The influence of granulation on super disintegrant performance.
The purpose of this study is to identify the causes of efficiency loss of super disintegrants following granulation or reworking. Two processes, precompression and prewetting, were proposed to simulate the processes during dry and wet granulation, respectively. The disintegration efficiency of the resulting disintegrant granules was tested in model formulations composed of dicalcium phosphate and lactose with the unprocessed disintegrants as controls. No significant difference was shown in the intrinsic swelling and the water uptake abilities of all super disintegrants following dry granulation. However, a significant decrease was observed for both Primojel and Polyplasdone XL10 in the rate of water being absorbed into the tablet matrix following wet granulation, but not for Ac-Di-Sol. United States Pharmacopeia (USP) disintegration testing without disc revealed a significant increase in disintegration time for tablets formulated with dry granulated Primojel and Polyplasdone XL10 and all wet granulated disintegrants. The increase in particle size following granulation appears to be the cause of the loss in disintegration efficiency. In conclusion, Ac-Di-Sol is less affected by both precompression and prewetting. The efficiency of Primojel and Polyplasdone XL10 is highly dependent on their particle size. Descreasing the particle size tends to increase their efficiency. Due to the size increase following granulation, a higher addition level of super disintegrant is required to ensure fast and uniform disintegration of tablets prepared by granulation.
Zhao
Na
N
Univeristy of Maryland School of Pharmacy, Baltimore, MD 21201, USA.
Augsburger
Larry L
LL
D002626:Chemistry, Pharmaceutical; D004339:Drug Compounding; D005079:Excipients; D007700:Kinetics; D010316:Particle Size; D019904:Polymethyl Methacrylate / Q000737:chemistry*; D011205:Povidone / Q000737:chemistry*; D011208:Powders; D012995:Solubility; D013213:Starch / Q000031:analogs & derivatives* / Q000737:chemistry; D013607:Tablets; D014867:Water / Q000737:chemistry
D005079:Excipients; D011208:Powders; D013607:Tablets; D014867:Water; D013213:Starch; D019904:Polymethyl Methacrylate; C048390:sodium starch glycolate; D011205:Povidone