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External preparation containing sirolimus as well as preparation method and application thereof
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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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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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[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...
[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.
[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 present invention relates to a new administration route of sirolimus, more specifically, to an external preparation of sirolimus, its preparation method and its use in preparing drugs for treating skin diseases, and belongs to the field of medical technology. Background technique [0002] Sirolimus, also known as rapamycin, is a macrolide antibiotic immunosuppressant. It is a macrolide antibiotic isolated from actinomycete culture fluid by the Ayerst Research Institute in 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 cells from entering the S phase from the G1 phase, and block the interaction between interleukin-2 (IL-2) and its receptors. The combination prevents Tc and Td cells from becoming sensitized T lymphocytes with immune response and exerting their immune effects. Sirolimus and tacrolimus are structural homologues an...
Claims
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Application Information
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