A paradigm shift in enteric coating: Achieving rapid release in the proximal small intestine of man

作者：Liu Fang; Basit Abdul W^*

来源：Journal of Controlled Release, 2010, 147(2): 242-245.

DOI：10.1016/j.jconrel.2010.07.105

• pH-sensitive polymers
• Methacrylic acid ethyl acrylate copolymer
• Enteric coatings
• Enteric polymers
• Gastric resistance
• Gamma scintigraphy
• Gastrointestinal transit

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 (R) L 30 D-55 neutralised to pH 6.0 in the presence of 10% citric acid, and an outer layer of standard EUDRAGIT (R) L 30 D-55. A conventional single coating of EUDRAGIT (R) L 30 D-55 was also applied to tablets for comparison purposes, with the identical coating formulation and thickness (5 mg/cm(2)) 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 coatings.

• 出版日期2010-10-15