History of disintegrants and the development process of E.C.G-505® & NS-300®

The concept of bioavailability was not penetrating widely before the 1950s, and there happened that eluted tablets were discharged to the outside of the body. However, the concept of bioavailability begun to penetrate into the pharmaceutical industry in Europe from the 1955s, and accordingly the elution time of drugs grew increasingly important. As the disintegration of granulated powders and tablets becomes important to control the elution time, with the importance of disintegrants increased, many disintegrants were studied and developed all over the world in the 1960s.

We, GOTOKU CHEMICAL CO., LTD. have sold “carboxymethyl cellulose sodium (hereinafter referred to as：CMC-Na)” since inception. Having had a detailed knowledge of cellulose derivatives, we anticipated development of disintegrants in Japan. In the 1960s, We, GOTOKU CHEMICAL bore the central part of research and development and developed a disintegrant “for the first time in Japan” which introduced Ca into Carboxymethyl Cellulose (CMC) and the disintegrant was launched into the market. This is “E.C.G-505®”.This disintegrant has the characteristics of constructing loose cross-linked structure by means of Ca chelating action.

After the success of the development of E.C.G-505®, we started developing the product focused on acid-type CMC. Initially acid-type CMC was considered as not suitable for a disintegrant because of scanty swelling property based on hydrogen bonding and counter ion property.   
However, it turned out from the subsequent research that acid-type CMC was the very excellent wicking type disintegrant and was put on the market by the product name of “NS-300®”. This disintegrant takes in fluids inside tablets by wetting phenomenon even in a case of a little wetting and is used as a lot of orally integrating tablets according to the speedy wetting time  

Since E.C.G-505® (Carmellose Calcium) was listed in JP in 1966, the international performance was
appreciated and listed in USP-NF, EP and recently in ChP.  
NS-300® was listed in JP in 1986 and after that in USP-NF and EP.

In response to the international performance and customers’ needs, both E.C.G-505® and NS-300® were registered with DMF* in U.S. and DMF* in China.

　*DMF： Drug Master File