JP2000095678A - Cataplasm base and cataplasm containing the same - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a base for cataplasm that has excellent extensibility and shape retention as well as moisture retention and skin adhesion. SOLUTION: This base for cataplasm is made of a thermally crosslinked carboxymethylcellulose sodium salt (for example, it is prepared by crosslinking carboxy-methylcellulose sodium salt with heat at 80-200 deg.C for 20-180 minutes.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to a base for cataplasms based on sodium carboxymethylcellulose and a cataplasm containing the same.

[0002]

2. Description of the Related Art In general, bases for cataplasms include spreadability,
Performance such as shape retention, water retention and skin adhesion is required.

[0003] In particular, the spreadability and the shape retention are important factors that determine the workability in the preparation of a cataplasm, but the spreadability and the shape retention are generally contradictory performances and are incompatible. . In other words, when considering the fluidity of the poultice paste as an index, it is better to increase the fluidity of the paste in order to improve the spreadability, but it is not preferable that the shape collapse occurs for shape retention, It means that the smaller the fluidity, the better.

Typical representatives conventionally used as bases for cataplasms are gelatin and sodium carboxymethylcellulose (hereinafter sometimes referred to as CMC).

[0005] However, gelatin-based bases
There is a problem in that the paste is easily affected by a change in climate and the paste softens in the summer and causes unpleasant stickiness when applied to the skin.

A paste using a CMC-based base is hardly affected by a change in climate, but has a problem in that the performance as a base for a poultice differs greatly depending on a change in the properties of the CMC used.

[0007]

SUMMARY OF THE INVENTION In view of the foregoing, it is an object of the present invention to provide a CMC having excellent spreadability, shape retention, water retention, skin adhesion, etc. It is an object to provide a base for poultices and a poultice.

[0008]

That is, the invention according to claim 1 relates to a base for a poultice comprising a heat-crosslinked sodium carboxymethylcellulose.

The invention according to claim 2 is characterized in that the thermally crosslinked carboxymethylcellulose sodium salt is prepared by converting carboxymethylcellulose sodium salt at 80 to 200 ° C.
The poultice according to claim 1, which is crosslinked by heating for 180 minutes.

Further, the invention according to claim 3 is the invention according to claims 1 to
2. A poultice comprising the base for poultices according to any one of (2) and a transdermally absorbable drug.

[0011]

BEST MODE FOR CARRYING OUT THE INVENTION The base material for a poultice according to the present invention is composed of thermally crosslinked CMC. By using such thermally crosslinked CMC, both spreadability and shape retention can be achieved. .

The thermally crosslinked CMC is obtained by subjecting the CMC to a heat treatment to form a crosslink. That is, as shown in the following reaction formula, free carboxylic acid groups present in small amounts in _{CMC (Cell-O-CH 2} -COOH)
Are reacted with unsubstituted hydroxyl groups (Cell-OH) in the CMC molecular chain by heat treatment at a high temperature to cross-link the CMC molecule with an ester bond. Here Cell
Represents a cellulose residue. _{Cell-O-CH 2 -COOH +} Cell-OH →
_{Cell-O-CH 2 -COO-} Cell

In order to cause the CMC to undergo an esterification crosslinking reaction by the heat treatment as described above, it is necessary that a free carboxylic acid group is present in the CMC. The means for obtaining CMC having such a free carboxylic acid group will be described later.

In the present invention, the raw material CMC for thermal crosslinking may be produced by any of the aqueous medium method and the solvent method.

Thermally Crosslinked CM Having Both Extensibility and Shape Retention
In order to obtain C, the degree of etherification,
It is preferable to use those having a 1% aqueous solution viscosity and a 1% aqueous solution pH in a specific range.

That is, the degree of etherification is preferably in the range of 0.6 to 1.5, more preferably 0.6 to 1.0. If the degree of etherification is less than the above range, the ductility tends to be particularly poor. On the other hand, if it exceeds the above range, the crosslinking effect is not sufficient, and the effect of improving shape retention tends to be hardly exhibited. It should be noted that such high etherification CMC
In order to obtain the compound (1), a large amount of monochloroacetic acid as an etherifying agent must be used, and there is also a problem that the cost of the raw material is high.

The viscosity of a 1% aqueous solution is 5 to 2000 mPa · s.
Is preferred, and particularly preferably 50 to 1000 m
Pa · s. If the 1% aqueous solution viscosity is less than the above range, the viscosity required for the cataplasm paste cannot be secured, and the shape retention tends to be poor. On the other hand, if it exceeds the above range, the viscosity of the paste is large, and the spreadability tends to be poor.

