JPS6317112B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention relates to a powder aerosol composition particularly suitable for pharmaceuticals, quasi-drugs, cosmetics, and the like. A powder aerosol composition is created by suspending and dispersing a solid powder that is insoluble in the liquefied propellant in the liquefied propellant using a surfactant or a suspending agent, and this is filled into a pressure-resistant container. It is known that the liquid is sprayed from an injection hole nozzle of the container. However, aerosol products filled with such powdered aerosol compositions have various problems.
For example, in the powder aerosol composition, it is generally difficult to sufficiently suspend and disperse solid powder such as a drug intended for spray application in the liquefied propellant, and even if it is possible, the suspension The stability of the condition is low, causing suspended particles to settle, float, or aggregate, which can clog the valve or actuator of the injection hole nozzle or prevent uniform spraying, or cause the drug to It also has a significant impact on the efficacy of drugs, making it impossible to obtain the desired medicinal effects. This tendency becomes even more pronounced when the amount of solid powder to be suspended is large. Specifically, the powder aerosol composition consists of powder particles of solid substances such as hydrocortisone, talc, aluminum compounds, various chain compounds, etc., alone or together with other esters, suspended and dispersed in a liquefied propellant. As the liquefied propellant, halogenated hydrocarbon gas, liquefied petroleum gas, dimethyl ether, a mixed gas thereof, or a liquefied gas obtained by adding other additive gases to these gases is used. However, the solid powder particles begin to separate or agglomerate immediately after the suspension operation, except in special cases. Therefore, in powder aerosol compositions, it is necessary to sufficiently suspend and disperse the solid particles using an appropriate suspending agent and to maintain this state stably. It is necessary to prevent particles from settling, flotation, agglomeration, etc., and to prevent adhesion to the walls of an aerosol container, formation of precipitates, and adhesion of precipitates. Conventionally, the following methods are known for obtaining a powder aerosol composition by suspending solid particles that are insoluble or poorly soluble in the liquefied propellant. (1) HLB (hydrophilicity - lipophilicity value) is approximately 10
A method of suspending solid particles in a liquefied propellant using a liquid non-ionic surfactant that is insoluble in the liquefied propellant as described below (Japanese Patent Publication No. 36
-Refer to Publication No. 14397). (2) A method in which solid particles insoluble in the liquefied propellant are dispersed in the liquefied propellant using lecithin, lanolin, cholesterol, or a derivative thereof dissolved in an ester of lower alcohol and higher fatty acid ( (See Special Publication No. 40-28956). (3) Using natural phospholipids and phosphoric acid esters that are soluble in liquefied propellants and higher alcohols with linear or side chains having 11 to 20 carbon atoms and liquid at room temperature, solid materials can be produced. A method of suspending particles in the propellant (see Japanese Patent Publication No. 14804/1983). (4) A method in which insoluble solid particles are suspended in a liquefied propellant using a liquid acetylated product of a partial ester with a long-chain fatty acid of a polyhydric alcohol (see Japanese Patent Publication No. 41-409) ). However, none of these methods can be said to have a satisfactory effect. That is, a sufficiently stable state of suspension and dispersion cannot always be obtained, or the types of suspending agents that can actually be used and the types of solid particles that can be suspended and dispersed are limited. Therefore, it is often difficult to apply conventional methods to aerosols for the human body, where the use of substances that are highly irritating to human skin should be avoided. For example, when solid particles are suspended and dispersed with an ester, isopropyl myristate has been mainly used as the ester, but this is highly irritating to the skin and cannot be used in large amounts in aerosols for human bodies. Can not. The present invention does not have the above-mentioned drawbacks, can always obtain a sufficient and stable suspension and dispersion state, can be suspended and dispersed in a wide range of types of solid particles, and can be applied to the human body. The purpose of the present invention is to provide a powder aerosol composition suitable for use as a powder aerosol composition. The present invention was completed based on the discovery, as a result of various studies, that jojoba oil has an excellent effect as a suspending agent and is not irritating to the skin. In the present invention, a powder aerosol composition is obtained by using a specific proportion of jojoba oil as a suspending agent and suspending and dispersing fine powder of a solid substance insoluble in the liquefied propellant. In addition, in the present invention, squalane, squalene, liquid paraffin, higher fatty acid ester, and other suspending aids or wetting agents can be used alone or in combination with jojoba oil as a suspending agent. . In the present invention, the proportion of jojoba oil used is within the range of 0.1 to 10% by weight based on the liquefied propellant,
