Puerarin nanocrystalline medical composition and preparation method thereof

A technology of puerarin and composition, applied in the puerarin nanocrystal pharmaceutical composition, puerarin nanocrystal pharmaceutical composition and its preparation field, can solve the problems of low encapsulation rate, enlargement and reunion that are difficult to recover Dissolved particle size and other issues to achieve good stability

Inactive Publication Date: 2013-07-24
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, nano-carrier drugs need to use carrier materials to disperse the drug in the carrier and nanometerize it, which has disadvantages such as safety: (1): carrier-based nano-preparations such as liposomes, nanoparticles, micelles, and nanocapsules Low encapsulation efficiency, leakage, instability, etc. are common, and are restricted by toxicity and carrier materials (currently only PLGA and PLA are included in the US Pharmacopoeia for artificially synthesized polyester carrier materials), which limits its clinical application; (2) Some methods require the addition of organic solvents during the preparation process, which is difficult to remove in the final preparation product, increasing the risk of medication for patients
[0010] However, because the puerarin nanocrystals in the nanocrystal mixture are easy to precipitate, agglomeration will occur, it will be difficult to redissolve or the particle size will increase, and the purpose of improving solubility and bioavailability cannot be achieved.
Therefore, it is still difficult to obtain a stable nanocrystal suspension

Method used

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  • Puerarin nanocrystalline medical composition and preparation method thereof
  • Puerarin nanocrystalline medical composition and preparation method thereof
  • Puerarin nanocrystalline medical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Example 1: Preparation of Puerarin Nanocrystal Suspension (1)

[0060] Prescription composition:

[0061]

[0062]

[0063] Preparation:

[0064] According to the above ratio, the main drug puerarin passes through a 100-mesh sieve, and the auxiliary materials pass through a 80-mesh sieve, and the particle size is tens of microns. Disperse the drug in water, then add hypromellose, sodium lauryl sulfate, and benzoic acid to make a coarse suspension, and then prepare a nanocrystal suspension by media milling at a speed of 4000 rpm. After 2 hours, the particle size can reach 250.4nm.

Embodiment 2

[0065] Example 2: Preparation of Puerarin Nanocrystal Suspension (2)

[0066] Prescription composition:

[0067]

[0068] Preparation:

[0069]According to the above ratio, the main drug puerarin passes through a 100-mesh sieve, and the auxiliary materials pass through a 80-mesh sieve, and the particle size is tens of microns. Disperse the drug in water, add hydroxypropyl cellulose, docusate sodium, and sodium benzoate to make a coarse suspension, and then prepare a nanocrystal suspension by a high-pressure homogenization method, with a high pressure of 1.5×10 5 kPa, after 15 cycles, the particle size can reach 358.4nm.

Embodiment 3

[0070] Embodiment 3: Puerarin nanocrystal suspension (3) and its preparation method

[0071] Prescription composition:

[0072]

[0073] Preparation:

[0074] According to the above ratio, the main drug puerarin passes through a 100-mesh sieve, and the auxiliary materials pass through a 80-mesh sieve, and the particle size is tens of microns. Disperse the drug in water, then add poloxamer, polyvinyl alcohol, and sorbic acid to make a coarse suspension, and then prepare a nanocrystal suspension by high-pressure micro-jet method, the number of cycles is 80 times, and the particle size can reach 385.9nm.

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Abstract

The invention belongs to the technical field of medicines and relates to a puerarin nanocrystalline medical composition and a preparation method and application thereof. Specifically, the puerarin composition is a puerarin nanocrystalline composition. The puerarin composition provided by the invention remarkably improves the solubility and bioavailabilityof puerarin and reduces or eliminates the food effect of the medicine, and is good in stability and can be prepared into various common preparation forms easily, the stability and effect of the medicine are improved, so that the composition has good prospect.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a puerarin nanocrystal medicinal composition and a preparation method thereof. The present invention also relates to the application of the puerarin nano crystal pharmaceutical composition. Background technique [0002] Puerarin (Pue) is the main isoflavone compound extracted from the dried root of Pueraria mirifica or Pueraria vine, chemical name 8-β-D-glucopyranose-4', 7-dihydroxyiso flavonoids. [0003] In recent years, domestic scholars have done a lot of research on the pharmacological effects and clinical applications of puerarin. The pharmacological effects of puerarin mainly include: improving microcirculation, slowing heart rate, lowering blood pressure, protecting myocardial ischemia-reperfusion injury, and antiarrhythmia , inhibit platelet aggregation and thrombosis, prevent atherosclerosis, improve coronary circulation, expand coronary arteries, etc. (Ma Jiajia, Li H...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K9/00A61K31/352A61K47/38A61K47/36A61K47/34A61K47/32A61K47/26A61K47/10A61P9/10A61P9/06A61P9/12A61P3/10A61P7/02
Inventor 郑爱萍张晓燕孙建绪魏丽莎
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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