Liposome spray and preparation method thereof

A technology of spray and liposome, applied in the field of liposome spray and its preparation, to achieve good antibacterial and antifungal effects, maintain drug stability, and promote drug absorption

Active Publication Date: 2011-11-30
ZHEJIANG HISUN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The technical problem to be solved in the present invention is to provide a new type of liposome spray-alcosome spray for the shortcomings of existing liposome sprays and ethosome preparations, which can promote the penetration of drugs faster. The skin or mucous membrane enters the deep tissue and blood circulation to exert quick-acting and long-acting therapeutic effects. This ethosome spray is suitable for a wide range of drugs, especially suitable for drugs with poor amphiphilicity or large molecular weight drugs, which can satisfy the needs of mucous membranes, The need for local or systemic treatment of skin, wounds, or cavities

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  • Liposome spray and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0024] Drugs with poor amphiphilicity or large molecular weight, such as oridonin, paclitaxel, curcumin, amphotericin B, dexamethasone, etc., are difficult to penetrate the complete skin, mucous membrane or biofilm barrier in the body, so the bioavailability is relatively low. Poor, it is difficult to play an effective therapeutic role. The first embodiment of the present invention utilizes natural phospholipid material egg yolk phospholipid and cholesterol as the main capsule material, hydroxyethyl starch as macromolecular aid dispersant, adds surfactant Tween 80 and antioxidant vitamin C, and adopts injection method to prepare Oridonin ethosome spray.

[0025] Preparation: Dissolve 20 mg of egg yolk phospholipid and 8 mg of cholesterol in 10 ml of ethanol, add 2 mg of Tween 80 and 8 mg of oridonin, and heat to 60°C to completely dissolve and form an organic phase. Another 0.05 g of hydroxyethyl starch (type 130 / 0.4) was dissolved in 20 ml of distilled water, and heated to 6...

Embodiment 2

[0030] The second implementation method of the present invention is basically the same as in Example 1, but the lipid material glyceryl monostearate is used as the main material to prepare oridonin ethosome spray.

[0031]Preparation: Dissolve 10 mg of glyceryl monostearate in 20 ml of ethanol, add 2 mg of Tween 80 and 8 mg of oridonin, and heat to 60°C to completely dissolve to form an organic phase. Another 0.05 g of hydroxyethyl starch (type 130 / 0.4) was dissolved in 10 ml of distilled water, and heated to 60° C. as the water phase. Inject the organic phase into the water phase, stir at 1000r / min for 10min to form a suspension of oridonin ethosome, cool to room temperature, add 10mg of vitamin C, fill it in a special bottle for spray, and obtain. Ethanol accounts for 60%-65% of the total volume of the spray solution.

[0032] Placement stability investigation: same as embodiment 1.

[0033] Experimental results showed that the initial particle size distribution of the ori...

Embodiment 3

[0035] The third embodiment of the present invention takes synthetic phospholipids as the main material, povidone is the macromolecule auxiliary dispersant, adds stabilizer propylene glycol, and adopts the injection method to prepare the curcumin elastosome spray.

[0036] Preparation: Dissolve 6 mg of hydrogenated soybean lecithin, 2 mg of dipalmitoylphosphatidylcholine (DPPC) phospholipid and 8 mg of cholesterol in 20 ml of ethanol, add 2 mg of Tween 80 and 6 mg of curcumin, and heat to 60 ° C to completely dissolve and form an organic phase. Another 50 mg of povidone (type K30) was dissolved in 5 ml of distilled water, and 20 mg of propylene glycol was added and heated to 60° C. as the water phase. Inject the organic phase into the water phase, stir at 1000r / min for 10min to form curcumin ethosome suspension, cool to room temperature, fill in a special spray bottle, and shake gently before use. Ethanol accounts for 75%-80% of the total volume of the spray solution.

[0037...

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Abstract

The invention relates to a novel liposome spraying agent and its preparation method. The spraying agent provided by the invention is prepared by the dispersion of medicine-loading ethosome in a solution system containing a macromolecular dispersing aid, and is used to helps raise the medicine loading capacity as well as the entrapment rate and promote medicines to penetrate through skin, mucous membrane or in vivo biomembrane barriers such that the medicines have long-acting effects. The novel liposome spraying agent has a wide medicine application range, especially is suitable for medicines of poor amphiphilicity or medicines of high molecular weight, and can be used to meet the requirement of treating local areas such as mucous membrane, skins, wounds and cavities or the whole body.

Description

【Technical field】 [0001] The invention belongs to the field of pharmaceutical preparations, more specifically, the invention relates to a liposome spray and a preparation method thereof. 【Background technique】 [0002] The skin and mucous membranes are a barrier for the human body to absorb drugs, and it is difficult for drugs with poor amphiphilicity or high molecular weight to penetrate the skin and mucous membranes into deep tissues and blood circulation to exert therapeutic effects. [0003] The current methods to promote drug penetration through the skin, mucous membrane or biofilm barrier in the body mainly rely on chemical absorption enhancers to increase drug absorption [Huang Jian, Gao Chunsheng, Mei Xingguo. Application of penetration enhancers in macromolecular drug mucosal drug delivery systems. Foreign Medicine: Pharmacy Volume. 2006, 33(6): 654-656]. Although chemical absorption enhancers can reduce the resistance of drugs passing through the skin and mucous m...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/12
Inventor 鲁翠涛赵应征
Owner ZHEJIANG HISUN PHARMA CO LTD
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