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

Bile salt modified cationic vitamin D3 oral liposome and its lyophilized preparation

A technology of liposome freeze-drying and vitamins, which is applied in the direction of liposome delivery, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., which can solve the problem of reduced drug efficacy, reduced drug dosage, and oral drug absorption Poor effect and liver metabolism and other problems, to achieve the effect of prolonging the action time, enhancing the adhesion ability, and avoiding drug degradation or leakage

Active Publication Date: 2020-08-04
JILIN UNIV
View PDF2 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the peristalsis of the gastrointestinal tract and the physical barrier formed by the mucus gel layer covering the surface of the mucosal epithelial cells, it also leads to poor absorption of oral drugs (4) liver metabolism
The influence of liver metabolizing enzymes will lead to a decrease in the drug dose and efficacy of drugs administered through the gastrointestinal tract into the systemic circulation

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
  • Bile salt modified cationic vitamin D3 oral liposome and its lyophilized preparation
  • Bile salt modified cationic vitamin D3 oral liposome and its lyophilized preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Weigh 123.75mg of soybean lecithin, 5.63mg of cationic material PEI-LA, 22.5mg of vitamin D3 and add 3mL of absolute ethanol, ultrasonic for 10min to make it fully dissolved, then stir in a water bath at 60°C with a magnetic stirrer at constant temperature, as Drug phase: Accurately weigh 56.25 mg of sodium glycocholate in 27 mL of phosphate buffer (pH 6.8), sonicate for 10 min to completely dissolve it as the water phase. Quickly add the drug phase into a round-bottomed flask of aqueous phosphate buffer (pH6.8), then remove the ethanol by rotary evaporation at 65°C and concentrate to 7.5 mL; Salt-modified cationic vitamin D3 oral liposomes. The lyoprotectant was added to the prepared preparation, pre-frozen at -70°C for 4 hours, and freeze-dried for 42 hours to obtain cholate-modified cationic oral vitamin D3 liposomes.

Embodiment 2

[0031] Accurately weigh 123.75mg of egg yolk lecithin, 5.63mg of cationic material PEI-LA, 22.5mg of vitamin D3 and add 3mL of absolute ethanol, ultrasonic for 10min to fully dissolve, then stir in a water bath at 60°C with a magnetic stirrer at constant temperature , as the drug phase; accurately weigh 22.50 mg of sodium glycocholate in 30 mL of phosphate buffer (pH 6.8), sonicate for 10 min to completely dissolve it, and use it as the water phase. Quickly add the drug phase into a round-bottomed flask of aqueous phosphate buffer (pH6.8), then remove the ethanol by rotary evaporation at 65°C and concentrate to 7.5 mL; Salt-modified cationic vitamin D3 oral liposomes. Add the lyoprotectant to the prepared preparation, pre-freeze at -70°C for 4 hours, and freeze-dry for 42 hours to obtain the cholate-modified cationic oral vitamin D3 liposome.

Embodiment 3

[0033]Accurately weigh 123.75mg of soybean lecithin, 5.63mg of cationic material PEI-LA, 22.5mg of vitamin D3, add 3mL of absolute ethanol, ultrasonic for 10min to fully dissolve, then stir in a water bath at 60°C with a magnetic stirrer at constant temperature, As the drug phase: Accurately weigh 90 mg of sodium glycocholate in 24 mL of phosphate buffer (pH 6.8), sonicate for 10 min to completely dissolve it, and use it as the water phase. Quickly add the drug phase into a round-bottomed flask of aqueous phosphate buffer (pH6.8), then remove the ethanol by rotary evaporation at 65°C and concentrate to 7.5 mL; Salt-modified cationic vitamin D3 oral liposomes. The lyoprotectant was added to the prepared preparation, pre-frozen at -70°C for 4 hours, and freeze-dried for 42 hours to obtain cholate-modified cationic oral vitamin D3 liposomes.

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
Login to View More

Abstract

The invention discloses a cholate modified cation vitamin D3 oral lipidosome and a freeze-drying preparation thereof. The method comprises the following steps: packing fat-soluble drug vitamin D3 into the lipidosome containing sodium glycocholate, using cationic material linolenic acid modified polymine (PEI-LA) for modifying the lipidosome surface, preparing into the oral vitamin D3 lipidosome with intestinal mucosa adhesion and preparing the freeze-drying preparation by freeze-drying, wherein the average grain size of the acquired preparation is within 160nm. According to the invention, an ethyl alcohol injection process-freeze-drying process is adopted for preparing and the acquired freeze-drying preparation can be further prepared into the oral preparations, such as, tablets and capsules. The prepared cholate modified lipidosome has the functions of increasing the drug solubility, prolonging the drug release time and increasing the oral-taking bioavailability of the drug.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a cholate-modified cationic vitamin D3 liposome and a freeze-dried preparation thereof. Background technique [0002] Vitamin D3 (Vitamin D3, VD3) is a fat-soluble vitamin, which belongs to a hormone precursor that acts on calcium and phosphorus metabolism, also known as "sunshine vitamin". Vitamin D3 has many effects, such as regulating calcium and phosphorus metabolism, improving the body's absorption of calcium and phosphorus; promoting the growth and calcification of human bones, promoting tooth development, and preventing osteoporosis; improving cardiovascular and cerebrovascular diseases; Phosphorus absorption, and increase phosphorus reabsorption through renal tubules; maintain normal levels of citrate in blood; improve immunity, anti-oxidation and other effects. [0003] However, because vitamin D3 is fat-soluble, insoluble in water, and h...

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 Patents(China)
IPC IPC(8): A61K9/127A61K47/28A61K47/34A61K31/593A61P3/02A61P19/10A61P9/00A61P3/00A61P7/00A61P37/04A61P39/06
CPCA61K9/0002A61K9/1274A61K9/1277A61K31/593A61K47/28A61K47/34
Inventor 李剑光范春宇孙亚厅毕野逯家辉滕乐生谢晶郝斐赵雅蓉赵秀婷
Owner JILIN UNIV
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