JP2001122804A - Pharmaceutical composition for external use comprising corn starch phosphate formulated therein - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a pharmaceutical composition for external use excellent in feeling of use. SOLUTION: This composition is obtained by formulating corn starch phosphate in a pharmaceutical composition for external use.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to a pharmaceutical composition for external use having an excellent feeling upon use.

[0002]

2. Description of the Related Art In the field of cosmetics, powder-containing products such as make-up products such as powdered white powder, blusher, and foundation have been used for a long time. However, the raw materials used as the powder are mainly clay minerals of natural origin, and examples thereof include kaolin, silicic anhydride, aluminum magnesium silicate, talc, mica and the like. Above all, in baby powder, the use of talc accounts for the majority, and the purpose is to reduce friction between skin. In foundations, etc., if talc, which has a particle shape in the form of a plate, is blended, poor spreading during application is felt,
In order to compensate for this, in recent years, polymers such as spherical silica, nylon powder, and series powder have been used.Moreover, depending on the purpose, the particle surface is modified or the particle shape is dared. Contains non-spherical powder.

[0003] These techniques are disclosed in, for example, Japanese Patent Application Laid-Open No. 7-20
No. 6,640, JP-A-11-130617, and the like. On the other hand, in pharmaceuticals, as a preparation for mixing powder with an external preparation, an antimycotic agent-containing powder agent is well known, but as with cosmetic powders, talc is used, Feeling poor slippage during application. Also, in pharmaceutical ointments and creams,
The fact is that efficacy is prioritized, and the feeling of use has not been so important until now. Until now, there has been an example in which a powder such as zinc oxide is blended as an active ingredient. However, in order to improve the usability, blending of a powder has generally not been attempted so far. Recently, aerosols containing a powder that protects the wound surface, such as zinc oxide, have been marketed, and talc, colloidal silica, or the like has been added to these as a dispersant.

[0004] Talc is mainly used as a topical powder for medical use. However, additives such as mica and magnesium oxide which are supplementarily added are also in the form of plate-like or columnar crystals, so that the feeling of use cannot be improved to some extent. Yes, but not enough. In addition, the stickiness of ointments and creams can reduce QOL (quality of life) such as adhesion to clothing and discomfort during application. Considering the case where starch is blended, the application of heat causes a gelatinization phenomenon called pregelatinization to form a gel and deteriorate the properties. When compounding powders to improve the feeling of use in aerosols, if the shape of the powder particles is needle-like or fibrous, clogging of the valve is considered, and if spherical fine powder is added, Although the improvement effect seems to be high, if the particle size is small, it is possible that fine powder may be inhaled from the mouth or nose during spraying.

[0005]

SUMMARY OF THE INVENTION Accordingly, an object of the present invention is to provide a pharmaceutical composition for external use having an excellent feeling upon use.

[0006]

Means for Solving the Problems The present inventors have conducted intensive studies in order to solve the above-mentioned problems, and as a result, by adding corn starch phosphate to the topical pharmaceutical composition, the feel of the topical pharmaceutical composition has been effectively improved. The present invention has been completed by finding out what can be done.

[0007]

BEST MODE FOR CARRYING OUT THE INVENTION Hereinafter, the present invention will be described in detail. Phosphate corn starch used in the present invention has the following formula:

[0008]

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Is a compound represented by the formula: However, other alkali metals such as potassium may be used instead of sodium. The preferred corn starch phosphate is the sodium salt. In pharmaceuticals, starch is commonly used as an additive (excipient, disintegrant, etc.) for an internal solid preparation, but it has been rarely added to an external preparation as an additive.

In the Japanese Pharmacopoeia, wheat starch, rice starch, potato starch, and corn starch are listed, and each starch is characterized by a particle diameter and a particle shape. Since the corn starch phosphate used in the present invention is based on corn starch, its particle size and particle shape are similar to those of corn starch. However, corn starch phosphate has a substantially spherical crystal form as compared with a plate-like crystal of a natural mineral such as talc, and provides good spreadability and slipperiness.

Also, corn starch phosphate is characterized in that it absorbs sweat and skin moisture when applied to the skin and can keep the skin dry for a long time. Even with ordinary corn starch, to use it in a dry state like a powder, you can expect a certain feeling of use improvement effect, but in the wet state, especially when affected by heat such as cream, Although gelatinization occurs as described above, corn starch phosphate does not cause swelling gelation even when heated due to its structure.

