Abstract
Present study attempts to overcome pH-dependent solubility, a limitation for oral delivery of poorly soluble BCS class-II drugs. A pH independent, patient compliant, dual working gastroretentive drug delivery system of model drug quetiapine fumarate (QF) was fabricated by unique combination approach of mucoadhesion and floating. Bilayer tablets comprising floating adhesive layer (FL) and matrix layer (ML) was systematically optimized by applying 32 full factorial experimental designs. Selected variables for FL: Polyox® 303WSR (X1FL) and alginate beads (X2FL), and for ML: HPMC K100M (X1ML) and fumaric acid (X2ML) were studied against responses for FL: floating lag time (R1FL), total floating time (R2FL) and adhesion force (R3FL) and for ML: percentage drug released at 2 h—Q2h (R1ML), 8 h—Q8h (R2ML), and 18 h—Q18h (R3ML), respectively. Optimized batch (OP) showed floating lag time (6.5 h), total floating time (14 h), adhesion force (0.82 N) and Q18h (>90 %). Pharmacokinetic study of OP and immediate release market product demonstrated improved bioavailability (~12 % higher AUC0–∞) of OP. In a nutshell, developed drug delivery system can be fabricated as a platform for QF and similar BCS class-II drugs with pH dependent solubility.
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Ahmed I, Ayres J (2007) Bioavailability of riboflavin from a gastric retention formulation. Int J Pharm 330(1–2):146–154
Al Remawia M, Al-akayleh F, Salem M, Al Shami M, Badwan A (2013) Application of excipient made from Chitosan-Xanthan as a single component for the controlled release of ambroxol tablet. J Excipients Food Chem 4(2):48–57
Awasthi R, Kulkarni GT (2014) Development of novel gastroretentive drug delivery system of gliclazide: hollow beads. Drug Dev Ind Pharm 40(3):398–408
Bomma R, Swamy Naidu R, Yamsani M, Veerabrahma K (2009) Development and evaluation of gastroretentive norfloxacin floating tablets. Acta Pharm 59(2):211–221
Chinthala S, Reddy K, Hadassah M, Metilda E, Sridevi S (2012) Formulation and evaluation of gastroretentive floating tablets of gabapentin using effervescent technology. Int J Pharm Biomed Res 3(4):202–208
Dash S, Murthy P, Nath L, Chowdhury P (2010) Kinetic modeling on drug release from controlled drug delivery systems. Acta Pol Pharm 67(3):217–223
Fassihi R, Ritschel W (1993) Multiple-layer, direct-compression, controlled-release system: in vitro and in vivo evaluation. J Pharm Sci 82(7):750–754
Gohel M, Parikh R, Aghara P, Nagori S, Delvadia R, Dabhi M (2009) Application of simplex lattice design and desirability function for the formulation development of mouth dissolving film of salbutamol sulphate. Curr Drug Deliv 6(5):486–494
ICH (2005) Q2(R1): validation of analytical procedures: text and methodology. In: ICH harmonised tripartite guideline international conference on harmonisation of technical requirements for registration of pharmaceuticals for human use
Jagdale S, Agavekar A, Pandya S, Kuchekar B, Chabukswar A (2009) Formulation and evaluation of gastroretentive drug delivery system of propranolol hydrochloride. AAPS PharmSciTech 10(3):1071–1079
Korsmeyer R, Gurny R, Doelker E, Buri P, Peppas N (1983) Mechanism of solute release from porous hydrophilic polymers. Int J Pharm 15(1):25–35
Krishnan V, Sasikumar S, Dass F, Vijayaraghavan R (2010) Effect of pore forming agents on the physical characteristics and release kinetics of levofloxacin hemihydrate from floating alginate drug delivery system—an in vitro study. Trends Biomater Artif Organs 24(3):139–145
