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External preparation for vascular abnormality treatment

An external agent and vascular technology, applied in the direction of cardiovascular system diseases, medical preparations containing active ingredients, drug combinations, etc., can solve problems such as vascular malformations with unknown causes, achieve simple administration, safe treatment, and eliminate increased blood vessels Effect

Pending Publication Date: 2021-09-28
OSAKA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The cause of most vascular tumors and vascular malformations is unknown, and no fundamental treatment has been established

Method used

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  • External preparation for vascular abnormality treatment
  • External preparation for vascular abnormality treatment
  • External preparation for vascular abnormality treatment

Examples

Experimental program
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Effect test

preparation example Construction

[0069] Examples of the preparation method of the external preparation include the following. (i) A gel can be prepared by gelling a solution containing sirolimus or a sirolimus derivative. (ii) An ointment can be prepared by mixing an ointment base with sirolimus or a sirolimus derivative. (iii) Patches, cataplasms, liniments, lotions and creams can be prepared according to known methods.

[0070] Hereinafter, gels, ointments, and creams will be specifically described.

[0071] (1) Gel

[0072] The external preparation for treating vascular abnormalities of the present invention may be a gel containing sirolimus or a sirolimus derivative.

[0073] When gelling a solution containing sirolimus or a sirolimus derivative, the solution may be gelled using a gelling derivatizing agent. Examples of the gelling derivatizing agent include carboxyvinyl polymers, carboxymethylcellulose, aluminum hydroxide, bentonite and the like.

[0074] The specific constitution of the carboxyviny...

manufacture example

[0135] [Manufacturing example: Preparation of sirolimus-containing gel]

[0136] Gels containing various concentrations of sirolimus were prepared. As a specific method, after adding and dissolving sirolimus in ethanol, water for injection was added and mixed to prepare a mixed solution. Carbomer (registered trademark) 934P NF was added and mixed to the mixed solution to prepare a homogeneous suspension. Tris was added and mixed as a neutralizing agent to the suspension to prepare a gel.

[0137] In addition, the components in 1 g of the gel other than sirolimus were 16 mg of Carbomer (registered trademark) 934P NF, 490 mg of water, 480 to 490 mg of ethanol, and 6 mg of tris.

[0138] More specifically, gels were prepared with the compositions of Production Examples 1 to 5 below.

manufacture example 1

[0139] Production Example 1: Gel containing 0.4% by weight of sirolimus (100 g in total)

[0140] Sirolimus 0.4g

[0141] Ethanol 48.4g

[0142] Water for injection 49g

[0143] Carbomer (registered trademark) 934P NF 1.6g

[0144] Trishydroxymethylaminomethane 0.6g

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Abstract

The present invention addresses the problem of providing an external preparation that can treat vascular abnormalities. The present invention is capable of treating vascular abnormalities (vascular deformation and vascular tumor) through transdermal or trans-mucosal membrane application of at least one selected from the group consisting of sirolimus and a sirolimus derivative. The sirolimus derivative may be everolimus, temsirolimus, ridaforolimus, zotarolimus, etc. This external preparation containing sirolimus and / or a sirolimus derivative has excellent therapeutic effect and is safe to use.

Description

technical field [0001] The present invention relates to the treatment of vascular abnormalities. Background technique [0002] Vascular abnormalities are broadly divided into two categories: vascular tumors and vascular malformations. The causes of most vascular tumors and vascular malformations are unknown, and fundamental treatments have not yet been established. Vascular tumors and vascular malformations are often called hemangiomas, but according to ISSVA (the International Society for the Study of Vascular Anomalies: International Society for the Study of Vascular Anomalies) advocated by the International Society for the Study of Vascular Anomalies Classification, the two are classified as different diseases. Although the classification is being standardized internationally, the traditional terminology is often used today. For example, strawberry hemangiomas are classified as infantile hemangiomas in the ISSVA classification. In addition, simple hemangiomas, telangi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P9/00A61P35/00A61P43/00A61P17/00A61K31/436A61K31/662
CPCA61P17/00A61P43/00A61P9/00A61P35/00A61K31/675A61K9/06A61K9/0014A61K47/44A61K31/436
Inventor 金田真理
Owner OSAKA UNIV
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