An attempt to stabilize nilvadipine solid dispersion by the use of ternary systems.
Firstly, we investigated the physical stability of nilvadipine (NIL)/crospovidone (cl-PVP) solid dispersion during storage (40 degrees C, 75% relative humidity) with powder x-ray diffraction, differential scanning calorimetry (DSC) and dissolution test. These studies indicated that recrystallization occurred during storage and that the dissolution of NIL greatly decreased, compared with that of the initial finding. Secondly, to improve the amorphous form physical stability of NIL, methylcellulose (MC) was added to NIL/cl-PVP solid dispersions as a dispersion carrier and NIL/cl-PVP/MC ternary solid dispersion systems were obtained by the solvent method. Powder x-ray diffraction and DSC studies indicated that the amorphous form physical stability of NIL clearly improved in the NIL/cl-PVP/MC solid dispersion systems during storage. Moreover, the dissolution properties of NIL/cl-PVP/MC solid dispersion systems were characterized by cl-PVP markedly enhancing the dissolution of NIL and MC inhibiting the change of the dissolution of NIL during storage. Finally, we obtained an ideal solid dispersion that was accompanied by a consistently higher rate of dissolution.
Hirasawa
Noriyuki
N
Medicinal Research Department, Nichi-iko Pharmaceutical Co., Ltd., Namerikawa, Japan. n-hirasawa@nichiiko.co.jp
Ishise
Sayoko
S
Miyata
Hitomi
H
Danjo
Kazumi
K
D004355:Drug Stability; D009543:Nifedipine / Q000031:analogs & derivatives* / Q000032:analysis / Q000737:chemistry*; D013678:Technology, Pharmaceutical / Q000379:methods*
C035100:nilvadipine; D009543:Nifedipine