Lohani S, Balkrishnan A, Bak A (2015) Selecting candidates with optimal oral exposure: the role of physicochemical and DMPK properties. AAPS Newsmagazine 18(3):36–37
Mehta DM, Shelat PK, Paejiya PB, Patel AJ, Barot BS (2011) Investigations of Plantago ovata husk powder as a disintegrating agent for development of famotidine tablets. Int J Pharm Sci Nanotech 4(2):1412–1417
Mehta DM, Paejiya PB, Barot BS, Shelat PK (2012) Investigation of the drug release modulating effect of acidifiers in modified release oral formulation of cinnarizine. Asian J Pharm Sci 7(3):193–201
Mehta DM, Parejiya PB, Barot BS, Suthar DD, Shelat PK (2013) Polyethylene oxide based pH-independent drug delivery system: formulation and optimization by central composite design. Drug Deliv Lett 3(3):220–232
Mehta DM, Parejiya PB, Patel HK, Shelat PK (2015) Development and validation of RP-HPLC method for determination of quetiapine fumarate in rabbit plasma. J Chem Pharm Res 7(11):773–777
Moore JW, Flanner HH (1996) Mathematical comparison of curves with an emphasis on in vitro dissolution profiles. Pharm Tech 20(6):64–74
Patel V, Prajapati B, Patel H, Patel K (2007) Mucoadhesive bilayer tablets of propranolol hydrochloride. AAPS PharmSciTech 8(3):E77
Peppas N (1985) Analysis of Fickian and non-Fickian drug release from polymers. Pharm Acta Helv 60(4):110–111
Prajapati S, Patel L, Patel D (2008) Gastric floating matrix tablets: design and optimization using combination of polymers. Acta Pharm 58(2):221–229
Reddy S, Satyanarayana P, Varma K, Raju N, Kumar S, Shanmugasundaram P (2011) Novel reverse phase HPLC method development and validation of quetiapine fumerate in bulk and tablet dosage form. Int J Pharm Ind Res 1(2):95–99
Singh B, Kim K (2000) Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention. J Control Release 63(3):235–259
Sinko PJ (2006) Martin’s physical pharmacy and pharmaceutical sciences: physical chemical and biopharmaceutical principles in the pharmaceutical sciences. Lippincott Williams & Wilkins, Philadelphia
Sonar G, Rao M, Mandsaurwale R, Vanshiv S (2009) Bioadhesive-floating matrix tablet of salbutamol sulphate using response surface methodology: optimization and in vitro evaluation. J Pharm Res 2(5):908–914
Streubel A, Siepmann J, Bodmeier R (2006) Drug delivery to the upper small intestine window using gastroretentive technologies. Curr Opin Pharmacol 6(5):501–508
USFDA (OGD) (2015) Dissolution methods. http://www.accessdata.fda.gov/scripts/cder/dissolution/. Accessed 25 Sep 2015
Varshosaz J, Tavakoli N, Roozbahani F (2006) Formulation and in vitro characterization of ciprofloxacin floating and bioadhesive extended-release tablets. Drug Deliv 13(4):277–285
Velhal A, Mirajkar S, Kuril V, Raghavan V, Deshpanday N (2011) Sustained release pharmaceutical compositions comprising quetiapine. US Patent US20110151002, p A1
Acknowledgments
The authors (D. M. Mehta, P. J. Parejiya, H. K. Patel, P. J. Trivedi, D. D. Suthar, P. K. Shelat) declare that they have no conlfict of interest. This work is a part of research project assisted by the INSPIRE Programme division (Department of Science and Technology—DST, Government of India, New Delhi). The authors are thankful to the DST for the same.
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Mehta, D.M., Parejiya, P.B., Patel, H.K. et al. Design, optimization and pharmacokinetics of novel prolonged gastroretentive drug delivery system of quetiapine fumarate. Journal of Pharmaceutical Investigation 46, 453–465 (2016). https://doi.org/10.1007/s40005-016-0237-0
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DOI: https://doi.org/10.1007/s40005-016-0237-0