Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Prostaglandin E1 long-circulation fat microsphere preparation for intravenous injection and preparation method thereof

A technology of alprostadil and lipid microspheres, which is applied in the direction of medical preparations containing active ingredients, pharmaceutical formulas, oil/fat/wax non-active ingredients, etc. It can solve the problem that the treatment effect of alprostadil is not very satisfying to patients, etc. question

Active Publication Date: 2010-05-05
XIAN LIBANG PHARMA
View PDF0 Cites 10 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Through clinical experiments, the therapeutic effect of the alprostadil drug prepared by the prior art is not very satisfactory to the patients, so we have invented a kind of alprostadil with good therapeutic effect and solved the existing problems of the prior art through long-term research preparation

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
  • Prostaglandin E1 long-circulation fat microsphere preparation for intravenous injection and preparation method thereof
  • Prostaglandin E1 long-circulation fat microsphere preparation for intravenous injection and preparation method thereof
  • Prostaglandin E1 long-circulation fat microsphere preparation for intravenous injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0098] Embodiment 1 The most preferred alprostadil lipid microsphere preparation of the present invention

[0099] Alprostadil 5.0mg

[0100] Soybean oil (for injection) 100.0g

[0101] Lecithin (for injection) 18.0g

[0102] Sodium Oleate 2.4g

[0103] Polyethylene Glycol-Phospholipid 20.0g

[0104] Vitamin E (for injection) 5.0g

[0105] Glycerin 22.1g

[0106] Add water for injection to 1000ml

[0107] Take alprostadil, soybean oil, add lecithin, vitamin E, polyethylene glycol-phospholipid (PEG-DSPE), under nitrogen protection, heat to 75 ℃, stir for about 10min to make the various lipid compounds added Fully dissolve, dissolve and mix. Another take 800ml water for injection, add glycerol and sodium oleate. Under nitrogen protection, the oil solution containing the drug was added to the aqueous solution of glycerol and sodium oleate under shear and stirring conditions to prepare colostrum, and the total amount was adjusted to 1000ml. Homogenize 5-8 times with a hig...

example 2

[0108] Example 2 Long-circulating alprostadil lipid microsphere pharmaceutical formulation with the highest alprostadil content (only soybean oil is used as an example)

[0109] prescription:

[0110] Alprostadil 1.0g

[0111] Soybean oil (for injection) 100.0g

[0112] Lecithin (for injection) 18.0g

[0113] Sodium Oleate 2.4g

[0114] Polyethylene Glycol-Phospholipid 20.0g

[0115] Vitamin E (for injection) 5.0g

[0116] Glycerin 22.1g

[0117] Add water for injection to 1000ml

[0118] Take 1.0 g of alprostadil and 100.0 g of soybean oil, add 18.0 g of lecithin and 20.0 g of polyethylene glycol-phospholipid (PEG-DSPE), under nitrogen protection, heat to 75 ° C, and stir for about 10 minutes to make the added Various lipid compounds are fully dissolved, then 5.0 g of vitamin E is added, dissolved and mixed. Another take 800ml of water for injection, add 22.1g of glycerol and 2.4g of sodium oleate. Under nitrogen protection, the oil solution containing the drug was a...

example 3

[0120] Example 3 Long-circulating alprostadil lipid microsphere pharmaceutical formulation with minimal polyethylene glycol-phospholipid content (only soybean oil is used as an example)

[0121] prescription:

[0122] Alprostadil 5.0mg

[0123] Soybean oil (for injection) 100.0g

[0124] Lecithin (for injection) 18.0g

[0125] Sodium Oleate 2.4g

[0126] Polyethylene Glycol-Phospholipid 2.0g

[0127] Vitamin E (for injection) 5.0g

[0128] Glycerin 22.1g

[0129] Add water for injection to 1000ml

[0130] Take 5.0 mg of alprostadil, 100.0 g of soybean oil, add 18.0 g of lecithin and 2.0 g of polyethylene glycol-phospholipid (PEG-DSPE), under nitrogen protection, heat to 75 ° C, and stir for about 10 min to make the added Various lipid compounds are fully dissolved, then 5.0 g of vitamin E is added, dissolved and mixed. Take another 800ml of water for injection and add 22.1g of glycerol. Under nitrogen protection, the oil solution containing the drug was added to the g...

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

PropertyMeasurementUnit
particle sizeaaaaaaaaaa
Login to View More

Abstract

The invention relates to a formula and a preparation method of a prostaglandin E1 long-circulation fat microsphere for intravenous injection. The preparation comprises the following components: (1) a prostaglandin E1 medicine; (2) vegetable oil (dissolving oil diluted by a medicine); (3) an emulsion surfactant; (4) an emulsion preparation stabilizing agent, an emulsifying agent, a particle diameter control agent and a polyoxyalkylene phospholipid derivative increasing the half life of the fat microsphere in blood; (5) oleic acid or oleate which is used as the emulsion preparation stabilizing agent or the emulsifying agent; (6) an antioxidant; and (7) a complex compound (glycerol) controlling the cation concentration.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a lipid microsphere preparation of alprostadil for intravenous injection and a preparation method thereof. technical background [0002] Alprostadil (prostaglandin E1, PGE1) is a kind of prostaglandin, which has the functions of dilating blood vessels, inhibiting platelet aggregation, inhibiting gastric acid secretion, stimulating intestinal and uterine smooth muscle, protecting liver and kidney function, inhibiting pancreatic exocrine secretion, and resisting lipid oxidation. effect, stimulate insulin secretion, etc. Main clinical applications: 1) Treatment of limb ulcers caused by chronic arterial occlusive disease (thromboangiitis obliterans, arteriosclerosis obliterans, etc.) obstacle. 2) Treatment of progressive systemic sclerosis, Kaplan's syndrome, skin ulcers caused by diabetes. 3) Recovery of subjective symptoms associated with peripheral blood flow disorder c...

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 Applications(China)
IPC IPC(8): A61K9/16A61K31/5575A61K47/44A61P9/00A61P9/10A61P17/00A61P43/00G01N30/36
Inventor 陈涛王汝涛王惟娇张阳
Owner XIAN LIBANG PHARMA
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com