optimization of extended zero-order release gliclazide tablets using D-optimal mixture design.

The objective of this study was to develop and optimize the gliclazide extended-release formulations by using simultaneously combination of two hydrophilic polymers: HPMC K 15M and sodium alginate as retardant. D-Optimal mixture design was employed to evaluate the effect of HPMC (X(1)), lactose (X(2)), and sodium alginate (X(3)) concentrations on the release rate of gliclazide from the matrices. The drug release percent at 3, 6, 9 and 12 h were the target responses and were restricted to 20-30, 45-55, 70-80 and 90-100%, respectively. Response surface methodology and multiple response optimization utilizing the polynomial equation were used to search for the optimal formulation with specific release rate at different time intervals. Validation of the optimization study indicated high degree of prognostic ability of response surface methodology. The mechanism of drug release from optimized extended-release matrix tablets was followed by the zero-order release pattern. This study demonstrated that D-optimal mixture experimental design facilitated the formulation and optimization of extended release hydrophilic matrix systems of gliclazide.

[1]  L. Chan,et al.  Investigation of the influence of mean HPMC particle size and number of polymer particles on the release of aspirin from swellable hydrophilic matrix tablets. , 2001, Journal of controlled release : official journal of the Controlled Release Society.

[2]  J. Crison,et al.  A Theoretical Basis for a Biopharmaceutic Drug Classification: The Correlation of in Vitro Drug Product Dissolution and in Vivo Bioavailability , 1995, Pharmaceutical Research.

[3]  Nicholas A. Peppas,et al.  A simple equation for description of solute release II. Fickian and anomalous release from swellable devices , 1987 .

[4]  T. Ohmura,et al.  Influence of physical factors in gastrointestinal tract on acetaminophen release from controlled-release tablets in fasted dogs , 1996 .

[5]  M. Khan,et al.  Optimization and characterization of controlled release multi-particulate beads coated with starch acetate. , 2005, International journal of pharmaceutics.

[6]  H. Tønnesen,et al.  Alginate in Drug Delivery Systems , 2002, Drug development and industrial pharmacy.

[7]  Matthew Roberts,et al.  The use of hypromellose in oral drug delivery , 2005, The Journal of pharmacy and pharmacology.

[8]  Ping I. Lee,et al.  Probing the Mechanisms of Drug Release from Hydroxypropylmethyl Cellulose Matrices , 1994, Pharmaceutical Research.

[9]  G. V. Patil,et al.  Release modulating hydrophilic matrix systems of losartan potassium: optimization of formulation using statistical experimental design. , 2007, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[10]  D. L. Massart,et al.  Itraconazole Formulation Studies of the Melt-Extrusion Process with Mixture Design , 2003, Drug development and industrial pharmacy.

[11]  J. Nunthanid,et al.  Alginate-based pellets prepared by extrusion/spheronization: a preliminary study on the effect of additive in granulating liquid. , 2007, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[12]  J. L. Gómez-Amoza,et al.  Atenolol release from hydrophilic matrix tablets with hydroxypropylmethylcellulose (HPMC) mixtures as gelling agent: effects of the viscosity of the HPMC mixture , 1996 .

[13]  Connie M. Borror,et al.  Mixture and mixture–process variable experiments for pharmaceutical applications , 2004 .

[14]  Y. Tsai,et al.  Optimization of sustained-release propranolol dosage form using factorial design and response surface methodology. , 2004, Biological & pharmaceutical bulletin.

[15]  M. Tuttle,et al.  Controlled release of water-soluble macromolecules from bioerodible hydrogels. , 1983, Biomaterials.

[16]  Chee Peng Lim,et al.  Use of Artificial Neural Networks to Predict Drug Dissolution Profiles and Evaluation of Network Performance Using Similarity Factor , 2000, Pharmaceutical Research.

[17]  Gao Li,et al.  Optimization of the preparation of nalmefene-loaded sustained-release microspheres using central composite design. , 2006, Chemical & pharmaceutical bulletin.

[18]  R Jochemsen,et al.  Complete bioavailability and lack of food‐effect on pharmacokinetics of gliclazide 30 mg modified release in healthy volunteers , 2002, Biopharmaceutics & drug disposition.