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Composition containing sophora flavescens extract for pulmonary administration as well as preparation method and application of composition

A technology for pulmonary administration and extract, applied in the field of compositions containing Sophora flavescens extract and its preparation, can solve the problems of poor drug sedimentation and retention effect, poor drug stability, etc., and achieves improved stability and bioavailability , Improve the effect of sedimentation and retention, good stability

Pending Publication Date: 2021-09-03
GUIZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, there are still some problems in the treatment of pulmonary diseases with pulmonary drug delivery, such as poor stability of the drug in the body, poor sedimentation and retention of the drug in the lungs, etc.

Method used

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  • Composition containing sophora flavescens extract for pulmonary administration as well as preparation method and application of composition
  • Composition containing sophora flavescens extract for pulmonary administration as well as preparation method and application of composition
  • Composition containing sophora flavescens extract for pulmonary administration as well as preparation method and application of composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Weigh 120 mg of soybean lecithin, 12 mg of cholesterol oleate, 6 mg of stearylamine, 12 mg of glyceryl trioleate, and 6 mg of polyethylene glycol monostearate in eggplant-shaped bottles, and add appropriate amount of dichloro Methane was vortexed to dissolve it completely; the organic solvent was removed by rotary evaporation under reduced pressure until the solution was about 0.5 mL. Add 0.5 mL of dichloromethane and 40 mg of oxymatrine, vortex to mix, and continue rotary evaporation for 20 min until a dry and uniform lipid film is formed on the bottle wall. Take out the eggplant-shaped bottle, add 4 mL of 0.01 mmol / L PBS solution to wash the membrane, and hydrate at 25°C for 1 hour to form a liposome primary emulsion. Sonicate the hydrated emulsion in a water bath for 1 min to obtain the Lip / ME solution. Incubate the Lip / ME solution with an equal volume of 40-100KDa hyaluronic acid solution (20mg / mL) at 25°C for 30 min to obtain the Lip / ME@ HA suspension.

[0043] F...

Embodiment 2

[0045] Example 2 Experimental study on tissue distribution in mice

[0046] The results of the in vivo tissue distribution study showed that the Lip / ME@HA obtained in Example 1 significantly improved the stability of Sophora flavescens extract in mice, prolonged the residence time of the drug in the lungs, and improved the bioavailability of the drug.

[0047] Experimental method: Nile red (NR) was loaded into Lip / ME@HA to form Lip / ME / NR@HA. 36 mice were divided into 2 groups with 18 mice in each group. After being anesthetized with urethane, the free Nile red solution (Free-NR) and Lip / ME / NR@HA were administered with a pulmonary administration quantitative nebulizer, respectively, with a dosage of 0.75 mg / kg. At 0.5, 1, and 2 hours after administration, 0.5 mL of blood was collected from the abdominal aorta and placed in a heparinized centrifuge tube; dissected, and the heart, liver, spleen, lung, and kidney were collected. Whole blood was centrifuged at 4°C, 6000r / min for ...

Embodiment 3

[0049] Example 3 Investigation of the therapeutic effect of Lip / ME@HA preparation on emphysema mice

[0050] The product of implementation example 1 is carried out the experimental study of drug efficacy in animals.

[0051] Preparation group: Lip / ME@HA group

[0052] Control group: normal group, model group, positive drug dexamethasone group

[0053] experimental method

[0054] SPF grade C57BL / 6 mice were randomly divided into 5 groups, normal group (Ctrl), model group (Model), low-dose Lip / ME@HA group (L-Lip / ME@HA), high-dose Lip / ME@ HA group (H-Lip / ME@HA) and positive control dexamethasone group (DEX). After anesthetized by intraperitoneal injection of urethane, 100 μL of porcine pancreatic elastin was injected into the airway on the 1st, 7th, 14th, 21st and 28th day using a pulmonary administration quantitative nebulizer. The Lip / ME@HA low-dose and high-dose groups were given Lip / ME@HA every other day using a pulmonary delivery quantitative nebulizer starting from the...

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Abstract

The invention discloses a composition containing a sophora flavescens extract for pulmonary administration as well as a preparation method and application of the composition. The composition is mainly prepared from the following components in parts by weight: 1 part of a radix sophorae flavescentis extract, 2 to 4 parts of soybean lecithin, 0.2 to 0.6 part of glyceryl trioleate, 0.2 to 0.4 part of cholesterol oleic acid, 0.1 to 0.2 part of polyethylene glycol monostearate, 0.1 to 0.2 part of a cationic material and 0.5 to 2 parts of hyaluronic acid. The composition is prepared by coating a sophora flavescens extract liposome with hyaluronic acid, can be used for pulmonary administration in a pulmonary administration manner, can avoid rapid onset of a first pass elimination effect, can significantly improve the stability of the sophora flavescens extract, can improve the bioavailability of the drug, can significantly reduce the toxic and side effects of the drug, and can improve the compliance of patients.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical compositions, and in particular relates to a composition containing Sophora flavescens extract for pulmonary administration, a preparation method and application thereof. Background technique [0002] Pulmonary diseases refer to primary lung diseases and related diseases. Common types of lung diseases include chronic obstructive pulmonary disease, emphysema, pulmonary hypertension, asthma, and viral pneumonia. Pulmonary diseases mainly involve the lungs. As the disease progresses, the lung function gradually declines, which may cause complications in other viscera. According to the "World Health Report" issued by the World Health Organization in 2018, the mortality rate of pulmonary diseases is the highest among non-infectious diseases in the world. Disease mortality ranks third in the ranking, second only to cardiovascular diseases and tumors. Due to factors such as air pollution, smoking...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/72A61K9/12A61K36/489A61K9/127A61K47/61A61P11/00A61P31/12A61P9/12A61P35/00
CPCA61K9/12A61K9/0073A61K36/489A61K9/127A61K47/61A61P11/00A61P31/12A61P9/12A61P35/00
Inventor 沈祥春彭剑青蔡梓民陶玲
Owner GUIZHOU MEDICAL UNIV
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