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External preparation containing rapamycin

A technology of rapamycin and external preparations, which is applied in the directions of medical preparations containing active ingredients, medical preparations without active ingredients, and aerosol delivery, etc. Rapamycin deterioration and other problems

Pending Publication Date: 2022-06-03
NOBELPHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In addition, rapamycin is easily deteriorated by oxidation and easily decomposed by the presence of water
Therefore, although a pharmaceutical preparation formulated with rapamycin and an antioxidant has been developed, it is difficult to disperse a fat-soluble antioxidant in an alcohol-free solution of rapamycin

Method used

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  • External preparation containing rapamycin
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0096] Hereinafter, the present invention will be described with reference to specific embodiments, but the present invention is not limited to the embodiments, and those skilled in the art will understand that the present invention may be used without departing from the scope or spirit of the present invention defined in the appended claims. Various changes and modifications are made in this embodiment below.

reference example 1

[0098] Sirolimus was mixed with each solvent shown in Table 1 in a ratio of sirolimus:solvent at 1:50 (weight ratio), heated in a water bath at about 50°C, irradiated with ultrasonic waves, and visually inspected. Observation confirmed the solubility. As a result, as shown in Table 1, it was not confirmed that sirolimus was dissolved in a single solvent.

[0099] [Table 1]

[0100] Solubility of sirolimus in each solvent

[0101] solvent Solubility Medium Chain Fatty Acid Triglycerides Insoluble (turbid liquid) Glycol Salicylate Insoluble (turbid liquid) Diethyl Sebacate Insoluble (turbid liquid) Diisopropyl Sebacate Insoluble (turbid liquid) Triacetin Insoluble (turbid liquid) Squalene Insoluble (turbid liquid) Propylene Glycol Insoluble (turbid liquid) Polyethylene Glycol (Macrogol 400) Insoluble (turbid liquid) 1,3-Butanediol Insoluble (turbid liquid)

[0102] (Quantitative test of sirolimus) ...

Embodiment 1

[0109] Example 1, Comparative Example 1

[0110] Using a mixed solvent obtained by mixing each solvent described in Table 1 and propylene glycol, the mixture was mixed so that sirolimus:solvent:propylene glycol was 1:50:25 (weight ratio), and heated in a water bath at about 50°C , and ultrasonic irradiation was carried out to prepare various preparations. Solubility was confirmed by visual observation of the obtained formulation.

[0111] The solubility results are shown in Table 2. The dissolution of sirolimus was confirmed by using a mixed solution of ethylene glycol salicylate, diethyl sebacate, and triacetin and propylene glycol.

[0112] [Table 2]

[0113] Solubility of Sirolimus to Mixtures of Each Solvent and Propylene Glycol (PG)

[0114] Test example solvent Solubility Comparative Example 1-1 Medium chain fatty acid triglycerides + PG Insoluble (white turbidity precipitates out) Example 1-1 Glycol Salicylate + PG dissolve Exa...

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Abstract

The present invention addresses the problem of providing a rapamycin-containing external preparation which has excellent stability and is effective in the treatment of skin diseases. Provided is an external preparation containing (a) rapamycin, (b) at least one substance selected from the group consisting of ethylene glycol salicylate, diethyl sebacate, and glyceryl triacetate, and (c) propylene glycol and / or polyethylene glycol, also provided are: an external preparation which further contains an antioxidant; and an external preparation which further contains a lipophilic solvent solution of an antioxidant.

Description

technical field [0001] The present invention relates to an external preparation containing rapamycin. Specifically, it relates to an external preparation containing rapamycin, excellent in stability, and effective for the treatment of skin diseases. Background technique [0002] Rapamycin (common name: sirolimus) is a macrolide produced by microorganisms. Rapamycin has an immunosuppressive effect, and thus has been used as a therapeutic drug for various diseases so far. For example, in addition to being used as an internal medicine for the treatment of lymphangioleiomyomatosis, in recent years, it is also used as an external preparation for the treatment of skin lesions accompanying tuberous sclerosis complex. [0003] On the other hand, although rapamycin is soluble in some organic solvents including ethanol, it is hardly soluble in or hardly soluble in many solvents including water. [0004] When using rapamycin as an external preparation, it is necessary to dissolve it...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K31/436A61K47/14A61K47/10A61P37/06A61P17/00
CPCA61K9/06A61K9/0014A61K31/436A61K47/14A61K47/10A61P37/06A61P17/00A61K31/05
Inventor 安泽亨井垣松男松本琢磨冰见论史
Owner NOBELPHARMA CO LTD
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