Investigation of the Biopharmaceutical Behavior of Theophylline Hydrophilic Matrix Tablets Using USP Methods and an Artificial Digestive System

This work aimed to investigate the biopharmaceutical behavior of hydrophilic matrix tablets of theophylline using different in vitro methods: USP II, USP IV, and a novel in vitro system simulating the gastrointestinal tract in man called the artificial digestive system (ADS). The potentiality of each method was evaluated by establishing in vitro/in vivo correlation. Using USP methods, the drug release was pH-independent and dependent on agitation intensity. Level A IVIVCs could be established using the different in vitro methods but one to one correlation was established only when the ADS method was used. For the prediction of in vivo drug dosage form behavior based on in vitro methods, the ADS showed a high predictability when compared to USP in vitro methods.

[1]  Eric Beyssac,et al.  A level A in vitro/in vivo correlation in fasted and fed states using different methods: applied to solid immediate release oral dosage form. , 2006, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

[2]  Melia Cd.  Hydrophilic matrix sustained release systems based on polysaccharide carriers. , 1991 .

[3]  M Alpsten,et al.  In vitro and in vivo erosion of two different hydrophilic gel matrix tablets. , 1998, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[4]  Scintigraphic study of the gastro-intestinal transit and correlations with the drug absorption kinetics of a sustained release theophylline tablet: I. Administration in fasting state , 1988 .

[5]  W. Bartoli,et al.  Gastric emptying of water and isocaloric carbohydrate solutions consumed at rest. , 1994, Medicine and science in sports and exercise.

[6]  S. Baumgartner,et al.  Quantitative evaluation of polymer concentration profile during swelling of hydrophilic matrix tablets using 1H NMR and MRI methods. , 2005, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[7]  M. Alric,et al.  Living recombinant Saccharomyces cerevisiae secreting proteins or peptides as a new drug delivery system in the gut. , 2004, Journal of biotechnology.

[8]  J. Leiper,et al.  Comparison of aspiration and scintigraphic techniques for the measurement of gastric emptying rates of liquids in humans. , 1992, Gut.

[9]  Christos Reppas,et al.  Dissolution Testing as a Prognostic Tool for Oral Drug Absorption: Immediate Release Dosage Forms , 2004, Pharmaceutical Research.

[10]  J. Maublant,et al.  Scintigraphic study of the gastro-intestinal transit of a sustained release theophylline tablet. II. Administration in non-fasting state , 1991 .

[11]  R. Löbenberg,et al.  Evaluation of Various Dissolution Media for Predicting In Vivo Performance of Class I and II Drugs , 1998, Pharmaceutical Research.

[12]  I. Khan,et al.  Dissolution testing for sustained or controlled release oral dosage forms and correlation with in vivo data: Challenges and opportunities , 1996 .

[13]  B. D. Rohera,et al.  Comparative evaluation of rate of hydration and matrix erosion of HEC and HPC and study of drug release from their matrices. , 2002, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

[14]  M. Sleisenger,et al.  Protein digestion and absorption in human small intestine. , 1979, Gastroenterology.

[15]  Monique Alric,et al.  A Dynamic Artificial Gastrointestinal System for Studying the Behavior of Orally Administered Drug Dosage Forms Under Various Physiological Conditions , 2004, Pharmaceutical Research.

[16]  Philippe Marteau,et al.  A Multicompartmental Dynamic Computer-controlled Model Simulating the Stomach and Small Intestine , 1995 .