Novel ointment

Abstract

To provide a novel ointment created by stably dissolving and mixing water-soluble active ingredients such as heparinoid for moisturizing purposes in an oleaginous ointment made of an oleaginous base.SOLUTION: The inventors of the present invention have discovered that by mixing a water-soluble active ingredient such as a heparinoid with an ointment base containing glycerin and a fat-soluble base such as Vaseline, it is possible to have the water-soluble active ingredient present in a dissolved state in the ointment, thereby forming a uniform and stable ointment, and thus completed the present invention.SELECTED DRAWING: None

Description

Technical Field

[0001] The present invention relates to an oily ointment containing water-soluble active ingredients such as heparin-like substances and urea, and particularly to an ointment used for improving dry skin and rough skin.

Background Art

[0002] Among the preparations for forming external preparations, there are ointments, creams, lotions, etc., and it is known that the ointment has the highest effect in protecting the skin and moisturizing the skin (Patent Document 1 and Patent Document 2).

[0003] There are ointments that use a water-soluble base (water-soluble ointment) and those that use an oily base such as petrolatum ointment (oily ointment). Although the water-soluble ointment has the merit of being easy to wash with water, it easily falls off from the skin due to sweat, etc., and is not as effective as the oily ointment in terms of "skin protection". On the contrary, although the oily ointment has a sticky feeling, it rarely falls off due to sweat, etc., and is considered to be the base with the most excellent skin protection effect.

[0004] When considering applying an active ingredient to the skin of a patient with skin damage, in order to avoid foreign matter invasion from the damaged part, it is necessary to apply a "preparation with a high protection effect", that is, an oily ointment. Therefore, for example, a moisturizer containing a heparin-like substance, which is a water-soluble active ingredient, is considered to be the most efficient when combined with an oily base such as petrolatum ointment.

[0005] However, when formulating a water-soluble active ingredient into an oily base, there was no method other than manufacturing by "dispersion" (uniformly mixing the powder of the active ingredient into the oil). In the case of ingredients with a coarse particle size, not only may the usability deteriorate, but also since the active ingredient is not dissolved, the effect of the active ingredient may not be obtained. Particularly in the case of heparin-like substances and urea, the particles are coarse, and there has been no product of an ointment (for example, petrolatum ointment) formulated into an oily base so far.

Prior Art Documents

Patent Document

[0006]

Patent Document 1

Patent Document 2

Summary of the Invention

Problems to be Solved by the Invention

[0007] An object of the present invention is to provide a novel ointment by stably dissolving and mixing a water-soluble active ingredient such as a heparin-like substance for moisturizing purposes in an oily ointment composed of an oily base.

Means for Solving the Problems

[0008] The inventors of the present invention have found that by mixing a water-soluble active ingredient such as a heparin-like substance into an ointment base containing glycerin and a lipophilic base such as petrolatum, the water-soluble active ingredient can be present in the ointment in a dissolved state, and a uniform and stable ointment can be formed, thus completing the present invention.

