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Composition and preparation of brain-targeted tanshinone oral oil-in-oil nanoemulsion

A technology of tanshinone and nanoemulsion, which is applied in the field of targeted preparation carriers, can solve the problems such as the limitation of the effect of diagnosis and treatment of the central nervous system, the difficulty of tanshinone entering the brain tissue, etc.

Inactive Publication Date: 2011-12-28
ANHUI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Tanshinone preparations currently on the market are oral capsules and injections, but after oral administration of capsules or injections, because the brain tissue is protected by the blood-brain barrier (BBB), it is difficult for tanshinone to enter the brain tissue, thereby causing cerebrovascular and central nervous system damage. (CNS) The effect of diagnosis and treatment has been greatly limited
Searches indicate that there are currently no brain-targeted oral tanshinone formulations

Method used

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Examples

Experimental program
Comparison scheme
Effect test

specific Embodiment 2

[0043] The tanshinone nanoemulsion used as brain targeting is characterized in that: the weight ratio of its components is:

[0044] salad oil 3g

[0045] Glycerin 2g

[0046] Lactate 1g

[0047] Span 2.8g

[0048] Tanshinone 0.6g.

[0049] Mix the above materials and stir gently until transparent.

specific Embodiment 3

[0050] The tanshinone inner rice milk used as brain targeting is characterized in that: the weight ratio of its components is:

[0051] Medium Chain Fatty Acid Glycerides 3g

[0052] Macrogol 400 2g

[0053] Oleic acid 1g

[0054] Polyoxyethylene phospholipids 1.8g

[0055] Tanshinone 1.5g.

[0056] Mix the above materials and stir gently until transparent.

[0057] Compared with the tanshinone suspension, the brain targeting index of the patented tanshinone nano-emulsion reached more than 3.6, and the brain tissue residence time was prolonged by 4 times after the above prescription was administered to rats. These results are the highest reported levels of tanshinone oral formulations in brain tissue known.

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Abstract

The invention relates to a brain-targeted tanshinone oral oil-in-oil type microemulsion preparation, which is suitable for preventing and treating cerebrovascular diseases and central nervous system diseases. The preparation of the present invention utilizes the combination of the characteristics of nanoparticles and the increase of the fat solubility of the preparation to promote the penetration of the drug through the blood-brain barrier, improve the selective enrichment of the drug in the brain, provide a higher concentration of the drug in the brain, and significantly increase the concentration of the drug in the brain. residence time, thereby improving the prevention and treatment of corresponding brain diseases.

Description

technical field [0001] The invention belongs to a targeted preparation carrier, in particular to a brain-targeted tanshinone oral oil-in-oil nanoemulsion, which can be used as a solvent or carrier for one or more brain active ingredients, and thus prepared into Nanoscale dispersed targeted formulations. Background technique [0002] Tanshinone has an obvious protective effect on cerebral ischemia-reperfusion injury, which is related to its protection of brain mitochondrial function, improvement of its energy metabolism, and antioxidant effect. At the same time, tanshinone can significantly reduce the expression of intercellular adhesion molecules and E-selectin on the surface of vascular endothelial cells after cerebral ischemia / reperfusion, reduce the infiltration of neutrophils in the tissue of cerebral ischemia, reduce the release of inflammatory mediators, and reduce the Improve blood-brain barrier permeability and reduce cerebral edema. Tanshinone is a highly effectiv...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/58A61P9/10A61P25/28
Inventor 鲁传华范燕妮
Owner ANHUI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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