Formulation and evaluation of taste masking sachets containing quetiapine fumarate
Quetiapine fumarate is a tetracyclic piperazino-azepine antidepressant agent. It is given with a dose of 15-45mg orally once a day. The absorption of this drug is rapid and complete. Due to first pass metabolism in the liver and metabolism in the gut wall, absolute bioavailability is about 50%. Peak blood concentrations are attained within about 2 hours after an oral dose. This leads to lower bioavailability of Quetiapine fumarate also having bitter taste. So to improve its bioavailability and to mask the taste solid dispersion technique was used using different carriers like PEG 6000, & Poloxamer. Results of prepared taste masking sachets by solid dispersion technique of Quetiapine fumarate by Fusion method & kneading method were discussed which includes solubility, drug content uniformity, and in vitro dissolution studies. Characterization in solid state was done by FT-IR studies. Finally by comparing all the formulations i.e., F1-F12 containing Quetiapine fumarate, Poloxamer and PEG 6000 in different ratios, Invitro drug release of Quetiapine fumarate with PEG 6000 in 1:3 by Fusion method shows 98.62% drug release at the end of 60mins. By comparing the release kinetics studies of best formulation of Quetiapine fumarate with zero order and first order we can say that the best formulation follows Zero order release kinetics studies.
Bauer M, Pretorius H, Constant E, Earley W, Szamosi J, Brecher M. Extended release quetiapine as adjunct to an antidepressant in patients with major depressive disorder: results of a randomized, placebo-controlled, double-blind study. J Clin Psychiatry. 2009;70:540-549.
El-Khalili N, Joyce M, Atkinson S, Buynak R, Datto C, Lindgren P, Eriksson H, Brecher M. Adjunctive extended release quetiapine fumarate (quetiapine XR) in patients with major depressive disorder and inadequate antidepressant response. Poster presented at: the 161st Annual Meeting of the American Psychiatric Association; May 3-8, 2008; Washington, DC
Brahmankar D. M., Jaiswal S.B., “Biopharmaceutics & Pharmaceutics”; First Edition, 1995, PP 335.
Watanabe Y., Ishikawa Y., Utoguchi N. and Matsumoto M., “Preparation and evaluation of tablets rapidly disintegrating in saliva containing bitter taste masked granules by the compression method”, Chem. Pharm. Bull., 1999, 47, PP 1451- 1457.
Sk. Benajeer et al. New Simple UV Spectrophotometric Method for Determination of Mirtazapine in Bulk and pharmaceutical dosage forms. International Journal of Pharma Sciences and Research (IJPSR) Vol 3 No 10 Oct 2012.
Karaşen, N & Altinöz, S. (2001). Determination of mirtazapine in tablets by UV spectrophotometric and derivative spectrophotometric methods. Journal of pharmaceutical and biomedical analysis. 24. 11-7.
Yajima T., Fukushima Y., Itai S., Kawashima K. Method of evaluation of the bitterness of clarithromycin dry syrup. Chem. Pharm. Bull. 2002;50:147–152. doi: 10.1248/cpb.50.147.
Gabriels M., Plaizier-Vercammen J. Design of a dissolution system for the evaluation of the release rate characteristics of artemether and dihydroartemisinin form tablets. Int. J. Pharm. 2004;274:245–260.
Liu C., Desai K. G. H., Liu C., Park H. J. Enhancement of dissolution rate of rofecoxib using solid dispersions with urea. Drug. Dev. Res. 2004;63:181–189.
Gohel M., Patel M., Amin A., Agrawal R., Dave R., Bariya N. Formulation, design and optimisation of mouth dissolve tablets of nimesulide using vacuum drying technique. AAPS PharmSciTech. 2004;5.
Roy GM: Taste masking in oral pharmaceuticals. Pharm. Tech. 1994; 18: 84‐99).
T.hayashida & M.Hatayama,”Carbohydrates as taste masking agents for oriental to drugs”, in JP 05 17,372 to Yoshitomi Pharmaceutical IndustriesLtd. (1993).
Chauhan B, Shimpi S, Paradkar A. Preparation and characterization of etoricoxib solid dispersions using lipid carriers by spray drying technique. AAPS Pharm Sci Tech 6 (3) (2005) 405-412.
Higuchi T. Mechanism of sustained action medication. Theroetical analysis of rate of release of solid drugs dispersed in solid matrices. J Pharm Sci 1963; 51: 1145-9.
Peppas NA. Analysis of Fickian and non-fickian drug release from polymer. Pharm Acta Helv 1985; 60: 110-11.
Marabathuni VJ, Dinesh P, Ravikumar R, Yamini P, Kiran PS, Hussain SP, Rao CM. Chitosan based sustained release mucoadhesive buccal patches containing amlodipine besylate (AMB). Asian J Res Pharm Sci. 2017 Jun 28;7:97-104.
Marabathuni VJ, Bhavani M, Lavanya M, Padmaja K, Madhavi N, Babu P, Rao CM. Formulation and evaluation of mouth dissolving Tablets of carbamazepine. Asian Journal of Pharmacy and Technology. 2017;7(3):137-43.
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