[0009] More specifically, the present application provides the following aspects in order to solve the above-mentioned problems: [1-1] An ointment containing a water-soluble active ingredient, glycerin, and an oily base; [1-2] The ointment according to [1-1], further containing a lipophilic emulsifier; [1-3] The ointment according to [1-1] or [1-2], containing 1 to 40% by weight of glycerin and 30% by weight or more of an oily base; [1-4] The ointment according to any one of [1-1] to [1-3], containing 1 to 6% by weight of glycerin and 90% by weight or more of an oily base; [1-5] The ointment according to any one of [1-1] to [1-4], wherein the water-soluble active ingredient is a component soluble in glycerin; [1-6] The water-soluble active ingredient is selected from the group consisting of heparin-like substances, urea, dipotassium glycyrrhizinate, sodium azulenesulfonate, cetylpyridinium chloride, panthenol, diphenhydramine hydrochloride, and benzethonium chloride, the ointment according to any one of [1-1] to [1-5]; [1-7] The water-soluble active ingredient is a heparin-like substance or urea, the ointment according to [1-6]; [1-8] The water-soluble active ingredient is 0.01 to 0.5% by mass of a heparin-like substance or 5.0 to 20.0% by mass of urea, the ointment according to [1-6]; [1-9] The oily base is petrolatum or a mixture of petrolatum and other oils, the ointment according to any one of [1-1] to [1-8]; [1-10] The other oils are one or more components selected from solid, semi-solid or liquid waxes, fatty acids, fatty acid esters, polyhydric alcohol fatty acid esters, higher alcohols, hydrocarbons, and silicone oils, the ointment according to [1-9]; [1-11] Containing polyglycerol fatty acid ester, glycerol fatty acid ester, or sorbitan fatty acid ester as a lipophilic emulsifier, the ointment according to any one of [1-2] to [1-10]; [1-12] The polyglycerol fatty acid ester is polyglyceryl-2 oleate, the ointment according to [1-11]; [1-13] It is 0.1 to 10% by weight of polyglyceryl-2 oleate, the ointment according to [1-12]; [2-1] A method for producing an ointment containing a water-soluble active ingredient, comprising the steps of: (a) dissolving the water-soluble active ingredient in glycerin; (b) mixing and kneading with an oily base; [2-2] In step (a), the water-soluble active ingredient is dissolved in glycerin while heating, the production method according to [2-1]; [2-3] In step (b), component B is heated, and then component A is mixed and kneaded with respect to component B, the production method according to [2-1] or [2-2]; [2-4] In the process (b), the method for production according to any one of [2-1] to [2-3], wherein a lipophilic emulsifier is previously contained in the component B; [2-5] The method for production according to [2-4], wherein in the process (b), while heating, a lipophilic emulsifier is dissolved in the oily base to prepare the component B. [Advantages of the Invention]

[0010] By dissolving a water-soluble active ingredient such as a heparin-like substance in glycerin, the water-soluble active ingredient can be mixed in a state of being dissolved in an ointment base containing a fat-soluble base such as petrolatum, and a uniform and stable ointment containing the water-soluble active ingredient dissolved therein can be formed. [Embodiments for Carrying Out the Invention]

[0011] According to the 17th revised Japanese Pharmacopoeia that has been in force in Japan since April 1, 2016, an ointment is a semi-solid preparation in which an active ingredient is dissolved or dispersed in a base and applied to the skin, and there are oleaginous ointments and water-soluble ointments. In the present invention, an oleaginous ointment, that is, an ointment based on an oleaginous base in which a water-soluble active ingredient is dissolved in the base, is provided.

[0012] Ointment base As the base used in producing the ointment in the present invention, an ointment base in which glycerin is dispersed in an oleaginous base can be used. The ointment base used in the present invention has the characteristic that it can contain a water-soluble active ingredient in a dissolved state.

[0013] Since the ointment base used in the present invention is intended for producing an oleaginous ointment, it is characterized by containing 30% by weight or more of an oleaginous base. As the oleaginous base used in the present invention, petrolatum or a mixture of petrolatum and other oil components can be used. The petrolatum in the present invention may be either yellow petrolatum or white petrolatum in the Japanese Pharmacopoeia, but white petrolatum is preferred.

[0014] As the oily base that can be optionally used in the present invention, a mixture of petrolatum and other oil components can be used. Examples of other oil components that can be used in the present invention include solid, semi-solid or liquid waxes, fatty acids, fatty acid esters, polyhydric alcohol fatty acid esters, higher alcohols, hydrocarbons, and silicone oils. When used as an oily base, one or more components selected from these can be mixed with petrolatum and used.

[0015] The above-described oily base itself cannot dissolve water-soluble active ingredients. In the present invention, in order to provide an oily ointment agent using an oily base in which a water-soluble active ingredient is dissolved in the base, it is characterized in that the ointment base contains a sufficient amount of glycerin to dissolve the water-soluble active ingredient. Specifically, the ointment base used in the present invention is characterized by containing 1 to 40% by weight of glycerin.

