CN114848593A - Foam composition and preparation method thereof - Google Patents
Foam composition and preparation method thereof Download PDFInfo
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- CN114848593A CN114848593A CN202210602957.8A CN202210602957A CN114848593A CN 114848593 A CN114848593 A CN 114848593A CN 202210602957 A CN202210602957 A CN 202210602957A CN 114848593 A CN114848593 A CN 114848593A
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/12—Aerosols; Foams
- A61K9/122—Foams; Dry foams
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/402—1-aryl substituted, e.g. piretanide
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/455—Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/20—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
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- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
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- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
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- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
Abstract
The application relates to the technical field of medicines, and provides a foam composition which comprises an effective dose of active ingredients and auxiliary materials, wherein the active ingredients comprise tretinoin medicines and/or pharmaceutically acceptable salts or esters thereof, and the auxiliary materials comprise a surfactant and an aqueous solvent. The foam compositions provided herein contain tretinoin drugs, which allow the foam compositions to be used to treat mild to severe skin disorders; the contained aqueous solvent can provide water and dissolve the tretinoin medicine; the surfactant has solubilization, can increase the solubility of the vitamin A acid drugs which are difficult to dissolve or insoluble in the aqueous solvent, and enables the foam composition to present good transparent appearance; the surfactant also has a foaming effect and forms an arrangement of two electron layers on the surface of the liquid film to surround the air to form a foam when the foam composition is dispensed by the actuator. Therefore, the propellant or gas is not needed, expensive production equipment and special distributors are not needed, and the cost is low.
Description
Technical Field
The application belongs to the technical field of medicines, and particularly relates to a foam composition and a preparation method thereof.
Background
Tretinoin is a compound related to vitamin A or retinoid, and tretinoin medicines are usually in various dosage forms such as emulsion, cream, gel and ointment, and are widely used for treating dermatosis such as acne. However, tretinoin creams and ointments have poor fluidity, are difficult to apply to the desired site of administration, are greasy, and have a large area of acne, and therefore, use over a large area can create an unpleasant experience. It also can block skin pores to induce acne formation, and has long-term administration for ensuring therapeutic effect and skin irritation effect. In addition, the existing tretinoin preparation has single function, has no beautifying effect and cannot play a role in moisturizing and nourishing.
The foaming agent of the tretinoin medicine has the characteristics of good spreadability, low density, easy control of dosage and the like, and can overcome the tolerance problem. However, the existing prescription of foam preparation requires the use of propellant or gas to generate foam, and the use of propellant or gas requires the use of a special container sealing system and a filling line to fill the propellant or gas into the container sealing system under pressure to generate foam, and the special container sealing system is expensive, resulting in high production cost of the product.
Therefore, the development of a propellant-free foaming agent of tretinoin having a cosmetic effect is a problem to be solved at present.
Disclosure of Invention
The present application aims to provide a foam composition and a method for preparing the same, aiming to solve the technical problem that the existing foam composition needs special production equipment and a dispensing container due to the use of propellant or gas.
In order to achieve the purpose of the application, the technical scheme adopted by the application is as follows:
in a first aspect, the present application provides a foam composition comprising an effective amount of an active ingredient comprising a retinoid drug and/or a pharmaceutically acceptable salt or ester thereof, and an excipient comprising a surfactant and an aqueous solvent.
In a second aspect, the present application provides a method of preparing a foam composition comprising the steps of:
s10: providing auxiliary materials, tretinoin medicaments and/or pharmaceutically acceptable salts or esters thereof;
s20: mixing the auxiliary materials with the tretinoin medicine and/or pharmaceutically acceptable salt or ester thereof to obtain the foam composition.
The foam composition provided by the first aspect of the application contains the tretinoin medicine and/or pharmaceutically acceptable salt or ester thereof as an active ingredient with effective dose, so that the foam composition can be used for treating mild to severe skin diseases; the contained aqueous solvent can provide water and can also dissolve the tretinoin medicine and/or pharmaceutically acceptable salt or ester thereof; the surfactant plays a role in solubilization, can increase the solubility of the vitamin A acid drugs which are difficult to dissolve or insoluble in an aqueous solvent and/or pharmaceutically acceptable salts or esters thereof in the aqueous solvent, and enables the foam composition to present a good transparent appearance; on the other hand, the surfactant has fixed hydrophilic and lipophilic groups, the hydrophilic groups are arranged inwards, and the lipophilic groups are arranged outwards (air), so that the hydrophilic groups and the lipophilic groups can be directionally arranged on the surface of the solution to form a bimolecular membrane structure. Therefore, when the foam composition is dispensed in the actuator, the surfactant is adsorbed at the interface between the solution of the foam composition and the air, and the surface tension of the solution is significantly lowered, thereby forming an electric double layer arrangement on the surface of the liquid film to surround the air to form bubbles, whereby a large number of bubbles can constitute the foam. Therefore, the foam composition can be dispensed and foamed by using a common actuator without using a propellant or gas and expensive production equipment and a special dispenser, and is low in cost.
According to the preparation method of the foam composition provided by the second aspect of the application, the auxiliary material and the tretinoin medicine and/or the pharmaceutically acceptable salt or ester thereof are mixed to obtain the foam composition. Therefore, the preparation method is simple to operate, low in cost and suitable for large-scale production and application.
Drawings
In order to more clearly illustrate the technical solutions in the embodiments of the present application, the drawings needed to be used in the embodiments or the prior art descriptions will be briefly described below, and it is obvious that the drawings in the following description are only some embodiments of the present application, and it is obvious for those skilled in the art to obtain other drawings without creative efforts.
FIG. 1 is a process flow diagram of a method of preparing a foam composition provided in the examples herein;
FIG. 2 is a schematic diagram of the mechanism of foam formation in a foam pump for a foam composition provided in the examples herein;
FIG. 3 is a mechanical drawing of foam formation in a drive chamber of a foam composition provided in the examples herein;
fig. 4 is a diagram of a container sealing system for a foam composition provided in the examples herein.
