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A puerarin nanocrystalline capsule and preparation method thereof

A technology of puerarin and nanocrystals, which is applied in capsule delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve the problems of low absolute bioavailability, poor solubility of puerarin, and difficulty in oral absorption, etc., to improve biological Utilization, oral convenience, and the effect of overcoming adverse reactions

Active Publication Date: 2021-05-28
易跃能
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved in the present invention is to overcome the poor solubility of puerarin, it is difficult to absorb when taken orally, and the absolute bioavailability is low (about 4%). Although the prior art can significantly improve the bioavailability of puerarin orally administered, it cannot To meet the requirements of oral administration (the absolute bioavailability of oral administration requires more than 20%), a puerarin nanocrystalline capsule and a preparation method thereof are provided

Method used

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  • A puerarin nanocrystalline capsule and preparation method thereof
  • A puerarin nanocrystalline capsule and preparation method thereof
  • A puerarin nanocrystalline capsule and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0045] Take 2g of puerarin and 4g of sodium lauryl sulfate, add it to 100mL of water, and stir evenly with a magnetic force; put the above mixed solution into a high-pressure milk homogenizer, control the temperature of the preparation process at 43°C, and circulate and homogenize 10 times under a pressure of 700Bar , to obtain a puerarin nanocrystal suspension; take the puerarin nanocrystal suspension, put it in a lyophilizer and pre-freeze it at -45°C and freeze-dry it (prefreeze at -45°C for 2h, keep it at -25°C for 4h, and - Sublimation and drying at 5°C for 14 hours, analysis and drying at 25°C for 2 hours out of the box) to obtain the freeze-dried product of puerarin nanocrystals; crush the freeze-dried product of puerarin nanocrystals through an 80-mesh sieve, and fill the powder into capsules to obtain puerarin Nanocrystalline capsules.

Embodiment 2

[0047] This example is basically the same as Example 1, except that the suspension of puerarin nanocrystals is changed from freeze-drying to spray-drying, and spray-drying is carried out at a flow rate of 8 rpm at an air inlet temperature of 180° C. to obtain puerarin Nanocrystalline powder, after filling the capsules, the puerarin nanocrystalline capsules are obtained.

Embodiment 3

[0049] Take the same puerarin nanocrystal suspension as in Example 1, add 6% mannitol, place it in a lyophilizer and freeze-dry it after pre-freezing at -20°C to obtain a puerarin nanocrystal freeze-dried product; The puerarin nanocrystal freeze-dried product is crushed through an 80-mesh sieve, and the powder is filled into capsules to obtain puerarin nanocrystal capsules.

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Abstract

The invention discloses a puerarin nano crystal capsule and a preparation method thereof. The preparation method is as follows: 1) Add puerarin and sodium lauryl sulfate (mass ratio ≥1:5 and <1:1.5) into water, and mix well to obtain a mixed solution; 2) Homogenize the mixed solution (40-45°C , 700-2000Bar) more than 5 times to obtain a suspension (particle size 150-500nm); 3) adopt method ① or ② to carry out: ① pre-freeze the suspension at -50-40°C for 1.5-2.5h, and then Incubate at -30--20°C for 3.5-4.5 hours, then sublimate and dry at -5°C for 12-16 hours, analyze and dry at 25°C for 1.5-2.5 hours, crush, sieve, and fill into capsules; ②Put the suspension in The temperature at the air inlet is 150-200°C and spray-dried, then filled into capsules. The capsule prepared by the invention meets the requirement of oral administration of puerarin.

Description

technical field [0001] The invention relates to a puerarin nanocrystal capsule and a preparation method thereof. Background technique [0002] Puerarin, also known as Pueraria lobata (Willd.) Ohwi root or Pueraria lobata (Willd.) Ohwi root or P. thunbergiana Benth. In the root. Puerarin is a colorless crystal; melting point 203-205°C; insoluble in water and organic solvents, soluble in water, methanol, and ethanol when heated, but insoluble in ethyl alcohol, chloroform, and benzene; not enzymatically hydrolyzed, It is also not easily hydrolyzed by dilute acid. [0003] Puerarin has the functions of promoting blood circulation and removing blood stasis, improving microcirculation, dilating coronary arteries and cerebrovascular vessels, reducing myocardial oxygen consumption, etc., and can obviously promote the cerebral circulation and peripheral circulation of animals and humans. It not only improves the normal brain microcirculation of the human body, but also has a signi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/48A61K31/352A61P9/10A61P9/00A61P27/16A61K47/20
Inventor 奉建芳涂亮星胡凯莉徐磊张艳
Owner 易跃能
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