Topical compositions
By adding a heparinoid to topical compositions with phosphocholine group-containing polymers and hydroxypropyl methylcellulose, the formation of precipitates and sediment is inhibited, ensuring a stable and aesthetically pleasing appearance.
Patent Information
- Application Number
- JP2023103320
- Authority / Receiving Office
- JP · JP
- Patent Type
- Patents
- Current Assignee / Owner
- Filing Date
- 2023-06-23
- Publication Date
- 2025-08-28
- Estimated Expiration
- 2036-12-28
AI Technical Summary
Topical compositions containing phosphocholine group-containing polymers and hydroxypropyl methylcellulose suffer from the formation of precipitates and sedimentation, leading to unsuitable external appearance for practical use.
Incorporation of a heparin-like substance, specifically a heparinoid, with phosphocholine group-containing polymers and hydroxypropyl methylcellulose in the composition to suppress the formation of floating matter and precipitates.
The composition effectively prevents the occurrence of floating matter and sediment, providing excellent appearance properties and stability during storage.
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Figure 0007730863000003
Abstract
Description
[Technical Field]
[0001] The present invention relates to a composition for external use that contains a phosphocholine group-containing polymer and hydroxypropylmethylcellulose, yet is capable of suppressing the formation of floating matter or precipitates and has excellent appearance properties. [Background technology]
[0002] Phosphocholine group-containing polymers such as 2-methacryloyloxyethyl phosphorylcholine-butyl methacrylate copolymer have been known to penetrate the stratum corneum, prevent moisture evaporation, support the skin's barrier function, and protect the skin from various irritants, and have attracted attention as ingredients for topical compositions. Therefore, various formulations of topical compositions containing phosphocholine group-containing polymers have also been investigated. For example, Patent Document 1 discloses a skin care product containing a phosphocholine group-containing polymer with a specific average molecular weight and specific structure, and polyethylene glycol and / or polyoxyethylene methyl glucoside with a specific average molecular weight. The composition is reported to have excellent slipperiness when applied to the skin and to have a good feel when used.
[0003] It is also known that when hydroxypropylmethylcellulose is added to a topical composition, properties such as viscosity and retention on the skin are improved.
[0004] In recent years, the requirements for the feel and functionality of topical compositions have been increasing, and if a topical composition can be provided that combines the effects of a phosphocholine group-containing polymer and hydroxypropyl methylcellulose, it is expected that consumer satisfaction with skin care will be increased.
[0005] On the other hand, in order to put a topical composition into practical use, it is necessary to give sufficient consideration not only to its functionality but also to its excellent appearance. However, in the prior art, the appearance of topical compositions containing phosphocholine group-containing polymers and hydroxypropylmethylcellulose has not been sufficiently studied. [Prior art documents] [Patent documents]
[0006] [Patent Document 1] Japanese Patent Application Laid-Open No. 2010-43018 Summary of the Invention [Problem to be solved by the invention]
[0007] The present inventors have conducted research aimed at commercializing a topical composition containing a phosphocholine group-containing polymer and hydroxypropyl methylcellulose, and have encountered a new problem: the topical composition containing a phosphocholine group-containing polymer and hydroxypropyl methylcellulose produces precipitates, causing cloudiness and sedimentation due to suspended matter, and failing to have an external appearance suitable for practical use.
[0008] Therefore, the object of the present invention is to provide a formulation technology that can suppress the occurrence of floating matter and precipitates in an external composition containing a phosphocholine group-containing polymer and hydroxypropyl methylcellulose, and that provides an external appearance with excellent properties. [Means for solving the problem]
[0009] The inventors have conducted extensive research to solve the above problems and have found that an external composition containing a heparin-like substance together with a phosphocholine group-containing polymer and hydroxypropyl methylcellulose can suppress the formation of floating matter or precipitates even during storage and can have excellent appearance properties.
