Calcium pectinate capsules for colon-specific drug delivery.
The calcium pectinate (CaP) capsule, a novel, colon-specific delivery system, was designed and developed using 5-fluorouracil (5-FU) as a model drug. Technically, CaP capsules were prepared by dipping a glass or stainless steel rod successively into pectin and calcium chloride solutions, followed by subsequent air-drying and coating. In vitro studies showed that the release of 5-FU from CaP capsules markedly increased in the presence of rat cecal contents, and the release characteristic was mainly associated with some capsule parameters such as calcium content, shell thickness, and coat amount. Gamma scintigraphic studies demonstrated that CaP capsules could pass through the stomach and small intestine intact and could release drug in colon. The 5-FU releasing characteristics acquired both from in vitro biomimic dissolution experiments and from healthy volunteers indicated that the newly developed CaP capsule possessed the ideal colon-specific drug delivery characteristic.
Xu
Chen
C
Institute of Functional Biomolecules, State Key of Pharmaceutical Biotechnology, Nanjing University, Nanjing, PR China.
Zhang
Jun Shou
JS
Mo
Yun
Y
Tan
Ren Xiang
RX
D000284:Administration, Oral; D000328:Adult; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage*; D002214:Capsules; D002432:Cecum; D003106:Colon / Q000000981:diagnostic imaging; D003110:Colonic Neoplasms / Q000188:drug therapy*; D016503:Drug Delivery Systems; D005472:Fluorouracil / Q000008:administration & dosage*; D006801:Humans; D008297:Male; D010368:Pectins / Q000737:chemistry* / Q000493:pharmacokinetics*; D011877:Radionuclide Imaging; D051381:Rats; D012995:Solubility
D000970:Antineoplastic Agents; D002214:Capsules; D010368:Pectins; D005472:Fluorouracil; C003181:polygalacturonic acid