Formula and preparation method of non-allergenic and painless novel propofol fatty microemulsion freeze-drying preparation

A technology for propofol fat and freeze-dried preparations, applied in freeze-dried delivery, pharmaceutical formulations, anesthetics, etc., can solve problems such as chemical instability, and achieve the effects of reducing vascular irritation, preventing oxidative degradation, and stabilizing preparations

Active Publication Date: 2015-04-22
XIAN LIBANG ZHAOXIN BIOTECH CO LTD
View PDF4 Cites 5 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, most of the excipients are unsaturated double bond compounds, and their chemical properties are not stable.

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
  • Formula and preparation method of non-allergenic and painless novel propofol fatty microemulsion freeze-drying preparation
  • Formula and preparation method of non-allergenic and painless novel propofol fatty microemulsion freeze-drying preparation
  • Formula and preparation method of non-allergenic and painless novel propofol fatty microemulsion freeze-drying preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0092] Example 1: Investigation on the applicability of ultrafiltration to common propofol fat microemulsion

[0093] Get the propofol fat microemulsion 1000mL that any embodiment prepares, get a small amount of sample analysis its water phase free propofol concentration. according to figure 2 Assemble the "ultrafiltration production equipment" and select the ultrafiltration cartridge with suitable pore size. The main factor in the selection is that the aqueous solution, especially the free propofol in the water phase, can pass freely, while the fat emulsion cannot pass through as the selection parameter. First, equilibrate the ultrafiltration column with isotonic buffer solution, then slowly input the propofol fat emulsion into the ultrafiltration column to adjust the column pressure. The aqueous solution containing free propofol passes through the ultrafiltration column and is effectively separated from the propofol fat microemulsion. The missing solution is replenished b...

Embodiment 2

[0094] Example 2: Investigation of the applicability of ultrafiltration to polyethylene glycol propofol fat microemulsion

[0095] Get according to the polyethylene glycol propofol fat microemulsion sample 1000mL prepared in embodiment 21-24, take a small amount and analyze its aqueous phase free propofol concentration. according to figure 2 Assemble the "ultrafiltration production equipment", select the ultrafiltration cartridge with the appropriate pore size, and use the water solution to pass through freely, but the fat emulsion cannot pass through as the selection parameter. First, equilibrate the ultrafiltration column with isotonic buffer solution, then slowly input the propofol fat emulsion into the ultrafiltration column to adjust the column pressure. The aqueous solution containing free propofol passes through the ultrafiltration column and is effectively separated from the propofol fat microemulsion. The missing solution is replenished by buffer solution. General...

Embodiment 3

[0100] Embodiment 3: the weight ratio of propofol and synthetic fatty acid glyceride is 1:12

[0101] prescription:

[0102]

[0103] Take 10.0 g of propofol and 120.0 g of glyceryl palmitate, add 12.5 g of phosphatidylcholine distearate, heat and stir for about 10-20 minutes and mix well. Another 700ml of water for injection was taken, and 22.0g of mannitol was added. Under nitrogen protection and stirring conditions, the propofol phospholipid oil solution was added to the mannitol aqueous solution, and the total amount was adjusted to 1000ml. Homogenize 7-8 times with a high-pressure homogenizer, the homogenization pressure is 100MPa, until the particle size is less than 180nm, adjust the pH to 6.0-8.0, filter, fill, and use a brown vial to prepare a freeze-dried preparation.

[0104] After the lyophilized preparation of propofol fat microemulsion prepared by the above method was reconstituted, the content of free propofol in the water phase was analyzed by ultracentrif...

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 diameteraaaaaaaaaa
particle diameteraaaaaaaaaa
particle sizeaaaaaaaaaa
Login to view more

Abstract

The invention discloses a formula and a preparation method of a non-allergenic and painless novel propofol fatty microemulsion freeze-drying preparation. The novel preparation comprises artificially synthesized phospholipid and artificially synthesized fatty acid glyceride, the presence of such allergic sources as a trace of protein in lecithin and soybean oil as natural sources is avoided, the uses of a metal complex EDTA, an antioxidant sulfite and thiosulfate is avoided, the allergic reaction caused by a metal complexing agent and sulfide is eliminated; a water phase free propofol is removed through various means in the formulation and preparation process, so that the injection pain is alleviated or eliminated and thus the safety of the preparation and the compliance of patients are improved.

Description

technical field [0001] The invention belongs to the series of medical medicines, and relates to the formulation and preparation of a freeze-dried preparation of medicine, in particular to the formulation and preparation of a non-allergenic and painless novel propofol fat microemulsion freeze-dried preparation. Background technique [0002] Propofol (also known as dipofol, propofol, 2,6-diisopropylphenol, see structure figure 1 ) is a hindered phenol with strong lipophilicity, and is mostly used in the form of fat emulsion preparations for clinical induction and maintenance of anesthesia [1] . Propofol, as a commonly used clinical intravenous anesthetic, has been widely used for its fast onset, short maintenance time, rapid recovery, fast metabolism, no accumulation, and high safety. [2] . [0003] With the increasing clinical use of propofol injection, the reports of adverse reactions are increasing [3] . The clinical manifestations of adverse reactions of propofol inje...

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): A61K9/107A61K9/19A61K31/05A61K47/24A61K47/14A61P23/00
Inventor 陈涛翟小刚刘红王汝涛惠民权王惟娇
Owner XIAN LIBANG ZHAOXIN BIOTECH CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap