TY - JOUR
T1 - A paradigm shift in enteric coating
T2 - achieving rapid release in the proximal small intestine of man
AU - Liu, Fang
AU - Basit, A.W.
PY - 2010
Y1 - 2010
N2 - The in vivo performance of a novel enteric double-coating technology designed to accelerate release in the proximal small intestine of humans was investigated. Tablet cores were coated with a double layer formulation consisting of an inner layer of EUDRAGIT® L 30 D-55 neutralised to pH 6.0 in the presence of 10% citric acid, and an outer layer of standard EUDRAGIT® L 30 D-55. A conventional single coating of EUDRAGIT® L 30 D-55 was also applied to tablets for comparison purposes, with the identical coating formulation and thickness (5 mg/cm2) as the outer layer of the double coating. Eight fasted volunteers received the double-coated and single-coated tablets in a two-way crossover study. The formulations were radiolabelled and followed by gamma scintigraphy; the disintegration times and positions were recorded. After leaving the stomach, tablets coated with the single-coating formulation showed a significant time delay before disintegration occurred in the mid to distal small intestine, with a mean disintegration time of 66 ± 22 min post gastric emptying. The double-coated tablets disintegrated earlier at 28 ± 6 min post gastric emptying with consistent disintegration in the proximal small intestine. The accelerated in vivo disintegration of the double-coating system can overcome the limitations of conventional enteric coating.
AB - The in vivo performance of a novel enteric double-coating technology designed to accelerate release in the proximal small intestine of humans was investigated. Tablet cores were coated with a double layer formulation consisting of an inner layer of EUDRAGIT® L 30 D-55 neutralised to pH 6.0 in the presence of 10% citric acid, and an outer layer of standard EUDRAGIT® L 30 D-55. A conventional single coating of EUDRAGIT® L 30 D-55 was also applied to tablets for comparison purposes, with the identical coating formulation and thickness (5 mg/cm2) as the outer layer of the double coating. Eight fasted volunteers received the double-coated and single-coated tablets in a two-way crossover study. The formulations were radiolabelled and followed by gamma scintigraphy; the disintegration times and positions were recorded. After leaving the stomach, tablets coated with the single-coating formulation showed a significant time delay before disintegration occurred in the mid to distal small intestine, with a mean disintegration time of 66 ± 22 min post gastric emptying. The double-coated tablets disintegrated earlier at 28 ± 6 min post gastric emptying with consistent disintegration in the proximal small intestine. The accelerated in vivo disintegration of the double-coating system can overcome the limitations of conventional enteric coating.
UR - http://www.scopus.com/inward/record.url?scp=77957021284&partnerID=8YFLogxK
U2 - 10.1016/j.jconrel.2010.07.105
DO - 10.1016/j.jconrel.2010.07.105
M3 - Article
AN - SCOPUS:77957021284
SN - 0168-3659
VL - 147
SP - 242
EP - 245
JO - Journal of Controlled Release
JF - Journal of Controlled Release
IS - 2
ER -