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Alprostadil injection and preparation method thereof

A technology of dil injection and alprostadil, which can be used in pharmaceutical formulations, emulsion delivery, and medical preparations containing active ingredients, etc., can solve problems such as cumbersome processes, reduced drug stability, and increased growth.

Inactive Publication Date: 2016-02-03
SHANGHAI SINE PHARMA LAB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] Chinese patent CN201110114324.4 proposes freeze-dried emulsion, but the addition of freeze-dried protective agent will reduce the stability of the drug, and after recovery, the particle size is large and the absorption effect is poor
[0007] Chinese patent CN200910058187.X increases the stability of the preparation by increasing the amount of surfactant poloxamer, but the use of poloxamer will increase the chance of hemolysis and bring safety hazards
[0008] Chinese patents CN201310655570.X and CN200910075878 provide the preparation method of alprostadil emulsion, wherein the oil phase is added to the water phase, sheared and stirred to form colostrum, and then the homogenization pressure is increased step by step, not only the process is cumbersome, but also the particle size of the emulsion is not uniform , poor stability

Method used

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  • Alprostadil injection and preparation method thereof
  • Alprostadil injection and preparation method thereof
  • Alprostadil injection and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0082] 1) Under the protection of nitrogen, add 18g of egg yolk lecithin and 1.2g of oleic acid into 100g of soybean oil, heat to 60°C, and stir at 4000 rpm to dissolve.

[0083] 2) Take 5 mg of alprostadil, dissolve it with 0.3 ml of absolute ethanol, add it into soybean oil and shear and dissolve it as the oil phase.

[0084] 3) Add 22.1 g of glycerol, an isotonic agent, into 300 ml of water for injection, heat to 60° C. and stir to dissolve, as the water phase.

[0085] 4) The above-mentioned oil phase and water phase are respectively added through a peristaltic pump, the oil phase addition speed is 10g / min, the water phase addition speed is 30g / min, sheared by an online shearing machine, the shear line speed is 40m / s, and water for injection is adjusted. The total amount reaches 1000ml to obtain colostrum. The colostrum is transferred to a high-pressure homogenizer and homogenized several times under a pressure of 1000 bar to obtain essence milk. Adjust the pH to 5.0-6.0...

Embodiment 2

[0087] 1) Under the protection of nitrogen, add 18g of egg yolk lecithin and 1.2g of oleic acid into 100g of soybean oil, heat to 60°C, and stir at 4000 rpm to dissolve.

[0088] 2) Take 5 mg of alprostadil, dissolve it with 0.3 ml of absolute ethanol, add it into soybean oil and shear and dissolve it as the oil phase.

[0089] 3) Add 22.1 g of glycerol, an isotonic agent, into 400 ml of water for injection, heat to 60° C. and stir to dissolve, as the water phase.

[0090] 4) The above-mentioned oil phase and water phase are respectively added through a peristaltic pump, the oil phase addition speed is 10g / min, the water phase addition speed is 40g / min, sheared by an online shearing machine, the shear line speed is 40m / s, and water for injection is adjusted. The total amount reaches 1000ml to obtain colostrum. The total amount of water for injection was adjusted to 1000ml, and the colostrum was transferred to a high-pressure homogenizer and homogenized several times under a p...

Embodiment 3

[0092] 1) Under the protection of nitrogen, add 18g of egg yolk lecithin and 1.2g of oleic acid into 100g of soybean oil, heat to 60°C, and stir at 4000 rpm to dissolve.

[0093] 2) Take 5 mg of alprostadil, dissolve it with 0.3 ml of absolute ethanol, add it into soybean oil and shear and dissolve it as the oil phase.

[0094] 3) Add 22.1 g of glycerol, an isotonic agent, into 500 ml of water for injection, heat to 60° C. and stir to dissolve, as the water phase.

[0095] 4) The above-mentioned oil phase and water phase were added through a peristaltic pump respectively, the oil phase was added at a speed of 10g / min, and the water phase was added at a speed of 50g / min, sheared by an online shearing machine, the shear line speed was 40m / s, and water for injection was adjusted. The total amount reaches 1000ml to obtain colostrum. The colostrum is transferred to a high-pressure homogenizer and homogenized several times under a pressure of 1000 bar to obtain essence milk. Adjus...

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Abstract

The invention provides an alprostadil injection and a preparation method thereof. The alprostadil injection is composed of alprostadil, oil for injection, an oleophylic emulsifying agent, an isotonic agent for injection and a stabilizing agent. The alprostadil injection contains alprostadil particles with an average particle size being 100-300nm and D90 being 150-350nm, and particle size change of the alprostadil injection is smaller than or equal to 10% after the alprostadil injection is placed for 12 months at the temperature of 2-8 DEG C.

Description

technical field [0001] The invention relates to an alprostadil injection emulsion and a preparation method thereof, in particular to a stable alprostadil injection emulsion and a preparation method thereof. Background technique [0002] Alprostadil, also known as prostaglandin E1, its chemical name is (1R,2R,3R)-3-hydroxy-2-[(E)-(3S)-3-hydroxy-1-octenyl]-5-oxo Cyclopentaneheptanoic acid, molecular formula: C 20 h 34 o 5 , molecular weight: 354.49. Alprostadil is a highly active endogenous physiological substance that can be synthesized in every tissue cell of the human body. [0003] Alprostadil has a variety of pharmacological effects: inhibiting platelet aggregation, thromboxane A2 generation, atherosclerotic lipid plaque formation and immune complexes, and can expand peripheral and coronary blood vessels, improve hemodynamics and blood rheology Inhibition of Ca in vascular smooth muscle cells 2+ , Inhibit the release of norepinephrine from vascular sympathetic nerve...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/5575
Inventor 房秋雨唐文燕施海斌史建国孙宁云张军东
Owner SHANGHAI SINE PHARMA LAB
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