[0012] As a substance similar to corn starch phosphate, sodium starch phosphate is present and is listed in the Official Food Additives. However, monosodium starch phosphate (type I) in which one glucose is bonded to one phosphoric acid includes sodium starch phosphate,
There is a diester form (II type) in which two glucoses are cross-linked via two phosphoric acids, and the solubility and gelatinization temperature differ depending on the ratio. The structure of corn starch phosphate is significantly different from that of sodium starch phosphate in that the esterification position is not at the 2-position hydroxyl group but at the 6-position. However, it does not dissolve in water and does not gelatinize. For comparison, a monoester compound (type I) and a diester compound (I
The structure with type I) is shown below.

[0013]

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Regarding the particle size of starches, for example,
Wheat starch is about 25-35 μm, rice starch is about 4-6 μm, and potato starch is about 70 μm.
9090 μm, and corn starch is about 9-18 μm.
m, compared to about 18 ~
It has a size of 20 μm, does not inhale from the nose or mouth, and does not deteriorate the feeling of use. Also,
Corn starch phosphate, when applied to the wound surface, has the function of absorbing body secretions, has no cytotoxicity, etc., and is excellent in tissue absorbability and compatibility, so it is considered to be a highly safe base. .

Phosphate corn starch having these characteristics is available from Dr. Hauser K.
G) is easily available on the market under the trade name CORNPO4, and among them, C suitable for external powder is
ORN PO4 PH “B”. The corn phosphate phosphate is, for example, 30 to 99.9% by weight, preferably 50 to 99% by weight in powders, and 0.5 to 5% by weight, preferably in ointments and creams, based on the weight of the pharmaceutical composition for external use. Is 1 to 3% by weight, and in the aerosol, 1
Suitably, it is incorporated in an amount of up to 10% by weight, preferably 3-7% by weight. As components other than corn starch phosphate, various drugs can be blended according to the dosage form.

In the case of a powder, a drug such as an antifungal agent, a bactericide, an astringent, an anti-inflammatory agent and the like can be added as an active ingredient together with corn starch phosphate. Examples of antifungal agents include ciclopirox olamine, tolnaftate, clotrimazole and the like. Examples of the bactericide include acrinol, benzalkonium chloride, and isopropylmethylphenol. Examples of the astringent include zinc oxide. As the anti-inflammatory agent, for example, glycyrrhizin and salts thereof can be blended.

These components are 0.5 to 5% by weight, preferably 1 to 2% by weight for the antifungal agent and 0.05 to 0.3% for the fungicide, based on the weight of the external pharmaceutical composition.
%, Preferably 0.1 to 0.2% by weight, for astringents 1 to 10% by weight, preferably 3 to 5% by weight, for anti-inflammatory agents 0.1 to 3% by weight, preferably 1 to 2% by weight.
It can be formulated in an amount of% by weight. If necessary, kaolin, zinc oxide, titanium oxide, talc and the like may be added to the external powder for medicine.

In the case of ointments and creams, steroids and nonsteroidal anti-inflammatory agents, antifungal agents, antihistamines, moisturizers, local anesthetics and the like can be blended. As steroids and non-steroidal anti-inflammatory drugs,
For example, hydrocortisone, prednisolone and its salts, indomethacin, glycyrrhetinic acid and the like can be mentioned. As the antifungal agent, components similar to powders can be blended. Examples of the antihistamine include chlorpheniramine maleate and diphenhydramine hydrochloride.
Examples of the humectant include urea and glycerin. As the local anesthetic, for example, dibucaine hydrochloride, lidocaine, and the like can be blended.

These components are present in an amount of 0.01 to 2% by weight, preferably 0.025 to 1% by weight for the anti-inflammatory agent and 0.5 to 1% by weight for the antifungal agent, based on the weight of the external pharmaceutical composition.
-5% by weight, preferably 1-2% by weight, 0.2-3% by weight, preferably 0.5-2% by weight for antihistanes, 4-30% by weight, preferably 10-10% for humectants.
-20% by weight, for local anesthetics 0.1-5% by weight,
Preferably, it can be blended in an amount of 0.2 to 2% by weight. Examples of additives for ointments and creams include white petrolatum, mineral oil such as liquid paraffin, higher fatty acids such as stearic acid, higher fatty alcohols such as cetanol and stearyl alcohol, fatty acid esters such as isopropyl myristate, and polyoxyethylene. Surfactants such as alkyl ethers and glycerin fatty acid esters, buffers such as citric acid and salts thereof, and preservatives such as parabens can be added.

