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A pharmaceutical aerosol composition

A technology of composition and aerosol applied in the field of pharmaceutical aerosol composition

Inactive Publication Date: 2020-05-12
LEO PHARMA AS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, tacrolimus is a complex highly functionalized molecule, resulting in the molecule being susceptible to degradation through reaction with pharmaceutical excipients or contaminants or with water, thus making the development of chemically stable formulations of tacrolimus a challenge. challenge

Method used

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  • A pharmaceutical aerosol composition
  • A pharmaceutical aerosol composition
  • A pharmaceutical aerosol composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0047] During the research leading up to the present invention, it was found that when dimethyl ether was used as a propellant, tacrolimus could be dissolved in the composition without adding a co-solvent while maintaining chemical stability. However, if Figure 1A As shown in , there is a linear relationship between the amount of dimethyl ether included in the composition and the vapor pressure inside the aerosol container, and ultimately the number of droplets with a size of 10 μm or less. For example, it has been found that when the amount of dimethyl ether in a composition further comprising 60 ml butane and 30 g of a hydrophobic carrier is 10 ml or the amount of dimethyl ether in a composition further comprising 50 ml of butane and 30 g of a hydrophobic carrier When it is 20ml, on the one hand, tacrolimus can be completely dissolved in the composition, and on the other hand, the spray rate of the composition discharged from the container can be adjusted so as to avoid form...

Embodiment 1

[0089] Compositions of the invention

[0090] Composition A

[0091]

[0092] Composition B

[0093]

[0094] Composition C

[0095]

[0096] Composition D

[0097]

[0098] Composition E

[0099]

[0100] Composition F

[0101]

[0102] Composition G

[0103]

[0104] Composition H

[0105]

[0106] Composition I

[0107]

[0108] Composition J

[0109]

[0110] Composition K

[0111]

[0112] Composition L (60:10)

[0113] components quantity Tacrolimus(*) 0.42mg (0.042%w / w) Edetate 0.042mg (0.0042%w / w) White Vaseline a

419.53 mg (41.95% w / w) Dimethyl ether 93.66mg (9.37w / w%) n-butane 486.35mg (48.65w / w%)

[0114] Composition M: (55:15)

[0115] components quantity Tacrolimus(*) 0.42mg (0.042%w / w) White Vaseline a

417mg (41.7%w / w) Dimethyl ether 139.6mg (13.96% w / w) n-butane 443 mg (44.3% w / w)

[0116] (*) Tacrolimus was added as t...

Embodiment 2

[0126] The chemical stability of tacrolimus in compositions A to I was tested and the following results were obtained.

[0127] Composition A

[0128]

[0129] Composition B

[0130]

[0131] Composition C

[0132]

[0133] Composition D

[0134]

[0135] Composition E

[0136]

[0137] Composition F

[0138]

[0139] Composition G

[0140]

[0141] Composition H

[0142]

[0143] Composition I

[0144]

[0145]

[0146] Composition J

[0147]

[0148] Composition K

[0149]

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Abstract

The present invention relates to a pharmaceutical aerosol composition comprising tacrolimus as the active ingredient and the use of the composition in the treatment of inflammatory dermal diseases. The aerosol composition comprise a propellant mixture and further a pharmaceutically acceptable hydrophobic carrier solubilized or suspended in said propellant mixture.

Description

technical field [0001] The present invention relates to a pharmaceutical aerosol composition containing tacrolimus as an active ingredient and the use of the composition in treating inflammatory skin diseases. Background technique [0002] Tacrolimus and pimecrolimus are immunosuppressive macrolides that have been approved as drugs. The drug inhibits calcineurin, resulting in inhibition of antigen-specific T cell activation and inhibition of inflammatory cytokine release. [0003] Tacrolimus has been approved for various indications, such as the treatment of transplant rejection, rheumatoid arthritis, ulcerative colitis, allergic conjunctivitis, and for the treatment of various orphan drug indications. In addition, tacrolimus has been approved for the treatment of atopic dermatitis. [0004] Atopic dermatitis (AD) is a chronic relapsing inflammatory skin disease with high prevalence in infancy, affecting 10% to 20% of children (Katoh, J. Dermatol. 36, 2009, pp. 367- 376 p...

Claims

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Application Information

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IPC IPC(8): A61K9/12A61K31/436A61K47/06
CPCA61K9/0014A61K9/12A61K31/436A61K47/06A61K47/08A61P17/00
Inventor L·B·詹森P·凯姆普K·彼得松G·霍伊
Owner LEO PHARMA AS
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