A kind of multivesicular liposome containing exenatide and its preparation method and application

A multivesicular liposome and exenatide technology, which is applied to medical preparations containing active ingredients, liposome delivery, and medical preparations without active ingredients, etc., can solve the problems of frequent administration, poor patient compliance, Fast release speed and other problems, to achieve the effect of reducing adverse reactions, high drug loading concentration, and improving compliance

Active Publication Date: 2011-12-14
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
View PDF3 Cites 10 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] Therefore, the technical problem to be solved in the present invention is to provide a new formulation of exenatide, which releases exenatide for the existing exenatide preparations, which have the def

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
  • A kind of multivesicular liposome containing exenatide and its preparation method and application
  • A kind of multivesicular liposome containing exenatide and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0054] Example 1

[0055] Step 1: Add 1mL containing 19.8mM (14.85mg) lecithin, 4.2mM (3.13mg) dipalmitoylphosphatidylglycerol, 30mM (11.61mg) cholesterol and 3.75mM (3.32mg) trioleic acid in a clean glass container A chloroform solution of glycerides. This solution is called the lipid phase.

[0056] Step 2: Add 1 mL of the inner aqueous phase of an aqueous solution of Exenatide 1 mg, 20 mM (4.20 mg) citric acid and 2.5% (25 mg) sucrose to the above glass container containing the lipid phase, and use a high-speed shearing machine Stir at 10,000 rpm for 10 minutes to obtain W / O colostrum.

[0057] Step 3: Place 5 mL of the outer aqueous phase solution containing 5.4% (w / v) (270 mg) glucose and 1% (50 mg) PVA on the colostrum layer, and then mix at a speed of 10,000 rpm for 10 seconds to obtain W / O / W type double emulsion.

[0058] Step 4: Transfer the double emulsion to a 250mL Erlenmeyer flask containing 5.4%(w / v)(270mg) glucose and 1%(50mg) PVA, 37℃ constant temperature water bat...

Example Embodiment

[0061] Example 2

[0062] Step 1: In a clean glass container, add 1 mL containing 5mM (3.96mg) hydrogenated soybean phospholipid, 0.5mM (0.38mg) dipalmitate phosphatidylserine, 10mM (3.87mg) cholesterol and 0.155mM (0.073mg) tricaprylin Ester in chloroform-ether (volume ratio 1:1) solution. This solution is called the lipid phase.

[0063] Step 2: Add 0.5 mL of the inner aqueous phase of an aqueous solution of Exenatide 5mg, 20mM (2.10mg) citric acid and 6% (30mg) sucrose into the above glass container containing the lipid phase, and use high-speed shearing The machine was stirred at a speed of 10,000 rpm for 10 minutes to obtain W / O colostrum.

[0064] Step 3: Place 7.5 mL of the outer aqueous solution containing 5.4% (w / v) (405 mg) glucose and 1% (75 mg) gelatin on the colostrum layer, and then mix at 4500 rpm for 40 seconds to obtain W / O / W type double emulsion.

[0065] Step 4: Transfer the double emulsion to a 250mL Erlenmeyer flask containing 9mL containing 5.4% (w / v) (486mg)...

Example Embodiment

[0068] Example 3

[0069] Step 1: Add 1 mL of dichloromethane solution containing 100 mM (75 mg) lecithin, 20 mM (8.49 mg) phosphatidic acid, 10 mM (3.87 mg) cholesterol and 13 mM (11.51 mg) triolein in a clean glass container. This solution is called the lipid phase.

[0070] Step 2: Add 1 mL of the inner aqueous phase of an aqueous solution containing 2.5 mg of Exenatide and 100 mM (21.01 mg) of citric acid to the above glass container containing the lipid phase, and stir with a high-speed shear at 10,000 rpm 10 minutes, get W / O colostrum.

[0071] Step 3: Place 20 mL of the outer aqueous phase solution containing 6% (w / v) (1200 mg) glucose and 1% (200 mg) hydroxymethyl starch on the colostrum layer, and then mix at 10,000 rpm for 10 seconds. Get W / O / W type double emulsion.

[0072] Step 4: Transfer the double emulsion to a 250mL Erlenmeyer flask containing 6% (w / v) (300mg) glucose and 1% (50mg) hydroxymethyl starch, 37℃ constant temperature water bath, make 8L / min A stream of ni...

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
Concentrationaaaaaaaaaa
Particle sizeaaaaaaaaaa
Encapsulation rateaaaaaaaaaa
Login to view more

Abstract

The invention discloses a multivesicular liposome containing exenatide, its preparation method and application. The multivesicular liposome comprises the following ingredients: 1 weight portions of exenatide, 0.1-200 weight portions of lipid component, 0.2-10 weight portions of pH regulator, 13-590 weight portions of osmotic pressure regulator, and 5-150 weight portions of auxiliary emulsifier, wherein, the lipid component comprises neutral phosphatide and cholesterol with the weight ratio of 0.4:1-19:1 and triglyceride which occupies 1-9 mol% of the lipid component. According to the invention, the exenatide for treating type II diabetes is prepared into a multivesicular liposome preparation. By utilizing the property of the active pharmaceutical ingredient exenatide that dissolving readily in water, the preparation process is carried out by directly dissolving exenatide in the internal aqueous phase and using multiple emulsion solvent evaporation method. The multivesicular liposome and the preparation method have the advantages of high utilization rate of raw materials, high drug-loading concentration, high entrapment rate of the medicine, good stability, good slow release, and good effect of decreasing blood sugar, thus reducing times and frequencies of usage, reducing adverse reactions, and improving patient compliance.

Description

technical field [0001] The invention belongs to the field of sustained-release preparations, in particular to a multivesicular liposome containing exenatide and its preparation method and application. Background technique [0002] According to the latest statistics from the International Diabetes Federation (IDF), the number of people with diabetes in the world exceeded 285 million in 2009, and there are 7 million new people with diabetes every year. It is estimated that in the next 20 years, the number of people with diabetes in the world will reach 440 million. The number of diabetic patients in my country ranks second in the world, second only to India. At present, there are about 70 million type 2 diabetic patients in my country. The average prevalence of type 2 diabetes in the urban population is 4.8%, but the complication control rate is less than 20%. Therefore, it is very important to research and develop an ideal clinical drug for diabetes. [0003] Exenatide (code...

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
IPC IPC(8): A61K9/127A61K38/17A61K47/28A61K47/44A61P3/10
Inventor 陈亭亭陆伟根徐成业杨耀杰
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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