In the ointment, the above components are based on the weight of the pharmaceutical composition for external use, 5 to 95% by weight, preferably 10 to 90% by weight for mineral oil, and for higher fatty acids and higher fatty alcohols, 1 to 30% by weight, preferably 2 to 20% by weight.
It can be present in an amount of 20% by weight, preferably 2-15% by weight. In creams, the above components are based on the weight of the external pharmaceutical composition, and mineral oils, higher fatty acids, higher fatty alcohols, fatty acid ester oils have a content of 1 to 30.
%, Preferably 2 to 20% by weight, for surfactants 1 to 10% by weight, preferably 2 to 8% by weight, for buffering agents 0.05 to 2% by weight, preferably 0.1 to 1% by weight.
% By weight, preservative is 0.05-0.3% by weight, preferably 0.1%
It can be incorporated in an amount of up to 0.2% by weight.

There are various types of aerosols,
A powder is mainly used in the case of a powder ejection preparation (a so-called powder spray type). In the case of this type, the required characteristics of the compounded powder are that the particle size is generally 50 μm or less, the particle shape is a spherical shape that is hardly clogged by accumulating in the valve hole, and the propellant Corn starch phosphate has these properties. In the case of aerosols, bactericides, antifungals,
Anti-inflammatory agents, astringents, anti-inflammatory analgesics, and the like can be blended, and specific examples include powders and the same components as in the case of ointments and creams. The proportions of these are the same as in the case of the powder. As an additive of the aerosol agent, a liquefied petroleum gas such as LPG, an ether system such as dimethyl ether, a fluorocarbon system such as fluorocarbon, or a compressed gas such as nitrogen or carbon dioxide can be blended as a propellant.

In the aerosol, these components are 20 to 80% by weight, preferably 30 to 60% by weight for LPG, and 20 to 60% by weight for dimethyl ether, based on the weight of the external pharmaceutical composition. %, Preferably 30
50% by weight, 0.2 to 5% for compressed gas such as nitrogen
%, Preferably 0.5 to 3% by weight.

[0023]

EXAMPLES Hereinafter, the present invention will be described in more detail with reference to Examples and Comparative Examples, but the scope of the present invention is not limited by these Examples and Comparative Examples.
In these examples and comparative examples, a sodium salt was used as corn starch phosphate.

Example 1 (Powder) Tolnaftate and corn starch phosphate (sodium salt) were uniformly stirred and mixed so as to have the following mixing ratio to prepare a scattered mixture.

Blending weight 1 g of tolnaftate 99 g of corn starch phosphate 100 g

Comparative Example 1 ( Powder) In the same manner as in Example 1,
Tonaphthate and talc were uniformly stirred so as to have the following composition to prepare a dispersion.

The mixing weight tolnaftate 1 g Talc 99 g total amount 100 g

Example 2 (Cream) According to a standard method for preparation of a cream, an emulsifier is dissolved in an oil phase, an aqueous phase in which a water-soluble component is dissolved is added, and the mixture is cooled while stirring and mixing. Phosphate corn starch is
After dispersing in water, the mixture is uniformly mixed with a cream base to produce.

Blending weight Corn starch phosphate 2 g Urea 10 g Cetanol 5 g Liquid paraffin 10 g Polyoxyethylene 1 g Cetyl ether methyl paraben 0.2 g Self-emulsifying monostearic acid 3 g Glycerin Purified water 100 g

[0030]

[Panel Test] With respect to the above Example 1 and Comparative Example 1, the feeling of use was evaluated using 10 panelists. The results are shown in Table 1 below.

[0031]

[Table 1] Table 1 Investigation results of the feeling of use of the external pharmaceutical composition (powders)

[0032]

The pharmaceutical composition for external use of the present invention, by blending corn starch phosphate, has a superior feeling in use as compared with the case of blending ordinary talc, as is clear from the panel test, The feeling can be improved.

 ──────────────────────────────────────────────────続 き Continued on the front page F term (reference) 4C076 AA06 AA17 AA24 AA30 CC31 EE38 4C083 AC022 AC072 AC182 AC392 AC482 AC682 AD241 CC01 CC05 DD08 DD17 DD22 DD31 EE06

Claims (2)

[Claims] 1. A pharmaceutical composition for external use characterized by containing corn starch phosphate. 2. The external pharmaceutical composition according to claim 1, which is a powder, an ointment, a cream, or an aerosol.