Prevention of small black spots on sugar-coated tablets containing aluminum acetylsalicylic acid.
Sugar-coated tablets containing aluminum acetylsalicylate gradually developed black spots on their surface. A factorial experiment was performed based on an L32 orthogonal array table in an attempt to halt this phenomenon. The factor responsible proved to be talc used to formulate the smooth coating layer over the subcoating layer containing aluminum acetylsalicylate. When HCl-treated talc was used as a filler for the smoothing layer, the black spots were markedly decreased. The spotting mechanism was considered to be due to hydrolysis of aluminum acetylsalicylate in the subcoating layer to salicylic acid and acetic acid, which sublimated into the pores of the smoothing layer. Then, ferrous ion substituted from magnesium ion in the talc molecule center was extracted by salicylic acid, acetic acid, and moisture. Finally, the ferrous ion was oxidized to ferric ion, and this produced an Fe3+ chelate compound together with salicylic acid.
Tomida
Y
Y
Production Division, Takeda Chemical Industries Ltd., Osaka, Japan.
Makino
T
T
D019342:Acetic Acid / Q000737:chemistry; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry; D001241:Aspirin / Q000737:chemistry*; D002241:Carbohydrates / Q000737:chemistry*; D002614:Chelating Agents / Q000737:chemistry; D004340:Drug Contamination / Q000517:prevention & control*; D004347:Drug Interactions; D005290:Ferric Compounds / Q000737:chemistry; D006813:Humidity; D006851:Hydrochloric Acid / Q000737:chemistry*; D008274:Magnesium / Q000737:chemistry; D020156:Salicylic Acid / Q000737:chemistry; D013608:Tablets, Enteric-Coated; D013627:Talc / Q000737:chemistry*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D002241:Carbohydrates; D002614:Chelating Agents; D005290:Ferric Compounds; D013608:Tablets, Enteric-Coated; D013627:Talc; D008274:Magnesium; D020156:Salicylic Acid; D019342:Acetic Acid; D006851:Hydrochloric Acid; D001241:Aspirin