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Breviscapine internal phase gelating polycystic lipidosome freeze-dried powder and preparation method thereof

A multivesicular liposome and breviscapine technology, which is applied in liposome delivery, freeze-drying delivery, powder delivery, etc., can solve the problems of short injection half-life, poor stability, poor absorption, etc., to delay drug release and reduce Fluidity, effect of reducing vesicle rupture

Inactive Publication Date: 2015-07-29
LINYI UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The technical problem to be solved by the present invention is to provide a kind of inner-phase coagulated breviscapine containing breviscapine in view of the current defects of poor oral absorption of breviscapine, short injection half-life, and poor stability of multivesicular liposomes as slow and controlled release drug delivery carriers. Gelled multivesicular liposome freeze-dried preparation, high encapsulation efficiency, slow release of breviscapine, good stability in vitro, greatly reducing the number and frequency of medication

Method used

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  • Breviscapine internal phase gelating polycystic lipidosome freeze-dried powder and preparation method thereof
  • Breviscapine internal phase gelating polycystic lipidosome freeze-dried powder and preparation method thereof
  • Breviscapine internal phase gelating polycystic lipidosome freeze-dried powder and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0038] Example 1 Preparation of breviscapine internal phase gelled polyvesicular liposome freeze-dried powder

[0039] Weigh 40 mg of phosphatidylcholine, 8.2 mg of triolein, 40 mg of cholesterol, add chloroform-ether (1:1) to dissolve in 2 ml, and use it as the lipid phase; weigh 400 mg of Poloxamer 407, 400 mg of Poloxamer 188 40mg, breviscapine 40mg, sucrose 40mg, arginine 8.7mg, add water to 2ml, adjust pH7.0 to dissolve, as the inner water phase; weigh 5.8mg lysine, glucose 30mg, add water to 4ml, as the outer water phase . Slowly add the inner water phase to the upper layer of the lipid phase, and shear for 8 minutes under the condition of a high-speed shear homogenizer at 10,000 rpm to form a water-in-oil emulsion; Cut down for 8 minutes to form a water-in-oil-in-water type double emulsion; blow dry the double emulsion with nitrogen to remove chloroform and ether therein, and obtain the scutellarin multivesicular liposome suspension; the obtained scutellarin multivesic...

Embodiment 2

[0041] Example 2 Preparation of breviscapine internal phase gelled multivesicular liposome lyophilized powder

[0042] Weigh soybean lecithin 38mg, triolein 10mg, dipalmitoylphosphatidylglycerol 10mg, cholesterol 40mg add chloroform-ether (1:1) to dissolve in 2ml, as lipid phase; weigh poloxamer 407 440mg, Poloxamer 188 70mg, breviscapine 40mg, sucrose 5mg, arginine 10.5mg, add water to 2ml, adjust pH7.0 to dissolve, as the internal water phase; weigh lysine 6mg, glucose 50mg, add water to 4ml, as the external aqueous phase. Slowly add the inner water phase to the upper layer of the lipid phase, and shear for 8 minutes under the condition of a high-speed shear homogenizer at 10,000 rpm to form a water-in-oil emulsion; Cut down for 8 minutes to form a water-in-oil-in-water type double emulsion; blow dry the double emulsion with nitrogen to remove chloroform and ether therein, and obtain the scutellarin multivesicular liposome suspension; the obtained scutellarin multivesicular...

Embodiment 3

[0044] Example 3 Preparation of breviscapine internal phase gelled multivesicular liposome lyophilized powder

[0045] Weigh soybean lecithin 47mg, tricaprylic glyceride 6mg, cholesterol 10mg add chloroform-ether (1:1) to dissolve in 2ml, as lipid phase; weigh poloxamer 407 380mg, poloxamer 188 10mg, scutellaria Add 40 mg of sucrose, 40 mg of sucrose, and 6.5 mg of histidine to 2 ml of water, adjust the pH to 7.0 to dissolve, and use it as the inner water phase; weigh 4 mg of polyvinyl alcohol, 20 mg of glucose, add water to 4 ml, and use it as the outer water phase. Slowly add the inner water phase to the upper layer of the lipid phase, and shear for 8 minutes under the condition of a high-speed shear homogenizer at 10,000 rpm to form a water-in-oil emulsion; Cut down for 8 minutes to form a water-in-oil-in-water type double emulsion; blow dry the double emulsion with nitrogen to remove chloroform and ether therein, and obtain the scutellarin multivesicular liposome suspensio...

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Abstract

The invention aims to provide breviscapine internal phase gelating polycystic lipidosome freeze-dried powder which is stable in internal and external properties, high in packaging rate and low in medicine release, and a preparation method thereof. The breviscapine internal phase gelating polycystic lipidosome disclosed by the invention comprises the following raw and auxiliary materials in parts by weight: 1 part of breviscapine, 0.95-1.18 parts of neutral phospholipid, 0.025-0.25 part of negative-charge phospholipid, 0.25-1 part of cholesterol, 0.15-0.25 part of triglyceride, 0.125-1 part of cane sugar, 0.163-0.263 part of an internal water phase assisting emulsifying agent, 9.5-10 parts of poloxamer 407, 0.25-1.75 parts of poloxamer 188, 0.5-1.25 parts of glucose, 0.1-0.15 part of an external water phase assisting emulsifying agent and 6-14 parts of a supporting agent.

Description

technical field [0001] The invention belongs to the field of sustained and controlled release preparations, in particular to a freeze-dried powder of breviscapine internal phase gelled multivesicular liposome and a preparation method thereof. Background technique [0002] Breviscapine is an active ingredient of flavonoids extracted from Breviscapine flower. The main components are scutellarin, a small amount of breviscapine and other flavonoid glycosides. It is an effective drug for treating cardiovascular and cerebrovascular diseases, angina pectoris and other diseases. It mainly treats cerebral thrombosis, cerebral infarction, paralysis after stroke, coronary heart disease, angina pectoris and other diseases with definite curative effect. The main component of scutellarin, scutellarin, has poor water solubility and low oral bioavailability. According to reports, when Beagle dogs were randomly orally administered scutellarin, the absolute oral bioavailability was only (0.40...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K9/127A61K31/7048A61K47/34A61P9/00A61P9/10
Inventor 李海刚
Owner LINYI UNIVERSITY
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