Detailed Description
In order to make the technical problems, technical solutions and advantageous effects to be solved by the present application more clearly apparent, the present application is further described in detail below with reference to the embodiments. It should be understood that the specific embodiments described herein are merely illustrative of the present application and are not intended to limit the present application.
In this application, the term "and/or" describes an association relationship of associated objects, meaning that there may be three relationships, e.g., a and/or B, which may mean: a alone, A and B together, and B alone. Wherein A and B can be singular or plural. The character "/" generally indicates that the former and latter associated objects are in an "or" relationship.
In the present application, "at least one" means one or more, "a plurality" means two or more. "at least one of the following" or similar expressions refer to any combination of these items, including any combination of the singular or plural items. For example, "at least one (a), b, or c", or "at least one (a), b, and c", may each represent: a, b, c, a-b (i.e., a and b), a-c, b-c, or a-b-c, wherein a, b, and c may be single or plural, respectively.
It should be understood that, in various embodiments of the present application, the sequence numbers of the above-mentioned processes do not mean the execution sequence, some or all of the steps may be executed in parallel or executed sequentially, and the execution sequence of each process should be determined by its function and inherent logic, and should not constitute any limitation to the implementation process of the embodiments of the present application.
The terminology used in the embodiments of the present application is for the purpose of describing particular embodiments only and is not intended to be limiting of the application. As used in the examples of this application and the appended claims, the singular forms "a", "an", and "the" are intended to include the plural forms as well, unless the context clearly indicates otherwise.
The weight of the related components mentioned in the description of the embodiments of the present application may not only refer to the specific content of each component, but also represent the proportional relationship of the weight among the components, and therefore, the content of the related components is scaled up or down within the scope disclosed in the description of the embodiments of the present application as long as it is scaled up or down according to the description of the embodiments of the present application. Specifically, the mass described in the specification of the embodiments of the present application may be a mass unit known in the chemical industry field such as μ g, mg, g, kg, etc.
The terms "first" and "second" are used for descriptive purposes only and are used for distinguishing purposes such as substances from one another, and are not to be construed as indicating or implying relative importance or implying any number of technical features indicated. For example, a first XX may also be referred to as a second XX, and similarly, a second XX may also be referred to as a first XX, without departing from the scope of embodiments of the present application. Thus, a feature defined as "first" or "second" may explicitly or implicitly include one or more of that feature.
The first aspect of the embodiments of the present application provides a foam composition, which includes an effective dose of an active ingredient and an adjuvant, wherein the active ingredient includes a retinoic acid drug and/or a pharmaceutically acceptable salt or ester thereof, and the adjuvant includes a surfactant and an aqueous solvent.
The foam composition provided by the embodiment of the application contains the tretinoin medicine and/or pharmaceutically acceptable salt or ester thereof as an active ingredient with effective dose, so that the foam composition can be used for treating mild to severe skin diseases; the contained aqueous solvent can provide water and can also dissolve the tretinoin medicine and/or pharmaceutically acceptable salt or ester thereof; the surfactant plays a role in solubilization, can increase the solubility of the vitamin A acid drugs which are difficult to dissolve or insoluble in an aqueous solvent and/or pharmaceutically acceptable salts or esters thereof in the aqueous solvent, and enables the foam composition to present a good transparent appearance; on the other hand, the surfactant has fixed hydrophilic and lipophilic groups, the hydrophilic groups are arranged inwards, and the lipophilic groups are arranged outwards (air), so that the hydrophilic groups and the lipophilic groups can be directionally arranged on the surface of the solution to form a bimolecular membrane structure. Therefore, when the foam composition is dispensed in the actuator, the surfactant is adsorbed at the interface between the solution of the foam composition and the air, and the surface tension of the solution is significantly lowered, thereby forming an electric double layer arrangement on the surface of the liquid film to surround the air to form bubbles, whereby a large number of bubbles can constitute the foam. Therefore, the foam composition can be dispensed and foamed by using a common actuator without using a propellant or gas and expensive production equipment and a special dispenser, and is low in cost.
In the examples, the compositions comprise, in weight percentages based on the total weight of the foam composition taken as 100%:
vitamin A acid medicine and/or its pharmaceutically acceptable salt or ester 0.001-5%
1 to 40 percent of surfactant
30-80% of aqueous solvent.
The tretinoin drugs and/or pharmaceutically acceptable salts or esters thereof in the examples may represent: the active component of the foam composition only contains the tretinoin medicine, or the active component of the foam composition only contains pharmaceutically acceptable salt or ester of the tretinoin medicine, or the active component of the foam composition contains both the tretinoin medicine and the pharmaceutically acceptable salt or ester thereof. The foam composition provided by the embodiment contains 0.001-5% of the tretinoin drug, so that the foam composition can be used for treating mild to severe skin diseases, contains 30-80% of an aqueous solvent, can make the foam composition contain water remarkably, can dissolve the tretinoin drug or pharmaceutically acceptable salt or ester thereof, reduces the using amount of a surfactant, contains 1-40% of the surfactant, can increase the solubility of the tretinoin drug or pharmaceutically acceptable salt or ester thereof which is insoluble or insoluble in the aqueous solvent, can make the foam composition present a good transparent appearance, can fully exert the drug effect of the tretinoin drug, and can play a foaming role, when the foam composition is distributed in an actuator, the surfactant is adsorbed on two-phase interfaces of a foam composition solution and air, the surface tension of the solution is obviously reduced, the double electronic layers are arranged on the surface of the liquid film to surround the air, a large number of bubbles are formed to form foam, and the volume fraction of gas in the foam can be increased, so that the stability of the foam can be improved, the elimination of liquid can be reduced, the emulsification can be delayed, and the foam composition has proper viscosity.
