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PGA1 ((13E,15S)-15-hydroxy-9-oxo-prosta-10,13-dien-1-oic acid)-containing lipid emulsion and preparation method thereof

A lipid emulsion and lipid technology, applied in the field of pharmaceutical preparations, can solve the problems of severe irritation of blood vessels, short validity period, poor stability of the main drug, etc., and achieve the effect of increasing curative effect

Active Publication Date: 2013-03-27
BEIJING TIDE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] For current PGA 1 The ubiquitous problems of poor stability of the main drug in water injections, severe irritation to blood vessels, and short validity period, the purpose of the present invention is to wrap the active ingredient PGA with lecithin with a soft shell structure 1 of oily solvents, thereby increasing the PGA 1 The stability of the main drug and the avoidance of PGA 1 The side effect of vascular stimulation, providing a PGA that can significantly prolong the effective period of the drug and avoid the defects of existing preparations 1 Lipid emulsion and preparation method thereof

Method used

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  • PGA1 ((13E,15S)-15-hydroxy-9-oxo-prosta-10,13-dien-1-oic acid)-containing lipid emulsion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Preheat 80g of soybean oil for injection to 60-70°C, add 15g of refined soybean lecithin, 1g of stabilizer (the mass ratio is oleic acid: coenzyme Q10=1:1), 5g of phosphatidylinositol, and stir with hand to form a uniform oil Slowly add 10mg of PGA1 API after the phase, stir at 60-70°C at high speed (8000 rpm) for 3 minutes to make it evenly dissolve in the oil phase; preheat 20g of glycerin for injection to 60-70°C with an appropriate amount Dilute with water for injection to form a uniform water phase; pour the above water phase into the mixer, slowly drop the oil phase into the water phase under the stirring condition of 10,000 rpm, stir for 10 minutes, and form milky white after uniform dispersion Colostrum; add the colostrum to the water for injection preheated to 60~70℃ to reach the full amount, transfer it to the high-pressure homogenizer, homogenize it for 8~10 times under the pressure of 10000~15000 Psi, and take samples to measure the particle size to The aver...

Embodiment 2

[0042] Preheat 100g of hydrogenated corn oil to 60-70°C, add 20g of egg yolk lecithin, 1.5g of stabilizer (mass ratio: cholesterol:vitamin E=1:1), 5g of sodium distearoylphosphatidylglycerol, and stir with a hand to form After the uniform oil phase, slowly add 20mg of PGA1 API, and stir at 60-70°C at high speed (8000 rpm) for 3 minutes to make it evenly dissolve in the oil phase; preheat 20g of glycerin for injection to 60 Dilute with water for injection at ~70°C to form a uniform water phase; pour the above water phase into the mixer, slowly drop the oil phase into the water phase under the stirring condition of 10,000 rpm, stir for 10 minutes, and disperse evenly Finally, milky white colostrum is formed; add the colostrum to the water for injection preheated to 60~70℃ to reach the full amount, transfer it to a high-pressure milk homogenizer, homogenize 8~10 times under the pressure of 10000~15000 Psi, and take samples for measurement particle size until the average particle ...

Embodiment 3

[0044] Preheat 100g cottonseed oil to 60-70℃, add 20g coconut oil C8 / C10 macrogol glyceride, 2g stabilizer (mass ratio is sodium oleate:vitamin C=1:1), 10g phosphatidylinositol , hand-held stirring to form a uniform oil phase, slowly add 30 mg of PGA1 raw material, and stir at 60-70 °C at high speed (8000 rpm) for 3 minutes to make it evenly dissolve in the oil phase; add 30 g of glycerin for injection with an appropriate amount Dilute with water for injection preheated to 60~70°C to form a uniform water phase; pour the above water phase into the mixer, slowly drop the oil phase into the water phase under the stirring condition of 10,000 rpm, and stir for 10 Minutes, evenly dispersed to form milky white colostrum; add the colostrum to the water for injection preheated to 60~70℃ to reach the full amount, transfer to the high-pressure milk homogenizer, and homogenize under the pressure of 10000~15000 Psi for 8~10 Once, take a sample and measure the particle size until the averag...

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Abstract

The invention provides a PGA1 ((13E,15S)-15-hydroxy-9-oxo-prosta-10,13-dien-1-oic acid)-containing lipid emulsion and a preparation method thereof, and in particular provides a PGA1 lipid emulsion preparation which is prepared by wrapping an oil component containing a main medicine PGA1 by a lipid agent which serves as a soft shell structure, wherein phosphatidylinositol or distearoyl phosphatidylglycerole sodium is added to the preparation, so that the stability of the main medicine PGA1 can be improved, and the main medicine PGA1 can be fused with the externally wrapped lipid agent structure better; and furthermore, the preparation prescription contains a stabilizer for improving the stability of the lipid agent structure. According to the PGA1-containing lipid emulsion, the phosphatidylinositol or distearoyl phosphatidylglycerole sodium is added and can be chemically combined with PGA1, so that the stability of PGA1 can be improved, PGA1 can be prevented from being damaged under the preparation conditions such as high temperature and high pressure, the useful life and the storage period of the medicine can be obviously prolonged, and adverse reaction such as vascular irritation and a plurality of defects such as toxic or side effect and inconvenience in use of conventional PGA1 preparation can be avoided.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a lipid emulsion, in particular to a PGA1 lipid emulsion capable of long-term stable storage and a preparation method thereof. Background technique [0002] The chemical name of prostaglandin A1 (PGA1) is (13E,15S)-15-Hydroxy-9-Oxo-Prosta-10,13-dien-1-Oic acid, which belongs to natural prostaglandin (PG) analogs. It is converted from cell membrane lipids in the body and is a highly active endogenous physiologically active substance. The clinical application of prostaglandin A1 in the treatment of essential hypertension, renal hypertension, diabetic hypertension and hypertension of pheochromocytoma has a significant antihypertensive effect. It has been reported in the literature that it can significantly reduce neuronal damage caused by ischemia, and in animal experiments, it has reduced the area of ​​cerebral infarction by more than 40%, especially after administration...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/5575A61P9/12
Inventor 程栎周丽莹王伟肖萱刘玉静张伟强杨明石
Owner BEIJING TIDE PHARMA
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