Evaluation of enteric coated tablet sensitive to pancreatic lipase. I. In vitro disintegration test.
We designed a new enteric coated preparation which is pH independent and functions by pancreatic lipase activity in the duodenum. Triolein (TO) and trilaurin (TL) were selected as lipase sensitive components and ethylcellulose (EC) was used as the support film for TO and TL. Tablets (330 mg, d = 10 mm) containing a model drug, sulfamethizole (SMZ), were coated with 1% each of TO, TL and EC solution by the fluidized bed coating technique. Disintegration tests were carried out in the media including JPXI 1st fluid (pH 1.2, JP-1), 2nd fluid (pH 6.8, JP-2) and JP-2 with gall powder and pancreatic lipase (JP-2-GL). The lag time of disintegration of the tablet (TOTL-Tab) coated 5-7 mg/tab with TO, TL and EC was about 10 min and all of the tablets disintegrated completely within 30 min in JP-2-GL. However, in the other media, which did not contain lipase, TOTL-Tab did not disintegrate for at least 2 h. It was confirmed that TO and TL in the coating film were digested by lipase. In addition, the tensil strength of the film decreased quickly after incubation in JP-2-GL. These results suggest that the application of TO, TL and EC to tablet coating is useful for an enteric release preparation sensitive to pancreatic lipase, even if patients have low gastric acidity or are taking antacids.
Yoshitomi
H
H
Faculty of Pharmacy and Pharmaceutical Sciences, Fukuyama University, Hiroshima, Japan.
Shizuku
Y
Y
Masuda
Y
Y
Itakura
R
R
Kanke
M
M
Okamoto
S
S
Nashihata
T
T
Goto
S
S
D002626:Chemistry, Pharmaceutical; D008049:Lipase / Q000378:metabolism*; D010179:Pancreas / Q000201:enzymology*; D012995:Solubility; D013608:Tablets, Enteric-Coated
D013608:Tablets, Enteric-Coated; D008049:Lipase