Particularly preferably, it is within the range of 0.1 to 5% by weight. In the present invention, the solid particles to be suspended and dispersed are optional, but include powder particles insoluble in the liquefied propellant,
Examples of particularly powdered drugs include prednisolone, hydrocortisone, derivatives thereof, tetrahydrozoline hydrochloride, dexamethasone, fradiomycin sulfate, aluminum fine powder, kaolin, talc, aluminum chlorohydroxide fine powder, titanium oxide, magnesium carbonate, magnesium silicate. , fish scale foil, titanium mica, mica, starch, synthetic polymer powders (nylon, polyethylene, etc.), magnesium, calcium and aluminum stearate, iron oxides such as red iron oxide, bentonite, etc., and particles of these is usually used in a particle size of 100 microns or less, preferably 5 to 30 microns. Furthermore, as the liquefied propellant, those commonly used for this purpose, ie, dichlorodifluoromethane, dichlorotetrafluoroethane, trichloromonofluoromethane, liquefied petroleum gas, dimethyl ether, etc. can be used. The powder aerosol composition of the present invention is as described above and free from the drawbacks of conventional products. That is, in the present invention, a powder aerosol composition is obtained using jojoba oil, which has not been previously known as a suspending agent for suspending solid particles in a liquefied propellant. Therefore, this jojoba oil has excellent suspending action as a suspending agent for suspending solid particles in the liquefied propellant used in aerosol products, and is therefore insoluble in the liquefied propellant. It is extremely easy to sufficiently uniformly suspend and disperse the solid particles in the liquefied propellant, and this sufficiently suspended and dispersed state remains stable for a long time and over a wide temperature range. maintained. Due to this excellent suspending action, there are few restrictions on the type of solid particles to be suspended and dispersed, and almost any substance can be reliably suspended and dispersed in any liquefied propellant. When carrying out the present invention, in many cases solid powders, which are chemicals to be suspended and dispersed, and jojoba oil, as well as auxiliaries and additives added as necessary, are placed under pressure together with the liquefied propellant in a pressure-resistant container. All you have to do is fill it in the container and mix well by shaking, and no other special consideration is required. The powder aerosol composition thus obtained is extremely stable, and hardly any sedimentation, floating or aggregation of suspended solid particles occurs even when left for a long time.
In rare cases, sedimentation may occur depending on the type of solid particles and dispensing conditions, but the dispersibility is extremely good and does not form a hard cake like conventional products, and can be shaken very lightly. A uniform suspension state can be easily restored by dynamic operation, for example, by inverting the container one to three times. The powder aerosol composition of the present invention is also suitable as an aerosol for human bodies. In other words, jojoba oil used as a suspending agent is mild to the skin, has no phototoxicity or dangerous toxicity, does not irritate the eye mucous membranes, and is not only harmless or non-toxic to the human body. , has the effect of suppressing allergic reactions, and allows the use of irritating substances such as isopropyl myristate in small amounts. In addition, it is more compatible with the skin than lanolin, cholesterol, etc., and is odorless and does not cause discomfort, and if used appropriately, may emit a pleasant fragrance. Furthermore, jojoba oil as a suspending agent as described above,
It is possible to obtain a product with the desired medicinal effect without any adverse effect on the efficacy of solid or liquid drugs that are mixed together. Moreover, there is no corrosive property to the aerosol container, and together with the ability to stably obtain a suspension and dispersion state as described above, extremely excellent quality as an aerosol product can be obtained. It can be suitably applied to powdered aerosol compositions used as external products, cosmetics, and others. The component compositions of powder aerosol compositions according to Examples and Comparative Examples of the present invention are shown in Tables 1 and 2, respectively.
Shown in the table. Since the manufacturing operation uses a conventional method, the explanation will be omitted. In addition, regarding the substance name in the table, "ACHO"
is aluminum chlorohydroxide,
"LPG" stands for liquefied petroleum gas, and "DME" stands for dimethyl ether. Regarding the stability of the contents, "〇" means good, "×" means poor, and regarding dispersibility, "◎" means It is uniform, "〇" means that there is some aggregation, and "×" means that there is significant aggregation.
Represents the number of clogs out of 50.

【table】

【table】

【table】

【table】

【table】

【table】

【table】

Claims (1)

[Claims] 1 Solid particles insoluble in the liquefied propellant are suspended and dispersed in the liquefied propellant using jojoba oil as a suspending agent, and the ratio of the jojoba oil to the liquefied propellant is 0.1 to 10% by weight. %.