[0010] That is, the present invention provides the following aspects. Item 1. A composition for external use comprising (A) a phosphocholine group-containing polymer, (B) hydroxypropyl methylcellulose, and (C) a heparinoid. Item 2. The topical composition according to Item 1, wherein the phosphocholine group-containing polymer (A) is a 2-methacryloyloxyethyl phosphorylcholine-butyl methacrylate copolymer. Item 3. The composition for external use according to Item 1 or 2, containing 0.01 to 5% by weight of the heparinoid (C). Item 4. The composition for external use according to any one of Items 1 to 3, further comprising (D) a polyhydric alcohol. Item 5. A method for suppressing the formation of suspended matter and / or precipitates in a topical composition containing a phosphocholine group-containing polymer and hydroxypropyl methylcellulose, comprising: The topical composition contains (A) a phosphocholine group-containing polymer, (B) hydroxypropyl methylcellulose, and (C) a heparinoid. A method for inhibiting the occurrence of floating matter and / or sediment in the topical composition. [Effects of the Invention]
[0011] The topical composition of the present invention contains a phosphocholine group-containing polymer and hydroxypropylmethylcellulose, yet is capable of suppressing the occurrence of floating matter and sediment, and can provide excellent appearance properties. DETAILED DESCRIPTION OF THE INVENTION
[0012] 1. External composition The topical composition of the present invention is characterized by containing a phosphocholine group-containing polymer (sometimes referred to as component (A)), hydroxypropyl methylcellulose (sometimes referred to as component (B)), and a heparinoid (sometimes referred to as component (C)). The topical composition of the present invention is described in detail below.
[0013] (A) Phosphocholine group-containing polymer A phosphocholine group-containing polymer is a polymer formed by polymerization of a monomer containing a phosphocholine group (hereinafter sometimes referred to as a "phosphocholine group-containing monomer"), and is a known component that has moisturizing properties, a barrier function for the stratum corneum, etc.
[0014] In the phosphocholine group-containing polymer used in the present invention, the type of phosphocholine group-containing monomer is not particularly limited, and examples thereof include monomers having a phosphocholine group and a vinyl group. More specific examples of phosphocholine group-containing monomers include 2-methacryloyloxyethyl phosphorylcholine and 2-methacryloyloxyethyl phosphorylethanolamine. In the phosphocholine group-containing polymer, the phosphocholine group-containing monomer may be contained alone or in combination of two or more. Among these phosphocholine group-containing monomers, 2-methacryloyloxyethyl phosphorylcholine is preferred from the viewpoint of more effectively suppressing the generation of suspended matter and precipitates.
[0015] The phosphocholine group-containing polymer used in the present invention may be a homopolymer consisting of one type of phosphocholine group-containing monomer, or may be a copolymer consisting of two or more types of monomers.
[0016] When the phosphocholine group-containing polymer is a copolymer, it may be a copolymer consisting of two or more types of phosphocholine group-containing monomers, or it may be a copolymer consisting of at least one type of phosphocholine group-containing monomer and at least one type of monomer other than the phosphocholine group-containing monomer.
[0017] The type of monomer other than the phosphocholine group-containing monomer contained in the phosphocholine group-containing polymer is not particularly limited, as long as it is pharmaceutically acceptable and capable of radical polymerization with the phosphocholine group-containing monomer, and examples thereof include monomers having a vinyl group. Specific examples of monomers other than phosphocholine group-containing monomers include alkyl (meth)acrylates such as methyl (meth)acrylate, ethyl (meth)acrylate, butyl (meth)acrylate, lauryl (meth)acrylate, stearyl (meth)acrylate, and 2-ethylhexyl (meth)acrylate; benzyl (meth)acrylate, phenoxyethyl (meth)acrylate, cyclohexyl (meth)acrylate, polypropylene glycol mono(meth)acrylate, polytetramethylene glycol mono(meth)acrylate, polypropylene glycol di(meth)acrylate, polytetramethylene glycol mono(meth)acrylate, polypropylene glycol polyethylene glycol mono(meth)acrylate, sodium methacrylate, and 2-hydroxy-3-methacryloyloxypropyltrimethylammonium. In the phosphocholine group-containing polymer, the monomers other than the phosphocholine group-containing monomer may be contained alone or in combination of two or more. Among these monomers other than the phosphocholine group-containing monomer, from the viewpoint of more effectively suppressing the generation of suspended matter and precipitates, preferred are alkyl(meth)acrylates and 2-hydroxy-3-methacryloyloxypropyltrimethylammonium, more preferred are alkyl(meth)acrylates having an alkyl group with 1 to 18 carbon atoms, even more preferred are alkyl(meth)acrylates having an alkyl group with 3 to 5 carbon atoms, and particularly preferred is butyl(meth)acrylate. In this specification, "(meth)acrylate" refers to methacrylate and / or acrylate.