[0016] The lower limit of the amount of glycerin to be included in the ointment base used in the present invention can be determined according to the amount of the water-soluble active ingredient and its solubility in glycerin. On the other hand, when glycerin is mixed and dispersed in the oily base, the resulting ointment base has a significantly lower viscosity compared to the oily base. According to the 17th revised Japanese Pharmacopoeia, an ointment is a semi-solid preparation and is supposed to have an appropriate viscosity for application to the skin. Therefore, also in the present invention, in consideration of this aspect, it is necessary to adjust the amount of glycerin mixed in the oily base. That is, the upper limit of the amount of glycerin to be included in the ointment base used in the present invention can be determined according to the viscosity of the ointment.

[0017] When it is desired to contain a water-soluble active ingredient in a small amount such as 0.01% by mass in an ointment base, the water-soluble active ingredient can be dissolved by including 1% by weight or more of glycerin to dissolve the water-soluble active ingredient. On the other hand, in order to dissolve a relatively large amount of a water-soluble active ingredient such as 20% by mass in an ointment base, increasing the amount of glycerin, which is a solvent for the water-soluble active ingredient, is more effective. However, as described above, if a large amount of glycerin with a low viscosity is blended, the "viscosity" of the base itself cannot be maintained, and separation occurs, resulting in loss of stability and inability to be used as an ointment. In the present invention, in order to maintain the viscosity of the ointment preparation, it is preferable that the glycerin contained in the ointment base be 40% by weight or less.

[0018] In the ointment base used in the present invention, glycerin exists in a state dispersed in an oily base. Therefore, over time, the oily base and glycerin may separate, and there is a possibility of losing quality stability. In order to enhance the stability of the ointment base containing the oily base and glycerin even when viewed over time, a lipophilic emulsifier can be further contained as a surfactant. As the lipophilic emulsifier, a nonionic surfactant having an HLB of 9.0 or less can be used. For example, · Glyceryl fatty acid esters (glyceryl myristate, glycerin monostearate, glycerin monooleate), · Polyglycerol fatty acid esters (polyglyceryl-2 oleate (diglyceryl monooleate), polyglyceryl-4 oleate (tetraglyceryl monooleate), decaglyceryl trioleate, decaglyceryl tristearate, decaglyceryl pentaoleate, decaglyceryl pentastearate, diglyceryl monostearate), · Sorbitan fatty acid esters (sorbitan monostearate, sorbitan monooleate, sorbitan sesquioleate, sorbitan trioleate), · Polyoxyethylene alkyl ethers (polyoxyethylene behenyl ether, polyoxyethylene cetyl ether, polyoxyethylene oleyl ether, polyoxyethylene stearyl ether), · Polyethylene glycol fatty acid ester (polyethylene glycol monooleate), · Propylene glycol fatty acid ester (propylene glycol monostearate), · Polyoxyethylene sorbitol fatty acid ester (polyoxyethylene sorbitol tetraoleate), · Polyoxyethylene hydrogenated castor oil (polyoxyethylene hydrogenated castor oil 5, polyoxyethylene hydrogenated castor oil 10), · Sucrose fatty acid ester (sucrose stearate, sucrose laurate) etc. can be used. Among these, in the present invention, it is preferable to use glycerin monostearate (a kind of glycerin fatty acid ester), polyglyceryl-2 oleate (a kind of polyglycerin fatty acid ester), and sorbitan monostearate (a kind of sorbitan fatty acid ester). When using the lipophilic emulsifiers exemplified in the present invention, each component can be used in an amount within the range approved for use as a pharmaceutical. When, for example, polyglyceryl-2 oleate is used when mixing with the ointment base, the amount of polyglyceryl-2 oleate varies depending on the amount of glycerin mixed in the base, but it may contain 0.1 to 10% by weight.

