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Lipid construct for delivery of insulin to a mammal

A construct and insulin technology, applied in drug delivery, liposome delivery, drug combination, etc., can solve unmet problems

Active Publication Date: 2008-08-06
SDG LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Accordingly, there remains an unmet need in the art for compositions and methods for controlling blood glucose levels in Type 1 and Type 2 diabetic patients

Method used

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  • Lipid construct for delivery of insulin to a mammal
  • Lipid construct for delivery of insulin to a mammal
  • Lipid construct for delivery of insulin to a mammal

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0154] In one embodiment, the amphiphilic lipid molecules include 1,2-distearoyl-sn-glyceryl-3-phosphocholine, cholesterol, cetyl phosphate, 1,2-dipalmitoyl-sn- Glyceryl-3-phosphoethanolamine-N-(Cap biotinyl); 1,2-Distearoyl-sn-glyceroyl-3-phosphoethanolamine, 1,2-dipalmitoyl-sn-glyceryl-3 -Phosphoethanolamine-N-(succinyl), 1,2-dipalmitoyl-sn-glyceryl-3-[phospho-rac-(1-glycerol)] (sodium salt), triethylammonium 2,3-di Acetoxypropyl 2-(5-((3aS,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanamido)ethyl phosphate and any A mixture of the aforementioned lipids.

[0155] Extended amphiphilic lipid molecules, also known as receptor binding molecules, comprise a proximal portion, a middle portion and a distal portion. The proximal portion links the extended lipid molecule to the construct, and the distal portion targets the construct to receptors displayed by hepatocytes. The proximal and distal sections are connected by an intermediate section. The composition of variou...

experiment Embodiment 1

Experimental Example 1: Pharmaceutical Composition 1

[0298] Lipid constructs include lipids 1,2-distearoyl-sn-glycero-3-phosphocholine, cholesterol, cetyl phosphate, 1,2-distearoyl-sn-glyceryl-3 -Phosphoethanolamine, 1,2-dipalmitoyl-sn-glyceryl-3-phosphoethanolamine-N-(succinyl), 1,2-dipalmitoyl-sn-glyceroyl-3-[phospho-rac-( 1-glycerol)] (sodium salt), a mixture of the receptor binding molecule 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine-N-(Cap biotinyl), and insulin.

experiment Embodiment 2

Experimental Example 2: Pharmaceutical Composition 2

[0299]Lipid constructs include lipids 1,2-distearoyl-sn-glycero-3-phosphocholine, cholesterol, cetyl phosphate, 1,2-distearoyl-sn-glyceryl-3 -Phosphoethanolamine, 1,2-dipalmitoyl-sn-glyceryl-3-phosphoethanolamine-N-(succinyl), 1,2-dipalmitoyl-sn-glyceroyl-3-[phospho-rac-( 1-glycerol)] (sodium salt), insulin, receptor binding molecule 1,2-dipalmitoyl-sn-glyceryl-3-phosphoethanolamine-N-(Cap biotinyl), and / or polychromium-poly (two)-[N-(2,6-(diisopropylphenyl)carbamoylmethyl)imino]diacetic acid] mixture. Lipid-anchored hepatocyte receptor-binding molecules 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine-N-(Cap biotinyl) and polychromium-poly(di)-[N-(2 , 6-(diisopropylphenyl)carbamoylmethyl)iminodiacetic acid] was added to the lipid construct at levels of 1.68%±0.5% by weight and 1.2%±0.5% by weight, respectively.

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Abstract

The instant invention is drawn to a hepatocyte targeted composition comprising interferon associated with a lipid construct comprising amphipathic lipid molecules and receptor binding molecule. The composition can comprise a mixture of free interferon and interferon associated with the complex. The composition can be modified to protect interferon and the complex from degradation. The invention also includes methods for the manufacture of the composition and loading interferon into the composition and recycling various components of the composition and methods of treating individuals infected with the hepatitis C and other hepatitis viruses.

Description

Background of the invention [0001] Diabetes is a condition that affects many people around the world. Treatments to control type 1 and type 2 diabetes are primarily aimed at normalizing blood sugar levels to prevent short- and long-term complications. Many patients require multiple daily insulin injections to control their diabetes. Several insulin products have been produced that control blood sugar levels at different time intervals. In an attempt to provide formulations that control glucose levels over longer periods of time, several products combine different forms of insulin. [0002] Previous attempts to normalize blood glucose levels in patients with type 1 and type 2 diabetes have focused on the subcutaneous administration of various time-released formulations of insulin, such as ultralente and humulin NPH insulin drugs . These formulations attempt to delay and then control the bio-distribution of insulin through modulation of insulin release to peripheral tissues,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127
CPCA61K9/0019A61K9/08A61K38/215A61K38/212A61K38/21A61K9/127A61K38/217A61P31/12A61P43/00A61P3/10Y02A50/30A61K38/28
Inventor J·R·劳W·B·格尔
Owner SDG LLC