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Pharmaceutical composition for skin

A composition and non-aqueous composition technology, applied in the field of pharmaceutical compositions for skin coating, can solve problems such as reduced skin penetration, achieve suitable transdermal absorbability, and achieve the effect of transdermal absorbability

Inactive Publication Date: 2018-01-02
MARUHO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, when using the ointment of patent document 2, compared with TACLONEX (registered trademark), vitamin D 3 The skin penetration of the compound (calcipotriol) was surprisingly increased, while that of the corticosteroid (betamethasone dipropionate) was decreased on the other hand

Method used

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  • Pharmaceutical composition for skin
  • Pharmaceutical composition for skin
  • Pharmaceutical composition for skin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0095] to develop vitamin D 3The composition was prepared for the purpose of a skin composition having the same percutaneous absorbability of the compound and the corticosteroid as a conventional product (hereinafter referred to as a single-dose product) containing each component alone. The reason is that single-dose products have been used for a long time in the clinical field, and their effectiveness and safety have been proven. Therefore, if a composition containing two active ingredients has absorbability of each active ingredient to the same degree as that of a single-dose product, it can be expected to exceed the effectiveness of each single-dose product. In addition, it has been demonstrated in non-clinical trials that there is no toxic interaction between the two active ingredients, so if the respective absorbability of the two active ingredients is to the same extent as the respective single-dose preparations, it is considered to ensure the same The same clinical saf...

Embodiment 2

[0114] [In vivo percutaneous absorption test using hairless mice]

[0115] The transdermal absorbability test of the compositions No.1 to No.4 produced in Example 1 was compared with a commercial product (Oxarol ointment: containing 0.0025% by weight of OCT) containing OCT alone, and a composition containing BBP alone. The transdermal absorbability of a commercial product (Antebate ointment: containing 0.05% by weight of BBP) was compared.

[0116] Plastic frame (4cm 2 ) fixed on hairless mice. After transdermally administering 20 mg of the sample into the frame, the frame was fixed with an adhesive bandage. After 1, 4 and 8 hours, the skin surface of the application part was wiped clean with cotton impregnated with 70% ethanol under anesthesia. After the hairless mice were bled to death, the skin of the application site was collected. After homogenizing the collected skin in acetonitrile, the liquid phase was collected. After the liquid phase was dried and solidified, ...

Embodiment 3

[0143] Compositions (ointments) shown in Table 5 were prepared. Compositions No. 5 and No. 6 in the table are compositions of the present invention, and No. 7 uses the polyoxypropylene-15-hard oil used in the examples of Patent Document 1 instead of the low-polarity ester oil. Comparative composition of fatty ether (PPG-15 stearyl ether).

[0144] Composition No.5 was manufactured according to Composition No.1. Compositions No.6 and No.7 except that octyl dodecyl myristate was replaced with oleyl oleate or PPG-15 stearyl ether, Manufactured according to composition No.1.

[0145] In addition, regarding the compositions of No. 5 to No. 7, the stability (survival rate after storage) of OCT and BBP was confirmed by the following method.

[0146] [Stability test of active ingredients (a) and (b) in the composition]

[0147]The contents of the active ingredients (a) and (b) after storing the composition for 8 weeks in a thermo-hygrostat set at 50°C were measured.

[0148] To ...

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Abstract

Provided is a formulation including a vitamin D3 compound and a corticosteroid as active ingredients, wherein the pharmaceutical composition for the skin has exceptional stability of each of the active ingredients and suitable percutaneous absorptivity of the active ingredients. The present invention provides a non-aqueous composition for the skin, wherein the composition contains (a) maxacalcitol, (b) at least one corticosteroid selected from the group consisting of betamethasone and esters thereof, (c) at least one low-polarity ester oil having an IOB value from 0.07 to less than 0.20, and (d) at least one non-polar liquid solvent.

Description

technical field [0001] The present invention relates to pharmaceutical compositions for skin useful for the treatment of inflammatory skin diseases, especially psoriasis. More specifically, the present invention relates to pharmaceutical compositions for skin application comprising an active vitamin D3 compound and a corticosteroid. Background technique [0002] Psoriasis is an inflammatory keratosis characterized by abnormal proliferation and abnormal keratinization of epidermal cells, inflammatory cell infiltration, and vascular proliferation. In addition, psoriasis is an intractable skin disease that progresses with repeated improvement and deterioration. In typical cases, silvery white scales are attached to red rashes slightly raised from the skin, accompanied by scalp-like Symptoms of rustling peeling. The basic method of psoriasis treatment is external therapy using topical drugs, and the mainstream therapy is vitamin D, which has the effect of inhibiting the prolif...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/593A61K9/06A61K31/573A61K47/06A61K47/14A61P17/00A61P17/06A61P43/00
CPCA61K47/06A61K47/14A61K31/573A61K9/06A61K9/0014A61K31/593A61K47/44
Inventor 江见英敏藤井正浩
Owner MARUHO