[0018] Specific examples of the phosphocholine group-containing polymers used in the present invention include polymethacryloyloxyethyl phosphorylcholine homopolymer, 2-methacryloyloxyethyl phosphorylcholine-butyl methacrylate copolymer (Polyquaternium-51), 2-methacryloyloxyethylene phosphorylcholine-butyl methacrylate-sodium methacrylate copolymer (Polyquaternium-65), 2-methacryloyloxyethyl phosphorylcholine-2-hydroxy-3-methacryloyloxypropyltrimethylammonium copolymer (Polyquaternium-64), and 2-methacryloyloxyethyl phosphorylcholine-stearyl methacrylate copolymer (Polyquaternium-61). In the above descriptions of the phosphocholine group-containing polymers, the names in parentheses indicate the cosmetic ingredient names.
[0019] In the topical composition of the present invention, the phosphocholine group-containing polymer may be used alone or in combination of two or more.
[0020] Among these phosphocholine group-containing polymers, from the viewpoint of more effectively suppressing the formation of suspended matter and sediment, preferred are 2-methacryloyloxyethyl phosphorylcholine-butyl methacrylate copolymer, polymethacryloyloxyethyl phosphorylcholine homopolymer, and 2-methacryloyloxyethyl phosphorylcholine-2-hydroxy-3-methacryloyloxypropyltrimethylammonium copolymer; more preferred are 2-methacryloyloxyethyl phosphorylcholine-butyl methacrylate copolymer and 2-methacryloyloxyethyl phosphorylcholine-2-hydroxy-3-methacryloyloxypropyltrimethylammonium copolymer; and particularly preferred are 2-methacryloyloxyethyl phosphorylcholine-butyl methacrylate copolymer.
[0021] In the topical composition of the present invention, the content of component (A) is not particularly limited and may be appropriately determined depending on the desired effect, but may be, for example, 0.025 to 1% by weight. From the viewpoint of more effectively suppressing the formation of suspended matter and precipitates, the content of component (A) is preferably 0.05 to 0.5% by weight, and more preferably 0.1 to 0.3% by weight.
[0022] (B) Hydroxypropyl methylcellulose Hydroxypropyl methylcellulose is a cellulose derivative and a compound also known as hypromellose.
[0023] The degree of substitution of the hydroxypropyl methylcellulose used in the present invention is not particularly limited and may be any of 1828, 2208, 2906, and 2910. From the viewpoint of more effectively suppressing phase separation, however, preferred are those with degrees of substitution of 2208, 2906, and 2910.
[0024] The viscosity of the hydroxypropyl methylcellulose used in the present invention is not particularly limited, but examples thereof include a viscosity of 1,000 mPa·s or more, preferably 1,000 to 200,000 mPa·s, in a 2 wt% aqueous solution (20°C). Here, the viscosity is a value measured using a Brookfield viscometer "TOKI SANGYO VISCOMETER TVB-10" (manufactured by Toki Sangyo Co., Ltd.) with a rotor M3 (rotation speed: 20 rpm, time: 1 min, unit: mPa·s).
