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Preparation method of compound nano lipidosome capable of improving bioavailability of catechinic acid

A nano-liposome and catechin technology, which is applied in liposome delivery, medical preparations containing active ingredients, drug combinations, etc., can solve the problem of low biofilm transfer rate, low bioavailability, and no probenecid and compound preparations of catechins to achieve the effect of enhancing bioavailability

Active Publication Date: 2014-01-29
浙江山屿海康养产业发展有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the key technical issues that restrict the efficient utilization of catechins or tea polyphenols have not been effectively resolved. bioavailability
However, there are no reports on the compound preparations composed of catechin and other active ingredients to exert synergistic effects.
At present, no compound preparation of probenecid and catechin has been reported

Method used

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  • Preparation method of compound nano lipidosome capable of improving bioavailability of catechinic acid
  • Preparation method of compound nano lipidosome capable of improving bioavailability of catechinic acid
  • Preparation method of compound nano lipidosome capable of improving bioavailability of catechinic acid

Examples

Experimental program
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Effect test

Embodiment 1

[0052] Embodiment 1, a kind of preparation method of the catechin compound nano-liposome that can improve catechin bioavailability, carries out following steps successively:

[0053] 1) Add 150mg of catechin and 1.6g of Tween80 to 20mL of 0.05mol / L phosphate buffered saline (PBS, pH7.0) and stir at 50°C until both catechin and Tween80 are dissolved; get catechin PBS solution;

[0054] 2) Dissolve 150mg of probenecid, 0.5g of egg yolk lecithin and 200mg of cholesterol in 10ml of dichloromethane, and use a syringe to inject the catechin obtained in step 1) at a temperature of 50°C at a certain speed (2ml / min) In the PBS solution, stir at constant temperature for 30 minutes to obtain a suspension;

[0055] 3) Put the suspension on a rotary evaporator to remove dichloromethane (heated in a water bath at 45°C); and then ultrasonically treat it under 380W power ultrasonic (frequency 28KHZ) for 10min to obtain catechin compound nanoliposomes of about 24.15 g.

Embodiment 2

[0056] Embodiment 2, the preparation of a kind of catechin compound nano liposome, carries out following steps successively:

[0057] 1) Add 150mg of catechin and 1.6g of Tween80 to 20mL of 0.05mol / L phosphate buffered saline (PBS, pH7.0) and stir at 50°C until both catechin and Tween80 are dissolved; get catechin PBS solution;

[0058] 2) Dissolve 100mg of probenecid, 0.5g of egg yolk lecithin and 200mg of cholesterol in 10ml of dichloromethane, and use a syringe to inject the catechin obtained in step 1) at a temperature of 50°C at a certain speed (2ml / min) In the PBS solution, stir at constant temperature for 30 minutes to obtain a suspension;

[0059] 3), the same as in Example 1; about 23.86 g of catechin compound nanoliposomes were obtained.

Embodiment 3

[0060] Embodiment 3, the preparation of a kind of catechin compound nano liposome, carries out following steps successively:

[0061] 1) Add 150mg of catechin and 1.6g of Tween80 to 20mL of 0.05mol / L phosphate buffered saline (PBS, pH7.0) and stir at 50°C until both catechin and Tween80 are dissolved; get catechin PBS solution;

[0062] 2) Dissolve 200mg of probenecid, 0.4g of egg yolk lecithin and 400mg of cholesterol in 10ml of dichloromethane, and use a syringe to inject the catechin obtained in step 1) at a temperature of 50°C at a certain speed (2ml / min) In the PBS solution, stir at constant temperature for 30 minutes to obtain a suspension;

[0063] 3), the same as in Example 1; about 24.21 g of catechin compound nanoliposomes were obtained.

[0064] Experiment 1. Detection of liposome encapsulation efficiency:

[0065] The suspension obtained in step 2) of Example 1, Example 2, and Example 3 was tested according to the above-mentioned method two, and the results were...

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Abstract

The invention discloses a preparation method of compound nano lipidosome capable of improving the bioavailability of catechin. The method comprises the following steps: 1) adding 100mg to 150mg of catechin and 1.0g to 2.0g of tween80 into 20ml of 0.05mol / L phosphate buffer (PBS, pH7.0) so as to obtain a mixture, and stirring the mixture at the temperature of 40-60 DEG C to obtain a catechin PBS solution; 2) weighing and dissolving 100mg to 200mg of probenecid, 0.1g to 0.5g of lecithin and 100mg to 500mg of cholesterol in 10ml to 20ml of dichloromethane so as to obtain a mixture I, injecting the mixture I into the catechin PBS solution obtained in step 1) by utilizing a syringe at the temperature of 40-60 DEG C so as to obtain a mixture II, and stirring the mixture II at a constant temperature to obtain a suspension; 3) evaporating the suspension in a rotating state to remove the dichloromethane; carrying out the ultrasonic treatment on the mixture by utilizing the ultrasonic of 350W to 400W for 8min to 12min to obtain the catechin compound nano lipidosome.

Description

technical field [0001] Catechin is the most important natural active ingredient in tea, which has various pharmacological and health-care activities. The invention relates to a preparation method of compound nano liposome capable of improving the bioavailability of catechin. Background technique [0002] Tea Polyphenols (Tea Polyphenols, TP) is the general term for polyphenols and their derivatives in tea, mainly composed of catechins, flavonoids, anthocyanins and phenolic acids, among which catechins account for the majority of tea polyphenols. The total amount is 60%-90%. Catechin has strong biological activity. A large number of studies have shown that catechin has various health care and pharmacological effects such as anti-oxidation, scavenging free radicals, anti-cardiovascular disease, antibacterial and anti-inflammatory. However, the key technical issues that restrict the efficient utilization of catechins or tea polyphenols have not been effectively resolved. bio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/353A61K9/127A61P19/06A61P19/02A61K31/195
Inventor 葛建韩宝瑜王梦馨
Owner 浙江山屿海康养产业发展有限公司
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