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  • The aim of this study was to develop a multiple-unit dosage system that released model drug into the colon, and also to evaluate the efficiency of the dosage form in human volunteers. The developed system combines pH-, time and biodegradable polymer-based mechanisms for drug targeting to the colon. Pellet cores containing caffeine as model drug and chitosan and microcrystalline cellulose as excipients were prepared by the extrusion/spheronization method. The prepared pellets were film coated with a pH-dependent polymer, Eudragit FS 30 D. The coating total weight gain was 28.83 % (w/w). Thanks to the application of an outer enteric film and the multiple unit design of the dosage form, the variability in gastric emptying was overcome, and a colon-specific targeting relied on the reproducibility of a small intestinal transit time, which was reported to be 3 +- 1 hours. A biodegradable polymer in the pellet core, chitosan, ensured the site-specific release of the model drug due to its solubility at the lower pH of the colonic region and by its biodegradability from the bacteria present. The efficiency of the system was confirmed by the in vivo testing of human saliva. The time of the first appearance of caffeine into the saliva, Tlag, was used as a parameter to estimate the disintegration time of the pellets into the gastrointestinal tract. The caffeine appeared in the saliva within 6.95 +- 1.12 hours (Tlag) in 9 volunteers. A comparison of the reported colon arrival times indicates that the developed system is applicable to colonic drug delivery.
  • The aim of this study was to develop a multiple-unit dosage system that released model drug into the colon, and also to evaluate the efficiency of the dosage form in human volunteers. The developed system combines pH-, time and biodegradable polymer-based mechanisms for drug targeting to the colon. Pellet cores containing caffeine as model drug and chitosan and microcrystalline cellulose as excipients were prepared by the extrusion/spheronization method. The prepared pellets were film coated with a pH-dependent polymer, Eudragit FS 30 D. The coating total weight gain was 28.83 % (w/w). Thanks to the application of an outer enteric film and the multiple unit design of the dosage form, the variability in gastric emptying was overcome, and a colon-specific targeting relied on the reproducibility of a small intestinal transit time, which was reported to be 3 +- 1 hours. A biodegradable polymer in the pellet core, chitosan, ensured the site-specific release of the model drug due to its solubility at the lower pH of the colonic region and by its biodegradability from the bacteria present. The efficiency of the system was confirmed by the in vivo testing of human saliva. The time of the first appearance of caffeine into the saliva, Tlag, was used as a parameter to estimate the disintegration time of the pellets into the gastrointestinal tract. The caffeine appeared in the saliva within 6.95 +- 1.12 hours (Tlag) in 9 volunteers. A comparison of the reported colon arrival times indicates that the developed system is applicable to colonic drug delivery. (en)
Title
  • The Development and In Vivo Evaluation of a Colon Drug Delivery System Using Human Volunteers
  • The Development and In Vivo Evaluation of a Colon Drug Delivery System Using Human Volunteers (en)
skos:prefLabel
  • The Development and In Vivo Evaluation of a Colon Drug Delivery System Using Human Volunteers
  • The Development and In Vivo Evaluation of a Colon Drug Delivery System Using Human Volunteers (en)
skos:notation
  • RIV/62157124:16370/12:43871001!RIV13-MSM-16370___
http://linked.open...avai/predkladatel
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
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http://linked.open...iv/cisloPeriodika
  • 2
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http://linked.open...aciTvurceVysledku
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http://linked.open...iv/duvernostUdaju
http://linked.open...titaPredkladatele
http://linked.open...dnocenehoVysledku
  • 130733
http://linked.open...ai/riv/idVysledku
  • RIV/62157124:16370/12:43871001
http://linked.open...riv/jazykVysledku
http://linked.open.../riv/klicovaSlova
  • Colonic drug delivery, in vivo evaluation, caffeine, chitosan, Eudragit FS 30 D (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • GB - Spojené království Velké Británie a Severního Irska
http://linked.open...ontrolniKodProRIV
  • [5C71DEC765E4]
http://linked.open...i/riv/nazevZdroje
  • Drug Delivery
http://linked.open...in/vavai/riv/obor
http://linked.open...ichTvurcuVysledku
http://linked.open...cetTvurcuVysledku
http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 19
http://linked.open...iv/tvurceVysledku
  • Muselík, Jan
  • Vetchý, David
  • Štembírek, Jan
  • Zimová, Lucie
http://linked.open...ain/vavai/riv/wos
  • 000299745700001
issn
  • 1071-7544
number of pages
http://bibframe.org/vocab/doi
  • 10.3109/10717544.2011.644350
http://localhost/t...ganizacniJednotka
  • 16370
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