External preparation containing sirolimus as well as preparation method and application thereof

An external preparation, the technology of sirolimus, applied in the field of medicine, achieves the effect of good drug absorption, high safety and good stability

Active Publication Date: 2016-06-15
WUHAN GENERAL HOSPITAL OF GUANGZHOU MILITARY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are no literature and patent reports about the topical application of sirolimus and the preparation of its topical preparations

Method used

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  • External preparation containing sirolimus as well as preparation method and application thereof
  • External preparation containing sirolimus as well as preparation method and application thereof
  • External preparation containing sirolimus as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0131] Single Cream Prescription:

[0132] component name

Dosage

Sirolimus

5g

stearic acid

40g

Glyceryl monostearate

40g

vaseline

20g

liquid paraffin

70g

Glycerin

50g

Triethanolamine

3g

Sodium dodecyl sulfate

3g

Laurocaprazine

2g

purified water

Appropriate amount

Full amount

1000g

[0133] Preparation Process:

[0134] (1) Oil phase: Accurately weigh stearic acid, glyceryl monostearate, vaseline, and liquid paraffin, heat and melt on a water bath, stir well, and keep warm at about 75°C;

[0135] (2) Water phase: Accurately weigh glycerin, triethanolamine, laurocapram, sodium lauryl sulfate and water, heat and stir in a water bath to dissolve, and heat to 75°C.

[0136] (3) Slowly add the above oil phase into the water phase, stir for 15 minutes, and keep stirring.

[0137] (4) Turn on the cooling water, start cooling down to about 5...

Embodiment 2

[0140] Single Cream Prescription:

[0141] components

Dosage

Sirolimus

10g

stearic acid

30g

Glyceryl monostearate

60g

vaseline

20g

liquid paraffin

30g

Glycerin

30g

Triethanolamine

5g

purified water

Appropriate amount

Full amount

1000g

[0142] Preparation Process:

[0143] (1) Oil phase: Accurately weigh stearic acid, glyceryl monostearate, vaseline, and liquid paraffin, heat and melt on a water bath, stir well, and keep warm at about 75°C;

[0144] (2) Water phase: Accurately weigh glycerin, triethanolamine, laurocaprazine and water, heat and stir in a water bath to dissolve, and heat to 75°C.

[0145] (3) Slowly add the above oil phase into the water phase, stir for 15 minutes, and keep stirring.

[0146] (4) Turn on the cooling water, start cooling down to about 55°C, add the prescribed amount of sirolimus, and continue stirring.

[0147] (5) When the...

Embodiment 3

[0149] Compound Cream Prescription:

[0150] components

Dosage

Sirolimus

1g

triamcinolone acetonide

2g

stearic acid

100g

liquid paraffin

120g

lanolin

20g

Glycerin

40g

Triethanolamine

8ml

purified water

Appropriate amount

quantity

1000g

[0151] Preparation Process:

[0152] Weigh stearic acid, liquid paraffin, and lanolin in the same container, heat to 80°C, stir well, and use it as the oil phase for later use; take glycerin, triethanolamine and water in another container, heat to 80°C, Stir well and use as the water phase for later use; add the oil phase to the water phase and stir, and when the temperature drops to 60°C, add the prescribed amount of sirolimus and triamcinolone acetonide, and stir evenly; Pack and serve.

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Abstract

The invention provides a new route of administration for sirolimus, namely that sirolimus is prepared into an external preparation for treating skin diseases. The external preparation is a prescribed preparation or compound preparation containing sirolimus, and the dosage form can be any one of pharmaceutical skin external dosage forms including cream, ointment, gel, spray, coating agent and the like, and can be any one of new external dosage forms including solid lipid nanoparticles and the like. The research shows that the external preparation containing sirolimus can be used for treating multiple immune and inflammatory skin diseases including atopic dermatitis, eczema, dermatitis, lichen planus, psoriasis, vitiligo, rosacea, sarcoidosis and the like, and is good in curative effect, high in safety and free of skin irritation. The external preparation is expected to become an important pharmaceutical preparation for clinically treating skin diseases following corticosteroids.

Description

technical field [0001] The invention relates to a new administration route of sirolimus, more specifically, relates to an external preparation of sirolimus, its preparation method and its application in the preparation of medicines for treating skin diseases, and belongs to the technical field of medicine. Background technique [0002] Sirolimus, also known as rapamycin, is a macrolide antibiotic immunosuppressant. It is a macrolide antibiotic isolated from the culture medium of actinomycetes by the Ayerst Research Institute of Canada in the early 1970s. The mechanism of sirolimus as an immunosuppressant is that it can block the late reaction (proliferation) of T lymphocyte activation, inhibit the cells from entering the S phase from the G1 phase, and block the interaction between interleukin-2 (IL-2) and its receptor. Combined, Tc and Td cells cannot become sensitized T lymphocytes with immune response and exert their immune function. Sirolimus and tacrolimus are structur...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/06A61K9/12A61K9/70A61K9/51A61K31/436A61K45/06A61K31/58A61K31/573A61P37/06A61P17/00A61P17/06A61K31/137
CPCA61K9/0014A61K9/06A61K9/12A61K9/51A61K9/7015A61K31/137A61K31/436A61K31/573A61K31/58A61K45/06A61K47/22A61K47/24A61K47/26A61K47/32A61K47/36A61K47/38A61K47/44A61K2300/00
Inventor 陈鹰刘宏潘明杰
Owner WUHAN GENERAL HOSPITAL OF GUANGZHOU MILITARY
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