The definition of the pH of a 1% aqueous solution is important for the presence of free carboxylic acid groups required for thermal crosslinking in the raw CMC. That is, the pH of the 1% aqueous solution is preferably in the range of 5.5 to 7.0, and particularly preferably 6.0 to 6.5. If the pH of the 1% aqueous solution exceeds the above range, the amount of free carboxylic acid groups required for thermal crosslinking is small, the crosslinking effect is not sufficient, and it is difficult to achieve both spreadability and shape retention. In addition, when a cataplasm is applied, it may lead to the occurrence of skin irritation and the like. On the other hand, when the pH of the 1% aqueous solution is less than the above range, the cataplasm paste becomes acidic due to the presence of free carboxylic acid groups not used for thermal crosslinking, which is not preferable.

As a method of obtaining CMC having a 1% aqueous solution pH in the above range, for example, CMC powder is dispersed in a solvent mainly composed of a water-soluble solvent such as lower alcohols such as methanol, ethanol and isopropyl alcohol, and acetic acid, An appropriate amount of an acid such as formic acid is added, mixed uniformly, then separated into a solid and a liquid by a centrifugation method, and the obtained solid is dried.

In the present invention, the degree of etherification is 0.6 to 1.5, and the viscosity of 1% aqueous solution is 5 to 2000 mPa.
It is preferable to thermally crosslink using CMC having a pH of 5.5% to 7.0% as a 1% aqueous solution. As the conditions for the thermal crosslinking, it is preferable to appropriately set the heating temperature and the heating time in order to appropriately perform the crosslinking.

That is, the heating temperature is preferably in the range of 80 to 200 ° C, particularly preferably 120 to 150 ° C. If the heating temperature is lower than the above range, crosslinking becomes insufficient or an extremely long time is required to achieve sufficient crosslinking. On the other hand, when the ratio exceeds the above range, the degradation of CMC becomes severe, and it becomes difficult to obtain a material having a predetermined viscosity.

The heating time is preferably in the range of 20 to 180 minutes, particularly preferably 30 to 150 minutes. Since the length of the heating time affects the degree of crosslinking, it is preferable to set an appropriate time within the above range in consideration of the heating temperature.

The heat treatment for thermal crosslinking is usually carried out by heating the raw material CMC in a powder state in an appropriate heating furnace. The heat treatment may be a batch type or a continuous type.

The poultice of the present invention comprises the heat-crosslinked C
A hydrogel containing a base for cataplasms composed of MC is used as an adhesive base, and a percutaneously absorbable drug is added thereto.

In the poultice of the present invention, as the adhesive base component, in addition to the thermally crosslinked CMC, sodium polyacrylate, polyhydric alcohols such as gelatin, glycerin, sorbitol, propylene glycol and ethylene glycol, and gum arabic And white inorganic pigments such as kaolin, talc, titanium oxide, aluminum hydroxide and aluminum silicate.

Transdermally absorbable drugs include methyl salicylate, glycol salicylate, diphenylhydrazines,
Analgesic and anti-inflammatory agents such as indomethacin, flurbiprofen and ketone profen, and oil refinement components such as camphor and menthol. These can be used alone or in combination of two or more.

The cataplasm of the present invention comprises a thermally crosslinked CM.
It can be produced by kneading C, other adhesive base components, a transdermal drug, and water to form a paste. The blending amount of the thermally crosslinked CMC is 10 × 1 at a paste viscosity of 50 ° C.
An amount in the range of 0 ^{4 to} 12 × 10 ⁴ mPa · s is preferable.

The poultice of the present invention is usually used as a molded poultice. The molding poultice comprises a support (packing), a paste formed by applying and spreading on the support, and a coating material (liner) for coating the paste. This molding poultice is generally used as an external preparation used for compresses.

[0029]

EXAMPLES Next, the base for a poultice and the poultice of the present invention will be described with reference to Examples and Comparative Examples, but the present invention is not limited thereto.

Examples 1 to 8 and Comparative Examples 1 to 8 <Production of thermally crosslinked CMC> 100 g of powders of various CMCs having different degrees of etherification and 1% aqueous solution were dispersed in 1000 g of 95% by weight methanol and obtained with a stirring rod. The resulting slurry was stirred. A 25% by weight aqueous acetic acid solution is added thereto in an amount of 1 to 50
g, and the mixture was homogenized, and then subjected to solid-liquid separation using a centrifuge. For the obtained CMC, the water content, the viscosity of a 1% aqueous solution, the degree of etherification, and the pH of a 1% aqueous solution were measured by the following measurement methods. Table 1 shows the results.

Next, the CMC was spread on a stainless steel vat, dried by heating at 105 ° C. for 2 minutes in a heating furnace, and further heated at 130 ° C. for 60 minutes to obtain a thermally crosslinked CMC.

