Stabilization of amorphous indomethacin by co-grinding in a ternary mixture.
Mechanochemical amorphization of indomethacin (IM) was substantially enhanced by grinding with SiO(2), talc and a Mg(OH)(2)-SiO(2) mixture. The rates of the mechanochemical amorphization were in the order of Mg(OH)(2)-SiO(2) mixture>talc>SiO(2). Amorphous state stability of IM compounded with the carrier was examined by crystallization behavior under the condition of 30 degrees C and 11% relative humidity. Superiority of the binary mixture as a carrier was explained in terms of the mechanically induced strong acidic sites of the carrier.
Watanabe
Tomoyuki
T
Product Development Laboratories, Sankyo Co. Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan. watatm@shina.sankyo.co.jp
Ohno
Ikumasa
I
Wakiyama
Naoki
N
Kusai
Akira
A
Senna
Mamoru
M
D002152:Calorimetry, Differential Scanning; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D003116:Color; D004339:Drug Compounding; D004355:Drug Stability; D005079:Excipients; D007202:Indicators and Reagents; D007213:Indomethacin / Q000737:chemistry*; D008276:Magnesium Hydroxide / Q000737:chemistry; D012822:Silicon Dioxide; D017550:Spectroscopy, Fourier Transform Infrared; D013314:Stress, Mechanical; D013816:Thermodynamics; D014961:X-Ray Diffraction
D005079:Excipients; D007202:Indicators and Reagents; D012822:Silicon Dioxide; D008276:Magnesium Hydroxide; D007213:Indomethacin