Enteric coated HPMC capsules designed to achieve intestinal targeting.
The enteric coating of HPMC capsules containing paracetamol was investigated. Two enteric polymers, Eudragit L 30 D-55 and Eudragit FS 30 D were studied, which are designed to achieve enteric properties and colonic release, respectively. The capsules were coated in an Accela Cota 10, and, as shown by optical microscopy, resulted in capsules with a uniform coating. Scanning electron microscopy of the surface of the capsules illustrate that, in contrast to gelatin, HPMC has a rough surface, which provides for good adhesion to the coating. Dissolution studies demonstrated that capsules coated with Eudragit L 30 D-55 were gastro resistant for 2 h at pH 1.2 and capsules coated with Eudragit FS 30 D were resistant for a further 1 h at pH 6.8. The product visualisation technique of gamma scintigraphy was used to establish the in vivo disintegration properties of capsules coated with 8 mg cm(-2) Eudragit L 30 D-55 and 6 mg cm(-2) Eudragit FS 30 D. For HPMC units coated with Eudragit L 30 D-55, complete disintegration occurred predominately in the small bowel in an average time of 2.4 h post dose. For HPMC capsules coated with Eudragit FS 30 D, complete disintegration did not occur until the distal small intestine and proximal colon in an average time of 6.9 h post dose.
Cole
Ewart T
ET
Capsugel Division of Pfizer Inc., Fabrikmattenweg 2, CH-4144 Arlesheim, Basel, Switzerland. ewart.cole@pfizer.com
Scott
Robert A
RA
Connor
Alyson L
AL
Wilding
Ian R
IR
Petereit
Hans U
HU
Schminke
Carsten
C
Beckert
Thomas
T
Cadé
Dominique
D
D002214:Capsules; D018592:Cross-Over Studies; D016503:Drug Delivery Systems / Q000379:methods*; D005260:Female; D006801:Humans; D007413:Intestinal Mucosa / Q000378:metabolism*; D007422:Intestines / Q000000981:diagnostic imaging / Q000187:drug effects*; D007785:Lactose / Q000008:administration & dosage* / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D008297:Male; D008747:Methylcellulose / Q000008:administration & dosage* / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D008855:Microscopy, Electron, Scanning; D010078:Oxazines; D011109:Polymethacrylic Acids / Q000008:administration & dosage / Q000493:pharmacokinetics; D011877:Radionuclide Imaging; D012995:Solubility; D013608:Tablets, Enteric-Coated
D002214:Capsules; D010078:Oxazines; D011109:Polymethacrylic Acids; D013608:Tablets, Enteric-Coated; C038300:methylmethacrylate-methacrylic acid copolymer; D008747:Methylcellulose; C071191:MK 458; D007785:Lactose