Application of a colon delivery capsule to 5-aminosalicylic acid and evaluation of the pharmacokinetic profile after oral administration to beagle dogs

Journal of Drug Targeting
T TakayaK Takada

Abstract

Pressure-controlled colon delivery capsule (PCC) containing 5-aminosalicylic acid (5-ASA) for the treatment of inflammatory bowel disease (IBD) was prepared and evaluated by an in vivo experiment using beagle dogs. As a reference drug, sulfasalazine (SASP), prodrug of 5-ASA, was used as a plain gelatin capsule preparation. After the oral administration of SASP at the does of 25.0 mg/kg, the mean time when the plasma 5-ASA concentration reaches to its maximum (Tmax) was 9.0 hr. In the case of 5-ASA administered in PCC, at the doses of 12.5 and 25.0 mg/kg, Tmaxs were 5.3 and 5.3 hr, respectively. Although the time for the first appearance of 5-ASA into the systemic circulation was almost the same value between SASP capsule and PCC containing 5-ASA, longer Tmax was observed from SASP capsule than from PCC. These results suggest that this 5-ASA preparation would be an useful dosage form for the therapy of IBD from the point of avoiding the side effect of sulfapyridine, one of the metabolites of SASP.

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Citations

May 15, 2013·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·F TalaeiA Saadatzadeh
Jun 4, 2013·International Journal of Pharmaceutics·Alessandra MaroniAndrea Gazzaniga
Aug 1, 1998·Journal of Controlled Release : Official Journal of the Controlled Release Society·T TakayaK Takada
Aug 1, 1998·Journal of Controlled Release : Official Journal of the Controlled Release Society·M MuraokaK Takada
Nov 5, 1998·Journal of Controlled Release : Official Journal of the Controlled Release Society·Z HuK Takada
Nov 16, 2002·International Journal of Pharmaceutics·Masataka KatsumaMuneo Fukui
Mar 15, 2003·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Q X CaiL P Gao
Aug 13, 2013·Expert Opinion on Drug Delivery·Takayuki YoshidaKazuhiro Sako
Dec 24, 2013·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Lisa WildeWerner Weitschies
May 9, 2001·The Journal of Pharmacy and Pharmacology·N ShibataK Takada
Nov 24, 2004·Advanced Drug Delivery Reviews·David R Friend
Oct 21, 1999·The Journal of Pharmacy and Pharmacology·Y YoshikawaK Takada
Oct 16, 2002·World Journal of Gastroenterology : WJG·Yi-Nuo PangZhi-Rong Zhang

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