Application of nilvadipine solid dispersion to tablet formulation and manufacturing using crospovidone and methylcellulose as dispersion carriers.
Nilvadipine (NIL) solid dispersion using crospovidone (Cross-linked-N-vinyl-2-pyrolidone, cl-PVP) and methylcellulose (MC) as carriers was applied to tablet formulation. Several grades of cl-PVP and MC were used, and their influence on tablet properties such as hardness, disintegration, dissolution and chemical stability were investigated. The agitation granulation method was used for preparation of solid dispersion granules, and the granules were compressed using a rotary tableting machine, and finally the obtained tablets were coated with film. As the particle size of cl-PVP decreased, hardness and apparent solubility were increased, while dissolution rate was lowered. When a higher viscosity grade of MC was used, hardness and dissolution rate were increased, and apparent solubility did not change. All batches of tablets were chemically stable at 40 degrees C, 75% relative humidity (R.H.) for six months. Finally, tablets with enhanced dissolution properties were obtained by using Polyplasdone XL-10 and Metolose SM-25 as the grades of cl-PVP and MC, respectively. These formulation tablets showed higher solubility and dissolution rate during storage as well as initial indicating good physical stability.
Hirasawa
Noriyuki
N
Research and Development Center, Nichi-iko Pharmaceutical Co, Ltd, Namerikawa, Japan. n-hirasawa@nichiiko.co.jp
Ishise
Sayoko
S
Miyata
Hitomi
H
Danjo
Kazumi
K
D004339:Drug Compounding; D004355:Drug Stability; D005079:Excipients / Q000737:chemistry*; D006244:Hardness; D008747:Methylcellulose / Q000737:chemistry*; D009543:Nifedipine / Q000031:analogs & derivatives / Q000737:chemistry*; D010316:Particle Size; D011205:Povidone / Q000737:chemistry*; D012995:Solubility; D013608:Tablets, Enteric-Coated
D005079:Excipients; D013608:Tablets, Enteric-Coated; C035100:nilvadipine; D008747:Methylcellulose; D011205:Povidone; D009543:Nifedipine