[0019] The ointment base produced in this way can dissolve the water-soluble active ingredient in the contained glycerin, so it can exhibit the unprecedented characteristic of being able to contain the water-soluble active ingredient in a dissolved state. In the present invention, during the production of the ointment, it is characteristic that the water-soluble active ingredient is contained in the ointment in a dissolved state, but it is preferable that the properties of the ointment, that is, the water-soluble active ingredient is contained in the ointment in a dissolved state, are stably maintained for 2 weeks or more, and it is more preferable that such properties of the ointment are stably maintained for 1 month or more.

[0020] Ointment containing water-soluble active ingredient As described above, since the ointment base used in the present invention can contain a water-soluble active ingredient in a dissolved state, in one aspect, the present invention can provide an ointment containing a water-soluble active ingredient, glycerin, and an oily base.

[0021] Regarding glycerin and the oily base contained as components in this aspect, they are as described above for the ointment base. One of the characteristics is that it contains 1 to 40% by weight of glycerin, and it is characterized by containing 30% by weight or more of the oily base.

[0022] In the present invention, when referring to a water-soluble active ingredient, as described above, it is preferably capable of dissolving in glycerin. Such water-soluble components include, but are not limited to, heparin-like substances, urea, dipotassium glycyrrhizinate, sodium azulenesulfonate, cetylpyridinium chloride, panthenol, diphenhydramine hydrochloride, and benzethonium chloride. Among these, heparin-like substances or urea can be exemplified as preferred ones. When, for example, a heparin-like substance is contained as the water-soluble active ingredient in the ointment, it is contained at 0.01 to 0.5% by mass, and when, for example, urea is contained, it is contained at 5.0 to 20.0% by mass.

[0023] In the present invention, when referring to a heparin-like substance, it is a substance having a structure or action similar to that of "heparin" having an anticoagulant effect, and is a substance called polysulfated chondroitin sulfate in substance. In the present invention, in particular, a mucopolysaccharide polysulfate ester conforming to the "heparin-like substance" listed in the Japanese Pharmaceutical Excipients Standard outside the Japanese Pharmacopoeia can be used.

[0024] Manufacture of the ointment of the present invention According to the 17th revised Japanese Pharmacopoeia, to produce an oily ointment, generally, an oily base such as fats and oils, waxes, and hydrocarbons such as paraffin is heated and melted, the active ingredient is added, mixed and dissolved or dispersed, and kneaded together until the whole becomes homogeneous.

[0025] Following this, the ointment containing the water-soluble active ingredient of the present invention can be produced by: (a) First, a step of dissolving the water-soluble active ingredient in glycerin (the product obtained in this step is referred to as Component A); (b) On the other hand, for the oily base and the lipophilic emulsifier, which is an optional component (this product is referred to as Component B), Component A is added in one or more portions and mixed by stirring until the whole becomes homogeneous and kneaded together. In the above step (a), when producing Component A (that is, dissolving the water-soluble active ingredient in glycerin), it may be dissolved while heating. Also, in the above step (b), when mixing and kneading Component A with Component B, it can also be carried out after heating Component B. Furthermore, in the above step (b), a lipophilic emulsifier, which is an optional component, can also be contained as Component B. In that case, the lipophilic emulsifier can be dissolved in the oily base while heating to obtain Component B, and then Component A can be mixed and kneaded. In this way, by mixing Component A with Component B and kneading until the whole becomes homogeneous, and then cooling while stirring, the ointment of the present invention can be produced.

[0026] Viscosity of the ointment of the present invention The viscosity of the ointment can be measured by a spreadability test method using a spread meter or a viscosity test method using a rotational viscometer described in the general test method of the Japanese Pharmacopoeia in accordance with the rheological measurement method of semi-solid preparations published by the Pharmaceuticals and Medical Devices Agency (PMDA). As described above, when a large amount of glycerin with a low viscosity is blended, the "viscosity" of the base itself cannot be maintained, and it will separate and lose stability, making it impossible to be used as an ointment. Therefore, the viscosity of the ointment produced according to the present invention is preferably measured using the above-described rotational viscometer, and the amounts of glycerin and the oily base are produced so that it becomes at least 7000 (mPas) during production.

