Quercetin hydroxypropyl Beta-cyclodextrin inclusion liposome, preparation method and application thereof

A technology of quercetin hydroxypropyl and cyclodextrin, which is applied in liposome delivery, drug combination, pharmaceutical formulation, etc., can solve the problems of limiting the application of β-cyclodextrin and low solubility, and improve bioavailability , extended cycle time, and broad application prospects

Inactive Publication Date: 2011-05-18
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

And β-cyclodextrin is the only cyclodextrin product that can be mass-produced in industry due to its simple production process and low cost. However, due to its C 2 、C 3 The formation of intramolecular hydrogen bonds between hydroxyl groups leads to its low solubility in water (1.85g / 100Ml, 20°C), which limits the application of β-cyclodextrin

Method used

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  • Quercetin hydroxypropyl Beta-cyclodextrin inclusion liposome, preparation method and application thereof
  • Quercetin hydroxypropyl Beta-cyclodextrin inclusion liposome, preparation method and application thereof
  • Quercetin hydroxypropyl Beta-cyclodextrin inclusion liposome, preparation method and application thereof

Examples

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Effect test

Embodiment 1

[0052] Example 1 Preparation of Quercetin Hydroxypropyl β-cyclodextrin Encapsulation Liposome and Freeze-dried Powder Injection of the Present Invention

[0053] Swell 0.5 g of hydroxypropyl β-cyclodextrin in absolute ethanol for 1 hour, then add 10 mg of quercetin, stir at 25°C for 0.5 hours to completely dissolve the quercetin, and obtain hydroxypropyl β-cyclodextrin quercetin After the dehydrated ethanol solution was added, 100 mg of soybean lecithin, 20 mg of cholesterol, and 6 mg of polyethylene glycol-distearic acid phosphatidylethanolamine were added. Wherein, the molecular weight of polyethylene glycol is 2000. Make a mixed solution, then add the above mixed solution dropwise at 60°C to 20ml of sucrose solution with a mass volume ratio of 2.5%, the volume ratio of absolute ethanol to sucrose solution is 1:4, and after magnetic stirring for 10min, remove the anhydrous solution by rotary evaporation. ethanol until the total volume of the solution is 10ml to form quercet...

Embodiment 2

[0054] Example 2 Preparation of Quercetin Hydroxypropyl β-cyclodextrin Encapsulation Liposome and Freeze-dried Powder Injection of the Present Invention

[0055] Swell 5 g of hydroxypropyl β-cyclodextrin in absolute ethanol for 2 hours to make a solution, then add 0.2 g of quercetin, stir at 50°C for 0.5 hours to completely dissolve the quercetin, and obtain hydroxypropyl β-cyclodextrin After dextrin quercetin dehydrated alcohol solution, add soybean lecithin 1g, cholesterol 0.2g, polyethylene glycol-distearate phosphatidylethanolamine 30mg wherein the molecular weight of polyethylene glycol is 2000, make mixed solution, again The above mixed solution was added dropwise at 60° C. to 0.2 L of sucrose solution with a mass volume ratio of 1.25%. The volume ratio of absolute ethanol to sucrose solution was 1:4, and after magnetic stirring for 20 min, the absolute ethanol was removed by rotary evaporation until the volume of the solution was 0.1 L to form quercetin hydroxypropyl β-...

Embodiment 3

[0056] Example 3 Preparation of Quercetin Hydroxypropyl β-cyclodextrin Encapsulation Liposome and Freeze-dried Powder Injection of the Present Invention

[0057] Swell 0.5 g of hydroxypropyl β-cyclodextrin in absolute ethanol for 1 hour to make a solution, then add 20 mg of quercetin, and ultrasonicate at 25°C for 5 minutes to completely dissolve the quercetin to obtain hydroxypropyl β-cyclodextrin After dextrin quercetin absolute ethanol solution, add soybean lecithin 100mg, cholesterol 20mg, polyethylene glycol-distearate phosphatidylethanolamine 2mg wherein the molecular weight of polyethylene glycol is 3000, make mixed solution, then Add 20ml of 2.5% sucrose solution (mass to volume ratio) dropwise to the above mixed solution at 65°C, the volume ratio of absolute ethanol to sucrose solution is 1:5, and after magnetic stirring for 10 min, remove absolute ethanol by rotary evaporation until the volume of the solution is 10ml forms quercetin hydroxypropyl β-cyclodextrin encap...

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Abstract

The invention relates to a quercetin hydroxypropyl Beta-cyclodextrin inclusion liposome, a preparation method and application thereof, belonging to the field of pharmaceutical preparation. The invention provides a medicine capable of improving the bioavailability of quercetin and a preparation method of the medicine. The medicine capable of improving the bioavailability of the quercetin is the quercetin hydroxypropyl Beta-cyclodextrin inclusion liposome which is prepared from the following components in parts by weight and a pharmaceutically-acceptable solvent: 1 part of quercetin, 1-100 parts of hydroxypropyl Beta-cyclodextrin, 5-50 parts of granulesten, 1-10 parts of cholesterol and 0.1-5 parts of polyethylene glycol-distearin phosphatidyl ethanolamine.

Description

technical field [0001] The invention relates to quercetin hydroxypropyl β-cyclodextrin inclusion complex liposome, a preparation method and application thereof, and belongs to the field of pharmaceutical preparations. Background technique [0002] Pulmonary fibrosis (PF) is a multi-caused disease characterized by diffuse alveolitis and alveolar structural disorder, which eventually leads to pulmonary interstitial fibrosis and respiratory failure. Clinically, pneumonia caused by radiation and chemotherapy drugs is a common complication, with an incidence rate of 36%-60%. There are a variety of causes including bacteria, dust, radioactive substances, and chemotherapy and radiation therapy. Its incidence rate is about 5 / 100,000. The average survival period after diagnosis of pulmonary fibrosis is about 2-4 years, and the 5-year survival rate is about 50-70%. At present, there is still a lack of specific treatment methods in clinical practice. In the past, the treatment of pu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K9/19A61K47/48A61K31/352A61P11/00A61K47/61
Inventor 陈俐娟魏于全
Owner SICHUAN UNIV
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