In the examples, the compositions comprise, in weight percentages based on the total weight of the foam composition taken as 100%:
vitamin A acid medicine and/or its pharmaceutically acceptable salt or ester 0.005-2%
1 to 40 percent of surfactant
40-70% of aqueous solvent.
The foam composition provided by the embodiment contains 0.005-2% of the tretinoin medicine, so that the foam composition can be used for treating mild to moderate skin diseases, contains 40-70% of an aqueous solvent, can remarkably contain water, can dissolve the tretinoin medicine or pharmaceutically acceptable salts or esters thereof, reduces the using amount of a surfactant, and contains 1-40% of the surfactant, so that on one hand, the solubility of the tretinoin medicine or pharmaceutically acceptable salts or esters thereof which is difficult to dissolve or insoluble in the aqueous solvent can be increased, the foam composition can present a good transparent appearance, the efficacy of the tretinoin medicine can be fully exerted, on the other hand, the foaming effect is achieved, the volume fraction of gas in the foam can be increased, and the stability of the foam is improved.
In an embodiment, the foam composition comprises 0.001-5% of a retinoid drug and/or a pharmaceutically acceptable salt or ester thereof. The tretinoin medicine and/or pharmaceutically acceptable salt or ester thereof are added as active ingredients with effective dose, so that the foam composition can be used for treating local skin diseases. In some embodiments, the foam composition may contain from 0.005 to 2% of a retinoid and/or a pharmaceutically acceptable salt or ester thereof. In other embodiments, the foam composition may contain from 0.01 to 1.0% of a retinoid and/or a pharmaceutically acceptable salt or ester thereof. In other embodiments, the foam composition may contain from 0.05 to 0.5% of a retinoid and/or a pharmaceutically acceptable salt or ester thereof. The percentage ranges provided in the examples herein for the retinoid drug and/or the pharmaceutically acceptable salt or ester thereof, allow the foam compositions to be used to treat mild to severe skin disorders.
In an embodiment, the tretinoin-based drug comprises at least one of tretinoin, tretinoin derivatives, adapalene derivatives, tazarotene derivatives, trefarotene derivatives. The tretinoin medicines provided by the embodiment can inhibit the keratinization process, can regulate and control cell differentiation, also has an anti-inflammatory effect, and can be used for treating mild to severe skin diseases, such as acne.
In the examples, the foam composition contains 1-40% surfactant. The addition of the surfactant can increase the solubility of the vitamin A acid drugs or pharmaceutically acceptable salts or esters thereof which are difficult to dissolve or insoluble in an aqueous solvent in the aqueous solvent, so that the foam composition presents good transparent appearance, simultaneously the vitamin A acid drugs can exert the maximum drug effect, and can also play a foaming role. The percentage of surfactant may be, but is not limited to, 1%, 5%, 10%, 15%, 20%, 25%, 30%, 35%, 40%. Within the percentage of the surfactant provided in the examples herein, the gas volume fraction in the foam can be increased, which can improve the stability of the foam.
In an embodiment, the surfactant comprises: at least one of docusate sodium, caprylic capric polyglycol glyceride (polyoxylglycero-8 glycerides, Labrasol), polyglycerol oleate (Polyglyceryl-3oleate, Plurol Oleique CC497), polyoxyethylene stearate, polyoxyethylene oleate polyglycol glyceride (Oleoyl polyoxyl-6glycerides, Labrafil M1944CS), medium-chain fatty acid triglyceride, isopropyl myristate, oleic acid, diethylene glycol monoethyl ether, polyoxyethylene alkyl ether, poloxamer, polyoxyethylene sorbitan fatty acid ester, sorbitan ester, polyoxyethylene castor oil derivative, and propylene glycol monocaprylate. Wherein, the polyoxyethylene alkyl ether is Brij series; the sorbitan esters are span series; the polyoxyethylene castor oil derivative may be polyoxyethylene 40 hydrogenated castor oil. The surfactants provided by the embodiment of the application have good wetting, solubilizing, emulsifying, foaming and other effects, and one or more of the surfactants can be added to increase the solubility of the hardly soluble or insoluble tretinoin drugs and/or pharmaceutically acceptable salts or esters thereof, so as to fully exert the drug effect. On the other hand, the foam composition can be endowed with the function of generating foam, and the stability of the foam is good.
In the examples, the foam composition contains 30-80% of an aqueous solvent. Adding an aqueous solvent to provide water to make the foam composition substantially hydrated and dissolve the tretinoin medicine and/or pharmaceutically acceptable salt or ester thereof; in some embodiments, the foam composition may contain 40-70% aqueous solvent. In some embodiments, the foam composition may contain 50-60% of an aqueous solvent. In some embodiments, the foam composition may contain 54-56% aqueous solvent.
In embodiments, the aqueous solvent comprises: at least one of water, propylene glycol and glycerol. In particular embodiments, the aqueous solvent may be water; the aqueous solvent may also include water, propylene glycol; the aqueous solvent may also include water, glycerol.
In embodiments, the adjuvant in the foam composition further comprises 1-20% of a solubilizer. The solubilizer is added to fully dissolve the hardly soluble or insoluble tretinoin drug and/or pharmaceutically acceptable salt or ester thereof, so as to increase the dispersion uniformity of the drug in the foam composition. In particular embodiments, the percentage of solubilizer may be, but is not limited to, 1%, 3%, 6%, 9%, 12%, 15%, 18%, 20%. The solubility of the drug is highest within the percentage ranges of the solubilizing agent provided in the examples herein.