[0025] In the topical composition of the present invention, commercially available hydroxypropyl methylcellulose can be used. Specific examples of commercially available hydroxypropyl methylcellulose include "Metolose 90SH-100SR", "Metolose 90SH-4000SR", "Metolose 90SH-15000SR", "Metolose 90SH-100000SR", "Metolose 65SH-50", "Metolose 65SH-400", "Metolose 65SH-1500", "Metolose 65SH-4000", "Metolose 60SH-50", "Metolose 60SH-4000", "Metolose 60SH-10000", and "Metolose TC" manufactured by Shin-Etsu Chemical Co., Ltd. -5E", "Metolose 90SH-100SR", "Metolose 90SH-4000SR", "Metolose 90SH-15000SR", "Metolose 90SH-100000SR", "Metolose TC-5M", "Metolose TC-5R", "Metolose TC-5S", "Metolose SB-4" manufactured by Dow Chemical Japan Co., Ltd.; "Methocel E4M", "Methocel E4M", "Methocel 40-100", "Methocel 40-101", "Methocel 40-202" manufactured by Matsumoto Yushi Pharmaceutical Co., Ltd.; and the like.
[0026] In the topical composition of the present invention, one type of hydroxypropyl methylcellulose may be used alone, or two or more types may be used in combination.
[0027] In the topical composition of the present invention, the content of component (B) is not particularly limited and may be appropriately determined depending on the viscosity and usability to be imparted to the topical composition, but may be, for example, 0.1 to 5% by weight. From the viewpoint of more effectively suppressing the formation of suspended matter and sediment, the content of component (B) is preferably 0.1 to 3% by weight, more preferably 0.3 to 2% by weight, and particularly preferably 0.3 to 1% by weight.
[0028] In the topical composition of the present invention, the ratio of component (B) to component (A) is determined depending on the respective contents of components (A) and (B), but may be, for example, 50 to 3,000 parts by weight of component (B) per 100 parts by weight of component (A).From the viewpoint of more effectively suppressing the formation of suspended matter and sediment, the ratio of component (B) to component (A) is preferably 100 to 2,500 parts by weight, more preferably 300 to 2,000 parts by weight, of component (B) per 100 parts by weight of component (A).
[0029] (C) Heparinoids Heparinoids are polysulfated mucopolysaccharides such as chondroitin polysulfate, and are known drugs known to have moisturizing, anti-inflammatory, and blood circulation promoting effects, etc. By including a heparinoid in the topical composition of the present invention, the occurrence of floating matter and precipitates that occur in the coexistence of a phosphocholine group-containing polymer and hydroxypropyl methylcellulose can be suppressed, and the composition can have excellent appearance properties.
[0030] The origin of the heparinoid used in the present invention is not particularly limited, and examples thereof include those obtained by polysulfating mucopolysaccharides, and those extracted from the tissues of edible animals (e.g., lungs containing tracheal cartilage from cattle, pigs, etc.). In the topical composition of the present invention, heparinoids listed in the Japanese Pharmacopoeia Non-Drug Standards are preferably used.
[0031] The content of component (C) in the topical composition of the present invention is not particularly limited, but may be, for example, 0.01 to 5% by weight. From the viewpoint of more effectively suppressing the formation of suspended matter and precipitates, the content of component (C) is preferably 0.05 to 3% by weight, more preferably 0.1 to 1% by weight, and particularly preferably 0.3 to 1% by weight.
[0032] In the topical composition of the present invention, the ratio of component (C) to component (A) is determined depending on the respective contents of components (A) and (B), but may be, for example, 100 to 2000 parts by weight of component (C) per 100 parts by weight of component (A).From the viewpoint of more effectively suppressing the formation of suspended matter and sediment, the ratio of component (C) to component (A) is preferably 200 to 1500 parts by weight, more preferably 300 to 1000 parts by weight, of component (C) per 100 parts by weight of component (A).
[0033] (D) Polyhydric alcohol In addition to the components (A) to (C), the topical composition of the present invention may optionally contain a polyhydric alcohol (sometimes referred to as (D)). The inclusion of a polyhydric alcohol may more effectively provide excellent appearance properties and may also enhance the moisturizing effect of component (A).
[0034] The polyhydric alcohol is not particularly limited as long as it is pharmaceutically or cosmetically acceptable, and examples thereof include 1,3-butylene glycol, ethylene glycol, propylene glycol, isoprene glycol, diethylene glycol, dipropylene glycol, polyethylene glycol, glycerin, etc. Among these polyhydric alcohols, 1,3-butylene glycol and propylene glycol are preferred.
