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Preparation method of prostaglandin E1

A technology of alprostadil and dil grease, which is applied in the field of preparation of alprostadil lipid microspheres, can solve problems such as insufficient binding force, achieve the effect of improving encapsulation efficiency, improving encapsulation efficiency, and reducing degradation products

Active Publication Date: 2010-03-10
辽宁中海康生物制药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But because the binding force between it and phospholipids is still not enough, there will still be about 10% or even more alprostadil dispersed in the water phase

Method used

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  • Preparation method of prostaglandin E1

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] prescription:

[0058] Alprostadil (PGE 1 ) 5mg

[0059] Refined soybean oil 100g

[0060] Egg yolk lecithin 12g

[0061] Oleic acid 1.8g

[0062] Glycerin 22.5g

[0063]

[0064] Add water for injection to 1000ml

[0065] crafting process:

[0066] (1) Get 20 mg of egg yolk lecithin, add ethanol to dissolve, add 5 mg of alprostadil, stir to dissolve, and evaporate ethanol with nitrogen while stirring;

[0067] (2) Preparation of the oil phase: heating the refined soybean oil to 70° C., adding egg yolk lecithin, oleic acid and step (1) alprostadil respectively, and stirring to dissolve it;

[0068] (3) Preparation of water phase: add glycerin to water to dissolve, and heat to 70°C;

[0069] (4) Preparation of colostrum: Add the oil phase of step (2) into the water phase of step (3), at a temperature of 70°C, high-speed shear dispersion, shear speed of 8000rpm, and time of 10 minutes to form colostrum, and quickly cool...

Embodiment 2

[0073] prescription:

[0074] Alprostadil 5mg

[0075] Refined soybean oil 50g

[0076] Medium Chain Triglycerides 50g

[0077] Egg yolk lecithin 12g

[0078] Oleic acid 1.8g

[0079] Glycerin 22.5g

[0080]

[0081] Add water for injection to 1000ml

[0082] crafting process:

[0083] (1) Get 20 mg of egg yolk lecithin, add ethanol to dissolve, add 5 mg of alprostadil, stir to dissolve, and evaporate the ethanol to dryness under reduced pressure;

[0084] (2) Preparation of oil phase: mix refined soybean oil and medium-chain triglycerides, heat to 70° C., add egg yolk lecithin, oleic acid and step (1) alprostadil respectively, and stir to dissolve it;

[0085] (3) Preparation of water phase: add glycerin to water to dissolve, and heat to 70°C;

[0086] (4) Preparation of colostrum: Add the oil phase of step (2) into the water phase of step (3), at a temperature of 70°C, high-speed shear dispersion, shear speed of 8000rpm, and tim...

Embodiment 3

[0090] Alprostadil 5mg

[0091] Cottonseed Oil 100g

[0092] Soy Lecithin 15g

[0093] Oleic acid 1.8g

[0094] Sucrose 120g

[0095] Appropriate amount of sodium hydroxide

[0096]

[0097] Add water for injection to 1000ml

[0098] (1) Get 50 mg of soybean lecithin, add ethyl acetate to dissolve, add 5 mg of alprostadil, stir to dissolve, evaporate ethyl acetate with nitrogen while stirring;

[0099] (2) Preparation of oil phase: heat cottonseed oil to 60°C, add soybean lecithin and oleic acid to dissolve, add step (1) alprostadil, stir to dissolve;

[0100] (3) Preparation of water phase: add sucrose into water to dissolve, and heat to 60°C;

[0101] (4) Preparation of colostrum: Add the oil phase of step (2) into the water phase of step (3), at a temperature of 60°C, high-speed shear dispersion, shear speed of 5000rpm, and a time of 30 minutes to form colostrum, and quickly cool down to 15 ~30°C, adjust the pH value to 4.0~...

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Abstract

The invention relates to a preparation method of prostaglandin E1 which is prepared by the following materials: alprostadil, oil for injection, emulsifier, stabilizer, isotonic agent and water for injection. The method comprises the following steps: firstly dissolving medical materials and phospholipids into suitable solvent and then adding to oil phase after removing solvent. The product preparedby the method has an obvious improvement on entrapment rate and reduces generation of degradation products.

Description

technical field [0001] The invention relates to a preparation method of alprostadil lipid microspheres. Background technique [0002] Alprostadil, also known as prostaglandin E 1 (PGE 1 ), is a highly active physiologically active substance that can inhibit platelet aggregation, thromboxane A 2 generation, atherosclerosis lipid plaque formation and the role of immune complexes, and can expand the pharmacological effects of peripheral and coronary vessels, mainly used for the treatment of chronic arterial occlusion (thromboangiitis obliterans, arteriosclerosis obliterans Etc.) limb ulcers and resting pain in limbs caused by microvascular circulation disorders, improving cardiovascular and cerebrovascular microcirculation disorders and adjuvant treatment of chronic hepatitis. The species currently on the market are alprostadil powder injection (cyclodextrin inclusion compound) and alprostadil injection (emulsion), and its properties are a kind of white milky liquid. During...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/5575A61P1/16A61P9/00A61P9/10
Inventor 黄海宋华先马红萍张占军程宇刘启悦
Owner 辽宁中海康生物制药股份有限公司
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