Dissolution difference between acidic and neutral media of acetaminophen tablets containing a super disintegrant and a soluble excipient. II.
The disintegration and dissolution of acetaminophen tablets containing sucrose and Ac-Di-Sol/Primojel was significantly different between acidic and neutral media. The purpose of this study was to investigate the mechanism of this phenomenon and to propose a way of reducing the dissolution difference between the two media. Tablets of different combinations of active ingredient, sucrose, and Ac-Di-Sol/Primojel were prepared and their dissolution in various media was evaluated. The dissolution differences were found to be largely related to the hydrophobicity of the active ingredient and pH difference of the two media. This difference was even more evident under the condition where acetaminophen, sucrose, and Primojel were combined. The dissolution difference was therefore attributed to the depressed function of Primojel in the acidic medium, the stronger binding of sucrose, the hydrophobicity of the active ingredient and pH difference of the two media. Increasing the concentration of Primojel or incorporating the surfactant in the tablet can thus greatly decrease the dissolution difference between acidic and neutral media.
Chen
C R
CR
Chia Nan College of Pharmacy and Science, Jen-Te Hsiang, Tainan Hsien, Taiwan.
Cho
S L
SL
Lin
C K
CK
Lin
Y H
YH
Chiang
S T
ST
Wu
H L
HL
D000082:Acetaminophen / Q000737:chemistry*; D004347:Drug Interactions; D005079:Excipients / Q000737:chemistry*; D006863:Hydrogen-Ion Concentration; D009994:Osmolar Concentration; D012967:Sodium Dodecyl Sulfate / Q000737:chemistry; D012995:Solubility; D013213:Starch / Q000031:analogs & derivatives / Q000737:chemistry; D013395:Sucrose / Q000737:chemistry; D013501:Surface-Active Agents / Q000737:chemistry; D013607:Tablets / Q000737:chemistry
D005079:Excipients; D013501:Surface-Active Agents; D013607:Tablets; D000082:Acetaminophen; D012967:Sodium Dodecyl Sulfate; D013395:Sucrose; D013213:Starch; C048390:sodium starch glycolate