[0035] These polyhydric alcohols may be used alone or in combination of two or more.
[0036] When the topical composition of the present invention contains component (D), its content may be appropriately set depending on the type of polyhydric alcohol used, etc., but may be, for example, 1% by weight or more, preferably 2 to 20% by weight, and more preferably 3 to 20% by weight.
[0037] water The topical composition of the present invention is prepared as an aqueous composition containing water. The content of water in the topical composition of the present invention may be appropriately determined depending on the formulation, but may be, for example, 5 to 95% by weight, preferably 5 to 90% by weight, and more preferably 10 to 90% by weight.
[0038] Other ingredients The topical composition of the present invention may contain, in addition to the above-mentioned components, other pharmacological components, if necessary. Examples of such pharmacological ingredients include antihistamines (diphenhydramine, diphenhydramine hydrochloride, etc.), local anesthetics (procaine, tetracaine, bupipacaine, mepipacaine, chloroprocaine, proparacaine, meprylcaine or salts thereof, orthocaine, oxethazaine, oxypolyethoxydecane, Scopolia extract, percaminpase, tesitdesitin, etc.), anti-inflammatory agents (dipotassium glycyrrhizinate, glycyrrhetinic acid, indomethacin, felbinac, diclofenac sodium, loxoprofen sodium, etc.), skin protectants (collodion, castor oil, etc.), blood circulation promoting ingredients (vanillyl nonylate amide, nicotinic acid benzyl ester, capsaicin, chili pepper extract, etc.), refreshing agents (menthol, camphor, etc.), vitamins (vitamin A, etc.), mucopolysaccharides (sodium chondroitin sulfate, glucosamine, etc.), etc.
[0039] Furthermore, the topical composition of the present invention may contain, as necessary, base materials or additives other than the above-mentioned components to obtain a desired formulation. Such base materials and additives are not particularly limited as long as they are pharmaceutically acceptable, and examples thereof include oils (olive oil, safflower oil, soybean oil, camellia oil, corn oil, rapeseed oil, sunflower oil, cottonseed oil, peanut oil, lard, squalane, fish oil, etc.), mineral oils (liquid paraffin, paraffin, gelling hydrocarbon, petrolatum, etc.), waxes (beeswax, carnauba wax, candelilla wax, ceresin, rice wax, microcrystalline wax, etc.), ester oils (isopropyl myristate, isopropyl adipate, diethyl sebacate, isopropyl sebacate, isopropyl palmitate, cetyl palmitate, ethyl oleate, etc.), oily bases such as fatty acid alkyl esters, fatty acids (stearic acid, oleic acid, palmitic acid, behenic acid, linoleic acid, lanolin, etc.), fatty acid esters (cetyl palmitate, isopropyl palmitate, ethyl linoleate, etc.), lower alcohols (ethanol, propanol, isopropanol, butanol, isobutanol, etc.), higher alcohols (stearyl alcohol, cetanol, behenyl alcohol, myristyl alcohol, oleyl alcohol, hexadecyl alcohol, lanolin alcohol, etc.), cholesterol, glyceryl tri-2-ethylhexanoate, cetyl 2-ethylhexanoate, silicone oils (dimethylpolysiloxane, cyclic silicone, etc.);Polyoxyethylene alkyl ethers such as POE (10-50 mol) phytosterol ether, POE (10-50 mol) dihydrocholesterol ether, POE (10-50 mol) 2-octyldodecyl ether, POE (10-50 mol) decyltetradecyl ether, POE (10-50 mol) oleyl ether, POE (2-50 mol) cetyl ether, POE (5-50 mol) behenyl ether, POE (5-30 mol) polyoxypropylene (5-30 mol) 2-decyltetradecyl ether, POE (10-50 mol) polyoxypropylene (2-30 mol) cetyl ether, and their phosphoric acid salts (e.g., sodium POE cetyl ether phosphate), POE (20-60 mol) sorbitan monooleate, and POE (10-60 mol) sorbitan monoisostearate Surfactants such as POE (10-80 mol) glyceryl monoisostearate, POE (10-30 mol) glyceryl monostearate, POE (20-100 mol) polyoxypropylene-modified silicone, POE