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Chloroquine liposomes freeze-dried powder injection and preparation method thereof

A technology of freeze-dried powder injection and chloroquine lipid, applied in the field of medicine, can solve the problems of poor chloroquine encapsulation rate, high cost, high price and the like, and achieve the effects of low cost, easy operation and good stability

Active Publication Date: 2008-10-15
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] It has been reported in foreign literature that the direct reverse evaporation method is used to prepare chloroquine liposomes in one step, but the phospholipid components used in this method must contain a certain proportion of negatively charged phospholipids in order to achieve an ideal drug encapsulation efficiency.
If only neutral natural phospholipids such as lecithin or soybean lecithin are used, the encapsulation efficiency of chloroquine is poor
In addition, in terms of product cost, negatively charged phospholipids are synthetic phospholipids, which are more expensive than ordinary natural phospholipids
It can be seen that this liposome preparation method has great limitations and high cost in the selection of phospholipids

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Weigh 500mg of soybean lecithin, 100mg of cholesterol and 20mg of vitamin E, dissolve in 20ml of ether, mix well, put the solution in a round-bottomed flask, and evaporate the organic solvent under reduced pressure with a rotary evaporator on a constant temperature water bath at 37-40°C , so that film-forming materials such as phospholipids form a uniform lipid film at the bottom of the flask; add 10ml of 0.1M citric acid-sodium citrate buffer solution (pH3.6) to the lipid film, and rotate on a rotary evaporator until the lipid film hydration changes into a milky white liposome suspension, ultrasonically crushed to reduce particle size. Weigh 10 mg of chloroquine phosphate, dissolve it in the liposome suspension, adjust the pH to 7.0 with disodium hydrogen phosphate, and leave it at room temperature for 20 minutes. The encapsulation efficiency is 93%, and the average particle size is 110 nm. 1000mg of trehalose was dissolved in the liposome suspension, sterile filtered ...

Embodiment 2

[0020] Weigh 420mg of dipalmitoylphosphatidylcholine (DPPC), 60mg of phosphatidylethanolamine (PE), 100mg of cholesterol and 20mg of vitamin E, dissolve in 10ml of ether, mix well, place the solution in a ground-mouthed round-bottomed flask, Use a rotary evaporator to evaporate the organic solvent under reduced pressure on a 37-40°C constant temperature water bath, so that the film-forming materials such as phospholipids form a uniform lipid film at the bottom of the flask; add 5ml of 0.1M citric acid-sodium citrate buffer solution (pH3. 6), rotate on a rotary evaporator until the lipid film is hydrated to become a milky white liposome suspension, and ultrasonically pulverize to reduce the particle size. Weigh 10 mg of chloroquine phosphate, dissolve it in the liposome suspension, adjust the pH to 7.0 with disodium hydrogen phosphate, and leave it at room temperature for 20 minutes. The encapsulation efficiency is 94%, and the average particle size is 200 nm. 1000mg of trehalo...

Embodiment 3

[0022] Weigh 1000mg of lecithin, 100mg of cholesterol and 20mg of vitamin E, dissolve in 100ml of ether, mix well, then add 20ml of 0.1M citric acid-sodium citrate buffer solution (pH3.6), the two are mixed to form an emulsion, and the emulsion is placed in In a round-bottomed flask with a ground mouth, use a rotary evaporator to evaporate the organic solvent under reduced pressure on a constant temperature water bath at 37-40°C until it becomes a milky white liposome suspension, and reduce the particle size by high-pressure emulsification. Weigh 10 mg of chloroquine phosphate, dissolve it in the liposome suspension, adjust the pH to 7.4 with disodium hydrogen phosphate, and leave it at room temperature for 20 minutes. The encapsulation efficiency is 90%, and the average particle size is 120 nm. 500mg of sucrose and 500mg of lactose were dissolved in the liposome suspension, sterile filtered (the pore size of the membrane filter was 220nm), divided into vials, and freeze-dried....

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Abstract

The invention provides a chloroquine liposome lyophilized powder for injection, comprising (by weight parts) the chloroquine or the salt formed by the chloroquine and acid 1part, phospholipid 2-100 parts, cholesterol 1-35 parts, vitamin E 0.5-5.0 and excipients. The preparation method comprises two steps, including the preparation of blank liposome, and the preparation of drug-carrying liposome through the pH gradient method. The injection has the advantages of reasonable design, wide carrier selection range, high drug entrapment efficiency, and good stability. The preparation method has the advantages of easy operation, low cost, and good controllability and repeatability.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a chloroquine liposome freeze-dried powder injection and a preparation method thereof. Background technique [0002] Since chloroquine was synthesized in the 1930s, it has been used as a safe, effective and inexpensive drug for the prevention and treatment of malaria parasite infection. At the same time, it also has anti-inflammatory, immunosuppressive and immunoregulatory effects, and is suitable for many diseases such as reducing fever, inhibiting arthritis, eliminating rashes, anticoagulation and lowering blood lipids. The most commonly used form clinically is its phosphate salt - chloroquine phosphate. It not only has obvious improvement effect in the treatment of systemic lupus erythematosus and rheumatoid arthritis, but also is a safe, effective and well-tolerated slow-acting antirheumatic drug. Studies in recent years have shown that chloroquine also has cer...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/4706A61K47/24A61K47/34A61P33/06A61P29/00A61P37/02A61K9/127
Inventor 邱利焱荆娜
Owner ZHEJIANG UNIV
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