JP2908226B2 - Method for selecting carboxymethylcellulose sodium salt to be used as base material for cataplasm - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to the selection of carboxymethylcellulose sodium salt (hereinafter abbreviated as CMC) to be used as an adhesive base for a cataplasm having excellent spreadability and shape retention.
It is about the method .

[0002]

2. Description of the Related Art The performance required of a base for cataplasms includes:
Examples include spreadability, shape retention, water retention, adhesion, and flexibility. Of these, spreadability and shape retention are important because they affect the workability during preparation and the retention of the dosage form.

[0003] In general, the extensibility and the shape retention have an opposite relationship. That is, an attempt to improve the spreadability results in poor shape retention. This means that it is better to increase the fluidity of the paste in order to improve the spreadability, considering the fluidity of the paste as an index, but on the other hand, it is not preferable for mold retention to cause mold flow Because it led to the result. Therefore, conventionally, in order to impart the spreadability and the shape retaining property, a technique utilizing a gelatin-based thermoplasticity has been dealt with (for example, JP-A-57-181020). This technique is intended to impart extensibility to a base at the time of a patch preparation by the thermoplasticity of gelatin so that the prepared patch retains shape retention. However, gelatin-based bases have been problematic because they are susceptible to changes in temperature and tend to soften when the temperature rises in summer and cause unpleasant stickiness when applied to the skin.

As a method for solving the above-mentioned problems, Japanese Patent Application Laid-Open No. 60-60854 has been proposed.
That is, 5 to 40 parts by weight of polyhydric alcohol, 1 to 10 parts of sodium polyacrylate, 1 to 10 parts of carboxymethyl cellulose, 0.01 to 30 parts of an aluminum compound, 1 to 10 parts of polyacrylate, 10 to 80 parts of water by weight And a method of using a solution containing an organic acid and adjusting the pH to 5 to 8 with an acid. According to this method, spreadability and shape-retaining property not depending on the thermoplasticity of gelatin can be obtained, and a base for patches having stable adhesive strength throughout the season can be obtained. However, although this method was useful, its quality was not stable depending on the CMC used, and thus an improvement was desired.

[0005]

The object of the invention is to solve the present invention, the specific viscosity
That can impart excellent spreadability and shape retention to the base for poultices from CMCs with different degrees of etherification and etherification
An object of the present invention is to develop a method for selecting a CMC to be used as a base material .

[0006]

Means for Solving the Problems The present inventors have conducted intensive studies on CMC which imparts excellent spreadability and shape retention to a base for a pubic agent, and as a result, the 1% viscosity was 50 to 50%. 500c
ps, degree of etherification 0.60 to 1.00 mol / C ₆
Transdermal Absorbent Using Hydrogel Containing CMC as Adhesive Base
CMC used as a base for cataplasms
In the printing industry, the PVI value (Printi) is an index for comprehensively evaluating the “stickiness” and “growth” of the printing paste.
ng Viscosity Index (print viscosity index) is selected by selecting a CMC having a specific range .
Exhibition found that the ductility and retention and the can be granted at the same time,
The present invention has been accomplished.

The PVT value used in the selection of the present invention is B
Measure the CMC solution at 25 ° C with an M-type viscometer (Tokyo Keiki Co., Ltd.)
The viscosity of the CMC solution prepared to have a viscosity of 0 rpm ± 10000 ± 500 cps was measured using the same viscometer at 6 rpm and 60 rpm.
Is a numerical value obtained by the following equation. PVI value = viscosity at 60 rpm / 6 viscosity at 6 rpm. In the present invention, a CMC having a 1% viscosity of 50 to 500 cps and a degree of etherification of 0.60 to 1.00 mol / C ₆
The reason for selecting a CMC having a PVI value of 0.40 to 0.60 was that the viscosity was less than 50 cps and the shape retention was poor,
If it exceeds 500 cps, the extensibility is inferior. If the degree of etherification is less than 0.60 mol / C ₆ , the spreadability is particularly poor. If the degree of etherification exceeds 1.00 mol / C ₆ , there is no significant adverse effect on the spreadability , shape retention, etc. This is because there remains a problem in terms of cost such as the necessity of using a large amount of monochloroacetic acid as an agent. Further, when the PVI value is less than 0.40 and more than 0.60, even if the viscosity and the degree of etherification are within the above-mentioned numerical limits, the spreadability and the shape retention are not satisfied at the same time. The object of the present invention is achieved when both are within the limited range. The CMC selected in the present invention has a 1% viscosity of a commercial product.
50-500 cps, degree of etherification 0.60-1.0
The PVI value of the CMC of 0 mol / C ₆ is 0.40 to 0.40.
What is in the range of 0.60 may be appropriately selected .