alkyl-modified silicone, polyethylene glycol monolaurate, polyethylene glycol monopalmitate, polyethylene glycol monostearate, polyethylene glycol dilaurate, polyethylene glycol dipalmitate, polyethylene glycol distearate, polyethylene glycol dioleate, polyethylene glycol diricinoleate, polyoxyethylene hydrogenated castor oil (5-100), polysorbate (20-85), glycerin fatty acid esters (glycerin monostearate, etc.), hydrogenated soybean phospholipids, and hydrogenated lanolin alcohol;Cooling agents (menthol, camphor, borneol, peppermint water, peppermint oil, etc.), preservatives (methylparaben, propylparaben, benzoic acid, sodium benzoate, sorbic acid, etc.), flavoring agents (citral, 1,8-sionel, citronellal, farnesol, etc.), coloring agents (tar dyes (Brown No. 201, Blue No. 201, Yellow No. 4, Yellow No. 403, etc.), cocoa pigments, chlorophyll, aluminum oxide, etc.), thickeners (carboxyvinyl polymer, polyvinylpyrrolidone, sodium alginate, ethyl cellulose, sodium carboxymethylcellulose, xanthan gum, carrageenan, etc.), pH adjusters (phosphoric acid, hydrochloric acid, citric acid, sodium citrate, succinic acid, etc.) Examples of additives include: carboxylic acid, tartaric acid, sodium hydroxide, potassium hydroxide, triethanolamine, triisopropanolamine, etc.), wetting agents (sodium dl-pyrrolidonecarboxylate solution, D-sorbitol solution, macrogol, etc.), stabilizers (dibutylhydroxytoluene, butylhydroxyanisole, sodium edetate, sodium metaphosphate, L-arginine, L-aspartic acid, DL-alanine, glycine, sodium erythorbate, propyl gallate, sodium sulfite, sulfur dioxide, chlorogenic acid, catechin, rosemary extract, etc.), antioxidants, UV absorbers, chelating agents, adhesives, buffers, solubilizers, solubilizers, and preservatives;
[0040] pH The pH of the topical composition of the present invention is not particularly limited and may be appropriately set taking into consideration irritation to the skin, etc., but is, for example, 3 to 8, preferably 3 to 7.
[0041] Formulation The formulation of the preventive or therapeutic agent of the present invention is not particularly limited, and may be either liquid or semi-solid (gel, paste) as long as it is in a dosage form that can be applied transdermally.
[0042] The topical composition of the present invention may be in any formulation, such as a topical skin drug (including quasi-drugs), a cosmetic, or a skin cleanser, as long as it is applied to the skin. Specific examples of the formulation of the topical composition of the present invention include topical skin drugs such as gels, creams, lotions, emulsions, liquids, patches, aerosols, ointments, and packs; cosmetics such as gels, creams, emulsions, skin lotions, lotions, and packs; and skin cleansers such as body shampoos, hair shampoos, and rinses. Among these formulations, topical skin drugs are preferred, and gels, lotions, and liquids are more preferred.
[0043] The topical composition of the present invention can exert moisturizing effects, stratum corneum barrier function, etc. based on the component (A) it contains, and can also exert moisturizing effects, anti-inflammatory effects, blood circulation promoting effects, etc. based on the component (C) it contains, so it is suitably used for purposes such as moisturizing, improving rough skin, preventing or treating dry skin diseases, and preventing or treating inflammatory skin diseases.
[0044] 2. Method for inhibiting the occurrence of floating matter and / or sediment in a topical composition The present invention further provides a method for inhibiting the formation of floating matter and / or precipitate in a topical composition containing (A) a phosphocholine group-containing polymer and (B) hydroxypropyl methylcellulose, characterized in that the method comprises incorporating (C) a heparin-like substance into the topical composition.
