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Apigenin vesicle preparation and its preparation technology

A technology of apigenin and vesicles, which is applied in the field of medicine, can solve the problems that have not been reported in domestic and foreign literature, and achieve the effects of improving bioavailability, obvious slow-release effect, and high encapsulation efficiency

Inactive Publication Date: 2008-04-23
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are also reports that apigenin is used to treat fatty liver, obesity and as a cartilage regeneration agent for the treatment of osteoarthritis (Chinese Patent Application No. 03127190.1 and 200480030411.X), but other studies on apigenin-related preparations and clinical applications have so far So far no domestic and foreign literature reports

Method used

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  • Apigenin vesicle preparation and its preparation technology
  • Apigenin vesicle preparation and its preparation technology
  • Apigenin vesicle preparation and its preparation technology

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Embodiment 1: the preparation of apigenin vesicle

[0030] prescription:

[0031] Apigenin 0.05g

[0032] Tween 80 0.5g

[0033] Cholesterol 0.25g

[0034] Proper amount of ethanol

[0035] Phosphate buffer at pH 7.4

[0036] Makes 100mL

[0037] Preparation process: Weigh the prescribed amount of apigenin, Tween 80 and cholesterol into a beaker, add an appropriate amount of ethanol to dissolve, and inject it into a phosphate buffer solution with a pH of 7.4 in a water bath at 55°C to prepare an apigenin vesicle solution. The encapsulation efficiency of the obtained vesicles was determined, and the encapsulation efficiency was 65.80%.

Embodiment 2

[0038] Embodiment 2: the preparation of apigenin vesicle

[0039] prescription:

[0040] Apigenin 0.05g

[0041] Span80 0.4g

[0042] Cholesterol 0.20g

[0043] Proper amount of ethanol

[0044] Phosphate buffer at pH 7.4

[0045] Makes 100mL

[0046] Preparation process: same as above, encapsulation efficiency is 60.68%.

Embodiment 3

[0047] Embodiment 3: the preparation of apigenin vesicle

[0048] prescription:

[0049] Apigenin 0.05g

[0050] Maize 0.50g

[0051] Cholesterol 0.20g

[0052] Proper amount of ethanol

[0053] Phosphate buffer at pH 7.4

[0054] Makes 100mL

[0055] Preparation process: Weigh the prescribed amount of apigenin, meze and cholesterol in a beaker, add an appropriate amount of ethanol and chloroform mixed solvent to dissolve, evaporate under reduced pressure to remove the organic solvent to form a thin film, add phosphate buffer, hydrate for 1 to 2 Hours, processed by a high-pressure homogenizer for 5 minutes, and passed through a 0.22um filter membrane to obtain an apigenin vesicle solution. The encapsulation efficiency of the obtained vesicles was determined, and the encapsulation efficiency was 68.62%.

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Abstract

The present invention provides an apigenin vesiculation preparation and its preparation process. Said preparation composition includes (by wt%) 0.25%-20% of apigenin, 40%-90% of non-ionic surface active agent, 8.7-48.8% of cholesterol and 2%-20% of lyophilization protection agent. The described non-ionic surface active agent can be Span-20, Span-40, Span-60, Span-80, Tween-20, Tween-60, Tween-80, benzozir, maizir, poloxamer or their mixture. Said invention can be made into preparations of injection, nose drops, ointment and oral liquor, etc, and can be prepared by adopting ethyl alcohol injection method, film dispersion method, inversed phase evaporation method, hydration method, extrusion method, mechanical method and pH gradient method.

Description

Technical field: [0001] The invention relates to the technical field of medicine, in particular to an apigenin vesicle preparation formed by a nonionic surfactant and apigenin and a preparation process thereof. Background technique: [0002] Apigenin (5,7,4'-trihydroxyflavone) belongs to flavonoids, widely present in the leaves of Apium graveolens var.dulce; the whole herb of Selaginella tamariscina; Cypress (Sabina chinensis) leaves. Apigenin has a variety of pharmacological activities: (1) Anti-tumor effect: Apigenin can cause breast cancer cells (MCF-7 and MDA-MB-468) to undergo G2 / M phase arrest. After the cells were treated with apigenin for 3 days, the growth of the cells was significantly inhibited, and the IC50 were 7.18 μg / ml and 8.19 μg / ml respectively; apigenin can selectively induce human prostate cancer cells and human leukemia cells HL-60 Cycle arrest and induce apoptosis. The mechanism of its induction of apoptosis may be realized through the release of cyt...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61K9/06A61K9/08A61K9/10A61K9/50A61K47/34A61P35/00A61P25/24A61P19/02A61P9/10A61P7/02A61K47/26A61K47/28
Inventor 陈大为刘丹胡海洋赵秀丽
Owner SHENYANG PHARMA UNIVERSITY
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