title: The development of Eudragit® NM-based controlled-release matrix tablets.
abstract: Eudragit® NM was investigated as a matrix former in combination with microcrystalline cellulose as an insoluble filler for preparing controlled-release tablets containing model drugs with different solubility.
  
  
  METHODS
  Three sets of matrix tablets differing in the drug-to-filler ratio (1:1, 2:1, and 4:1) and polymer amount with diltiazem hydrochloride (freely soluble) or caffeine (sparingly soluble) were prepared. Samples were evaluated by the dissolution test at pH 6.8 corresponding to the upper part of the small intestine; the selected samples were tested at a changing pH level to better simulate in vivo conditions.
  
  
  RESULTS
  The prepared matrix tablets fulfilled all the requirements of the European Pharmacopoeia. Tablets with Eudragit® NM showed excellent mechanical characteristics. In vitro studies showed that the set 1:1 was the most suitable for the sustained release of a freely soluble drug concerning the burst effect and the total drug amount released within 12 hours. The significant effect of the drug-to-filler ratio and polymer amount on the dissolution profile was confirmed by similarity factor analysis. A faster drug release was observed during the dissolution test within changing pH levels because of the pH-dependent solubility of diltiazem. A prolonged release of the sparingly soluble drug was not achieved, and a trend for fast disintegration was observed.
  
  
  CONCLUSIONS
  The combination of Eudragit®NM with microcrystalline cellulose as an insoluble filler seems to be suitable only for freely soluble drugs, when the amount of the drug and the filler is similar.
authors: Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, Czech Republic.
authors: Kateřina
authors: K
authors: Dvořáčková
authors: Rasa
authors: R
authors: Kalėdaitė
authors: Jan
authors: J
authors: Gajdziok
authors: Miloslava
authors: M
authors: Rabišková
authors: Martina
authors: M
authors: Bajerová
authors: Jan
authors: J
authors: Muselík
authors: Robertas
authors: R
authors: Lažauskas
authors: Rimantas
authors: R
authors: Pečiūra
authors: Jurga
authors: J
authors: Bernatonienė
mesh_terms: D002482:Cellulose / Q000737:chemistry*; D003692:Delayed-Action Preparations / Q000737:chemistry*; D015195:Drug Design; D011109:Polymethacrylic Acids / Q000737:chemistry*; D012995:Solubility; D013607:Tablets
chemical_list: D003692:Delayed-Action Preparations; D011109:Polymethacrylic Acids; D013607:Tablets; C038300:methylmethacrylate-methacrylic acid copolymer; D002482:Cellulose