In an embodiment, the solubilizer comprises at least one of benzyl alcohol, phenoxyethanol, Hexylene glycol (Hexylene glycol), diethylene glycol monoethyl ether, dimethyl sulfoxide, and propylene carbonate. The solubilizing effect of the solubilizing agents provided in the embodiments of the present application is the best, which is beneficial to fully dissolving the retinoic acid drugs and/or pharmaceutically acceptable salts or esters thereof, and fully exerting the pharmacodynamic action of the retinoic acid drugs.
In embodiments, the adjunct of the foam composition further comprises 1-20% of a dispersing medium. The addition of the dispersion medium can fully and uniformly disperse the insoluble or insoluble tretinoin medicaments and/or pharmaceutically acceptable salts or esters thereof, and can further increase the dispersion uniformity of the tretinoin medicaments in the foam composition. In particular embodiments, the percentage of dispersion medium may be, but is not limited to, 1%, 3%, 6%, 9%, 12%, 15%, 18%, 20%. Within the percentage content range of the dispersion medium provided by the embodiment of the application, the drug effect of the tretinoin drug reaches the highest.
In an embodiment, the dispersion medium comprises at least one of polyethylene glycol, dimethyl isosorbide, butylene glycol, isopropyl myristate, N-methyl-2-pyrrolidone, dodecanol. The dispersion medium provided by the embodiment of the application has the best dispersion effect, is favorable for fully dispersing the tretinoin medicament and/or the pharmaceutically acceptable salt or ester thereof, and is favorable for improving the dispersion uniformity of the tretinoin medicament in the foam composition.
In an embodiment, the auxiliary materials in the foam composition further comprise: at least one of hydrophobic solvent, foam stabilizer, antioxidant and humectant. The hydrophobic solvent contained in the foam composition provided by the embodiment can form a milky matrix under the synergistic action of water and a surfactant, so that a milky foam composition can be formed; the foam stabilizer can increase the viscosity of the foam composition and can increase the stability of foam formed after the foam composition is dispensed; the antioxidant contained in the foam composition can effectively delay or prevent the foam composition from oxidative deterioration, and can further improve the stability of the foam composition; the moisturizer can provide skin moisturizing effect and hydration effect for skin, and is beneficial to skin rejuvenation and recovery of pathological symptoms to healthy skin.
In a specific embodiment, the auxiliary material in the foam composition may further include any one of a hydrophobic solvent, a foam stabilizer, an antioxidant, and a humectant. In other embodiments, the auxiliary materials in the foam composition may further include any two or more of a hydrophobic solvent, a foam stabilizer, an antioxidant, and a humectant.
In the examples, the hydrophobic vehicle comprises 1-40% by weight of the total foam composition. The hydrophobic solvent can form a milky matrix under the synergistic action of water and surfactant, and a milky foam composition can be obtained. In particular embodiments, the percentage of hydrophobic vehicle may be, but is not limited to, 1%, 5%, 10%, 15%, 20%, 25%, 30%, 35%, 40%. Within the percentage of hydrophobic vehicle provided in the examples herein, it is advantageous to form a creamy foam composition that provides optimal foam stability after dispensing.
In embodiments, the hydrophobic vehicle comprises: at least one of almond oil, sesame oil, isopropyl myristate, shea butter, mineral oil, olive oil, soybean oil, oleoyl oleate, isopropyl palmitate, lanolin, silicon dioxide dimethicone, and diisopropyl adipate. In a specific embodiment, the hydrophobic vehicle may comprise any one of almond oil, sesame oil, isopropyl myristate, shea butter, mineral oil, olive oil, soybean oil, oleoyl oleate, isopropyl palmitate, lanolin, simethicone, dimethicone, and diisopropyl adipate. In other embodiments, the hydrophobic vehicle may also comprise two or more of almond oil, sesame oil, isopropyl myristate, shea butter, mineral oil, olive oil, soybean oil, oleoyl oleate, isopropyl palmitate, lanolin, silica dimethicone, and diisopropyl adipate.
In an embodiment, the foam stabilizer comprises 1-40% by weight of the total foam composition. The addition of the foam stabilizer can reduce the drainage of liquid, delay emulsification and enable the foam composition to have the most appropriate viscosity. In particular embodiments, the percentage of foam stabilizer may be, but is not limited to, 1%, 5%, 10%, 15%, 20%, 25%, 30%, 35%, 40%. Within the percentage ranges of the foam stabilizer provided in the examples herein, the viscosity of the foam composition is optimized and the stability of the foam is optimized.
In an embodiment, the foam stabilizer comprises: at least one of acacia, methylcellulose, hydroxypropyl methylcellulose, ethylcellulose, hydroxypropyl cellulose, xanthan gum, polyacrylic acid polymer, and carbomer polymer. The foam stabilizer using the high molecular weight polymers provided in this example can increase the viscosity of the foam composition and the stability of the foam formed after dispensing. In a specific embodiment, the foam stabilizer may contain any one of acacia, methylcellulose, hydroxypropylmethylcellulose, ethylcellulose, hydroxypropylcellulose, xanthan gum, polyacrylic acid polymer, and carbomer polymer. In other embodiments, the foam stabilizer may contain any two or more of acacia, methylcellulose, hydroxypropylmethylcellulose, ethylcellulose, hydroxypropylcellulose, xanthan gum, polyacrylic acid polymer, and carbomer polymer.
In embodiments, the antioxidant comprises 0.01 to 0.5% by weight of the total foam composition. The antioxidant is added, so that the oxidative deterioration of the foam composition can be effectively delayed or prevented, the stability of the foam composition is improved, and the storage time is prolonged. In particular embodiments, the percentage of antioxidant may be, but is not limited to, 0.01%, 0.1%, 0.2%, 0.3%, 0.4%, 0.5%.
In an embodiment, the antioxidant comprises at least one of dibutylhydroxytoluene, butylhydroxyanisole, ascorbyl palmitate, ascorbic acid, DL-alpha-tocopherol. The antioxidants provided by the embodiment are widely used antioxidants, can be used independently or in combination, and can endow the foam composition with excellent oxidation resistance and stability.