[0027] Enclosing the ointment of the present invention in a container The active ingredient of the present invention is a water-soluble active ingredient, and since it is an ointment dissolved in glycerin as a solvent and having a viscosity of at least 7000 (mPas) during production, it is preferably enclosed in any available tube (for example, an aluminum tube, an aluminum laminate tube, a resin (for example, polyethylene) tube), a plastic jar container, a glass container, etc.

[0028] Hereinafter, the present invention will be specifically shown by way of examples. The examples shown below do not limit the present invention by any means.

Example

[0029] Example 1: Manufacture of an ointment containing a water-soluble active ingredient In this example, studies were conducted for the purpose of producing an ointment containing a water-soluble active ingredient.

[0030] First, the water-soluble active ingredient was dissolved in glycerin by heating (this product is called Component A), while the oily base was dissolved by heating (this product is called Component B). Component A was added to Component B in one or multiple portions and mixed by stirring, and after mixing and kneading until the whole became homogeneous, it was further cooled while stirring to produce the ointment in this example. In this example, a heparin-like substance was used as the water-soluble active ingredient.

[0031] Specifically, the raw materials of Component A and the raw materials of Component B were weighed at the ratios described in the table and dissolved by heating at 70 to 80°C respectively. Then, Component A was gradually added to Component B while stirring and mixed with a disperser (manufactured by Mizusawa Industries), and then cooled while stirring to obtain an ointment. After that, it was filled into a plastic sealed container and stored for 2 weeks to 1 month in an environment of 40°C and 75RH%.

[0032] The solubility during production was evaluated according to the following evaluation criteria. 「Evaluation Criteria」 〇: No insoluble matter △: Signs of insoluble matter can be seen ×: There is insoluble matter.

[0033] The presence of "insoluble matter" in the ointment according to this standard was confirmed visually. Specifically, for the ointment of each production example, a sample after production was taken into a stainless-steel container, spread thinly, and the presence of insoluble matter was confirmed visually.

[0034] The stability of the ointment was classified according to the following evaluation criteria after storing the ointment for 2 weeks to 1 month: "Evaluation Criteria" 〇: No separation △: Signs of separation are observed ×: Separation.

[0035] "Separation" of the ointment according to this standard was confirmed by microscopic observation. Specifically, for the samples of the ointments of each comparative example and each production example stored for 2 weeks to 1 month in an environment of 40 °C and 75% RH constant, a small amount was taken into a preparation, and microscopic observation was performed to confirm the presence or absence of separation between the liquid part and the solid part.

[0036] The viscosity of the ointment at the time of production of each production example or comparative example was measured using a viscosity test method by the rotational viscometer method described in the general test method of the Japanese Pharmacopoeia, using "HAAKE Viscotester iQ Air" manufactured by Thermo Fisher Scientific.

[0037] The data for the ointments of each comparative example and each production example were summarized in the following table. The numerical values in the table all indicate weight %, and "-" indicates that it has not been evaluated.

[0038]

Table 1

[0039] As a result of the investigation in this example, when using 0.3% by weight of a heparin-like substance as the water-soluble active ingredient, by dissolving the water-soluble active ingredient in 1.0% to 40% by weight of glycerin and then mixing it with petrolatum, which is an oily base, it was possible to make the water-soluble active ingredient present in the ointment in a dissolved state without containing a surfactant (see Production Examples 1 to 4). Also, when the water-soluble active ingredient was dissolved in 0.7% by weight of glycerin, it was not possible to make the water-soluble active ingredient present in the ointment in a dissolved state during production (Comparative Example 4).

[0040] However, when not containing glycerin, or when using propylene glycol or butylene glycol as the solvent for the water-soluble active ingredient instead of glycerin, it was not possible to make the water-soluble active ingredient present in the ointment in a dissolved state (see Comparative Examples 1 to 3).

[0041] Example 2: Examination of the stability of an ointment containing a water-soluble active ingredient In this example, investigations were conducted for the purpose of improving the stability during storage of the ointment containing the water-soluble active ingredient.

