Improved carrier system for cyclosporin pharmaceutical compositions

A technology of cyclosporine and composition, which is applied in the field of microemulsion concentrate carrier system, and can solve the problems of poor bioavailability of cyclosporin, etc.

Inactive Publication Date: 2004-06-16
BIOMAX
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The present inventors have discovered a system that overcomes the problem of limited solubility and thus poor bioavailability of cyclosporine

Method used

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  • Improved carrier system for cyclosporin pharmaceutical compositions

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Ingredient mg

[0047] Cyclosporin 100

[0048] Lauroglycol 90 280

[0049] Cremophore EL 225

[0050] Miglyol 812 15

[0051] Alpha-tocopherol 5

[0052] Total 625

[0053] This example uses the aforementioned ingredients in the indicated amounts. The cyclosporin is dissolved in a propylene glycol monoester / diester of lauric acid with a monoester content of not less than 90%. Then polyoxyethylene 35 castor oil (Cremophore EL) as a surfactant was added and mixed with it at room temperature for several minutes until the solution was uniform. Then the triacetin and alpha-tocopherol are added and mixed until a homogeneous mixture is obtained.

[0054] The solution was then stored for 6 weeks to ensure that no crystallization occurred.

[0055] To verify the formation of an emulsion, add 1 part of the formulation to 10 parts of water and stir slowly. The drug does not precipitate or crystallize, and the resulting solution forms a fine emuls...

Embodiment 2

[0058] According to the method of Example 1, except that the formula contains the following ingredients:

[0059] Ingredient mg

[0060] Cyclosporine 25

[0061] Lauroglycol 90 80

[0062] Cremophore EL 50

[0063] Miglyol 812 7.5

[0064] Alpha-tocopherol 2.5

[0065] Total 165

Embodiment 3

[0067] According to the method of Example 1, except that the formula contains the following ingredients:

[0068] Ingredient mg

[0069] Cyclosporin 100

[0070] Lauroglycol 90 300

[0071] Cremophore EL 230

[0072] Miglyol 12 10

[0073] Alpha-tocopherol 5

[0074] Total 645

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Abstract

A homogeneous cyclosporin composition containing a pharmaceutically effective amount of cyclosporin in association with a pharmaceutical carrier, said carrier comprising a drug solubilizing effective amount of mono or diester of propylene glycol of lauric acid with monoester content of at least 90%, a non-ionic surfactant and a dispersing agent. The composition described herein provides greater solubility of cyclosporin and cyclosporin capsule shell stability.

Description

Invention field [0001] The present invention relates to a microemulsion concentrate carrier system of a pharmaceutical composition containing cyclosporin. Background of the invention [0002] Cyclosporine is a kind of unique structure, cyclic, poly-N-methylated undecapeptide, with general pharmacology, especially immunosuppressive, anti-inflammatory and / or anti-parasitic (such as anti-malaria and anti- other Protozoa) activity. The first cyclosporin isolated is the naturally occurring fungal metabolite cyclosporin, which is also known as cyclosporin A or cyclosporin. [0003] Cyclosporin is highly lipophilic and only slightly soluble in water, but easily soluble in organic solvents such as methanol, ethanol, chloroform, etc. Due to its limited solubility in water, the bioavailability of oral cyclosporin is very low. Poor bioavailability can lead to ineffective treatments and the need to use higher doses and lead to the possibility of undesirable side effects. W...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K9/48A61K9/64A61K38/13
CPCA61K38/13A61K9/4858A61K9/1075A61P29/00A61P33/02A61P33/06A61P37/06
Inventor E·E·林恩
Owner BIOMAX
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