Alprostadil lipid nanosphere injection and preparation method thereof

A technology of dil lipid and alprostadil, which is applied in blood diseases, pharmaceutical formulations, emulsion delivery, etc., can solve problems affecting the clinical application of products, increase blood circulation time, and shorten pharmacological action time, so as to reduce pulmonary circulation. Inactivation and blood clearance, reduced blood clearance, reduced effect of pulmonary circulation inactivation

Active Publication Date: 2011-08-10
SHENYANG WANJIA INST OF BIOLOGICAL TECH RES
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Because alprostadil is not heat-resistant, the product may be completely degraded by autoclaving. Even if a short-term high temperature method is used, the product will produce degradation products that may be as high as 60%, and the phospholipid degradation products due to high heat will continue to affect the main drug. Stability shortens the shelf life of the product. For example, the products that are already on the market are produced in this way. The technical defects of the products have greatly affected the clinical application of the products.
Chinese patent 200410021253.3, alprostadil freeze-dried emulsion and its preparation method, although part of the disclosed technical scheme involves the similar combination of injection oil and emulsifier of this patent, and lists the drug alprostadil in one of the examples of the patent , soybean oil, soybean lecithin, HS15, pure water, etc., but the purpose is to prepare freeze-dried milk, so a large amo...

Method used

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  • Alprostadil lipid nanosphere injection and preparation method thereof
  • Alprostadil lipid nanosphere injection and preparation method thereof
  • Alprostadil lipid nanosphere injection and preparation method thereof

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Experimental program
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Embodiment 1

[0034] Alprostadil lipid nanosphere injection of the present invention is prepared from the following raw materials in parts by weight: 0.03 g of alprostadil, 90 g of medium-chain oil, 40 g of soybean lecithin, polyethylene glycol dodecahydroxy hard Prepared from 50g of fatty acid ester, 20g of glycerin and 800g of water.

[0035] In a sterile workshop or a 100-class purification workshop, weigh 90g of medium-chain oil for injection, add 40g of sterile soybean lecithin and 50g of sterile polyethylene glycol lauryl hydroxystearate into it, and heat it to 60 Mix well at -70°C, then add 30mg of the main drug alprostadil to dissolve it; add 800g of water for injection at 60-70°C and 20g of injection-grade glycerin, keep warm at 60-70°C, and shear and stir to form The colostrum is then placed in a high-pressure homogenizer, circulated 3-4 times under a pressure of 20-100 MPa, cooled to room temperature, filtered through a 0.45 μm filter membrane, and then filtered through a 0.22 μm...

Embodiment 2

[0037] Alprostadil lipid nanosphere injection of the present invention is prepared from the following raw materials according to the ratio of parts by weight: 0.002g of alprostadil, 40g of medium chain oil, 26g of egg yolk lecithin, polyethylene glycol dodecahydroxy hard Fatty acid ester 25g, glycerin 22g, water 890g.

[0038] In a sterile workshop or a 100-grade purification workshop, weigh 40g of medium-chain oil for injection, add 26g of sterile egg yolk lecithin and 25g of sterile polyethylene glycol lauryl hydroxystearate into it, and heat it to 60 -70°C, mix well, then add 2mg of the main drug alprostadil to it, make it dissolve, keep warm at 60-70°C; add 890g of water for injection at 60-70°C and 22g of injection-grade glycerin, keep warm to 60-70°C ℃, shear and stir to form colostrum, then put it into a high-pressure homogenizer, cycle 8 times under a pressure of 20-100MPa, cool to room temperature, filter with a 0.45μm filter membrane, and then filter with a 0.22μm fi...

Embodiment 3

[0040] Alprostadil lipid nanosphere injection of the present invention is prepared from the following raw materials in parts by weight: 0.06 g of alprostadil, 42 g of medium chain oil, 28 g of soybean oil, 30 g of soybean lecithin, polyethylene glycol Lauryl hydroxystearate 40g, glycerin 22g, water 838g.

[0041] In a sterile workshop or a 100-grade purification workshop, weigh 42g of medium-chain oil for injection and 28g of soybean oil for injection according to the weight ratio, and add 30g of sterile soybean lecithin and sterile polyethylene glycol dodecahydroxyl to it. Stearate 40g, heat it to 60-70°C, mix well, then add 60mg of the main drug alprostadil to it, dissolve it, keep warm at 60-70°C; add 60-70°C water for injection 838g and injection grade The mixture of 22g glycerin is kept at 60-70°C, sheared and stirred to form colostrum, then placed in a high-pressure homogenizer, circulated 10 times under a pressure of 20-100MPa, cooled to room temperature, and filtered t...

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Abstract

The invention belongs to the technical field of medicines, and discloses an alprostadil lipid nanosphere injection and a preparation method thereof. The alprostadil lipid nanosphere injection is prepared from the following raw materials in parts by weight: 0.002-0.2 part of alprostadil, 40-100 parts of oil for injection, 20-40 parts of emulsifier, 25-50 parts of cosurfactant, 20-30 parts of glycerol, and 780-890 parts of water. The alprostadil lipid nanosphere injection provided by the invention has the particle size smaller than 100 nm, can be sterilized by aseptic filtration, overcomes the instability shortcoming of alprostadil, and improves product stability. Meanwhile, the lipid nanosphere has the particle size smaller than 100 nm, so that the alprostadil lipid nanosphere injection is more favorable for in vivo non-resveratrol (RES) tissue distribution of alprostadil, reduction of pulmonary circulation inactivation and blood removal, and long-term in vivo circulation of alprostadil. The alprostadil lipid nanosphere injection is suitable for surgical treatment of heart diseases and cranial nerve diseases.

Description

technical field [0001] The invention relates to an alprostadil lipid nanosphere injection and a preparation method thereof. The preparation is mainly used for injection administration and treatment of cardiovascular and cranial neurosurgery diseases, and belongs to the technical field of medicines. Background technique [0002] Alprostadil is a vasodilator with definite curative effect and a human physiological substance, which is widely used clinically in the treatment of coronary heart disease, vasculitis, sequelae of cerebral thrombosis, severe hepatitis, thrombosis, and erectile dysfunction. It also has a good effect on ulcerative diseases, such as diabetic ulcers and ulcers caused by extremity ischemia. [0003] Alprostadil is extremely unstable chemically, is unstable to water and heat, and is easy to degrade. Alprostadil is administered intravenously in the body, and blood can be inactivated by more than 90% once it passes through the pulmonary circulation, and the f...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/5575A61K47/44A61K47/34A61P9/14A61P9/10A61P1/16A61P7/02A61P15/10A61P17/02A61P25/00A61K47/14
Inventor 董英杰艾莉王会芳李乐
Owner SHENYANG WANJIA INST OF BIOLOGICAL TECH RES
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