In embodiments, the humectant comprises 1 to 40% by weight of the total foam composition. The humectant can provide skin moistening effect and hydration effect to skin, and is beneficial to skin rejuvenation and recovery of pathological symptoms to healthy skin. In particular embodiments, the humectant may be present in a percentage amount of, but not limited to, 1%, 5%, 10%, 15%, 20%, 25%, 30%, 35%, 40%. The emollient effect of the foam composition is optimized within the ranges of the humectant percentages provided in the examples herein.
In an embodiment, the humectant comprises at least one of propylene glycol, glycerin, sodium hyaluronate, urea, sodium lactate, sorbitol, butylene glycol, panthenol, sodium pyrrolidone carboxylate, trehalose. In particular embodiments, the moisturizer may contain any one or more of propylene glycol, glycerin, sodium hyaluronate, urea, sodium lactate, sorbitol, butylene glycol, panthenol, sodium pyrrolidone carboxylate, trehalose.
In an embodiment, the foam composition further comprises: at least one of a penetration enhancer, a wetting agent, a colorant, a chelating agent, and a preservative. The penetration enhancer contained in the foam composition provided by the embodiment interacts with stratum corneum lipid to change the arrangement structure of the stratum corneum lipid, enhance the permeability and improve the solubility of the drug; the moisturizer can moisten skin and keep moisture of skin; the coloring agent can color the foam composition, modify and beautify the appearance of the foam composition and adjust the influence of certain ingredients on the color of the foam composition; the chelating agent and the preservative contained in the foam composition can improve the stability of the foam composition under the synergistic action, and are beneficial to prolonging the shelf life and preventing bacterial contamination. The foam composition can be added with any one or more of a penetration enhancer, a wetting agent, a coloring agent, a chelating agent and a preservative, so as to further improve the efficacy of the foam composition, and the specific addition amount is within the concentration range approved by FDA IIG or the use concentration range of common auxiliary materials.
In embodiments, the foam composition produces bubbles of 0.1 to 3mm in size when dispensed and the foam composition produces a foam with a gas volume fraction of 50 to 90% when dispensed. Foam stability is best provided in the size range and gas volume fraction range of the bubbles provided in this example.
In an embodiment, the foam composition may be dispensed using a conventional actuator that converts a liquid into a foam and then applies the foam to the skin surface. Expensive production equipment and special distributors are not needed, and the cost is low.
In a second aspect, embodiments of the present application provide a method of preparing a foam composition, comprising the steps of:
s10: providing auxiliary materials, tretinoin medicaments and/or pharmaceutically acceptable salts or esters thereof;
s20: mixing the auxiliary materials with the tretinoin medicine and/or pharmaceutically acceptable salt or ester thereof to obtain the foam composition.
According to the preparation method of the foam composition provided by the embodiment of the application, the auxiliary material and the tretinoin medicine and/or the pharmaceutically acceptable salt or ester thereof are mixed to obtain the foam composition. Therefore, the preparation method is simple to operate, low in cost and suitable for large-scale production and application.
In step S10, the auxiliary material includes a surfactant and an aqueous solvent. The tretinoin drug and/or pharmaceutically acceptable salt or ester thereof can be represented as: only the tretinoin drug exists, only the pharmaceutically acceptable salt or ester of the tretinoin drug exists, and the tretinoin drug and the pharmaceutically acceptable salt or ester thereof exist at the same time.
In step S20, the method of mixing the auxiliary materials and the retinoic acid drugs and/or their pharmaceutically acceptable salts or esters may be performed by conventional manufacturing processes, such as mixing under stirring or homogenization, and will not be described herein again for brevity.
In an embodiment, the formulation of the foam composition may include any one of water-based foam, hydroalcoholic foam, emulsion foam, and oily foam.
In the secured position, the liquid dosing chamber (a) is filled with liquid, as shown in fig. 2 and 3. Closing the ball valve (b) of the chamber and releasing the steel spring (c). When pressed, the air in the medicine chamber is compressed by the piston (d). At the same time, the aperture of the piston in the air dosing chamber is closed by means of a diaphragm valve (e). The steel spring is compressed and the ball valve of the liquid metering chamber is closed. The formulation in the formulation dosing chamber and the air in the air dosing chamber are transferred through the suction tube (f) and compressed by a foam generator with a double screen (g). In the discharge position, the compression steel spring moves the piston of the air dosing chamber in a fixed position. The diaphragm valve of the air dosing chamber was opened and the dosing chamber was filled with air. The ball valve of the liquid dosing chamber is opened and the empty dosing chamber can be filled with the formulation.
As shown in fig. 4, the main components of the dispenser are a reservoir, an air and liquid dosing chamber, a piston with holes and a diaphragm valve, a foam generator with a double screen and a foam generating head.
The foam pump uses specialized plumbing to facilitate the smooth extraction of liquid from the bottle as foam. The foam pump has two specific chambers, one for the liquid (drawn out of the pump container by a suction tube) and the other for the liquid. The liquid and air were driven through the same small nozzle and stainless steel mesh. Thus, in the absence of propellant in the container sealing system, foam is formed in the foaming pump.
The following description will be given with reference to specific examples.
Example 1
The embodiment of the application provides a foam composition and a preparation method thereof.
The foam composition comprises the following components in percentage by weight based on the total weight of the foam composition as 100 percent:
a method of preparing a foam composition comprising the steps of:
s10: adding docusate sodium into a mixed solution of propylene glycol and glycerol, and uniformly stirring to obtain a mixed solution;
s20: adding adapalene into the mixed solution obtained in the step S10, and uniformly dispersing to obtain an adapalene dispersion solution;
s30: firstly, adding polyoxyethylene sorbitan fatty acid ester into water for dissolving, and then adding into a mixed solution of polyglycerol oleate, caprylic/capric polyethylene glycol glyceride and sorbitan ester for homogenizing for 30min to obtain a mixture;
s40: and adding the adapalene dispersion liquid into the mixture obtained in the step S30, homogenizing for 30min, and then continuously stirring the stock solution for 30min to obtain the foam composition.
