A novel pH- and time-dependent system for colonic drug delivery.
A novel pH- and time-dependent delivery system was developed for delivering drugs to the colon. In vitro studies showed that this novel system could release the drug at a predetermined time, which was mainly controlled by the coating layers of the system. The delayed time of the press-coating layer was controlled by its erosion rate, which followed Hixson-Crowell equation. A proper selection of such factors as the viscosity grade of HPMC and tablet hardness, etc., can help reproduce the drug release profile as expected. The transit profiles in two healthy volunteers by gamma scintigraphy demonstrated that the tablets were able to pass through the stomach and small intestine intact and could safely reach the distal end of the small intestine, where the system began to release the drug contained in the core tablet. For both of the volunteers, disintegration of the tablets occurred in the ascending colon, which had highlighted the potential of this system for colonic drug delivery.
Qi
Meiling
M
Department of Clinical Pharmacology, North Taiping Road Hospital, Beijing, China. mlqi@bit.edu.cn
Wang
Peng
P
Wu
Dezheng
D
D000328:Adult; D003106:Colon / Q000000981:diagnostic imaging / Q000378:metabolism*; D005079:Excipients / Q000737:chemistry; D006244:Hardness; D006801:Humans; D006863:Hydrogen-Ion Concentration; D065347:Hypromellose Derivatives; D008297:Male; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D011877:Radionuclide Imaging; D012995:Solubility; D013213:Starch / Q000031:analogs & derivatives* / Q000737:chemistry; D013608:Tablets, Enteric-Coated; D013997:Time Factors; D014011:Tinidazole / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D014783:Viscosity
D005079:Excipients; D013608:Tablets, Enteric-Coated; D014011:Tinidazole; D065347:Hypromellose Derivatives; D008747:Methylcellulose; D013213:Starch; C034848:carboxymethyl starch