Film coated tablets (ColoPulse technology) for targeted delivery in the lower intestinal tract: Influence of the core composition on release characteristics

Autor: Frans Stellaard, Jos G. W. Kosterink, R.C.A. Schellekens, Jan H. Baltink, Henderik W. Frijlink, Herman J. Woerdenbag, Ellen M. Woesthuis
Přispěvatelé: Pharmaceutical Technology and Biopharmacy, Guided Treatment in Optimal Selected Cancer Patients (GUTS), Biopharmaceuticals, Discovery, Design and Delivery (BDDD), Targeted Gynaecologic Oncology (TARGON)
Rok vydání: 2010
Předmět:
Water uptake
eudragit
Chemistry
Pharmaceutical
Pharmaceutical Science
Lower Gastrointestinal Tract
magnesium stearate
chemistry.chemical_compound
Drug Delivery Systems
Coating
drug delivery system
Organic chemistry
Magnesium stearate
glucose
Disintegration
starch glycolate sodium
Mesalamine
drug release
silicon dioxide
benzoic acid
povidone
Anti-Inflammatory Agents
Non-Steroidal
article
tablet disintegration
General Medicine
Hydrogen-Ion Concentration
alpha lactose
cellulose
Microcrystalline cellulose
priority journal
Pharmaceutical Preparations
croscarmellose sodium
mesalazine
Sodium benzoate
Tablets
Enteric-Coated
microcrystalline cellulose
Algorithms
water transport
Materials science
copper sulfate
Colon delivery
Colon
Film coating
Color
bicarbonate
engineering.material
Excipients
Polymethacrylic Acids
Suspensions
Hardness
Humans
delayed release formulation
Cellulose
intestine
Croscarmellose sodium
Water transport
Reproducibility of Results
citric acid
Pulsatile delivery
Solubility
chemistry
Chemical engineering
medical technology
engineering
Zdroj: Pharmaceutical development and technology, 17(1), 40-47
ISSN: 1097-9867
1083-7450
DOI: 10.3109/10837450.2010.513986
Popis: The design of a film coating technology which allows a tablet to deliver the drug in the ileocolonic segment would offer new treatment possibilities. The objective is to develop a platform technology that is suitable for a broad range of drug compounds. We developed a coated tablet with a delayed, pulsatile release profile based on a pH-sensitive coating technology (ColoPulse). The production process was validated, and the effect of core composition on the in vitro release and water uptake investigated. The release profile of the standard tablet core composition, based on the use of cellulose as a filler, was independent of the coat thickness in a range of 9.013.2mg/cm2. The release profile of a coated tablet was strongly influenced when cellulose was partly replaced by the model substance glucose (loss of sigmoidal release), citric acid (stabilization), sodium bicarbonate (destabilization) or sodium benzoate (destabilization). The film coating takes up water when below the pH-threshold. However, this did not cause early disintegration of the coating. The ColoPulse technology is successfully applied on tablets. The in vitro release characteristics of the coated tablets are influenced by the composition of the core. © 2012 Informa Healthcare USA, Inc.
Databáze: OpenAIRE
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