JPS59176247A - Method for preventing decomposition of water-soluble azunole - Google Patents

Abstract

PURPOSE:To prevent the decomposition of water-soluble azunole or a drug containing the same, and to keep its drug action for a long period, by sealing the drug together with a disoxidation agent. CONSTITUTION:The decomposition of water-soluble azunole of formula having excellent anti-inflammatory action, histamine-release suppressing action, etc. is prevented, and the activities of the compound are maintained for a long period, by sealing the azunole or a drug containing the same together with a disoxidation agent [e.g. Ageless (commercial name of a product of Mitsubishi Gas Chemical Co.) packed with a gas-permeable material such as paper, cloth or perforated plastic film, etc.]. It is preferable to use a disoxidation agent capable of absorbing 200-1,000ml of oxygen per 1kg of the water-soluble azulene or 500-1,000 tablets of the drug or 500g of the granules of the drug.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a method for preventing the decomposition of water-soluble aznol and maintaining its medicinal efficacy for a long period of time.

Water-soluble Azunol [chemical name: sodium 2-1,4-dimefh-7-i7globylazulene-3-sulfonate] is a compound represented by the following formula (1), and has excellent anti-inflammatory and histamine release inhibitory effects. etc., and are currently widely used in clinical practice.

Water-soluble Aznol is generally formulated in the form of tablets or granules, but water-soluble Aznol is unstable to heat and decomposes when stored at room temperature. It decomposes into [chemical name: 1゜4-dimethyl-7-inglobil azulene], resulting in decreased medicinal efficacy and loss of commercial value.

Therefore, conventionally, water-soluble Azunol and formulations containing the same have been stored at low temperatures (5° C. or lower) to prevent this decomposition. However, it is extremely complicated and difficult to preserve drugs at temperatures below 5° C. during the storage and distribution process, and an advantageous preservation method has been desired.

Although it has been known that water-soluble Azunol is decomposed by heat, no research has been conducted on other causes of hair loss. Therefore, the inventor of the present invention conducted extensive research on its stability from various viewpoints and found that water-soluble Azunol is decomposed in the presence of oxygen.Therefore, if it is packaged with an oxygen scavenger, it will prevent decomposition at room temperature and will last for a long time. The present invention was completed by discovering that it can be stably maintained for a long period of time.

That is, the present invention provides a method for preventing the decomposition of water-soluble Azunol, which comprises sealing and packaging water-soluble Azunol or a preparation containing the same together with an oxygen absorber.

In the method of the present invention, the oxygen scavenger used is one packaged with a breathable material such as paper, cloth, or plastic with pores. It is commercially available as (trade name manufactured by Toagosei Kagaku Co., Ltd.), Secur (trade name manufactured by Nippon Soda Co., Ltd.), etc.

1. To carry out the method of the invention, the oxygen scavenger is made immiscible with the water-soluble Aznol or its formulation and sealed in its packaging container.

For example, the packaged oxygen scavenger may be sealed together with water-soluble Azunol or its preparation in a non-breathable container, such as a bottle or an aluminum, Variron, or Boblon bag.

The amount of oxygen scavenger varies depending on the form of the preparation, but usually water-soluble azulene bulk powder I, Ky, @ agent 500 to 1000 tablets,
Preferably, an oxygen scavenger is used which has an oxygen absorption capacity of about 200 to 1000 m per 500 f of granules.

In this case, the water-soluble azunol can be stably maintained without being decomposed for a long period of time even at room temperature, as shown in the Examples below, with extremely simple operations.

Next, an example will be given and explained.

Example 1 Water-soluble Azunol 500f and [Ageless Z-100
041 pieces (oxygen absorption amount: 10,100 O) were placed in a 0.81-volume glass bottle with a lid, stored at various temperatures, and the residual rate was examined. In addition, only water-soluble Azunol 500f was added to O,
As a control, S was placed in a glass bottle with a lid.

The residual rate of water-soluble Azunol was measured by the following method. That is, adding 60 - of water to the sample 0.1f, approximately 2
Shake for 0 minutes and add water to make exactly 100-. Take this solution 10- and add water to make it 50m, use it as a sample solution,
The absorbance (A) is measured at an oil length of 10 mm and a wavelength of 570 nm to determine the content, and the initial content is set to 100 to determine the residual rate.

The content rate during measurement and the results are shown in Table 1-Tlj (product of the present invention) and Table 1-(
2) As shown in the table (control).

Table 1-(1) Table 1-(2) Margins below the present invention Comparative Example 2 (1) Tablet water-soluble Azunol 2 (■) Lactose 42 Crystalline cellulose 40 Corn starch 12 Sodium hydrogen carbonate 0.5 Gum arabic 3 Stearin & Calcium One tablet was made by a conventional method from a composition of 0.5 or more.

(11) 1,000 tablets and “Vitalo 7 LH”
-1000J 1 (0.5 m) was placed in a glass bottle with a lid and stored at 30°C for 6 months, but no decomposition of water-soluble azunol was observed.

Example 3 (1) Granules Water-soluble Azunol 10 (■) Lactose 784.9 Mannitol 200 Sodium bicarbonate 5 T-menthol kO11 Granules 1y were prepared from the above composition by a conventional method.

(11) The above granules 500f and “Sekurujin-100”
Put 1 piece of 0J into an aluminum bag of O, St capacity, seal it, and add 30
Although it was stored at ℃ for 6 months, no decomposition of water-soluble azunol was observed.

that's all Applicant Taiyo Pharmaceutical Co., Ltd.

Claims (1)

[Claims] 1. A method for preventing the decomposition of water-soluble Azunol, which comprises sealingly packaging water-soluble Azunol or a preparation containing the same together with an oxygen absorber.