[0042] First, the water-soluble active ingredient was dissolved in glycerin by heating (this product is referred to as Component A). On the other hand, the oily base and the lipophilic emulsifier, which is an optional component, were dissolved by heating (this product is referred to as Component B). Component A was added to Component B in one or multiple portions and mixed by stirring. After mixing and kneading until the whole became homogeneous, it was further cooled while stirring to produce the ointment in this example. In this example, a heparin-like substance was used as the water-soluble active ingredient, and polyglyceryl-2 oleate (a kind of polyglycerol fatty acid ester), glycerin stearate (a kind of glycerol fatty acid ester), or sorbitan stearate (a kind of sorbitan fatty acid ester) was used as the lipophilic emulsifier.

[0043] The production of the ointment and subsequent storage were carried out in the same manner as in Example 1. Also, the solubility during production and the stability of the ointment after storage for 2 weeks to 1 month were both evaluated based on the same criteria as those described in Example 1.

[0044] The data for the ointments of each comparative example and each production example were summarized in the following table. All the numerical values in the table represent weight %, and "-" indicates that no evaluation was made.

[0045]

Table 2

[0046] As a result of the examination in this example, when 0.3 wt% of a heparin analogue as a water-soluble active ingredient was dissolved in 12 wt% of glycerin and then mixed with petrolatum, which is an oily base, there was no difference in solubility during production regardless of the presence or absence of a surfactant in the ointment, and although a decrease in stability was observed in Production Example 3, there was no significant difference in stability up to 2 weeks after production (see Production Examples 3, 5 to 7).

[0047] On the other hand, when a lipophilic emulsifier is added as a surfactant to the ointment, the water-soluble active ingredient can be present in the ointment in a dissolved state even after storage for 1 month after preparation (see Production Examples 5 to 7). In particular, when polyglyceryl-2 oleate is added as a lipophilic emulsifier, the water-soluble active ingredient can be present in the ointment in a dissolved state without separation of Component A and Component B even after storage for 1 month after preparation (see Production Example 5).

[0048] However, even when polyglyceryl-2 oleate was mixed with petrolatum, which is an oily base, the water-soluble active ingredient could not be present in the ointment in a dissolved state when glycerin was not contained (see Comparative Example 5).

[0049] Example 3: Examination of the surfactant content in an ointment containing a water-soluble active ingredient In this example, studies were conducted for the purpose of examining the content of a lipophilic emulsifier that can be contained as an optional component in an ointment containing a water-soluble active ingredient.

[0050] First, a water-soluble active ingredient was dissolved in glycerin by heating (this product is referred to as Component A). On the other hand, an oily base and a lipophilic emulsifier as an optional component were dissolved by heating (this product is referred to as Component B). Component A was added to Component B in one or multiple portions and mixed by stirring. After mixing and kneading until the whole became homogeneous, it was further cooled while stirring to produce the ointment in this example. In this example, a heparin-like substance was used as the water-soluble active ingredient, and polyglyceryl-2 oleate was used as the lipophilic emulsifier.

[0051] The production of the ointment and subsequent storage were carried out in the same manner as in Example 1. Also, the solubility during production and the stability of the ointment after storage for 2 weeks to 1 month were evaluated based on the same criteria as those described in Example 1.

[0052] The data for the ointments of each comparative example and each production example were summarized in the following table. All the numerical values in the table indicate weight %, and "-" indicates that it was not evaluated.

[0053]

Table 3

[0054] As a result of the study in this example, when 0.3 wt% of a heparin-like substance as a water-soluble active ingredient was dissolved in various wt% of glycerin and then mixed with petrolatum as an oily base, when 0.1 to 10 wt% of polyglyceryl-2 oleate as a lipophilic emulsifier as a surfactant was added to the ointment, even after storage for 1 month after adjustment, the water-soluble active ingredient could be present in the ointment in a dissolved state without separation of Component A and Component B (see Production Examples 5, 8 to 11).

