title: Preparation and evaluation of pectin-based colon-specific pulsatile capsule in vitro and in vivo.
abstract: The purpose of this study was to develop and evaluate a colon-specific, pulsatile drug delivery system, which consists of an impermeable capsule body filled with a 5-aminosalicylic acid rapid-disintegrating tablet and a pectin-based erodible plug placed in the opening of the capsule body. To obtain an appropriate gel-forming ability and suitable lag time for the colon-specific drug delivery, high-methoxy pectin (HM-pectin) was formulated with lactose and lowmethoxy pectin (LM-pectin) with HPMC to prepare the plug tablet. In order to evaluate the lag time, prior to the rapid drug release, both the formulation of the plug tablet and in vitro release medium were studied. The lag time prior to the rapid drug release was mainly determined by the HM-pectin/lactose or LM-pectin/HPMC ratio. The addition of pectinase or rat cecal content into the release medium shortened the lag time significantly, which predicted the probable enzyme sensitivity of pectin plug tablet. In vivo studies showed that the plasma concentration of drug can only be detected 6h after oral administration of the pulsatile capsule, which indirectly proved the colon-specific characteristics. These results show that the pulsatile capsule may have the therapeutic action for colon-specific drug delivery.
authors.affiliation: Chongqing Key Laboratory of Biochemistry & Molecular Pharmacology, School of pharmacy, Chongqing medical university, Chongqing 400016, China.
authors.forename: Jing
authors.initials: J
authors.lastname: Liu
authors.forename: Liangke
authors.initials: L
authors.lastname: Zhang
authors.forename: Yuntao
authors.initials: Y
authors.lastname: Jia
authors.forename: Wenjing
authors.initials: W
authors.lastname: Hu
authors.forename: Jingqing
authors.initials: J
authors.lastname: Zhang
authors.forename: Huiming
authors.initials: H
authors.lastname: Jiang
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000493:pharmacokinetics; D002214:Capsules; D003106:Colon / Q000378:metabolism*; D004285:Dogs; D016503:Drug Delivery Systems; D005079:Excipients / Q000737:chemistry; D005260:Female; D005782:Gels; D065347:Hypromellose Derivatives; D066298:In Vitro Techniques; D007785:Lactose / Q000737:chemistry; D008297:Male; D019804:Mesalamine / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D010368:Pectins / Q000737:chemistry*; D020551:Pulse Therapy, Drug; D051381:Rats; D017207:Rats, Sprague-Dawley; D013607:Tablets; D013997:Time Factors
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D002214:Capsules; D005079:Excipients; D005782:Gels; D013607:Tablets; D065347:Hypromellose Derivatives; D019804:Mesalamine; D010368:Pectins; D008747:Methylcellulose; D007785:Lactose