, referred to as EGCG] has good free radical scavenging, anti-oxidation, anti-mutation, anti-aging, anti-radiation, anti-virus, anti- Anti-cancer, lowering blood fat and cholesterol, anti-atherosclerosis, antibacterial, lowering blood sugar, lowering blood pressure and other health care and pharmacological effects. [0003] However, due to the instability of EGCG, it is very easy to absorb moisture, oxidize, have low bioavailability, poor absorption, and cause irritation to the gastrointestinal tract. Long-term use will reduce the content of metals such as iron in the body and other shortcomings limit the application of EGCG. Simple tea polyphenols and metal...

Claims

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Application Information

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IPC IPC(8): A61K31/353A61K47/32A61K9/00A61P19/10
Inventor 许东晖梅雪婷许实波
Owner SUN YAT SEN UNIV
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