[0008] as a component of Pas <br/>-up agents for bases to use CMC in more selected in the present invention, 1% viscosity, in addition to etherification degree and PVI value of CMC within the range, Examples thereof include polyhydric alcohols such as sodium polyacrylate, glycerin, sorbitol, propylene glycol and ethylene glycol, adhesives such as gum arabic, and white inorganic pigments such as kaolin and titanium oxide.
Further, as a transdermal absorption agent for preparing a poultice by mixing with the above-mentioned poultice base, methyl salicylate, glycol salicylate, diphenhydramines, indomethacin, flurbiprofen, ketoneprofen and camphor, menthol, etc. Of the essential oil component alone or a mixture thereof.

[0009]

EXAMPLES The present invention will be described in detail below, but the present invention is not limited by these.

Example 1 1% viscosity: 168 cps, degree of etherification: 0.81 mol
1 / C ₆ , a CMC having a PVI value of 0.46 is selected, and the components and proportions shown in Table 1 are placed in a mortar in the order of CMC, sodium polyacrylate, and kaolin, and powder-mixed. Then, glycerin is added and mixed well. The mixture was kneaded well while gradually adding water to obtain a base paste for a poultice.

Example 2 1% viscosity: 300 cps, degree of etherification: 0.88 mol
1 / C ₆ , a CMC having a PVI value of 0.53 was selected, and the components and ratios shown in Table 1 were prepared in exactly the same procedure as in Example 1 to prepare a base paste for a poultice. Obtained.

Comparative Example 1 1% viscosity: 800 cps, degree of etherification: 0.65 mol
Using CMC having a l / C ₆ and a PVI value of 0.42, the components and ratios shown in Table 1 were prepared in exactly the same procedure as in Example 1 to prepare a base paste for a poultice. Obtained.

Comparative Example 2 1% viscosity: 30 cps, degree of etherification: 0.85 mol
/ C ₆ , using a CMC with a PVI value of 0.56, Table 1
Were prepared in exactly the same procedure as in Example 1 to obtain a cataplasm base paste.

Comparative Example 3 1% viscosity: 190 cps, degree of etherification: 1.39 mol
Using CMC having a l / C ₆ and a PVI value of 0.59, the components and ratios shown in Table 1 were prepared in exactly the same manner as in Example 1 to prepare a base paste for a poultice. Obtained.

Comparative Example 4 1% viscosity: 324 cps, degree of etherification: 0.40 mo
1 / C ₆ , using a CMC having a PVI value of 0.45, the components and proportions shown in Table 1 were prepared in exactly the same procedure as in Example 1 to prepare a base paste for a poultice. Obtained.

Comparative Example 5 1% viscosity: 215 cps, degree of etherification: 0.70 mol
Using CMC having a l / C ₆ and a PVI value of 0.67, the components and the proportions shown in Table 1 were prepared in exactly the same procedure as in Example 1 to prepare a base paste for a poultice. Obtained.

Comparative Example 6 1% viscosity: 375 cps, degree of etherification: 0.68 mol
1 / C ₆ , using a CMC having a PVI value of 0.32, the components and proportions shown in Table 1 were prepared in exactly the same procedure as in Example 1 to prepare a base paste for a poultice. Obtained.

From the above Examples 1 and 2 and Comparative Examples 1 to 6
Table 2 shows the performance of the obtained paste. Shown in Table 2
So, the following CMCBy selectingExtensibility and
A base for cataplasms that simultaneously satisfies mold retention
Has been demonstrated. (1) 1% viscosity 50 to 500 cps (2) Degree of etherification 0.60 to 1.00 mol
/C ₆  (3) PVI value 0.40 to 0.60

[0019]

[Table 1]

[0020]

[Table 2]

Retainability: Put the paste in a tube having a tip diameter of 8 mm,
Extruded in a strand on a glass plate.
After standing for a time, the state of the strand was evaluated in comparison with that immediately after. ：: No dripping at all ○: Almost no dripping Δ: Slight dripping ×: Marked dripping Extensibility: A fixed amount of paste was placed on a stage and stretched with a glass rod, and the spread area was measured and measured in cm ² / g. Expressed. The gap between the stage and the glass rod is 0.5 mm
And

[0022]

As described in detail above , when a CMC having a 1% viscosity, a degree of etherification and a PVI value within a specific range as shown in Table 1 is selected and used, a base for a poultice is obtained. It has been found that a paste having excellent spreadability and shape retention can be obtained when used as an agent, and the present invention has been completed.

Continuation of the front page (56) References JP-A-62-138538 (JP, A) JP-A-59-110647 (JP, A) JP-A-59-53411 (JP, A) JP-A-59-108045 (JP, A) , A) JP-A-63-93717 (JP, A) (58) Fields investigated (Int. Cl. ⁶ , DB name) A61K 9/70

Claims (1)

(57) [Claims] 1. A 1% viscosity of 50 to 500 cps,
Viscosity hydrogel that Le degree is carboxymethyl cellulose sodium salt 0.60~1.00mol / _{C 6}
Base for cataplasm containing transdermal drug as base material
Carboxymethylcellulose sodium salt used for
Carboxymethyl that to, PVI value used in a base for poultices, characterized in <br/> be selected ones of 0.40 to 0.60
How to select chill cellulose salts.