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Apitoxin liposome preparation and preparation method thereof

A liposome preparation and melittin technology, applied in the preparation of melittin liposome preparation, the field of melittin liposome preparation, can solve the problem that melittin vascular irritation can not be completely eliminated, and improve the bioavailability , prolong the cycle time, improve the effect of compliance

Inactive Publication Date: 2011-05-04
安徽省百春制药有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the course of the experiment, it was found that ordinary liposomes of melittin still cannot completely eliminate the blood vessel irritation of melittin

Method used

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  • Apitoxin liposome preparation and preparation method thereof
  • Apitoxin liposome preparation and preparation method thereof
  • Apitoxin liposome preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] Take by weighing 1.2g soybean lecithin (purity is greater than 92% phosphatidylcholine), 150mg cholesterol is dissolved in 50ml ethanol, ultrasonic, dissolves; Under 50 ℃, 400rpm magnetic stirring conditions, above-mentioned solution is slowly injected into 90ml isotonic saline ( Containing 5% poloxamer 188, which is percentage by weight, the same below), the two are mixed and stirred for 2 hours until the ethanol is completely evaporated to dryness to obtain a liposome coarse suspension, which is homogenized under high pressure to reduce the particle size (5000psi, 3 times), that is. Finally, 60 mg of melittin was dissolved in 30 ml of isotonic saline (containing 5% poloxamer 188), then mixed with the above solution, and 12 g of lactose was added to dissolve in the mixed solution, after sterile filtration (membrane filter pore size 0.2 μm) , the subsequent filtrate is dispersed without sub-packing in vials, and freeze-dried.

[0069] After the freeze-dried liposomes w...

Embodiment 2

[0075] Weigh 1g of soybean lecithin (purity greater than 93%), and dissolve 200mg of cholesterol in dichloromethane, place the solution in a ground eggplant-shaped bottle, and evaporate it under reduced pressure on a rotary evaporator on a constant temperature water bath at 25°C at 100rpm. Organic solvent, so that phospholipids and cholesterol form a uniform film on the bottom of the bottle, and then put it in a vacuum desiccator to evacuate overnight, and set aside. In addition, 100 mg of melittin was dissolved in 200 ml of isotonic 5% glucose solution (containing 2% poloxamer 188), this solution was added to the above-mentioned eggplant-shaped bottle, and the membrane was washed by rotating at 37 ° C until milky white lipids were formed. Body suspension, homogenized under high pressure, reduced particle size (5000psi, 3 times), that is. Dissolve 20 g of trehalose in liposomes, filter aseptically (the pore size of the membrane filter is 0.2 μm), divide the filtrate into vials...

Embodiment 3

[0078] After the subsequent filtrate after aseptic filtration in Example 1 is subpackaged in vials, through repeated freezing and thawing (freezing temperature is -50 ℃, freezing time is 3h, melting temperature is 4 ℃, melting time is 30min, repeated freezing and thawing The number of times is 2 times), freeze-dried to obtain freeze-dried powder injection.

[0079] After the freeze-dried liposomes were stored at 4°C for 3 months, the melittin content was 95.9%. After adding an appropriate amount of injection-grade isotonic glucose solution, the liposome encapsulation efficiency was 96.8%, and the particle size was 214nm. The encapsulation efficiency remained basically unchanged after being diluted with 5% glucose solution or 0.9% normal saline for 8 hours.

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Abstract

The invention relates to the field of medicine preparation, in particular to a melittin lipidosome preparation. The lipidosome preparation is composed of one part of melittin, 5-40 parts of phospholipid, 1.3-10 parts of cholesterin and 10-140 parts of poloxamer. The invention also discloses the preparing method of the melittin lipidosome preparation. The melittin lipidosome preparation not only can delay the medicine release in the lipidosome, prong the circulating time in the blood and improve the bioavailability of the medicine, but also can obviously reduce the side effect of the medicine and improve the adaptability of a patient.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a melittin liposome preparation, and also discloses a preparation method of the melittin liposome preparation. Background technique [0002] Bee venom (bee venom) is a transparent venom with aromatic odor secreted by worker bee venom glands. It is a complex mixture, mainly containing protein polypeptides, enzymes, biogenic amines and other substances, of which peptides, Enzymes and non-peptides constitute the main active components of bee venom. Peptides include melittin, the main substance of apalmin response. Enzymes mainly include more than 55 kinds of enzyme substances, of which phospholipase A 2 It is the main substance that produces allergic reactions after bee stings. Non-peptides include histamine, various biogenic amines that are associated with pain following bee stings. [0003] Among the bee venom, the most researched is the bee venom hemolytic peptide, ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/17A61K9/127A61K47/24A61P35/00
Inventor 柯学程文显陈真郭青龙王长江杨勇
Owner 安徽省百春制药有限公司
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