The effect of cross-linking on the in vivo disintegration of hard gelatin capsules.
OBJECTIVE
To evaluate if the cross-linking of gelatin affects in vivo capsule disintegration.


METHODS
Scintigraphic investigation in nine healthy volunteers to provide for a real time visualisation of capsule disintegration.


RESULTS
The moderately stressed capsules failed the USP dissolution specification for acetaminophen capsule when tested in water and conventional SGF but passed with the addition of pepsin. Moderately stressed capsules started to disintegrate at 10 +/- 6 minutes (range 6 to 24 minutes) compared to 8 +/- 2 minutes (range 5 to 11 minutes) for the unstressed capsule.


CONCLUSIONS
The results of the study clearly demonstrate that with the incisive technique of gamma scintigraphy there are no differences in the in vivo disintegration properties of moderately stressed and unstressed capsules.
Pharmaceutical Profiles Limited, Highfields Science Park, Nottingham, UK.
J
J
Brown
N
N
Madit
E T
ET
Cole
I R
IR
Wilding
D
D
Cadé
D000082:Acetaminophen / Q000008:administration & dosage / Q000493:pharmacokinetics; D018712:Analgesics, Non-Narcotic / Q000008:administration & dosage / Q000493:pharmacokinetics; D002214:Capsules / Q000008:administration & dosage / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D003432:Cross-Linking Reagents / Q000737:chemistry; D018592:Cross-Over Studies; D004064:Digestive System / Q000378:metabolism; D005260:Female; D005780:Gelatin / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D006801:Humans; D007091:Image Processing, Computer-Assisted / Q000379:methods; D008297:Male; D016037:Single-Blind Method
D018712:Analgesics, Non-Narcotic; D002214:Capsules; D003432:Cross-Linking Reagents; D000082:Acetaminophen; D005780:Gelatin