JP2002145780A5 - - Google Patents

Description

[0007]
Grayed Li Kosaminogurikan such chondroitin sulfate is a kind of high molecular polysaccharide, to form a hydrogel lumps in water. In particular, when the concentration of grayed Li Kosaminogurikan high, easily hydrogel mass is produced. The formation of a hydrogel mass is likely to be promoted particularly in a low pH environment, and the formed hydrogel mass is poorly soluble and blocks the ingress of water inside the mass. Therefore, when the taken formulation contains water in the gastrointestinal tract to form a hydrogel, the permeation of water into the solid preparation is impeded, resulting in the delay of disintegration time, and the release of the active ingredient is inhibited. Therefore, when designing a solid preparation, it is necessary to consider its disintegration characteristics.

[0010]
Another object of the present invention is to provide a method for improving the disintegration properties of the solid preparation and a solid preparation which can inhibit the formation of hydrogel lumps be a solid preparation comprising a grayed re Kosaminogurikan such as chondroitin sulfate.

[0011]
Still another object of the present invention, even if pH is changed, it is possible to suppress the gel formation grayed Li Kosaminogurikan acids is to provide a method for improving the disintegration properties of the solid preparation.

[0013]
That is, the preparation of the present invention is a preparation containing a vitamin B1 and is effective for stabilizing the vitamin B1, for example, at a ratio of 0.1 parts by weight or more to 1 part by weight of the vitamin B1. While containing amino sugars (glucosamine or its salt etc.) , it further contains glycosaminoglycans . In addition, the preparation of the present invention is a preparation containing a vitamin B1 and an amino sugar, and further contains glycosaminoglycans, and the content of the vitamin B1 is 0.001 to 30% by weight with respect to the whole. %. Such a preparation of the present invention may be a solution, but contains glycosaminoglycans (such as hyaluronic acid, chondroitin and their salts) which are easily formed as a gel because disintegrability can be improved by amino sugars. In some cases, it is advantageously applied to solid formulations. That is, the formulation of the present invention may be a solid form preparations.

[0014]
This onset Ming embraces is blended aminosugar the solid preparation containing glycosaminoglycans, a method of improving the disintegration properties of the solid preparation.

[0027]
As mentioned above, the solid preparation of the present invention may further contain glycosaminoglycans (mucopolysaccharide or acidic mucopolysaccharide). The glycosaminoglycans can be used as an active ingredient (bioactive ingredient or pharmacologically active ingredient) of the preparation. Glycosaminoglycans are a series of acidic polysaccharides including amino sugars, including, for example, hyaluronic acid, chondroitin, jaruronic acid, heparan, keratan or salts thereof. The salt of glycosaminoglycans, (such as the sodium salt such as sodium hyaluronate) alkali metal salts, sulfuric smell Li Kosaminogurikan (chondroitin sulfate A (chondroitin 4-sulfate), chondroitin sulfate B (dermatan sulfate), chondroitin sulfate Chondroitin sulfate such as C (chondroitin 6-sulfate), heparin, heparan sulfate, keratan sulfate I, keratan sulfate II and the like can be exemplified. Incidentally, sulfuric smell Li Kosaminogurikan are sodium, potassium, calcium, magnesium, iron, metal salts such as manganese, may also be a salt such as ammonium salt. These glycosaminoglycans can be used alone or in combination of two or more.

[0043]
【Effect of the invention】
In the present invention, vitamin B1s can be effectively stabilized by amino sugars. Also, it is a solid preparation comprising a grayed re Kosaminogurikan such chondroitin sulfate, can suppress the formation of hydrogel lumps, can improve disintegration. In particular, the disintegration dependence by pH is small, and the disintegration of the solid preparation can be effectively improved even if the pH is changed.

[0057]
In all tablets, the disintegration time tended to be prolonged due to the decrease in pH, but in Test Example 1 containing glucosamine, the disintegration was high at any pH. In Comparative Examples 1 and 2, particularly, the disintegration time at low pH is slow, and the formation of a hydrogel mass of sodium chondroitin sulfate can not be suppressed. The results are shown in Table 1.

[0058]
[Table 1]

[0059]
Test example 2
Thiamine nitrate 3 parts by weight (made by Takeda Yakuhin Kogyo Co., Ltd.), glucosamine hydrochloride 100 parts by weight (made by Yaizu Fisheries Co., Ltd.), 0.5 parts by weight of magnesium stearate (made by Taihei Kagaku Sangyo Co., Ltd.) uniformly mixed Then, a mixture of tablet components was prepared. The mixture was subjected to rotary tableting to obtain circular tablets (diameter 8.5 mm, weight 270 mg, hardness 5 kg (measured by digital hardness tester)) as in Example 1 .

[0060]
The tablets of Test Example 2 and Comparative Example 3 were put in a glass bottle and stored at 50 ° C. in the dark for 2 weeks. Thereafter, the residual amount of thiamine nitrate in the tablet was measured by high performance liquid chromatography (HPLC) according to a conventional method. In Test Example 2, the residual ratio (the residual amount of thiamine nitrate in the tablet / initial thiamine nitrate amount in the tablet) Comparative Example 3 was 95.3%, compared to 99.8%).

[0061]
In addition, the tablet of Test Example 2 was put in a glass bottle, stored at 40 ° C., protected from light for 1 month, 3 months and 6 months, and the residual rate of thiamine nitrate was measured in the same manner. Even after 6 months, it was a high survival rate of 99.9%. Thus, glucosamine was shown to be effective in the long-term stabilization of thiamine nitrate.

Claims (7)

It is a preparation containing vitamin B1s, containing 0.1 parts by weight or more of amino sugars with respect to 1 part by weight of vitamins B1, and further containing glycosaminoglycans . A preparation comprising a vitamin B1 and an amino sugar, wherein the preparation further comprises glycosaminoglycans, and the content of the vitamin B1 is 0.001 to 30% by weight based on the whole. The preparation according to claim 1 or 2, wherein the amino sugar is glucosamine or a salt thereof . Preparation according to claim 1 or 2, wherein the solid form preparations. Glycosaminoglycans are hyaluronic acid, chondroitin and preparations according to claim 1, wherein at least one member selected from the salts thereof. The preparation according to claim 1 , wherein the preparation comprises 0.1 part by weight or more of aminosugars with respect to 1 part by weight of glycosaminoglycans. A method of incorporating amino sugars into a solid preparation containing glycosaminoglycans to improve the disintegration of the solid preparation.