JPS59152310A - Oral cavity composition - Google Patents

Abstract

PURPOSE:An oral cavity composition useful as toothpaste, paint for affected part of gum, etc. having stability for a long period, showing an inhibitory action on plasmin in prevention and relief of pyorrhea alveolaris, obtained by using carrageenan as a viscous agent, blending it with leupeptin. CONSTITUTION:In adding stably leupeptin having an inhibitory action on serine protease to an oral cavity composition, 0.5-3.0wt%, preferably 1.0-2.0wt% carrageenan as a viscous agent based on total amount of the oral cavity composition and 0.0001-1.0wt%, preferably 0.001-0.1wt% leupeptin as a drug based on the total amount of the oral cavity composition are blended with other components.

Description

DETAILED DESCRIPTION OF THE INVENTION Field of Industrial Application The present invention (-1, 1 cavity composition, further details 1-< is a medicinal agent for the prevention and remission of chronic marginal 1-1 periodontitis, and 1) [1] relates to oral compositions such as toothpastes and gingival topical preparations stably containing iveptin.

BACKGROUND OF THE INVENTION Chronic marginal periodontitis, so-called alveolar pyorrhea, is one of the major diseases in the dental field, and its treatment is a very important problem in terms of cavity hygiene.

In recent years, the fibrinolytic system (fibrinolytic system) has progressed in the gingiva of the teeth (3) where inflammatory symptoms such as protrusion, swelling, redness, and 4:lI+l1jj, which are symptoms of pyorrhea, occur. It has been revealed that (oral surgery - 135
Vol., p. 818, 1973), a substance that inhibits plasmin, an enzyme that initiates the fibrinolytic system, is used as a medicinal agent for preventing and relieving alveolar leakage (can be incorporated into 21st cavity compositions). Typical examples of such medicinal agents include:
Examples include epsilon aminocaproic acid and fnexamic acid. However, epsilon-aminocaproic acid and l-pyrugizamic acid have the disadvantage that, although they are stable, they have a low plasmin suppressing effect when added to a c1 cavity composition.

On the other hand, as rJIJJ quality with high plasmin suppressing effect,
Leupeptin, a peptide isolated from the culture solution of actinomycetes, is known. However, when leupeptin is incorporated into oral compositions, other formulation ingredients, particularly
In the oral cavity, compositions are extremely unstable due to the influence of thickeners, which are essential ingredients for caking purposes, and 1-2 viscosity increases to maintain their dosage form.1-2 - Conventionally, leupeptin has been stably formulated.1. 1 l 1i'> xl+sei・1 does not match ru.

Purpose of the Invention In view of these two circumstances, the present inventors conducted a parental control (jl cocoon) to create an L1 cavity silk composition stably containing leupeptin, and as a result, unexpectedly Also, Tsu'hq
, [-1 Of the divine thickeners that can be distributed in the Nail 911 product, only Kara--Nan is different from Il Temple, and it is tl to l-1 Ipeptin. It was discovered that leupeptin is maintained at a constant level17, leading to the completion of the present invention.

The oral composition of the present invention contains a medicinal agent and 1-fibebutin at 1° and carrageenan at 1 and 1-2. 4';'rhui. According to the present invention, leupeptin is administered in the 1-1 cavity preparation for a long period of 1fFl', and a fixed value of 1fFl'A51. ．． 4. - Zurukotokateki, 1m - row 1fJ 2 reach no 11bo, slow tW K
The high virasmin suppressing effect of -'f- can be utilized.

1) As mentioned in article 11, leupeptin is one of the low-molecular weight peptides isolated from the culture of actinomycetes.
Vol. 2, No. 6, p. 283, 1.9694F-'), which is a substance that has a serine protease inhibitory effect. In the present invention, usually manual labor 1. Both leupeptin and I4
11. An example of this is Streptomyces roscus.
), Strea 1-Myces roseochromogens (Sc
reptomyccs roscollromoge
ns), Streatomycey, -A#hiV4-Cli(
Streptornycesalbireticul
i), Streptomyces fist thiortheus (5trc
pto+nyces thiolutcus), S1
(St.
reptomycesIavcndulac), S)
- Leptomyces novolitoei sis (Strept.
omyces nol) oricocnsis), which can be isolated from the nutrient solution of &+1 eyebrows. The compounding layer has one rule: i11 to 0.0001 to 1.0% (TFI%, the same applies hereinafter) to the entire button composition.
, preferably 0.001 to 0.1%.

