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Alprostadil lipid complexes and micelle composition thereof for injection

A technology of dil lipid and alprostadil, which is applied in the direction of drug combination, drug delivery, and medical preparations of non-active ingredients, etc., can solve the problems of difficulty in normalizing the pharmacological activity and instability of alprostadil, etc., and achieve improved injection efficiency. Safety, reducing the inactivation of alprostadil, and increasing the effect of stability

Inactive Publication Date: 2009-05-27
SHENYANG WOSEN PHARMA INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, many domestic pharmaceutical companies have produced alprostadil for injection, but alprostadil is very unstable in water and prone to degradation. In addition, alprostadil also has many adverse reactions, which makes it difficult for its pharmacological activity to play normally.

Method used

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  • Alprostadil lipid complexes and micelle composition thereof for injection
  • Alprostadil lipid complexes and micelle composition thereof for injection
  • Alprostadil lipid complexes and micelle composition thereof for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Take 10mg of alprostadil, 2.0g of egg yolk lecithin, 400mg of sodium cholesterol sulfate, and 10mg of vitamin E, and dissolve them in methanol at 30°C as the organic phase; dissolve 0.5g of PEG400 in 90ml of water for injection, and heat to 30°C as the water phase , inject the organic phase into the water phase under stirring at 30°C, continue to stir for 5 minutes, and then evaporate the methanol under reduced pressure to obtain the alprostadil lipid complex with blue opalescence and the micelle composition for injection thereof. Make up with water to a total volume of 100ml, and filter to sterilize with a 0.22μm microporous membrane.

[0043] Add 5% (w / v) trehalose to the obtained alprostadil lipoplex and the aqueous dispersion of the micelle composition for injection, freeze-dry under aseptic operation, and divide into packages to obtain.

[0044] The lyophilized preparation was diluted with physiological saline, and its average particle diameter measured was 72.8 ± ...

Embodiment 2

[0046] Take 20mg of alprostadil, 3.0g of soybean lecithin, and 500mg of sodium cholesterol sulfate, and dissolve them in absolute ethanol at 35°C as the organic phase; dissolve 1.0g of PEG200 in 90ml of water for injection, heat to 35°C as the water phase, and Under stirring at 35°C, inject the organic phase into the water phase, continue to stir for 10 minutes, and then evaporate the ethanol under reduced pressure to obtain the alprostadil lipid complex with blue opalescence and its micelle composition for injection, which is replenished with water for injection. When the total volume reaches 100ml, it is sterilized by filtering through a 0.22μm microporous membrane, and then aliquoted.

Embodiment 3

[0048] Take 500 mg of alprostadil, 10 g of soybean lecithin, and 5 g of sodium cholesterol sulfonate, and dissolve them in tetrahydrofuran at 35 ° C as the organic phase; dissolve 5 g of poloxamer 188 in 950 ml of water for injection, heat to 35 ° C as the water phase, and Under stirring, inject the organic phase into the water phase, continue to stir for 10 minutes, and then evaporate the tetrahydrofuran under reduced pressure to obtain the alprostadil lipid complex with blue opalescence and the micelle composition for injection thereof, and add water for injection to make up to the total concentration. The volume is 1000ml, and it is sterilized by filtration through a 0.22μm microporous membrane.

[0049] Add 5% (w / v) trehalose to the obtained alprostadil lipoplex and the aqueous dispersion of the micelle composition for injection, freeze-dry under aseptic operation, and divide into packages to obtain.

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Abstract

The invention belongs to the pharmaceutical preparation field and relates to an alprostadil lipid compound, a micellar compound used in the injection of the alprostadil lipid compound and a preparation method of the alprostadil lipid compound. The alprostadil lipid compound and the micellar compound used in the injection of the alprostadil lipid compound are composed of alprostadil with a therapeutic dose, phospholipid, cholesterol sulfate or / and similar cholesterol derivative, additive and injection water. The alprostadil lipid compound and the micellar compound used in the injection of the alprostadil lipid compound have the advantages of small side effect, low blood vessel simulation, high drug-loading rate, narrow particle size distribution, capability of filtering and degerming, good pharmaceutical stability, etc.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to an alprostadil lipid complex and a micelle composition for injection thereof. More specifically, the present invention relates to a kind of alprostadil lipoplex and its injectable micelle composition that can improve drug encapsulation efficiency, reduce irritation, filter sterilization, and stable storage and its injection Micellar compositions and methods for their preparation. Background technique [0002] Alprostadil (PGE 1 ), also known as prostaglandin E 1 , is a highly active endogenous physiologically active substance, which has obvious pharmacological effects such as expanding peripheral and coronary vessels, inhibiting platelet aggregation, and inhibiting the formation of atherosclerotic lipid plaques. It is used for the treatment of myocardial infarction, thrombotic Phlebitis, obliterative arteriosclerosis, chronic arterial occlusive disease such as thromboa...

Claims

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Application Information

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IPC IPC(8): A61K31/5575A61K9/00A61K47/24A61P7/02A61P9/10A61P9/14
Inventor 德瑞克·王贺晓玲徐飒
Owner SHENYANG WOSEN PHARMA INST
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