Example 2
The embodiment of the application provides a foam composition and a preparation method thereof.
The foam composition comprises the following components in percentage by weight based on the total weight of the foam composition as 100 percent:
a method of preparing a foam composition comprising the steps of:
s10: adding docusate sodium into a mixed solution of propylene glycol and glycerol, and uniformly stirring to obtain a mixed solution;
s20: adding tazarotene into the mixed solution obtained in the step S10, and uniformly dispersing to obtain a tazarotene dispersion solution;
s30: firstly, adding polyoxyethylene sorbitan fatty acid ester into water for dissolving, and then adding into a mixed solution of polyglycerol oleate, caprylic/capric polyethylene glycol glyceride and sorbitan ester for homogenizing for 30min to obtain a mixture;
s40: and (4) adding the tazarotene dispersion liquid into the mixture obtained in the step S30, homogenizing for 30min, and then continuously stirring the stock solution for 30min to obtain the foam composition.
Example 3
The embodiment of the application provides a foam composition and a preparation method thereof.
The foam composition comprises the following components in percentage by weight based on the total weight of the foam composition as 100 percent:
a method of preparing a foam composition comprising the steps of:
s10: adding docusate sodium into a mixed solution of propylene glycol and glycerol, and uniformly stirring to obtain a mixed solution;
s20: adding the trefariptin into the mixed solution obtained in the step S10, and uniformly dispersing to obtain a trefariptin dispersion solution;
s30: firstly, adding polyoxyethylene sorbitan fatty acid ester into water for dissolving, and then adding into a mixed solution of polyglycerol oleate, caprylic/capric polyethylene glycol glyceride and sorbitan ester for homogenizing for 30min to obtain a mixture;
s40: and adding the trofavudine dispersion liquid into the mixture obtained in the step S30, homogenizing for 30min, and then continuously stirring the stock solution for 30min to obtain the foam composition.
Example 4
The embodiment of the application provides a foam composition and a preparation method thereof.
The foam composition comprises the following components in percentage by weight based on the total weight of the foam composition as 100 percent:
a method of preparing a foam composition comprising the steps of:
s10: adding adapalene into oleic acid for dissolving to obtain a first adapalene solution;
s20: uniformly mixing diethylene glycol monoethyl ether, sorbitan esters and isopropyl myristate, adding the mixture into the first adapalene solution, and uniformly stirring to obtain a second adapalene solution;
s30: and adding the polyoxyethylene sorbitan fatty acid ester into water for dissolving, and then adding the polyoxyethylene sorbitan fatty acid ester into the second adapalene solution for uniformly stirring to obtain the foam composition.
Example 5
The embodiment of the application provides a foam composition and a preparation method thereof.
The foam composition comprises the following components in percentage by weight based on the total weight of the foam composition as 100 percent:
a method of preparing a foam composition comprising the steps of:
s10: adding tazarotene into medium-chain fatty acid triglyceride, stirring and dissolving to obtain a tazarotene solution;
s20: firstly, uniformly stirring diethylene glycol monoethyl ether, polyoxyethylene 40 hydrogenated castor oil, caprylic capric acid polyethylene glycol glyceride and propylene glycol, and then uniformly mixing with a tazarotene solution to obtain a tazarotene microemulsion;
s30: adding water into the tazarotene microemulsion, and uniformly stirring to obtain the foam composition.
Example 6
The embodiment of the application provides a foam composition and a preparation method thereof.
The foam composition comprises the following components in percentage by weight based on the total weight of the foam composition as 100 percent:
a method of preparing a foam composition comprising the steps of:
s10: adding tazarotene into propylene glycol monocaprylate, stirring and dissolving to obtain a first tazarotene solution;
s20: firstly, uniformly stirring polyoxyethylene sorbitan fatty acid ester, medium-chain fatty acid triglyceride, sorbitan ester, caprylic/capric polyethylene glycol glyceride and diethylene glycol monoethyl ether, and then adding the mixture into a first tazarotene solution to be uniformly stirred to obtain a second tazarotene solution;
s30: adding water into the second tazarotene solution and stirring uniformly to obtain the foam composition.
Example 7
The embodiment of the application provides a foam composition and a preparation method thereof.
The foam composition comprises the following components in percentage by weight based on the total weight of the foam composition as 100 percent:
a method of preparing a foam composition comprising the steps of:
s10: adding trefavudine into benzyl alcohol, stirring and dissolving to obtain a first trefavudine solution;
s20: firstly, uniformly stirring polyoxyethylene stearate, polyethylene glycol oleate, propylene glycol and diethylene glycol monoethyl ether, then adding the mixture into a first trefarine solution, and uniformly stirring to obtain a second trefarine solution;
s30: and adding water into the second trefariptin solution, and uniformly stirring to obtain the foam composition.
Example 8
The embodiment of the application provides a foam composition and a preparation method thereof.
The foam composition comprises the following components in percentage by weight based on the total weight of the foam composition as 100 percent:
a method of preparing a foam composition comprising the steps of:
s10: adding trefavudine into benzyl alcohol, stirring and dissolving to obtain a first trefavudine solution;
s20: uniformly stirring caprylic/capric polyethylene glycol glyceride, polyglycerol oleate and medium-chain fatty acid triglyceride, then adding the mixture into the first trebrogliptin solution, and uniformly stirring to obtain a second trebrogliptin solution;
s30: and adding water into the second trefariptin solution, and uniformly stirring to obtain the foam composition.
