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Alprostadil lipid nanosphere injection and preparation method thereof

A technology of dil lipid and alprostadil, which is used in blood diseases, pharmaceutical formulations, emulsion delivery, etc., can solve the problems of increasing blood circulation time, affecting clinical application of products, shortening pharmacological action time, etc., and reducing blood clearance. , reduce pulmonary circulation inactivation and blood clearance, reduce the effect of pulmonary circulation inactivation

Active Publication Date: 2012-09-26
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 amount of freeze-drying protective agent mannitol is added and the freeze-drying process is adopted, so that the particle size of the emulsion cannot be less than 100nm , the actual particle size of the emulsion disclosed in the description of the invention reaches 166nm and 188nm. In addition, the key point is that in this patent, there is no technical solution for the combination of medium chain oil and emulsifier, so that it is impossible to obtain such small particle size lipid nanoparticles ball effect
[0006] The main pharmacological and physiological advantages of the disclosed alprostadil emulsion patent and the already-marketed liposphere product are that compared with intravenous administration of the original drug, it reduces the inactivation of lung enzymes, increases blood circulation time, and can specifically However, due to the phagocytosis of RES tissues, it will be quickly cleared from the blood, resulting in shortened pharmacological action time

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

Examples

Experimental program
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Effect test

Embodiment 1

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

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

Embodiment 2

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

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

Embodiment 3

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

[0041] In a sterile workshop or a class 100 purification workshop, weigh 42 g of medium chain oil for injection and 28 g of soybean oil for injection according to the weight ratio, add 30 g of sterile soybean lecithin and sterile polyethylene glycol dodecyl 40g stearate, heat it to 60-70℃, mix well, add 60mg of main drug alprostadil to it, dissolve it, keep at 60-70℃; add 838g water for injection at 60-70℃ and injection grade The mixed solution of 22g glycerol was kept at 60-70°C, sheared and stirred to form colostrum, then put into a high-pressure homogenizer, circulated 10 times under the pressure of 20-100MPa, cooled to room temperature, and used a ...

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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 ismore 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 and administration for the treatment of cardiovascular and neurosurgical 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. The drug is widely used in the clinical treatment of coronary heart disease, vasculitis, cerebral thrombosis sequelae, severe hepatitis, thrombosis and erectile dysfunction. It also has a good curative effect on ulcerative diseases, such as diabetic ulcers and ulcers caused by ischemia of extremities. [0003] Alprostadil is chemically unstable, unstable to water and heat, and easily degraded. When alprostadil is administered intravenously in vivo, more than 90% of the blood can be inactivated through the pulmonary circulation once, and the first-pass eff...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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