CMC Measurement Method About 2 g of a water sample is accurately weighed into a weighing bottle, dried in a constant temperature dryer at 105 ° C. for 3 hours, and the water content is calculated from the weight loss. Moisture (% by weight) = (weight loss g / sample g) × 100

1% aqueous solution viscosity A sample was weighed to prepare a 1% by weight aqueous anhydride solution, and the aqueous solution was prepared.
Measure at 5 ° C. with a BM type viscometer.

Degree of etherification About 1 g of an anhydrous sample is accurately weighed and incinerated in a magnetic crucible. After cooling, transfer to a 500 ml beaker and add N / 1
50 ml of sulfuric acid and about 250 ml of water are added and boiled for 30 minutes. After cooling, the excess acid is titrated with N / 10 potassium hydroxide using phenolphthalein as an indicator and calculated by the following equation. A = (number of blank ml−number of sample titration ml) × N / 1
0 Potassium hydroxide strength / sample g degree of etherification = 162A / 10000-80A

PH of 1% aqueous solution The pH of a 1% aqueous solution is measured with a pH meter.

<Pop preparation test> Thermal crosslinking C obtained above
A poultice was prepared using MC as follows. First, a solution A and a solution B having the following compositions were prepared.

Solution A Component weight parts Aluminum silicate 15 Talc 7.5 Glycerin 45 Thymol 0.15 Methyl salicylate 0.75 Thermally crosslinked CMC X

The above-mentioned components were used in a three-one-motor two-blade 7
Liquid A was prepared by kneading at 50 rpm for 3 minutes at 00 rpm. In addition, about the thermally crosslinked CMC, the viscosity of the obtained cataplasm paste is 10 × 10 ^{4 to} 12 × 10 ⁴ m.
The addition amount X was appropriately determined according to the viscosity of the thermally crosslinked CMC used so as to obtain Pa · s. The viscosity of the cataplasm paste was measured using a BH type viscometer rotor No. Measured at 50C at 7-20.

Solution B Component Weight parts Lactic acid 1.5 Gelatin 9 Water 90

A liquid B was prepared by kneading the above components.

Next, by adding the total amount of the solution B to the total amount of the solution A and kneading the mixture at 50 ° C. for 10 minutes, the viscosity of the paste as a poultice becomes 10 × 10 ^{4 to} 12 × 10 ⁴ mPa.
S (50 ° C.).

Immediately, 10 g of the above paste was applied to a cotton flannel (6c
m.times.10 cm), and spread. The spread surface was coated with a polyvinylidene chloride film to prepare a molded cataplasm, and the molded cataplasm was placed in a laminate bag and sealed.

Then, a 200 g weight was placed on the entire surface of the cotton flannel and allowed to stand at 25 ° C. for 30 days, and the following items were evaluated for this evaluation sample. Evaluated at times). Table 1 shows the results.

(Spreadability) Easiness of spread when the paste was spread on cotton flannel was evaluated by touch. Those that can be spread smoothly ◎ The paste is too hard or too soft and takes much time for work ○ The one that paste was too hard or too soft to spread enough △

(Shape Retention) With respect to the cotton flannel to which the paste was applied, it was visually observed whether or not the paste spread out more than the size of the cotton flannel (6 cm × 18 cm). No spread of the paste was observed ◎ Little spread of the paste was observed ○ Some spread of the paste was slightly observed △ Some spread of the paste was clearly observed ×

(Water retention) The state of water bleeding on the back side of the cotton flannel coated with the paste was evaluated by touch. Water bleeding is not felt at all ◎ Water bleeding is hardly felt ○ Water bleeding is slightly felt △ Water bleeding is clearly felt ×

(Skin Adhesion) The paste surface of the cotton flannel coated with the paste was allowed to adhere to the skin and allowed to stand for 5 minutes, and then resistance was observed when the paste was gently peeled off. Those who felt strongly adhered ◎ Those who felt closely adhered ○ Those who felt weakly adhered △ Those which did not adhere ×

[0048]

[Table 1]

[0049]

According to the present invention, the use of a thermally crosslinked CMC as a base for a poultice makes it possible to attain both contradictory performances such as spreadability and shape retention, and furthermore to provide a water repellent and skin adhesive excellent excellence. Can be obtained.

Claims (3)

[Claims] 1. A base for a poultice comprising a thermally crosslinked sodium carboxymethylcellulose. 2. The poultice according to claim 1, wherein the thermally crosslinked carboxymethylcellulose sodium salt is obtained by heating and crosslinking carboxymethylcellulose sodium salt at 80 to 200 ° C. for 20 to 180 minutes. 3. A poultice comprising the base for a poultice according to claim 1 and a transdermally absorbable drug.