[0055] Example 4: Examination of water-soluble active ingredients In this example, the stability of water-soluble active ingredients other than heparin-like substances during storage was confirmed.

[0056] First, each water-soluble active ingredient was dissolved in glycerin by heating (this product is referred to as Component A), while an oily base and a lipophilic emulsifier were dissolved by heating (this product is referred to as Component B). Component A was added to Component B in one or multiple portions and mixed by stirring. After mixing and kneading until the whole became homogeneous, it was further cooled with stirring to produce the ointment in this example. In this example, heparin-like substances, urea, diphenhydramine hydrochloride, panthenol, sodium azulenesulfonate, cetylpyridinium chloride, benzethonium chloride, or dipotassium glycyrrhizinate were used as water-soluble active ingredients, and polyglyceryl-2 oleate was used as a lipophilic emulsifier.

[0057] The production of the ointment and subsequent storage were carried out in the same manner as in Example 1. Also, the solubility during production and the stability of the ointment after storage for 2 weeks to 1 month were evaluated based on the same criteria as those described in Example 1.

[0058] The data on the ointments of each comparative example and each production example were summarized in the following table. All the numerical values in the table represent weight %, and "-" indicates that it was not evaluated.

[0059]

Table 4

[0060] As a result of the study in this example, after dissolving water-soluble active ingredients at their desired concentrations in 12 wt% glycerin in the same manner as in Production Example 3, mixing them with petrolatum, which is an oily base, and further adding 2 wt% of polyglyceryl-2 oleate, a lipophilic emulsifier, as a surfactant to the ointment, it was possible to keep the water-soluble active ingredients dissolved in the ointment without separation of Component A and Component B even after storage for 1 month after preparation (see Production Examples 12 to 18).

Industrial Applicability

[0061] By using an ointment base containing glycerin provided by the present invention and a fat-soluble base such as petrolatum, a uniform and stable ointment containing a water-soluble active ingredient dissolved in the ointment can be provided. Further, an ointment containing a lipophilic emulsifier as an optional component for the purpose of improving the stability after production can be provided.

Claims

1. An ointment containing a water-soluble active ingredient, glycerin, and an oily base.

2. The ointment according to Claim 1, further containing a lipophilic emulsifier.

3. The ointment according to Claim 1 or 2, containing 1 to 40% by weight of glycerin and 30% by weight or more of an oily base.

4. The ointment according to any one of Claims 1 to 3, containing 1 to 6% by weight of glycerin and 90% by weight or more of an oily base.

5. The ointment according to any one of Claims 1 to 4, wherein the water-soluble active ingredient is a component soluble in glycerin.

6. The ointment according to any one of Claims 1 to 5, wherein the water-soluble active ingredient is selected from the group consisting of heparin-like substances, urea, dipotassium glycyrrhizinate, sodium azulenesulfonate, cetylpyridinium chloride, panthenol, diphenhydramine hydrochloride, and benzethonium chloride.

7. The ointment according to Claim 6, wherein the water-soluble active ingredient is a heparin-like substance or urea.

8. The ointment according to Claim 6, wherein the water-soluble active ingredient is 0.01 to 0.5% by mass of a heparin-like substance or 5.0 to 20.0% by mass of urea.

9. The ointment according to any one of Claims 1 to 8, wherein the oily base is petrolatum or a mixture of petrolatum and other oils.

10. The ointment according to Claim 9, wherein the other oils are one or more components selected from solid, semi-solid or liquid waxes, fatty acids, fatty acid esters, polyhydric alcohol fatty acid esters, higher alcohols, hydrocarbons, and silicone oils.

11. The ointment according to any one of Claims 2 to 10, containing a polyglycerol fatty acid ester, a glycerol fatty acid ester, or a sorbitan fatty acid ester as a lipophilic emulsifier.

12. The ointment according to Claim 11, wherein the polyglycerol fatty acid ester is polyglyceryl-2 oleate.

13. The ointment according to Claim 12, which is 0.1 to 10% by weight of polyglyceryl-2 oleate.

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