• Abhisek Pal


Objective: Seroquel is an antipsychotic drug with plasma half-life of 6 hrs and poor oral bioavailability (9%) due to extensive first-pass
metabolism. A present work is an attempt to improve oral bioavailability of seroquel by solid dispersions (SDs) (to improve the aqueous
solubility and dissolution rate) so as to facilitate faster onset of action. Seroquel is a biopharmaceutical classification system Class II drug having
low solubility (1.28 µg/ml).
Methods: In the present investigation, an attempt was made to prepare SD with water-soluble carriers like polyethylene glycol (PEG 6000) PEG 6000
and PEG 4000. The SDs were prepared by melting method and physical mixing method by using PEG 6000 and PEG 4000 in the ratio 1:1, 1:3 and
1:5 respectfully. The prepared dispersions were evaluated for their physicochemical and dissolution characteristics. All the dispersions were easy to
prepare, and the powder mass obtained in various formulations were free flowing under dry conditions. Physicochemical properties of the products
were characterized by Fourier infrared spectroscopy which reveals that there is no interaction between drug and polymer. In vitro dissolution
profiles of Seroquel formulations of physical mixtures (PMs) and melting methods were studied using Lab India Disso 2000 dissolution apparatus
employing paddle method. 500 ml of 6.2 phosphate buffer was used as dissolution medium maintained at 37±0.50°C, and the stirrer rotation was
kept at 50 rpm. Aliquots were withdrawn at different time intervals and measured for the absorbance for Seroquel at 244 nm using ultra violet-visible
spectrophotometer with a reference to suitably constructed standard plot.
Results and Discussions: Mixture of drug:PEG 6000 in (1:3) ratio prepared by melting method gives the highest drug release (93.55%) than PM
(88.12%) and pure drug (39.75%) in 60 minutes. The dissolution of all the preparation follows Higuchi order kinetics.
Conclusion: It is concluded that in melting method, due to the fineness, amorphous state of the drug, particle size reduction and absence of aggregation,
dissolution rate increases but in PMs only a marginal increase in dissolution rate because the size reduction process is not effective.
Keywords: Dissolution, Solid dispersion, Seroquel.



Sweetman SC. Martindale, the Complete Drug Reference. 35


London, UK: Pharmaceutical Press; 2007.

Moore MD, Wildfong PL. Aqueous solubility enhancement through

engineering of binary solid composites: Pharmaceutical applications.

J Pharm Innov 2009;4(1):36-49.

Jinno J, Kamada N, Miyake M, Yamada K, Mukai T, Odomi M, et al.

Effect of particle size reduction on dissolution and oral absorption of a

poorly water-soluble drug, cilostazol, in beagle dogs. J Control Release


Bansal K, Pant P, Rao PR, Padhee K, Sathapathy A, Kochhar PS.

Micronization and dissolution enhancement of norethindrone. Int J Res

Pharm Chem 2011;1(3):315-9.

Habib MJ. Historical background of solid dis person. In: Pharmaceutical

Solid Dispersion Technology. Lancaster, USA, PA: Technomic

Publishing Company, Inc.; 2001. p. 17604, 2-3.161.

Debuigne F, Cuisenaire J, Jeunieau L, Masereel B, Nagy JB. Synthesis

of nimesulide nanoparticles in the microemulsion epikuron/isopropyl

myristate/water/n-butanol (or isopropanol). J Colloid Interface Sci


Jacobs C, Kayser O, Müller RH. Production and characterisation of

mucoadhesive nanosuspensions for the formulation of bupravaquone.

Int J Pharm 2001;214(1-2):3-7.

Kayser O, Olbrich C, Yardley V, Kiderlen AF, Croft SL. Formulation of

amphotericin B as nanosuspension for oral administration. Int J Pharm


Kocbek P, Baumgartner S, Kristl J. Preparation and evaluation of


nanosuspensions for enhancing the dissolution of poorly soluble drugs.

Int J Pharm 2006;312(1-2):179-86.

Liversidge GG, Conzentino P. Drug particle size reduction for

decreasing gastric irritatancy and enhancing absorption of naprxen in

rats. Int J Pharm 1995;125(2):309-13.