[0045] In this method, the types and contents of (A) to (C) used, the types and contents of other ingredients to be blended, the formulation form of the topical composition, etc. are the same as those in "1. Topical composition" above. [Example]
[0046] The present invention will be explained in more detail below by showing examples, but the present invention is not limited to these examples. Test Example 1. Preparation of topical composition A gel-type topical composition was prepared with the composition shown in Table 1. Specifically, a predetermined amount of hydroxypropyl methylcellulose, heparinoid, and propylene glycol was added to purified water and uniformly dispersed and dissolved, and then a predetermined amount of 2-methacryloyloxyethylphosphocholine-butyl methacrylate copolymer was added and mixed to obtain a gel-type topical composition.
[0047] 2. Evaluation of appearance The appearance of each of the obtained external compositions was visually inspected immediately after production, and the appearance properties were evaluated. In addition, after storing each of the obtained external compositions at 20°C under light-shielded conditions for 1 hour, the appearance was visually inspected and the appearance properties were evaluated. The appearance properties were evaluated according to the following criteria. <Evaluation criteria for appearance properties> (prevention of precipitation) ⊚: No precipitate was observed immediately after preparation or after storage. ○: A slight amount of precipitate was observed immediately after preparation, but the precipitate disappeared after storage. △: A slight amount of precipitate was generated immediately after preparation, and the precipitate remained even after storage. ×: A significant amount of precipitate was generated immediately after preparation, and the precipitate remained even after storage. (Suppression of floating matter) ⊚: No floating matter was generated immediately after preparation or after storage, and no cloudiness was observed. ○: Immediately after preparation, a small amount of floating matter was generated, causing slight turbidity, but after storage, the floating matter disappeared and no turbidity was observed. △: A small amount of floating matter was generated immediately after preparation, causing slight cloudiness, and the floating matter remained even after storage, and the solution remained cloudy. ×: A significant amount of floating matter was generated immediately after preparation, causing noticeable cloudiness, and even after storage, the floating matter remained and the solution remained significantly cloudy.
[0048] 3.Results The results are shown in Table 1. When hydroxypropyl methylcellulose was contained alone (Reference Example 1), no floating matter or precipitate was observed, but when 2-methacryloyloxyethylphosphocholine-butyl methacrylate copolymer and hydroxypropyl methylcellulose were used in combination (Comparative Examples 1 and 2), significant floating matter and precipitate were observed. In contrast, when a heparinoid was contained together with 2-methacryloyloxyethylphosphocholine-butyl methacrylate copolymer and hydroxypropyl methylcellulose (Examples 1 to 8), the occurrence of floating matter and precipitate was sufficiently suppressed.
[0049] [Table 1]
[0050] Prescription example The topical compositions (liquid) shown in Table 2, the topical compositions (lotion) shown in Table 3, and the topical compositions (gel) shown in Table 4 were prepared. The external appearance of the obtained topical compositions was evaluated in the same manner as in the above test examples, and it was found that the occurrence of floating matter and precipitation was sufficiently suppressed in all cases.
[0051] [Table 2]
[0052] [Table 3]
[0053] [Table 4]
Claims
1. A composition for external use comprising (A) 2-methacryloyloxyethyl phosphorylcholine / butyl methacrylate copolymer, (B) hydroxypropyl methylcellulose, (C) a heparinoid, and water.
2. The topical composition according to claim 1, containing 0.01 to 5% by weight of the (C) heparinoid.
3. The topical composition according to claim 1 or 2, further comprising (D) a polyhydric alcohol.
4. A method for suppressing the formation of floating matter and / or precipitates in a topical composition containing 2-methacryloyloxyethyl phosphorylcholine / butyl methacrylate copolymer and hydroxypropyl methylcellulose, comprising: The topical composition contains (A) 2-methacryloyloxyethyl phosphorylcholine / butyl methacrylate copolymer, (B) hydroxypropyl methylcellulose, and water, as well as (C) a heparinoid. A method for inhibiting the occurrence of floating matter and / or sediment in the topical composition.
Citation Information
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