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Alprostadil liposome microsphere preparation

A technology of lipid microspheres and dill fat, which is applied in the field of pharmaceutical preparations and can solve the problems of short validity period and poor stability

Inactive Publication Date: 2010-06-02
BEIJING TIDE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Aiming at the problems of poor stability and short validity period generally existing in the current alprostadil preparations, the purpose of the present invention is to provide a drug that can significantly prolong the validity period of the drug and avoid Alprostadil lipid microsphere injection with defects in existing preparations and preparation method thereof

Method used

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  • Alprostadil liposome microsphere preparation
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040]Preheat 80g of soybean oil for injection to 60-70°C, add 20g of refined soybean lecithin, 1g of stabilizer (mass ratio is oleic acid: coenzyme Q10 = 1:1), stir with hand to form a uniform oil phase, then slowly add 7mg of prostaglandin Dil raw material, stir at 60-70°C at high speed (8000 rpm) for 3 minutes to make it evenly dissolve in the oil phase; dilute 20g of glycerin for injection with an appropriate amount of water for injection preheated to 60-70°C Finally, a uniform water phase is formed; the above water phase is poured into the mixer, and the oil phase is slowly dropped into the water phase under the stirring condition of 10000 rpm, stirred for 10 minutes, and milky white colostrum is formed after uniform dispersion; Add the colostrum to the water for injection preheated to 60-70°C to reach the full amount, transfer it to a high-pressure homogenizer, homogenize it for 5-8 times under the pressure of 5000-15000Psi, take samples to measure the particle size until...

Embodiment 2

[0042] Preheat 100g of soybean oil for injection to 60-70°C, add 25g of refined soybean lecithin, 1.5g of stabilizer (mass ratio: cholesterol:vitamin E=1:1), stir with hand to form a uniform oil phase, then slowly add 7mg of prostaglandin Dil raw material, stir at 60-70°C at high speed (8000 rpm) for 3 minutes to make it evenly dissolve in the oil phase; dilute 20g of glycerin for injection with an appropriate amount of water for injection preheated to 60-70°C Finally, a uniform water phase is formed; the above water phase is poured into the mixer, and the oil phase is slowly dropped into the water phase under the stirring condition of 10000 rpm, stirred for 10 minutes, and milky white colostrum is formed after uniform dispersion; Add the colostrum to the water for injection preheated to 60-70°C to reach the full amount, transfer it to a high-pressure homogenizer, homogenize it for 5-8 times under the pressure of 5000-15000Psi, take samples to measure the particle size until th...

Embodiment 3

[0044] 100g soybean oil for injection is preheated to 60~70 ℃, adds the mixture (mass ratio of 5: 1) of 20g refined lecithin and polyoxyethylene castor oil, 2g stabilizer (mass ratio is sodium oleate: Vitamin C = 1: 1), after hand-held stirring to form a uniform oil phase, slowly add 15 mg of alprostadil bulk drug, and stir at a high speed (8000 rpm) at 60 to 70 ° C for 3 minutes to make it evenly dissolve in the oil phase; Glycerin for injection is diluted with an appropriate amount of water for injection preheated to 60-70°C to form a uniform water phase; pour the above water phase into the mixer, and slowly drop the oil phase into the In the water phase, stir for 10 minutes to form milky white colostrum after uniform dispersion; add the colostrum to the water for injection preheated to 60-70°C to reach the full amount, transfer it to a high-pressure homogenizer, and place it under a pressure of 5000-15000Psi Homogenize 5 to 8 times, take samples to measure the particle size...

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Abstract

The invention provides an alprostadil liposome microsphere preparation, in particular to an alprostadil liposome microsphere preparation containing a stabilizing agent, wherein the stabilizing agent contains a component A and a component B; the component A is selected from one or more of oleic acid, sodium oleate and cholesterol; the component B is selected from one or more of vitamin E, coenzymes Q10, propylgallate, ascorbyl palmitate and vitamin C. The stabilizing agent can guarantee that alprostadil is in a relatively stable weak acidic environment, prevent the alprostadil from being oxidized and degraded, reduce the interfacial tension of oil phases and water phases of the microsphere preparation, stabilizes phospholipids bimolecular films of liposome microspheres and has the dual functions of improving the chemical stability and the preparation stability of active medicaments so as to greatly reduce the degradation rate of the alprostadil, obviously prolong the validity period and the storage life of medicaments and avoid the defects of adverse reactions, toxic and side effects, inconvenient use, and the like of the traditional alprostadil preparations.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to an alprostadil lipid microsphere preparation, in particular to an alprostadil lipid microsphere preparation containing a stabilizer. Background technique [0002] Alprostadil (PGE 1 ), also known as prostaglandin E1, the chemical name is (1R, 2R, 3R)-3-hydroxy-2[(E)-(3S)-3-hydroxy-1-octenyl]-5-oxocyclopentyl Alkaneheptanoic acid, which belongs to natural prostaglandin (PG) analogs, is a highly active endogenous physiologically active substance, which can be synthesized in various tissue cells of the human body. [0003] PGE 1 It has a variety of pharmacological activities: it can significantly expand peripheral and coronary vessels, improve hemodynamics and hemorheology; inhibit platelet aggregation, reduce platelet hyperreactivity and thromboxane A (TXA) levels; inhibit free Ca of vascular smooth muscle cells 2+ , Inhibit the release of norepinephrine from vascular ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/5575A61K47/44A61K47/14A61K47/22A61K47/28A61K47/34A61P7/02A61P9/00A61P9/10
Inventor 刘红星张扬程栎杨青松王伟周丽莹肖萱
Owner BEIJING TIDE PHARMA
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