Example 9
The embodiment of the application provides a foam composition and a preparation method thereof.
The foam composition comprises the following components in percentage by weight based on the total weight of the foam composition as 100 percent:
the difference between the preparation method of the foam composition and the embodiment 8 is that in step S30 of this embodiment, xanthan gum is first added into water to be hydrated for 1 hour, and then added into the second trefariptin solution to be uniformly stirred, so as to obtain the foam composition.
Example 10
The embodiment of the application provides a foam composition and a preparation method thereof.
The foam composition comprises the following components in percentage by weight based on the total weight of the foam composition as 100 percent:
the difference between the preparation method of the foam composition and the embodiment 8 is that in step S30 of this embodiment, hydroxypropyl methylcellulose is added into water to be hydrated for 1 hour, and then added into the second trefariptin solution to be uniformly stirred, so as to obtain the foam composition.
Example 11
The embodiment of the application provides a foam composition and a preparation method thereof.
The foam composition comprises the following components in percentage by weight based on the total weight of the foam composition as 100 percent:
a method of preparing a foam composition comprising the steps of:
s10: adding adapalene into oleic acid for dissolving to obtain a first adapalene solution;
s20: uniformly stirring caprylic/capric polyethylene glycol glyceride, polyglycerol oleate and medium-chain fatty acid triglyceride, then adding the mixture into the first adapalene solution, and uniformly stirring to obtain a second adapalene solution;
s30: adding xanthan gum into water for hydration for 1 hour, then adding the xanthan gum into the second adapalene solution, and uniformly stirring to obtain the foam composition.
Example 12
The embodiment of the application provides a foam composition and a preparation method thereof.
The foam composition comprises the following components in percentage by weight based on the total weight of the foam composition as 100 percent:
a method of preparing a foam composition comprising the steps of:
s10: dissolving Tazaro river into medium-chain fatty acid triglyceride to obtain a first Tazaro river solution;
s20: uniformly stirring caprylic/capric polyethylene glycol glyceride, polyglycerol oleate and benzyl alcohol, and then adding the mixture into the first Tizarojiang solution to be uniformly stirred to obtain a second Tizarojiang solution;
s30: adding xanthan gum into water for hydration for 1 hour, and then adding the xanthan gum into a second Tazaro river solution to be uniformly stirred to obtain the foam composition.
And (3) relevant performance test analysis:
foam appearance: the foam compositions provided in examples 1-12 were visually inspected for the appearance of foam formed.
Apparent viscosity: the apparent viscosity of the foam composition before foam formation was determined using a Brookfield viscometer LV-3C, at 5rpm for 1 min.
The foam quality is as follows: the foam quality was analyzed visually, taking into account the parameters: milky or non-milky foam, bubble size, thick, thin, dark, watery, non-watery. Wherein the rating scale is specified as follows:
dry foam, large bubbles, difficult to spread on the skin upon application as very poor (-);
no milky foam, large bubbles, became thin as a water sample when smeared, which was poor (-);
less milky foam, large bubbles, becoming thin as water when smeared is general (+);
medium creamy foam, medium bubble size, dullness and thinning to reasonably good (++);
rich milky foam, large bubbles, slower rate of darkening upon use and maintaining good milky (+++);
very rich milky foam, small bubbles, did not turn dull when applied and retained rich milky was excellent (+++).
Foaming power: foaming force measured using a glass graduated cylinder with a stopper was 250mL in volume. Measuring 5mL of the foam composition into a glass measuring cylinder with a plug, adding 25mL of purified water, mixing the solution under the condition of not forming foam, and dissolving the foam composition into the purified water; the solution volume was further adjusted to 50mL with purified water and the whole solution was heated to 30 ℃. Shake 12 times upside down in a stoppered glass cylinder. After completion, the stoppered glass cylinder was allowed to stand for 5 minutes and the volume of foam and solution was measured. Foaming force was calculated from the difference between the final volume of the foam after shaking and the initial volume (50 mL).
Foam stability: the glass cylinder with the plug containing the foam was left to stand for 30 minutes and the volume was recorded. The difference between the final volume after 30 minutes and the initial 50mL volume is the foam stability value.
Specific gravity: and calculating the ratio of the density of the foam to the density of pure water at room temperature, and calculating the specific gravity of the foam. The foam was pumped into a pycnometer and the density was calculated and simultaneously compared to the density of water.
TABLE 1
| Examples | Foam appearance | Apparent viscosity | Quality of foam | Foaming power | Foam stability | Specific gravity of foam |
| Example 1 | Milk foam rich in white | 5610 | ++++ | 160 | 75 | 0.086 |
| Example 2 | White rich milk foam | 5480 | ++++ | 155 | 81 | 0.095 |
| Example 3 | White rich creamy foam | 5240 | ++++ | 158 | 78 | 0.091 |
| Example 4 | White milky foam | 5890 | ++++ | 135 | 60 | 0.150 |
| Example 5 | White milky foam | 5980 | +++ | 141 | 63 | 0.136 |
| Example 6 | White rich creamy foam | 5260 | ++++ | 153 | 76 | 0.101 |
| Example 7 | White rich creamy foam | 5110 | ++++ | 148 | 73 | 0.141 |
| Example 8 | White milky foam | 5790 | +++ | 144 | 65 | 0.138 |
| Example 9 | White rich creamy foam | 5340 | ++++ | 152 | 83 | 0.098 |
| Example 10 | White milky foam | 5920 | +++ | 146 | 67 | 0.137 |
| Example 11 | White rich creamy foam | 5460 | ++++ | 154 | 76 | 0.090 |
| Example 12 | White rich creamy foam | 5340 | ++++ | 153 | 81 | 0.101 |
Table 1 shows the performance test results of the foam compositions provided in examples 1-12 of the present application, and it can be seen from Table 1 that the foam compositions provided in examples 1-12 have apparent viscosities of 5110-5920, foaming forces of 135-160, foam stabilities of 60-83, and foam specific gravities of 0.086-0.150, which indicates that the foam compositions provided in the present application have suitable viscosities, good foaming forces, and good stability of the formed foams. In addition, the foam compositions provided in examples 1-3, 6, 7, 9, 11, and 12 formed milky white foam with excellent foam quality, in addition to the white milky foam formed by the foam compositions provided in examples 4, 5, 8, and 10, which showed good foam quality and that the foam compositions provided herein could be dispensed and formed into milky white foam with only a common actuator without the use of a propellant or gas.