Carrageenan 1l-j: Normally viscous (any type used as the circumferential side may be used; in general, from the viewpoint of stability in the morning, it is 05 to 3.0% with a force of 11 to 3.0% over the entire oral cavity during the morning). <(・”, distributed at a rate of 1(] to 20%).

The (11-stop silk paraboloid) of the present invention is prepared and polished for one hour according to the conventional method.
) 11 This month 1...Sta fill, which one can be used in the gum application part 1 . For example, 7:I-Al l'+1.1 of 1% minced meat, chrycerin, nruby-ru, etc., calcium diphosphate, calcium carbonate, 7k 'I'l-aluminum hydrosilicic acid, Abrasives such as calcium pyrophosphate, insoluble sthorium metaphosphate, 1-lium wauryl sulfate, 1-lium N-acyl sarcosicina, foaming agents such as nistyl, algyl jetanolamide, etc. Agents, 1'', ``taste'', fragrance A: 1 and 1 and 2, oxda, monofluorophosphate no 1, l JI hum, ri 1 colhexidine, other anti-inflammatory fi 11, etc.
You may also mix in some of the medicinal ingredients of the mountain.

To add to the effectiveness of the invention, we tested the modulating effect of carrageenan on leupeptin.1. Here are the results.

1. λl test-1 Dissolve 1 evane 2 m2' in water 1 Inl 17, 1 volume axillary c), 2mi water solution of various viscosity (11 agents) f 0.8 mp was added and incubated at 37℃ for 40 days. Dilute this 9-preserved solution to 0 times with water and add 2 ml of the solution to Q, lM, l-+1s salt N.
Add 0.02% trypsin solution Q.l ml to 1.7 rnl of buffer solution, 0.1% ゛N''-bensoyl-7 luginine balani,
After reacting at 37 °C for 30 minutes, 20% vinegar m ] +
The reaction was stopped by changing the amount of (n/) JIJ. The amount of free 1-danitroanilide was measured by the absorbance at a wavelength of 41Qnm, and from this value the activity of leupeptin 1'/U:. 9
It's out. In the same way, the activity of leupeptin before storage is expressed, and the activity of leupeptin after storage (71) is 1.
%) to 7"c. Na, !A1 light and 1~, total of $11 1',]; The same test was conducted on the system without t+l addition. The results are shown in Table 1.

Table 1 As shown in Table 1, among the viscous ingredients of each type, leupeptin is specifically and stably maintained in the bath using carrageenan.

Test-2 According to the conventional method 1, leupeptin combination wire tooth 1 prescribed by Rigi
Fu and gingival liniments were prepared.

Toothpaste formulation 1% Calcium diphosphate 450 Lithium lauryl sulfate 1.5 ml 200 Carrageenan
1゜-ritsukalin sodium
015 incense 41
't.

Roybeno°Sin 0.001
Water] Adjusted to 00% 41 momme Gingival liniment Prescription Ingredients % Carrageenan 1. (1 Glycerin 40.0 Leupeptin
0.01 water
1. After storing the obtained toothpaste and gum liniment at 37°C for 40 days, the leupeptin activity of the sample was calculated in the same manner as in Test 1 above, and compared with the activity immediately after preparation. The remaining activity rate of leupeptin was investigated.

As a result, the residual activity rate was 83% for the toothpaste and 85% for the gingiva liniment, indicating that leupeptin remained stable in both formulations.

The present invention will be explained in detail by referring to a real sister example.1. <Explain.

Real persimmon example 1 A toothpaste with the following formulation was manufactured according to a conventional method.

Ingredients % dibasic calcium phosphate, 45.0 ton
Ruby Tor
250 carrageenan
lO lauryl sulfate)-lium 15 zaccarinum 1 nm 0.2fF
t'1 1.0 water 10(n%
Adjusted to '人屏1ju12 Conventional method V (according to %), a gingival liniment with the following formulation was manufactured 1-/this.

Claims (1)

[Claims] (1) Leupeptin and mucilage +j) as medicinal agents and carrageenan as one agent.
- 1-lumen silk composition.