JPS60163811A - External application pharmaceutical containing propranolol - Google Patents

Abstract

PURPOSE:The titled application pharmaceutical, obtained by incorporating propranolol (beta-blocking agent) in a plaster consisting essentially of a water-soluble high polymer, water and a specific oily component, supporting the resultant mixture on a support, e.g. a flannel, and capable of improving the disadvantage of the well-known pharmaceuticals for administration in a constant dose. CONSTITUTION:An external application pharmaceutical, containing propranolol, constituted of a plaster consisting essentially of the propranolol useful for preventing and treating angina pectoris or arrhythmia, a water-soluble high polymer, e.g. sodium polyacrylate, water and an oily component, e.g. isopropyl myristate, having percutaneous absorptivity for the above-mentioned drug and a support consisting of a flannel, nonwoven fabric or plastic sheet, capable of administration in a constant dose without fear of staining clothing, etc., and having individual tackiness of the plaster to the skin and no disadvantage of causing side effects, e.g. rash, in the affected application site due to no required sealed administration.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention provides a topical patch containing propranolol, and more specifically, a paste containing propranolol, a water-soluble polymer compound, water, and an oily component that has the effect of promoting transdermal absorption of drugs; A propranolol-containing external patch comprising a support made of flannelette, nonwoven fabric, or plastic sheet and holding the above-mentioned paste.

Propranolol is a drug that has a β-blocking action and is used for the prevention and treatment of angina pectoris, arrhythmia, etc. Conventionally, propranomil has been administered orally or by injection, but it has had side effects such as hypersensitivity, hypotension, analgesia, and nausea, so it has been necessary to use it with caution. In recent years, in order to improve these disadvantages associated with oral or injection administration, ointments containing propranolol, or patches containing inibrobranolol in a polymer matrix as a type of so-called drug delivery system have been developed. Attempts are being made to develop transdermal absorption preparations. However, with ointments, it is difficult to quantify the dose, and they also have drawbacks such as staining clothes.In addition, in patch patches, the matrix itself does not have the strength to stick to the skin, and non-breathable adhesive tape (2) Since the matrix is administered in a sealed manner to the skin, it has the drawback of causing side effects such as skin irritation in the area where it is applied.

The inventors of the present invention have conducted intensive research to solve the above-mentioned drawbacks of conventional formulations such as ointments and patches, and have found that a water-soluble polymer compound, water, and an oily component that has the effect of promoting transdermal absorption of drugs. Propranolol can be administered in a fixed amount by containing propranolol in a plaster that is required for one person and holding it on a support made of flannelette, nonwoven, cloth, or plastic sheet. The present invention has been completed based on the discovery that it is possible to obtain an external patch that does not cause staining, has adhesive properties to the skin, and does not require sealed administration.

Water-soluble polymer compounds such as sodium polyacrylate, carboxyvinyl polymer, carboxymethylcellulose, polyvinyl alcohol, polyvinylpyrrolidone,
Sodium alginate, gelatin, etc. interact with water to form a pasty or gel-like substance. Due to its nature, this product has adhesive properties to the skin and contains moisture, so plasters based on this product can be applied directly to the skin without using an adhesive sheet or the like. In addition, it hydrates the skin and facilitates transdermal absorption of Z1 propranolol contained in the paste. Therefore, the water-soluble polymer compound used in the present invention can be any compound that becomes paste-like or gel-like when it interacts with water.

In the present invention, the above-mentioned paste further contains an oily component. This promotes transdermal absorption of the drug contained in the paste, that is, propranolol, and preferably one that dissolves propranolol is suitable. Oil-based ingredients that have this effect include plant and animal side products, hydrocarbons such as liquid paraffin and squalane, alcohols such as isostearyl alcohol and 2-octyldodecanol, isopropyl myristate, and olein. Octyldodenyl acid, octyldodecyl myristate,
Esters such as isostearyl isostearate, glycerin fatty acid ester, medium chain fatty acid triglyceride, etc. can be used in the present invention.

The above-mentioned base 1: The paste obtained by adding propranolol can be used by itself as the paste (3) of the patch targeted by the present invention, but if necessary, Th
[In addition to the four ingredients, for example, excipients such as kaolin and bentonite are used to improve the shape retention of the paste; propylene glycol and glycerin are used to increase the moisturizing properties of the paste;
Humectants such as 3-butylene glycol and polyethylene glycol, and other additives such as emulsifiers, surfactants, and oxidative rainproofing agents may be incorporated into the paste. The type and amount of these additives to be blended can be arbitrarily selected depending on the application site of the patch, the symptoms, etc.

The active ingredient, propranolol, is mixed into the paste so that it is dispersed as evenly (partially) as possible.

In that case, the concentration of propranolol in the paste can be selected within a wide range. Propranolol, which is mixed into the bone body, moves through the moisture of the plaster and is constantly supplied to the plaster surface.

As a result, when this serum is applied to the skin, propranolol is constantly administered from the surface of the application, along with the effects of the oily components and water that have the effect of promoting transdermal absorption. It will be absorbed transdermally and provide the desired therapeutic effect to the patient.

The plaster is held on a support made of flannel, nonwoven fabric, or plastic sheet. This support keeps the propranolol-containing paste in a certain shape and prevents staining of clothes during administration, and is preferably in the form of a breathable sheet, but polyethylene film, It may also be a non-breathable film such as a polypropylene film or a polyurethane film.

Further, the method of holding the paste on the support is not particularly limited, and for example, the paste may be held on the support (spreading, coating, etc.).

The patch of the present invention is administered by applying it to the body, especially the chest, and since the paste containing propranolol is held on a sheet-like support (2), by cutting it into an appropriate size and aligning it. The dosage can be adjusted appropriately depending on the disease state, etc., and it is extremely convenient and useful in practical treatment.

Furthermore, this patch has self-adhesive properties and can be applied directly to the skin, eliminating the need for sealed administration, and the sheet-like support is permeable to moisture and air, resulting in side effects such as rash. It is easy to store and carry.

Examples 0.5 parts of propranolol, 4.0 parts of sodium polyacrylate, 20.0 parts of glycerin, 2.0 parts of carboxyvinyl polymer, 10.0 parts of isopropyl myrinutate, 5.0 parts of kaolin, and 58.5 parts of water. The paste is uniformly mixed to obtain a paste, which is spread on a nonwoven fabric made of polyester and rayon, and then cut to an appropriate size to obtain a patch.

In order to investigate the administration effect of the patch of the above example, the hair on the chest skin of rabbits was cut in a circular ≦2 area 100 - area, where the patch of the example was applied for 1.2 days after application. .4.6.
8. Blood was collected after 10 and 12 hours, and the drug concentration in the plasma of each blood was measured using high performance liquid chromatography. The measurement results are shown in the table below.

As is clear from the results of the above measurements, it can be seen that the patch of the present invention produces excellent administration effects.

Claims (1)

[Claims] A paste containing propranolol, a water-soluble polymer compound, water, and an oily component that has the effect of promoting transdermal absorption of drugs;
A propranol-containing external patch comprising a support such as flannelette, nonwoven fabric, or plastic sheet for holding the above-mentioned paste.