The above description is only exemplary of the present application and should not be taken as limiting the present application, as any modification, equivalent replacement, or improvement made within the spirit and principle of the present application should be included in the protection scope of the present application.
Claims (10)
1. A foam composition comprises an effective dose of active ingredients and auxiliary materials, and is characterized in that the active ingredients comprise tretinoin drugs and/or pharmaceutically acceptable salts or esters thereof, and the auxiliary materials comprise surfactants and aqueous solvents.
2. The foam composition according to claim 1, comprising the following components in weight percent, based on the total weight of the foam composition taken as 100 percent:
vitamin A acid medicine 0.001-5%
1 to 40 percent of surfactant
30-80% of aqueous solvent.
3. The foam composition according to claim 1, comprising the following components in weight percent, based on the total weight of the foam composition taken as 100 percent:
vitamin A acid medicine 0.005-2%
1 to 40 percent of surfactant
40-70% of aqueous solvent.
4. The foam composition of any one of claims 1 to 3, wherein the tretinoin-based drug comprises at least one of tretinoin, tretinoin derivatives, adapalene derivatives, tazarotene derivatives, trefarotene derivatives; and/or
The surfactant includes: at least one of docusate sodium, caprylic/capric macrogol glyceride, polyglycerol oleate, polyoxyethylene stearate, oleic macrogol glyceride, medium-chain fatty triglyceride, isopropyl myristate, oleic acid, diethylene glycol monoethyl ether, polyoxyethylene alkyl ether, poloxamer, polyoxyethylene sorbitan fatty acid ester, sorbitan ester, polyoxyethylene castor oil derivative, and propylene glycol monocaprylate; and/or
The aqueous solvent includes: at least one of water, propylene glycol and glycerol.
5. The foam composition of claim 4, wherein the auxiliary material further comprises: 1-20% of a solubilizer; wherein the solubilizer comprises at least one of benzyl alcohol, phenoxyethanol, hexanediol, diethylene glycol monoethyl ether, dimethyl sulfoxide and propylene carbonate; or
The auxiliary materials also comprise: 1-20% of a dispersing medium; wherein the dispersion medium comprises at least one of polyethylene glycol, dimethyl isosorbide, butanediol, isopropyl myristate, N-methyl-2-pyrrolidone and dodecanol.
6. The foam composition of claim 5, wherein the auxiliary material further comprises: at least one of hydrophobic solvent, foam stabilizer, antioxidant and humectant.
7. The foam composition of claim 6, wherein said hydrophobic vehicle comprises 1-40% of the total weight of said foam composition; and/or
The foam stabilizer accounts for 1-40% of the total weight of the foam composition; and/or
The antioxidant accounts for 0.01 to 0.5 percent of the total weight of the foam composition; and/or
The humectant accounts for 1-40% of the total weight of the foam composition.
8. The foam composition of claim 6, wherein the hydrophobic vehicle comprises: at least one of almond oil, sesame oil, isopropyl myristate, shea butter, mineral oil, olive oil, soybean oil, oleoyl oleate, isopropyl palmitate, lanolin, silicon dioxide dimethicone, and diisopropyl adipate; and/or
The foam stabilizer comprises: at least one of acacia, methylcellulose, hydroxypropyl methylcellulose, ethylcellulose, hydroxypropyl cellulose, xanthan gum, polyacrylic acid polymer, and carbomer polymer; and/or
The antioxidant comprises at least one of dibutyl hydroxy toluene, butyl hydroxy anisol, ascorbyl palmitate, ascorbic acid and DL-alpha-tocopherol; and/or
The humectant comprises at least one of propylene glycol, glycerin, sodium hyaluronate, urea, sodium lactate, sorbitol, butylene glycol, panthenol, sodium pyrrolidone carboxylate, and trehalose.
9. The foam composition according to any one of claims 5 to 8, wherein the foam composition further comprises: at least one of a penetration enhancer, a wetting agent, a colorant, a chelating agent, and a preservative; and/or
The foam composition generates bubbles when dispensed in a size of 0.1 to 3 mm; and/or
The foam composition has a gas volume fraction of 50-90% that produces foam when dispensed.
10. A process for the preparation of a foam composition according to any one of claims 1 to 9, comprising the steps of:
providing the auxiliary material, the tretinoin medicine and/or pharmaceutically acceptable salt or ester thereof;
and mixing the auxiliary material and the tretinoin medicine and/or pharmaceutically acceptable salt or ester thereof to obtain the foam composition.
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010116078A1 (en) * | 2009-04-06 | 2010-10-14 | Pierre Fabre Dermo-Cosmetique | Foaming pharmaceutical composition that does not contain a propellant gas |
| CN105392473A (en) * | 2013-07-11 | 2016-03-09 | 宝丽制药股份有限公司 | External-use composition producing foamed state upon use |
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010116078A1 (en) * | 2009-04-06 | 2010-10-14 | Pierre Fabre Dermo-Cosmetique | Foaming pharmaceutical composition that does not contain a propellant gas |
| CN105392473A (en) * | 2013-07-11 | 2016-03-09 | 宝丽制药股份有限公司 | External-use composition producing foamed state upon use |
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