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Alprostadil lyophilized microemulsion, and preparation method and application thereof

A technology of alprostadil and freeze-dried microemulsion, applied in the field of alprostadil freeze-dried microemulsion and its preparation, can solve the problems of insufficient clinical safety and stability of preparations, complicated process of alprostadil dry emulsion, etc. Duration of efficacy, reduced irritation, reduced impurity content

Active Publication Date: 2012-11-07
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The technical problem to be solved in the present invention is exactly to provide a kind of new alprostadil preparation and preparation method thereof for existing alprostadil dry emulsion process complexity, the deficiency of clinical safety and stability of preparation

Method used

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  • Alprostadil lyophilized microemulsion, and preparation method and application thereof
  • Alprostadil lyophilized microemulsion, and preparation method and application thereof
  • Alprostadil lyophilized microemulsion, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] prescription:

[0024]

[0025] crafting process:

[0026] (1) Mix and heat MCT, alprostadil, oleic acid, glycerin and Solutol HS 15 to dissolve them all, as the oil phase, add glucose to water, stir to dissolve, and use it as the water phase;

[0027] (2) At 30-50°C, slowly add the water phase to the oil phase while stirring to form a microemulsion, and then stir for 0.5h to form a stable and uniform microemulsion;

[0028] (3) adjust the pH of the microemulsion to 6.0-7.0, then pass the microporous membrane of the gained microemulsion through a 0.22 μm microporous membrane, and filter and sterilize;

[0029] (4) Finally, the sterilized microemulsion is freeze-dried to remove moisture, and then under the protection of nitrogen, the freeze-dried product is covered with an aluminum cover and taken out of the box;

[0030] (5) Steps (1) to (4) are all operated under nitrogen protection.

Embodiment 2

[0032] prescription:

[0033]

[0034] crafting process:

[0035] (1) Mix and heat MCT, alprostadil, oleic acid, glycerin, and Cremophor RH 40 to dissolve them all, as the oil phase, add glycine, mannitol, etc. into water, stir to dissolve, and use it as the water phase;

[0036] (2) At 30-50°C, slowly add the water phase to the oil phase while stirring to form a microemulsion, and then stir for 0.5h to form a stable and uniform microemulsion;

[0037] (3) adjust the pH of the microemulsion to 6.0-7.0, then pass the microporous membrane of the gained microemulsion through a 0.22 μm microporous membrane, and filter and sterilize;

[0038] (4) Finally, the sterilized microemulsion is freeze-dried to remove moisture, and then under the protection of nitrogen, the freeze-dried product is covered with an aluminum cover and taken out of the box;

[0039] (5) Steps (1) to (4) are all operated under nitrogen protection.

Embodiment 3

[0041] prescription:

[0042]

[0043] crafting process:

[0044] (1) MCT, alprostadil, sodium oleate, glycerin, and Tween 80 are mixed and heated to make them all dissolve, and as the oil phase, lactose, trehalose, etc. are added to water, stirred to dissolve, and used as the water phase;

[0045] (2) At 30-50°C, slowly add the water phase to the oil phase while stirring to form a microemulsion, and then stir for 0.5h to form a stable and uniform microemulsion;

[0046] (3) adjust the pH of the microemulsion to 6.0-7.0, then pass the microporous membrane of the gained microemulsion through a 0.22 μm microporous membrane, and filter and sterilize;

[0047] (4) Finally, the sterilized microemulsion is freeze-dried to remove moisture, and then under the protection of nitrogen, the freeze-dried product is covered with an aluminum cover and taken out of the box;

[0048] (5) Steps (1) to (4) are all operated under nitrogen protection.

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Abstract

The invention discloses an alprostadil lyophilized microemulsion, and a preparation method and application thereof. The alprostadil lyophilized microemulsion includes: by weight percentage, 0.001% -0.1% of alprostadil, 1.0% -10.0% of grease, 1.0% -20.0% of an emulsifier, 1.0%-20.0% of co-emulsifier, 0.3% -1.6% of a stabilizer, 50.0% -90.0% of a cryoprotectant, and 0.0005 %-0.50 % of a pH conditioning agent. The aforementioned components are prepared into a microemulsion with particle size of 10 nm-50 nm. The microemulsion is filtrated and sterilized, then lyophilized, and ultimately prepared into an injection-used alprostadil lyophilized product with high stability, small re-dissolution particle size (average particle size within 50-100 nm) and good safety. The lyophilized microemulsion is characterized in that: microemulsion drops have a small particle size; the microemulsion can successfully realize filtration and sterilization before lyophilization; the impurity content is low; the side effects are less; the lyophilized product has physical stability and good security and has no hemolysis, irritation, allergy and other toxic irritant reactions; and the storage and transportation is convenient. Before use, adding an appropriate amount of water for injection, glucose solution or physiological saline as need, the lyophilized microemulsion is hydrated, oscillated, diluted, and redissolved into the microemulsion for use of intravenous injection.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a freeze-dried alprostadil microemulsion and a preparation method and application thereof. Background technique [0002] Alprostadil, also known as prostaglandin E1 (PGE 1 ), has high-efficiency and extensive physiological activities. This product not only has the effect of obviously dilating blood vessels, but also inhibits platelet aggregation, reduces blood viscosity and red blood cell aggregation, improves microcirculation, protects vascular endothelium, prevents the formation of atherosclerotic plates and improves nerve function. damage etc. After intravenous injection, it is weakly combined with plasma protein, and its half-life is 5-10 minutes. It is completely metabolized in the body, and 68% of the dose is metabolized by the first-pass effect of the liver, and excreted by the kidney in the form of metabolites. The drug is white needle-like crystal...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K9/107A61K31/5575A61P7/02A61P9/00A61P9/10
Inventor 何军刘洁杨亚妮陈允发
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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