FORMULATION AND IN-VITRO EVALUATION OF GASTRO-RETENTIVE FLOATING TABLETS CONTAINING QUETIAPINE FUMARATE

Authors

  • P Poornima Jawaharlal Nehru Technological University, Kukatpally, Hyderabad-500072, Telangana, India
  • K Abbulu CMR College of Pharmacy, Kandlakoya (V), Medchal Road, Hyderabad-501401, Telangana, India
  • K Mukkanti Jawaharlal Nehru Technological University, Kukatpally, Hyderabad-500072, Telangana, India

Abstract

The present study was focused on Gastro-retentive tablets of Quetiapine fumarate using hydrophilic polymers HPMC K 250 PH PRM, HPMC K 750 PH PRM and HPMC K 1500 pH PRM as release retarding agents. WSR 301 was chosen as resin, Sodium bicarbonate was used as effervescent agents. FTIR studies revealed that there is no interaction between the drug and polymers used for the formulation. The tablets were prepared by direct compression method and the release rate was found to decrease with proportional increase in the ratio of polymer to drug. Quetiapine fumarate has good water solubility and is absorbed well from stomach and therefore is a very good drug to be formulated into gastro retentive floating dosage form. In-vitro release profile of Quetiapine fumarate and marketed product when compared, the optimized formulation F19 showed drug release of 98.61% within 24 h whereas 96.78% of the drug was released from the marketed product within 1h. The major mechanism of drug release follows zero order kinetics and non fickian transport by coupled diffusion and erosion. Such a formulation of Quetiapine fumarate with extended drug release over 24 hours probably is the best formulation for the treatment of Schizophrenia with only one oral tablet a day thus minimizing the side effects with low drug dose. The optimized formulation remained stable when subjected to accelerated stability studies.

Keywords:

Quetiapine Fumarate, Floating tablets, HPMC, Schizophrenia.

DOI

https://doi.org/10.25004/IJPSDR.2017.090605

References

1. Whitehead, L, Fell JT, Collett JH. Development of a Gastroretentive Dosage Form. European Journal of Pharmaceutical Sciences. 1996; 4 (1): 182.
2. Mojaverian P, Vlasses PH, Kellner PE, Rocci ML Jr. Effects of gender, posture and age on gastric residence time of an indigestible solid: pharmaceutical considerations. Pharm. Res. 1988; 5(10): 639–644.
3. Deshpande AA, Rhodes CT, Shah NH, Malick AW. Controlled release drug delivery system for prolonged gastric residence: an overview. Drug Dev. Ind. Pharm. 1996; 22(6): 531- 539.
4. Hwang SK, Park H, Park K. Gastric retentive drug delivery systems. Crit. Rev. Ther. Drug Carrier Syst. 1998; 15(3): 243–284.
5. Gruber P, Rubinstein A, Li VH, Bass P, Robinson JR. Gastric emptying of non-digestible solids in the fasted dog. J. Pharm. Sci. 1987; 76(2): 117–122.
6. Desai S, Bolton S. A Floating Controlled Release Drug Delivery System: In vitro–In vivo Evaluation. Pharma. Res. 1993; 10 (9):1321-1325.
7. Li S, Lin S, Chien TW, Daggy BP, Mirchandani HL. Statistical optimization of gastric floating system for oral controlled delivery of calcium. AAPS PharmSciTech. 2001; 2(1):E1.
8. Li S, Lin S, Daggy BP, Mirchandani HL, Chien TW. Effect of formulation variables on the floating properties of gastric floating drug delivery system. Drug Dev Ind Pharm. 2002; 28(7):783-793.
9. Martindale – The Complete Drug Reference -35th Edition, Chicago Pharmaceutical Press, London, 2007.
10. Rama Rao T, Bala Krishna K, Hussain MA, Anjum M, Azizurrahman M. Formulation and Evaluation of Gastroretentive Floating Tablets of Quetiapine Fumarate. RJPBCS. 2014; 5 (5): 380-389.
11. Nasrin N, Asaduzzaman M, Mowla R, Rizwan F, Alam A. A Comparative Study of Physical Parameters of Selected Ketorolac tromethamine tablets available in the Pharma Market of Bangladesh. Journal of Applied Pharmaceutical Science. 2008; 1(8): 101-103.
12. Penners G, Lustig K, Jorg PVG, inventors. Expandable pharmaceutical forms. US patent 5 651-985. July 29, 1997.
13. Phuapradit W, Bolton S. Influence of tablet density on oral absorption of sustained release acetaminophen matrix tablets. Drug Dev Ind Pharm. 1991; 17:1097-1107.
14. Phuapradit W. Influence of Tablet Buoyancy on Oral Absorption of Sustained Release Acetaminophen Matrix Tablets [dissertation]. [Thesis]. Jamaica, NY: St John’s University; 1989.
15. Małgorzata W, Marcin Z, Aleksandra A. Tasting cetirizine-based microspheres with an electronic tongue. Sensors and Actuators B Chemical. 2016; 238: 1190-1198.
16. Janssen M, Timur UT, Woike N, Welting TJ, Draaisma G, Gijbels M, van Rhijn LW, Mihov G, Thies J, Emans PJ. Celecoxib-loaded PEA microspheres as an auto regulatory drug-delivery system after intra-articular injection. J Control Release. 2016 Dec 28; 244(Pt A):30-40.
17. Tyagi LK, Kori ML. Stability Study and In-vivo Evaluation of Lornoxicam Loaded Ethyl Cellulose Microspheres. Int. J. Pharm. Sci. Drug Res. 2014; 6(1): 26-30.
18. Singh K, Kumar A, Langyan N, Ahuja M . Evaluation of mimosa pudica seed mucilage as sustained-release excipient. AAPS PharmSciTech 2009; 10: 1121-1127.
19. Peppas NA Analysis of Fickian and non-Fickian drug release from polymers. Pharm ActaHelv. 1985; 60: 110-111.
20. Siepmann J, Kranz H, Bodmeier R, Peppas NA. HPMC-matrices for controlled drug delivery: a new model combining diffusion, swelling, and dissolution mechanisms and predicting the release kinetics. Pharm Res. 1999; 16: 1748-1756.

Published

01-11-2017
Statistics
Abstract Display: 456
PDF Downloads: 485
Dimension Badge

How to Cite

“FORMULATION AND IN-VITRO EVALUATION OF GASTRO-RETENTIVE FLOATING TABLETS CONTAINING QUETIAPINE FUMARATE”. International Journal of Pharmaceutical Sciences and Drug Research, vol. 9, no. 6, Nov. 2017, pp. 315-22, https://doi.org/10.25004/IJPSDR.2017.090605.

Issue

Section

Research Article

How to Cite

“FORMULATION AND IN-VITRO EVALUATION OF GASTRO-RETENTIVE FLOATING TABLETS CONTAINING QUETIAPINE FUMARATE”. International Journal of Pharmaceutical Sciences and Drug Research, vol. 9, no. 6, Nov. 2017, pp. 315-22, https://doi.org/10.25004/IJPSDR.2017.090605.