Sharma D. A review on innovative approaches to enhance solubility

and dissolution rate of hydrophobic drugs. Novel Sci Int J Pharm Sci


Sanghvi R, Evans D, Yalkowsky SH. Stacking complexation by

nicotinamide: A useful way of enhancing drug solubility. Int J Pharm


Loftsson T, Brewster ME. Pharmaceutical applications of

cyclodextrins 1. Drug solubilization and stabilization. J Pharm Sci


Podlogar F, Gasperlin M, Tomsic M, Jamnik A, Rogac MB. Structural

characterisation of water–Tween 40/Imwitor 308–isopropyl myristate

microemulsions using different experimental methods. Int J Pharm


Serajuddin AT. Salt formation to improve drug solubility. Adv Drug

Deliv Rev 2007;59(7):603-16.

Murali Mohan Babu GV, Prasad ChD, Ramana Murthy KV. Evaluation

of modified gum karaya as carrier for the dissolution enhancement of

poorly water-soluble drug nimodipine. Int J Pharm 2002;234(1-2):1-17.

Keck CM, Müller RH. Drug nanocrystals of poorly soluble drugs

produced by high pressure homogenisation. Eur J Pharm Biopharm


Salvadori B, Capitani G, Mellini M, Dei L. A novel method to

prepare inorganic water-soluble nanocrystals. J Colloid Interface Sci


Sekiguchj K, Obi N. Studies on absorption of eutectic mixture. I.

A comparison of the behavior of eutectic mixture of sulfathiazole

and that of ordinary sulfathiazole in man. Chem Pharm Bull


Dhirendra K, Lewis S, Udupa N, Atin K. Solid dispersions: A review.

Pak J Pharm Sci 2009;22:234-46.

Shinde S.S, Patil M. V, Amol S. Solid Dispersions of Poorly Water

Soluble Drug Using Spray Drying Technique. Int J Drug Del 2013;


Serajuddin AT. Solid dispersion of poorly water-soluble drugs: Early

promises, subsequent problems, and recent breakthroughs. J Pharm Sci


Chiou WL, Riegelman S. Pharmaceutical applications of solid

dispersion systems. J Pharm Sci 1971;60(9):1281-302.

Patel M, Tekade A, Gattani S, Surana S. Solubility enhancement

of lovastatin by modified locust bean gum using solid dispersion

techniques. AAPS Pharm Sci Tech 2008;9(4):1262-9.

Gupta P, Bansal AK. Spray drying for generation of a ternary

amorphous system of celecoxib, PVP, and meglumine. Pharm Dev

Technol 2005;10(2):273-81.

Chauhan B, Shimpi S, Paradkar A. Preparation and evaluation of

glibenclamide-polyglycolized glycerides solid dispersions with silicon

dioxide by spray drying technique. Eur J Pharm Sci 2005;26(2):219-30.

Paradkar A, Ambike AA, Jadhav BK, Mahadik KR. Characterization of

curcumin-PVP solid dispersion obtained by spray drying. Int J Pharm


Broadhead J, Edmond Rouan SK, Rhodes CT. The spray drying of

pharmaceuticals. Drug Dev Ind Pharm 1992;18:1169-206.

Takeuchi H, Nagira S, Yamamoto S, Kawashima Y. Solid dispersion

particles of tolbutamide prepared with fine silica particles by the spraydrying

method. Powder Technol


Weuts I, Kempen D, Verreck G, Decorte A, Heymans K, Peeters J,

et al. Study of the physicochemical properties and stability of solid

dispersions of loperamide and PEG6000 prepared by spray drying. Eur

J Pharm Biopharm 2005;59(1):119-26.

Fahr A, Liu X. Drug delivery strategies for poorly water-soluble drugs.

Expert Opin Drug Deliv 2007;4(4):403-16.



How to Cite

Mohanty, S., and A. Pal. “DISSOLUTION ENHANCEMENT OF SEROQUEL BY SOLID DISPERSION TECHNIQUES”. Asian Journal of Pharmaceutical and Clinical Research, vol. 9, no. 4, July 2016, pp. 284-7, https://innovareacademics.in/journals/index.php/ajpcr/article/view/12166.



Original Article(s)