Unlock instant, AI-driven research and patent intelligence for your innovation.

A kind of alprostadil fat emulsion for injection

A technology of dil fat and alprostadil, which is applied in the field of alprostadil fat emulsion for injection, can solve the problems of high price, short validity period, and limited sources, and achieve the effect of solving particle size changes

Active Publication Date: 2019-07-23
BEIJING LANDAN PHARMA TECH
View PDF4 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Because alprostadil injection exists in the form of emulsion, there is still a part of the drug that will degrade when it meets water, resulting in the following quality problems: (1) the degradation product PGA of alprostadil injection 1 The content of X-ray is as high as 60% (National Standard WS1-(X-041)-2002Z-2008); (2) The validity period is short, only 12 months (0~5℃)
Although human albumin can solve the problem of freeze-drying protection, its source is limited and expensive, which is not suitable for the wide clinical application of this product
[0007] In order to solve this problem in the patent document CN201010168597.2, cyclodextrins and sugars are used together as a freeze-drying protectant to increase the stability of the drug. The principle is that the cyclodextrin wraps the drug to increase the stability without It is said that cyclodextrin itself has certain nephrotoxicity and hemolysis when used for intravenous injection. It is said that after the cyclodextrin wraps the drug, it increases the water solubility, and the drug will be distributed in a larger proportion in the water phase instead of the oil phase. Therefore, there are hidden dangers in the safety of preparations

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • A kind of alprostadil fat emulsion for injection
  • A kind of alprostadil fat emulsion for injection
  • A kind of alprostadil fat emulsion for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] prescription:

[0030]

[0031] Process:

[0032] (1) Preparation of water phase: add sucrose into water to dissolve, heat to 65°C, add phosphatidylcholine (PC-98T, Shanghai Everite) for high-speed shear dispersion, and set aside;

[0033] (2) Preparation of the oil phase: heat the refined soybean oil to 65°C, add egg yolk phosphatidylglycerol (EPG, Shanghai Everett) for high-speed shear dispersion, add alprostadil, and stir to dissolve it;

[0034] (3) Preparation of colostrum: Add the oil phase of step (2) into the water phase of step (1), at a temperature of 65°C, high-speed shear dispersion, shear speed of 10,000 rpm, and time of 15 minutes, to form colostrum;

[0035] (4) High-pressure homogenization: Adjust the pH of the colostrum in step (3) to 6.9-7.1, and then use a microfluidizer for high-pressure homogenization 3 times at a pressure of 1000-1200 bar;

[0036] (5) Preliminary filtration: Prefilter the refined milk in step (4) through a 0.45 μm filter memb...

Embodiment 2

[0040]

[0041]

[0042] Process:

[0043] (1) Preparation of water phase: add sucrose into water to dissolve, heat to 65°C, add phosphatidylcholine (PC-98T, Shanghai Everite) for high-speed shear dispersion, and set aside;

[0044] (2) Preparation of the oil phase: heat the refined soybean oil to 65°C, add egg yolk phosphatidylglycerol (EPG, Shanghai Everett) for high-speed shear dispersion, add alprostadil, and stir to dissolve it;

[0045] (3) Preparation of colostrum: Add the oil phase of step (2) into the water phase of step (1), at a temperature of 65°C, high-speed shear dispersion, shear speed of 10,000 rpm, and time of 15 minutes, to form colostrum;

[0046] (4) High-pressure homogenization: Adjust the pH of the colostrum in step (3) to 6.9-7.1, and then use a microfluidizer for high-pressure homogenization 3 times at a pressure of 1000-1200 bar;

[0047] (5) Preliminary filtration: Prefilter the refined milk in step (4) through a 0.45 μm filter membrane;

[00...

Embodiment 3

[0051] prescription:

[0052]

[0053] Process:

[0054] (1) Preparation of water phase: add sucrose into water to dissolve, heat to 65°C, add phosphatidylcholine (PC-98T, Shanghai Everite) for high-speed shear dispersion, and set aside;

[0055] (2) Preparation of the oil phase: heat the refined soybean oil to 65°C, add egg yolk phosphatidylglycerol (EPG, Shanghai Everett) for high-speed shear dispersion, add alprostadil, and stir to dissolve it;

[0056] (3) Preparation of colostrum: Add the oil phase of step (2) into the water phase of step (1), at a temperature of 65°C, high-speed shear dispersion, shear speed of 10,000 rpm, and time of 15 minutes, to form colostrum;

[0057] (4) High-pressure homogenization: Adjust the pH of the colostrum in step (3) to 6.9-7.1, and then use a microfluidizer for high-pressure homogenization 3 times at a pressure of 1000-1200 bar;

[0058] (5) Preliminary filtration: Prefilter the refined milk in step (4) through a 0.45 μm filter memb...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention provides an alprostadil fat emulsion for injection. The alprostadil fat emulsion comprises, by weight, 1 part of alprostadil, 2, 000 to 8, 000 parts of oil for injection, 1, 200 to 2, 400 parts of phosphatidylcholine, 1 to 9 parts of phosphatidylglycerol and 12, 000 to 24, 000 parts of a freeze-drying protective additive. The alprostadil fat emulsion for injection improves stability of alprostadil and particle size stability before and after freeze-drying, and a freeze-dried product has a better physical form.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an alprostadil fat emulsion for injection. Background technique [0002] Alprostadil injection was first listed in Japan, using fat emulsion drug loading technology, consisting of drug, soybean oil, refined egg yolk lecithin, oleic acid, glycerin and pH regulator, and its preparation method is to dissolve the drug in fatty oil In the method, refined lecithin is used as emulsifier, oleic acid is used as auxiliary emulsifier, O / W type drug-loaded fat emulsion is prepared by high-pressure homogenization, and the average particle size of the emulsion is 200nm. Alprostadil injection adopts the drug-loading method of fat emulsion, and the drug is encapsulated in the oil phase, which greatly reduces the occurrence of irritation. It has the following advantages: (1) Targeting: It has a higher affinity to the blood vessel wall of the inflammatory site, can deposit on the wall o...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K9/19A61K31/5575A61K47/24A61P9/10A61P9/12
Inventor 不公告发明人
Owner BEIJING LANDAN PHARMA TECH